agenticx/DrugbankRawParquet · Datasets at Hugging Face

DB00677

Isoflurophate

An irreversible cholinesterase inhibitor with actions similar to those of echothiophate. It is a powerful miotic used mainly in the treatment of glaucoma. Its vapor is highly toxic and it is recommended that only solutions in arachis oil be used therapeutically. (From Martindale, The Extra Pharmacopoeia, 29th ed, p1330)

liquid

For use in the eye to treat certain types of glaucoma and other eye conditions, such as accommodative esotropia.

Isoflurophate is used as ocular drops in the treatment of chronic glaucoma. Isoflurophate is an organophosphorus compound that acts as an irreversible cholinesterase inhibitor. As such, it displays parasympathomimetic effects. Isoflurophate is used in the eye to treat certain types of glaucoma and other eye conditions, such as accommodative esotropia. They may also be used in the diagnosis of certain eye conditions, such as accommodative esotropia. Isoflurophate damages the acetylcholinesterase enzyme and is therefore irreversible, however, pralidoxime can displace organophosphates such as isoflurophate from acetylcholinesterase, but only if administered before isoflurophate damages (alkylates) the enzyme.

The mechanism of isoflurophate's action involves the irreversible inhibition of cholinesterase.

null

Signs of overdose include increased sweating, loss of bladder control, muscle weakness, nausea, vomiting, diarrhea, or stomach cramps or pain, shortness of breath, tightness in chest, or wheezing, slow or irregular heartbeat, unusual tiredness or weakness, watering of mouth.

null

Organic compounds

Organic acids and derivatives

Organic phosphoric acids and derivatives

Phosphate esters

[ "approved", "investigational", "withdrawn" ]

[]

[ "Humans and other mammals" ]

[]

[]

[ "Diflupyl", "Floropryl", "Fluopryl", "Neoglaucit" ]

[]

[ "P22303", "P06276", "P02787" ]

[ "P06276" ]

[ "P02768" ]

[]

DB00678

Losartan

Losartan is an angiotensin II receptor blocker (ARB) used to treat hypertension.[L7423] Angiotensin-converting enzyme (ACE) inhibitors are used for a similar indication but are associated with a cough.[L7423] When patients with ACE inhibitor associated coughs are switched to ARBs like losartan, they have an incidence of cough similar to placebo or [hydrochlorothiazide].[L7423] Losartan is available as losartan potassium oral tablets as well as a combination tablet of losartan potassium and hydrochlorothiazide.[L7423,L7426] Patients taking losartan should have their renal function and potassium levels monitored.[L7423] Losartan was granted FDA approval on 14 April 1995.[L7423]

solid

Losartan is indicated to treat hypertension in patients older than 6 years, reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy (though this benefit may not extend to patients with African heritage), and to treat diabetic nephropathy with elevated serum creatinine and proteinuria in patients with type 2 diabetes and hypertension.[L7423] Losartan with hydrochlorothiazide is indicated to treat hypertension and to reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy (though this benefit may not extend to patients with African heritage).[L7426,L45663]

Losartan is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke.[A1033,L7423,L7426] Losartan has a long duration of action as it is given once daily.[L7423,L7426] Patients taking losartan should be regularly monitored for hypotension, renal function, and potassium levels.[L7423,L7426]

Losartan reversibly and competitively prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland.[L7423,L7426] Losartan and its active metabolite bind the AT1 receptor with 1000 times more affinity than they bind to the AT2 receptor.[L7423,L7426] The active metabolite of losartan is 10-40 times more potent by weight than unmetabolized losartan as an inhibitor of AT1 and is a non-competitive inhibitor.[L7423,L7426] Losartan's prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure.[L7423,L7426] Angiotensin II would otherwise bind to the AT1 receptor and induce vasoconstriction, raising blood pressure.[L7423,L7426]

Losartan is approximately 33% orally bioavailable.[A1033,L7423,L7426] Losartan has a Tmax of 1 hour and the active metabolite has a Tmax of 3-4 hours.[A1033,L7423,L7426] Taking losartan with food decreases the Cmax but does only results in a 10% decrease in the AUC of losartan and its active metabolite.[A1033,L7423,L7426] A 50-80mg oral dose of losartan leads to a Cmax of 200-250ng/mL.[A1033]

Losartan is metabolized to an aldehyde intermediate, E-3179, which is further metabolized to a carboxylic acid, E-3174, by cytochrome P450s like CYP2C9.[A1033] Losartan can also be hydroxylated to an inactive metabolite, P1.[A1033] Approximately 14% of losartan is metabolized to E-3174.[A1033] Losartan can be metabolized by CYP3A4, CYP2C9, and CYP2C10.[A1033] Losartan can also be glucuronidated by UGT1A1, UGT1A3, UGT1A10, UGT2B7, and UGT 2B17.[A415]

The oral TDLO in mice is 1000mg/kg and in rats is 2000mg/kg.[L7423,L7426] In humans the TDLO for men is 10mg/kg/2W and for women is 1mg/kg/1D.[L7441] Symptoms of overdose are likely to include hypotension, tachycardia, or bradycardia due to vagal stimulation.[L7423,L7426] Supportive treatment should be instituted for symptomatic hypotension.[L7423,L7426] Hemodialysis will not remove losartan or its active metabolite due to their high rates of protein binding.[L7423,L7426]

The terminal elimination half life of losartan is 1.5-2.5 hours while the active metabolite has a half life of 6-9 hours.[A1033]

Losartan is 98.6-98.8% protein bound and the active metabolite (E-3174) is 99.7% protein bound in serum.[A1033]

A single oral dose of losartan leads to 4% recovery in the urine as unchanged losartan, 6% in the urine as the active metabolite.[L7423,L7426] Oral radiolabelled losartan is 35% recovered in urine and 60% in feces.[L7423,L7426] Intravenous radiolabelled losartan is 45% recovered in urine and 50% in feces.[L7423,L7426]

The volume of distribution of losartan is 34.4±17.9L and 10.3±1.1L for the active metabolite (E-3174).[A1033]

Losartan has a total plasma clearance of 600mL/min and a renal clearance of 75mL/min.[A1033] E-3174, the active metabolite, has a total plasma clearance of 50mL/min and a renal clearance of 25mL/min.[A1033]

Organic compounds

Benzenoids

Benzene and substituted derivatives

Biphenyls and derivatives

[ "approved" ]

[ "C09CA", "C09C", "C09", "C", "C09DA", "C09D", "C09", "C", "C09DB", "C09D", "C09", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "1.31", "description": "Cozaar 100 mg Tablet", "unit": "tablet" }, { "cost": "1.31", "description": "Cozaar 25 mg Tablet", "unit": "tablet" }, { "cost": "1.31", "description": "Cozaar 50 mg Tablet", "unit": "tablet" }, { "cost": "1.72", "description": "Losartan potassium 25 mg tablet", "unit": "tablet" }, { "cost": "1.92", "description": "Cozaar 25 mg tablet", "unit": "tablet" }, { "cost": "2.26", "description": "Losartan potassium 50 mg tablet", "unit": "tablet" }, { "cost": "2.5", "description": "Cozaar 50 mg tablet", "unit": "tablet" }, { "cost": "2.65", "description": "Hyzaar 50-12.5 tablet", "unit": "tablet" }, { "cost": "2.97", "description": "Hyzaar 50-12.5 mg tablet", "unit": "tablet" }, { "cost": "3.14", "description": "Losartan potassium 100 mg tablet", "unit": "tablet" }, { "cost": "3.41", "description": "Cozaar 100 mg tablet", "unit": "tablet" }, { "cost": "3.54", "description": "Losartan Potassium-HCTZ 100-12.5 mg tablet", "unit": "tablet" }, { "cost": "3.54", "description": "Losartan Potassium-HCTZ 100-25 mg tablet", "unit": "tablet" }, { "cost": "3.61", "description": "Hyzaar 100-12.5 tablet", "unit": "tablet" }, { "cost": "3.61", "description": "Hyzaar 100-25 tablet", "unit": "tablet" }, { "cost": "3.87", "description": "Hyzaar 100-12.5 mg tablet", "unit": "tablet" }, { "cost": "3.91", "description": "Hyzaar 100-25 mg tablet", "unit": "tablet" }, { "cost": "78.05", "description": "Losartan Potassium-HCTZ 30 50-12.5 mg tablet Bottle", "unit": "bottle" }, { "cost": "211.78", "description": "Losartan Potassium 90 50 mg tablet Bottle", "unit": "bottle" } ]

[ { "approved": "1993-05-11", "country": "United States", "expires": "2010-11-11", "number": "5210079" }, { "approved": "1997-03-04", "country": "United States", "expires": "2009-03-04", "number": "5608075" }, { "approved": "2003-02-11", "country": "Canada", "expires": "2011-06-07", "number": "2085584" }, { "approved": "1995-01-24", "country": "Canada", "expires": "2012-01-24", "number": "1334092" } ]

(2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanol | 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole | Losartan | EPO-R | AGTR1A | AGTR1B | Angiotensin II type-1 receptor | AT1 receptor | AT1AR | AT1BR | AT2R1 | AT2R1B | (R)-limonene 6-monooxygenase | (S)-limonene 6-monooxygenase | (S)-limonene 7-monooxygenase | 1.14.14.1 | Cholesterol 25-hydroxylase | CYP2C10 | CYPIIC9 | Cytochrome P-450MP | Cytochrome P450 MP-4 | Cytochrome P450 MP-8 | Cytochrome P450 PB-1 | S-mephenytoin 4-hydroxylase | 1,4-cineole 2-exo-monooxygenase | 1,8-cineole 2-exo-monooxygenase | 1.14.14.1 | Albendazole monooxygenase (sulfoxide-forming) | Albendazole sulfoxidase | Cholesterol 25-hydroxylase | CYP3A3 | CYPIIIA3 | CYPIIIA4 | Cytochrome P450 3A3 | Cytochrome P450 HLp | Cytochrome P450 NF-25 | Cytochrome P450-PCN1 | Nifedipine oxidase | Quinine 3-monooxygenase | (R)-limonene 6-monooxygenase | (S)-limonene 6-monooxygenase | (S)-limonene 7-monooxygenase | 1.14.14.1 | CYPIIC17 | CYPIIC19 | Cytochrome P450-11A | Cytochrome P450-254C | Fenbendazole monooxygenase (4'-hydroxylating) | Mephenytoin 4-hydroxylase | 2.4.1.17 | Bilirubin-specific UDPGT isozyme 1 | GNT1 | hUG-BR1 | UDP-glucuronosyltransferase 1-1 | UDP-glucuronosyltransferase 1A isoform 1 | UDPGT 1-1 | UGT1 | UGT1-01 | UGT1.1 | UGT1*1 | UGT1A1 | 2.4.1.17 | GNT1 | UDP-glucuronosyltransferase 1-3 | UDP-glucuronosyltransferase 1-C | UDP-glucuronosyltransferase 1A isoform 3 | UDPGT 1-3 | UGT-1C | UGT1 | UGT1-03 | UGT1.3 | UGT1*3 | UGT1A3 | UGT1C | 2.4.1.17 | GNT1 | UDP-glucuronosyltransferase 1-10 | UDP-glucuronosyltransferase 1-J | UDPGT 1-10 | UGT-1J | UGT1 | UGT1-10 | UGT1.10 | UGT1*10 | UGT1A10 | UGT1J | 2.4.1.17 | 3,4-catechol estrogen-specific UDPGT | UDP-glucuronosyltransferase 2B9 | UDPGT 2B7 | UDPGT 2B9 | UDPGTh-2 | UGT2B7 | UGTB2B9 | 2.4.1.17 | C19-steroid-specific UDP-glucuronosyltransferase | C19-steroid-specific UDPGT | UDPGT 2B17 | UGT2B17 | 1.14.14.1 | CYPIIC8 | Cytochrome P450 form 1 | Cytochrome P450 IIC2 | Cytochrome P450 MP-12 | Cytochrome P450 MP-20 | S-mephenytoin 4-hydroxylase | ATP-binding cassette sub-family B member 1 | MDR1 | Multidrug resistance protein 1 | P-glycoprotein 1 | PGY1 | Phospholipid transporter ABCB1 | hOAT1 | hPAHT | hROAT1 | OAT1 | Organic anion transporter 1 | PAH transporter | PAHT | Renal organic anion transporter 1 | OATL4 | Organic anion transporter 4-like protein | Renal-specific transporter | RST | URAT1 | Urate anion exchanger 1 | Urate:anion antiporter SLC22A12 | Glucose transporter type 9 | GLUT-9 | GLUT9 | Urate transporter | 7.6.2.- | ATP-binding cassette sub-family B member 11 | BSEP

[ "Act Losartan", "Act Losartan", "Act Losartan", "Act Losartan/hct", "Act Losartan/hct", "Act Losartan/hct", "Ag-losartan", "Ag-losartan", "Ag-losartan", "Ag-losartan Hctz", "Ag-losartan Hctz", "Apo-losartan", "Apo-losartan", "Apo-losartan", "Apo-losartan/hctz", "Apo-losartan/hctz", "Apo-losartan/hctz", "Auro-losartan", "Auro-losartan", "Auro-losartan", "Auro-losartan HCT", "Auro-losartan HCT", "Auro-losartan HCT", "Bio-losartan", "Bio-losartan", "Bio-losartan", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Cozaar", "Dom-losartan", "Dom-losartan", "Dom-losartan", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar", "Hyzaar DS", "Ipg-losartan", "Ipg-losartan", "Ipg-losartan", "Jamp-losartan", "Jamp-losartan", "Jamp-losartan", "Jamp-losartan Hctz", "Jamp-losartan Hctz", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan", "Losartan HCT", "Losartan HCT", "Losartan HCT DS", "Losartan Pot/hctz", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan 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Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan Potassium", "Losartan potassium", "Losartan Potassium", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 100 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 25 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "LOSARTAN POTASSIUM 50 mg", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and 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potassium and Hydrochlorothiazide", "Losartan potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and 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Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium HCTZ", "Losartan potassium Tablets, 100 mg", "Losartan potassium Tablets, 100 mg", "Losartan potassium Tablets, 100 mg", "Losartan potassium Tablets, 100 mg", "Losartan potassium Tablets, 100 mg", "Losartan potassium Tablets, 25 mg", "Losartan potassium Tablets, 25 mg", "Losartan potassium Tablets, 25 mg", "Losartan potassium Tablets, 25 mg", "Losartan potassium Tablets, 25 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan potassium Tablets, 50 mg", "Losartan Potatssium", "Losartan-hctz", "Losartan-hctz", "Losartan-hctz", "Losartan/hct", "Losartan/hct", "Losartan/hct", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losatan Potassium", "Losatan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Losortan Potassium", "Mar-losartan", "Mar-losartan", "Mar-losartan", "Mint-losartan", "Mint-losartan", "Mint-losartan", "Mint-losartan/hctz", "Mint-losartan/hctz", "Mint-losartan/hctz DS", "Mylan-losartan", "Mylan-losartan", "Mylan-losartan", "Mylan-losartan Hctz", "Mylan-losartan Hctz", "Mylan-losartan Hctz", "PHL-losartan", "PHL-losartan", "PHL-losartan", "PMS-losartan", "PMS-losartan", "PMS-losartan", "PMS-losartan-hctz", "PMS-losartan-hctz", "PMS-losartan-hctz", "Priva-losartan", "Priva-losartan", "Priva-losartan", "Ratio-losartan Hctz", "Sandoz Losartan", "Sandoz Losartan", "Sandoz Losartan", "Sandoz Losartan HCT", "Sandoz Losartan HCT", "Sandoz Losartan HCT DS", "Septa-losartan", "Septa-losartan", "Septa-losartan", "Septa-losartan Hctz", "Septa-losartan Hctz", "Taro-losartan", "Taro-losartan", "Taro-losartan", "Teva-losartan", "Teva-losartan", "Teva-losartan", "Teva-losartan/hctz", "Teva-losartan/hctz", "Teva-losartan/hctz", "Van-losartan", "Van-losartan", "Van-losartan", "Van-losartan-hctz", "Van-losartan-hctz" ]

[ "Lortaan" ]

[ "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Hyzaar", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Hyzaar", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Pot/hctz", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium HCTZ", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Hyzaar", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan potassium and Hydrochlorothiazide", "Losartan potassium and Hydrochlorothiazide", "Losartan potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan potassium and hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "LOSARTAN POTASSIUM and HYDROCHLOROTHIAZIDE", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Hyzaar", "Hyzaar", "Losartan potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Hyzaar", "Hyzaar DS", "Hyzaar", "Sandoz Losartan HCT", "Sandoz Losartan HCT DS", "Teva-losartan/hctz", "Sandoz Losartan HCT", "Apo-losartan/hctz", "Apo-losartan/hctz", "Apo-losartan/hctz", "Teva-losartan/hctz", "Teva-losartan/hctz", "Mylan-losartan Hctz", "Mylan-losartan Hctz", "Mylan-losartan Hctz", "Act Losartan/hct", "Act Losartan/hct", "Act Losartan/hct", "Mint-losartan/hctz", "Mint-losartan/hctz", "Mint-losartan/hctz DS", "PMS-losartan-hctz", "PMS-losartan-hctz", "PMS-losartan-hctz", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losartan Potassium and Hydrochlorothiazide", "Van-losartan-hctz", "Van-losartan-hctz", "Losartan-hctz", "Losartan-hctz", "Losartan-hctz", "Ratio-losartan Hctz", "Jamp-losartan Hctz", "Jamp-losartan Hctz", "Auro-losartan HCT", "Auro-losartan HCT", "Auro-losartan HCT", "Losartan/hctz", "Losartan/hctz", "Losartan/hctz", "Losartan HCT", "Losartan HCT", "Losartan HCT DS", "Septa-losartan Hctz", "Septa-losartan Hctz", "Losartan/hct", "Losartan/hct", "Losartan/hct", "Losartan Potassium and Hydrochlorothiazide", "Ag-losartan Hctz", "Ag-losartan Hctz", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide", "Losartan Potassium and Hydrochlorothiazide" ]

[ "P19235", "P30556" ]

[ "P11712", "P08684", "P33261", "P22309", "P35503", "Q9HAW8", "P16662", "O75795", "P10632" ]

[ "P02768" ]

[ "P08183", "Q4U2R8", "Q96S37", "Q9NRM0", "O95342" ]

DB00679

Thioridazine

A phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. It has little antiemetic activity. Thioridazine has a higher incidence of antimuscarinic effects, but a lower incidence of extrapyramidal symptoms, than chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p618). Thioridazine was withdrawn worldwide in 2005 due to its association with cardiac arrythmias.

solid

For the treatment of schizophrenia and generalized anxiety disorder.

Thioridazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Thioridazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.

Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect, depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

60%

Hepatic

LD50=956-1034 mg/kg (Orally in rats); Agitation, blurred vision, coma, confusion, constipation, difficulty breathing, dilated or constricted pupils, diminished flow of urine, dry mouth, dry skin, excessively high or low body temperature, extremely low blood pressure, fluid in the lungs, heart abnormalities, inability to urinate, intestinal blockage, nasal congestion, restlessness, sedation, seizures, shock

21-25 hours

95%

null

Organic compounds

Organoheterocyclic compounds

Benzothiazines

Phenothiazines

[ "approved", "withdrawn" ]

[ "N05AC", "N05A", "N05", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.01", "description": "Thioridazine HCl 150 mg tablet", "unit": "tablet" }, { "cost": "1.14", "description": "Thioridazine HCl 200 mg tablet", "unit": "tablet" }, { "cost": "11.16", "description": "Thioridazine hcl powder", "unit": "g" }, { "cost": "0.33", "description": "Thioridazine 10 mg tablet", "unit": "tablet" }, { "cost": "0.35", "description": "Thioridazine HCl 10 mg tablet", "unit": "tablet" }, { "cost": "0.45", "description": "Thioridazine HCl 15 mg tablet", "unit": "tablet" }, { "cost": "0.47", "description": "Thioridazine 25 mg tablet", "unit": "tablet" }, { "cost": "0.49", "description": "Thioridazine HCl 25 mg tablet", "unit": "tablet" }, { "cost": "0.58", "description": "Thioridazine 50 mg tablet", "unit": "tablet" }, { "cost": "0.61", "description": "Thioridazine HCl 50 mg tablet", "unit": "tablet" }, { "cost": "0.67", "description": "Thioridazine 100 mg tablet", "unit": "tablet" }, { "cost": "0.69", "description": "Thioridazine HCl 100 mg tablet", "unit": "tablet" } ]

[]

[ "Mellaril", "Mellaril", "Mellaril Tab 100mg", "Mellaril Tab 10mg", "Mellaril Tab 200mg", "Mellaril Tab 25mg", "Mellaril Tab 50mg", "Novo-ridazine (thioridazine Oral Suspension) - 2 mg/ml", "Novo-ridazine 100mg", "Novo-ridazine 10mg", "Novo-ridazine 25mg", "Novo-ridazine 50mg", "Novo-ridazine Tab 200mg", "PMS Thioridazine Tab 50mg", "PMS-thioridazine 100mg/tab USP", "PMS-thioridazine 10mg/tab USP", "PMS-thioridazine Solution 30mg/ml", "PMS-thioridazine Solution 5mg/ml", "PMS-thioridazine Tab 25mg", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Hydrochloride", "Thioridazine Oral Sus 2mg/ml", "Thioridazine Tab 10mg", "Thioridazine Tab 25mg", "Thioridazine Tab 50mg" ]

[ "Aldazine", "Mallorol", "Malloryl", "Meleril", "Mellaril-S", "Mellerets", "Mellerette", "Melleretten", "Melleril", "Novoridazine", "Orsanil", "Ridazin", "Ridazine", "Sonapax", "Thioril" ]

[]

[ "P14416", "P21728", "P35348", "P35368", "P28223", "Q12809" ]

[ "P05181", "P10635", "P33261" ]

[]

DB00680

Moricizine

An antiarrhythmia agent used primarily for ventricular rhythm disturbances.

solid

Used to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.

Moricizine is used to treat irregular heartbeats (arrhythmias) and to maintain a normal heart rate. It acts on the heart muscle to improve the heart's rhythm. Moricizine has potent local anesthetic activity and membrane stabilizing effect. Decreases excitability, conduction velocity, and automaticity as a result of slowed atrioventricular (AV) nodal and His-Purkinje conduction. Decreases the action potential duration (APD) in Purkinje fibers; also decreases the effective refractory period (ERP) but to a lesser extent than the APD, so the ERP/APD ratio is increased. Decreases the maxiumum rate of Phase 0 depolarization (V max ), but does not affect action potential amplitude or maximum diastolic potential. Does not affect atrial, AV nodal, or left ventricular refractory periods and has minimal effect on ventricular repolarization (evidenced by the overall decrease in JT interval). Has no effect on sinoatrial (SA) nodal or intra-atrial conduction and only minimal effect on sinus cycle length and sinus node recovery time. In the Vaughan Williams classification of antiarrhythmics, moricizine is considered to be a class I agent. It has properties of class IA, IB, and IC agents but does not clearly belong to any of the three subclasses. It has less effect on the slope of phase 0 and a greater effect on action potential duration and effective refractory period than class IC agents.

Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes.

Well absorbed, absorption is complete within 2 to 3 hours. Significant first-pass metabolism results in an absolute bioavailability of approximately 38%. Administration within 30 minutes after a meal slows the rate, but does not affect the extent of absorption, although peak plasma concentrations are reduced.

Hepatic and extensive, to at least 26 metabolites, none accounting for as much as 1% of the administered dose. Two metabolites may be pharmacologically active but are present in extremely small quantities. Moricizine induces its own metabolism (it induces hepatic cytochrome P-450 activity).

Symptoms of overdose include vomiting, unconsciousness, and severe low blood pressure.

2 hours (range 1.5-3.5 hours).

Approximately 95%.

Less than 1% of orally administered Ethmozine® is excreted unchanged in the urine. Approximately 56% of the administered dose is excreted in the feces and 39% is excreted in the urine.

* 300 L

null

Organic compounds

Organoheterocyclic compounds

Benzothiazines

Phenothiazines

[ "approved", "investigational", "withdrawn" ]

[ "C01BG", "C01B", "C01", "C" ]

[ "Humans and other mammals" ]

[]

[ "Ethmozine", "Ethmozine", "Ethmozine" ]

[ "Etmozins" ]

[]

[ "Q14524" ]

[]

DB00681

Amphotericin B

Amphotericin B shows a high order of in vitro activity against many species of fungi. Histoplasma capsulatum, Coccidioides immitis, Candida species, Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus are all inhibited by concentrations of amphotericin B ranging from 0.03 to 1.0 mcg/mL in vitro. While Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible. Pseudallescheria boydii and Fusarium sp. are often resistant to amphotericin B. The antibiotic is without effect on bacteria, rickettsiae, and viruses.

solid

Used to treat potentially life threatening fungal infections.

Amphotericin B shows a high order of in vitro activity against many species of fungi. Histoplasma capsulatum, Coccidioides immitis, Candida species, Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus are all inhibited by concentrations of amphotericin B ranging from 0.03 to 1.0 mcg/mL in vitro. While Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible. Pseudallescheria boydii and Fusarium sp. are often resistant to amphotericin B. The antibiotic is without effect on bacteria, rickettsiae, and viruses.

Amphotericin B is fungistatic or fungicidal depending on the concentration obtained in body fluids and the susceptibility of the fungus. The drug acts by binding to sterols (ergosterol) in the cell membrane of susceptible fungi. This creates a transmembrane channel, and the resultant change in membrane permeability allowing leakage of intracellular components. Ergosterol, the principal sterol in the fungal cytoplasmic membrane, is the target site of action of amphotericin B and the azoles. Amphotericin B, a polyene, binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.

Bioavailability is 100% for intravenous infusion.

Exclusively renal

Oral, rat: LD50 = >5 gm/kg. Amphotericin B overdoses can result in cardio-respiratory arrest.

An elimination half-life of approximately 15 days follows an initial plasma half-life of about 24 hours.

Highly bound (>90%) to plasma proteins.

null

* 39 +/- 22 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day at Day 1] * 17 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 1 mg/kg/day 3-20 days later] * 51 +/- 44 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day at Day 1] * 22 +/- 15 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 2.5 mg/kg/day 3-20 days later] * 21 +/- 14 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day at Day 1] * 11 +/- 6 mL/hr/kg [febrile neutropenic cancer and bone marrow transplant patients receiving infusion of 5 mg/kg/day 3-20 days later]

Organic compounds

Organic oxygen compounds

Organooxygen compounds

Carbohydrates and carbohydrate conjugates

[ "approved", "investigational" ]

[ "G01AA", "G01A", "G01", "G", "A07AA", "A07A", "A07", "A", "A01AB", "A01A", "A01", "A", "J02AA", "J02A", "J02", "J" ]

[ "Various Fungus Species" ]

[ { "cost": "12.0", "description": "Abelcet 5 mg/ml vial p-f", "unit": "ml" }, { "cost": "24.5", "description": "Amphotericin b 50 mg vial", "unit": "vial" }, { "cost": "29.99", "description": "Amphotericin b powder", "unit": "g" }, { "cost": "72.5", "description": "Fungizone Iv 50 mg/vial", "unit": "vial" }, { "cost": "93.33", "description": "Amphotec 50 mg vial", "unit": "vial" }, { "cost": "160.0", "description": "Amphotec 100 mg vial", "unit": "vial" }, { "cost": "188.4", "description": "Ambisome 50 mg vial", "unit": "vial" } ]

[ { "approved": "1997-03-25", "country": "Canada", "expires": "2014-03-25", "number": "1339008" }, { "approved": "1995-09-05", "country": "Canada", "expires": "2012-09-05", "number": "1336890" }, { "approved": "2002-06-18", "country": "United States", "expires": "2019-06-18", "number": "6406713" }, { "approved": "1999-02-23", "country": "United States", "expires": "2016-02-23", "number": "5874104" }, { "approved": "1999-10-12", "country": "United States", "expires": "2016-10-12", "number": "5965156" } ]

[ "Abelcet", "Abelcet", "AmBisome", "AmBisome", "Amphotec", "Amphotec", "Amphotec", "Amphotec", "Amphotec 100 mg", "Amphotec 50 mg", "Amphotericin B", "Amphotericin B", "Amphotericin B", "Amphotericin B", "Amphotericin B for Injection, USP", "Fungizone", "Fungizone" ]

[ "Abelect", "Ampho-Moronal", "Amphocil", "Amphocin", "Amphotericin", "Fungilin", "Fungisome", "Fungizone Intravenous", "Halizon" ]

[ "Abelcet" ]

[]

DB00682

Warfarin

Warfarin is an anticoagulant drug normally used to prevent blood clot formation as well as migration. Although originally marketed as a pesticide (d-Con, Rodex, among others), Warfarin has since become the most frequently prescribed oral anticoagulant in North America. Warfarin has several properties that should be noted when used medicinally, including its ability to cross the placental barrier during pregnancy which can result in fetal bleeding, spontaneous abortion, preterm birth, stillbirth, and neonatal death. Additional adverse effects such as necrosis, purple toe syndrome, osteoporosis, valve and artery calcification, and drug interactions have also been documented with warfarin use. Warfarin does not actually affect blood viscosity, rather, it inhibits vitamin-k dependent synthesis of biologically active forms of various clotting factors in addition to several regulatory factors.

solid

**Indicated** for:[label,L6616] 1) Prophylaxis and treatment of venous thromboembolism and related pulmonary embolism. 2) Prophylaxis and treatment of thromboembolism associated with atrial fibrillation. 3) Prophylaxis and treatment of thromboembolism associated with cardiac valve replacement. 4) Use as adjunct therapy to reduce mortality, recurrent myocardial infarction, and thromboembolic events post myocardial infarction. **Off-label** uses include: 1) Secondary prevention of stroke and transient ischemic attacks in patients with rheumatic mitral valve disease but without atrial fibrillation.[A179182]

Warfarin is an anticoagulant, as such it disrupts the coagulation cascade to reduce frequency and extent of thrombus formation.[label,L6616] In patients with deep vein thrombosis or atrial fibrillation there is an increased risk of thrombus formation due to the reduced movement of blood.[T622] For patients with cardiac valve disease or valve replacements this increased coagulability is due to tissue damage. Thrombi due to venous thrombosis can travel to the lungs and become pulmonary emboli, blocking circulation to a portion of lung tissue. Thrombi which form in the heart can travel to the brain and cause ischemic strokes. Prevention of these events is the primary goal of warfarin therapy. Limitation of thrombus formation is also a source of adverse effects. In patients with atheroscelotic plaques rupture typically results in thrombus formation.[A179212] When these patients are anticoagulated plaque rupture can allow the escape of cholesterol from the lipid core in the form of atheroemboli or cholesterol microemboli. These emboli are smaller than thrombi and block smaller vessels, usually less than 200 μm in diameter. The consequences of this are varied and depend on the location of the blockage. Effects include visual disturbances, acute kidney injury or worsening of chronic kidney disease, central nervous system ischemia, and purple or blue toe syndrome.[label,A179212] Blue toe syndrome can be reversed if it has not progressed to tissue necrosis but the other effects of microemboli are often permanent. Antocoagulation appears to mediate warfarin-related nephropathy, a seemingly spontaneous kidney injury or worsening of chronic kidney disease associated with warfarin therapy.[A179215] Nephropathy in this case appears to be due to increased passage of red blood cells through the glomerulus and subsequent blockage of renal tubules with red blood cell casts. This is worsened or possibly triggered by pre-existing kidney damage. Increased risk of warfarin-related nephropathy occurs at INRs over 3.0 but risk does not increase as a function of INR beyond this point. Warfarin has been linked to the development of calciphylaxis.[label] This is thought to be due to warfarin's inhibition of [vitamin K](VKA) recycling as VKA is needed for the carboxylation of matrix Gla protein.[A179218] This protein is an anti-calcification factor and its inhibition through preventing the carboxylation step in its production leads to a shift in calcification balance in favor of calciphylaxis. Tissue necrosis can occur early on in warfarin therapy.[label] This is attributable to half lives of the clotting factors impacted by inhibition of vitamin K recycling.[label,A179221] Proteins C and S are anticoagulation factors with half lives of 8 and 24 hours respectively. The coagulation factors IX, X, VII, and thrombin (factor II) have half lives of 24, 36, 6, and 50 hours respectively. This means proteins C and S are inactivated sooner than pro-coagulation proteins, with the exception of factor VII, resulting in a pro-thrombotic state for the first few days of therapy. Thrombi which form in this time period can occlude arterioles in various locations, blocking blood flow and causing tissue necrosis due to ischemia.

Warfarin is a [vitamin K] antagonist which acts to inhibit the production of vitamin K by vitamin K epoxide reductase.[label,A179221,T116] The reduced form of vitamin K, vitamin KH2 is a cofactor used in the γ-carboxylation of coagulation factors VII, IX, X, and thrombin. Carboxylation induces a conformational change allowing the factors to bind Ca2+ and to phospholipid surfaces. Uncarboxylated factors VII, IX, X, and thrombin are biologically inactive and therefore serve to interrupt the coagulation cascade. The endogenous anticoagulation proteins C and S also require γ-carboxylation to function. This is particularly true in the case of thrombin which must be activated in order to form a thrombus. vitamin KH2 is converted to vitamin K epoxide as part of the γ-carboxylation reaction catalyzed by γ-glutamyl carboxylase. Vitamin K epoxide is then converted to vitamin K1 by vitamin K epoxide reductase then back to vitamin KH2 by vitamin K reductase. Warfarin binds to vitamin K epoxide reductase complex subunit 1 and irreversibly inhibits the enzyme thereby stopping the recycling of vitamin K by preventing the conversion of vitamin K epoxide to vitamin K1. This process creates a hypercoagulable state for a short time as proteins C and S degrade first with half lives of 8 and 24 hours, with the exception of factor VII which has a half life of 6 hours.[A179221] Factors IX, X, and finally thrombin degrade later with half lives of 24, 36, and 50 hours resulting in a dominant anticoagulation effect.[A179221] In order to reverse this anticoagulation vitamin K must be supplied, either exogenously or by removal of the vitamin K epoxide reductase inhibition, and time allowed for new coagulation factors to be synthesized.[label,A179221,T116] It takes approximately 2 days for new coagulation factors to be synthesized in the liver. Vitamin K2, functionally identical to vitamin K1, is synthesized by gut bacteria leading to interactions with antibiotics as elimination of these bacteria can reduce vitamin K2</sub supply and result in a greater anticoagulation effect.[T116]

Completely absorbed from the GI tract. The mean Tmax for warfarin sodium tablets is 4 hours.[label,L6616,A2460]

Metabolism of warfarin is both stereo- and regio-selective.[A2460] The major metabolic pathway is oxidation to various hydroxywarfarins, comprising 80-85% of the total metabolites. CYP2C9 is the major enzyme catalyzing the 6- and 7-hydroxylation of S-warfarin while 4'-hydroxylation occurs through CYP2C18 with minor contributions from CYP2C19. R-warfarin is metabolized to 4'-hydroxywarfarin by CYP2C8 with some contirbuting by CYP2C19, 6- and 8-hydroxywarfarin by CYP1A2 and CYP2C19, 7-hydroxywarfarin by CYP1A2 and CYP2C8, and lastly to 10-hydroxywarfarin by CYP3A4. The 10-hydroxywarfarin metabolite as well as a benzylic alcohol metabolite undergo an elimination step to form dehydrowarfarin. The minor pathway of metabolism is the reduction of the ketone group to warfarin alcohols, comprising 20% of the metabolites. Limited conjugation occurs with sulfate and gluronic acid groups but these metabolites have only been confirmed for R-hydroxywarfarins.

**LD50 Values** Mouse: 3 mg/kg (Oral), 165 mg/kg (IV), 750 mg/kg (IP)[L6622] Rat: 1.6 mg/kg (Oral), 320 mg/kg (Inhaled), 1400 mg/kg (Skin)[L6622] Rabbit: 800 mg/kg (Oral)[L6622] Pig: 1 mg/kg (Oral)[L6622] Dog: 3 mg/kg (Oral)[L6622] Cat: 6 mg/kg (Oral)[L6622] Chicken: 942 mg/kg (Oral)[L6622] Guinea Pig: 180 mg/kg (Oral)[L6622] **Overdose** Doses of 1-2 mg/kg/day over a period of 15 days have been fatal in humans.[L6625] Warfarin overdose is primarily associated with major bleeding particularly from the mucous membranes, gastrointestinal tract, and genitourinary system.[label,L6625] Epistaxis, ecchymoses, as well as renal and hepatic bleeding are also associated. These symptoms become apparent within 2-4 days of overdose although increases in prothrombin time can be observed within 24 hours. Treatment for overdosed patients includes discontinuation of warfarin and administration of [vitamin K]. For more urgent reversal of anticoagulation [prothrombin] complex concentrate, blood plasma, or [coagulation factor VIIa] infusion can be used.[label] Patients can be safely re-anticoagulated after reversal of the overdose. **Carcinogenicity & Mutagenicity** The carcinogenicity and mutagenicity of warfarin have not been thoroughly investigated.[label] **Reproductive Toxicity** Warfarin is known to be a teratogen and its use during pregnancy is contraindicated in the absence of high thrombotic risk.[label,L6625] Fetal warfarin syndrome, attributed to exposure during the 1st trimester, is characterized by nasal hypoplasia with or without stippled epiphyses, possible failure of nasal septum development, and low birth weight. Either dorsal midline dysplasia or ventral midline dysplasia can occur. Dorsal midline dysplasia includes agenisis of the corpus callosum, Dandy-Walker malformations, midline cerebellar hypoplasia. Ventral midline dysplasia is characterized by eye anomalies which can potentially include optic atrophy, blindness, and microphthalmia. Exposure during the 2nd and 3rd trimester is associated with hypoplasia of the extremities, developmental retardation, microcephaly, hydrocephaly, schizencephaly, seizures, scoliosis, deafness, congenital heart malformations, and fetal death. The critical exposure period is estimated to be week 6-9 based on case reports. Effects noted in the Canadian product monograph include developing a single kidney, asplenia, anencephaly, spina bifida, cranial nerve palsy, polydactyl malformations, corneal leukoma, diaphragm hernia, and cleft palate.[L6616] **Lactation** Official product monographs mention a study in 15 women.[label,L6616] Warfarin was not detected in the breast milk of any woman and 6 infants were documented as having normal prothrombin times. The remaining 9 infants were not tested. Another study in 13 women using doses of 2-12 mg also revealed no detectable warfarin in breast milk.[L6628] A woman who mistakenly took 25 mg of warfarin for 7 days while breastfeeding presented to an emergency room with an INR of 10 and prothrombin time of over 100 s. Her infant had a normal INR of 1.0 and prothrombin time of 10.3. The infant in this case has an increased prothrombin time of 33.8 s three weeks previous but this was judged not to be due to warfarin exposure.

R-warfarin is cleared more slowly than S-warfarin, at about half the rate.[label] T1/2 for R-warfarin is 37-89 hours. T1/2 for S-warfarin is 21-43 hours.

99% bound primarily to albumin.[label,L6616,A2460]

The elimination of warfarin is almost entirely by metabolism with a small amount excreted unchanged.[label,L6616,A2460] 80% of the total dose is excreted in the urine with the remaining 20% appearing in the feces.[A2460]

Vd of 0.14 L/kg.[label,L6616,A2460] Warfarin has a distrubution phase lasting 6-12 hours.[L6616] It is known to cross the placenta and achieves fetal serum concentrations similar to maternal concentrations.

Clearance of warfarin varies depending on CYP2C9 genotype.[label,L6616] The \*2 and \*3 alleles appear in the Caucasian population at frequencies of 11% and 7% and are known to reduce clearance warfarin. Additional clearance reducing genotypes include the \*5, \*6, \*9 and \*11 alleles. Genotypes for which population clearance estimates have been found are listed below. \*1/\*1 = 0.065 mL/min/kg \*1/\*2, \*1/\*3 = 0.041 mL/min/kg \*2/\*2, \*2/\*3, \*3/\*3 = 0.020 mg/min/kg

Organic compounds

Phenylpropanoids and polyketides

Coumarins and derivatives

Hydroxycoumarins

[ "approved" ]

[ "B01AA", "B01A", "B01", "B" ]

[ "Humans and other mammals" ]

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Tablet", "unit": "tablet" }, { "cost": "0.33", "description": "Taro-Warfarin 7.5 mg Tablet", "unit": "tablet" }, { "cost": "0.35", "description": "Coumadin 2 mg Tablet", "unit": "tablet" }, { "cost": "0.43", "description": "Coumadin 3 mg Tablet", "unit": "tablet" }, { "cost": "0.43", "description": "Coumadin 4 mg Tablet", "unit": "tablet" }, { "cost": "0.49", "description": "Jantoven 1 mg tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Coumadin 10 mg Tablet", "unit": "tablet" }, { "cost": "0.53", "description": "Jantoven 2.5 mg tablet", "unit": "tablet" }, { "cost": "0.53", "description": "Jantoven 3 mg tablet", "unit": "tablet" }, { "cost": "0.56", "description": "Jantoven 2 mg tablet", "unit": "tablet" }, { "cost": "0.56", "description": "Jantoven 4 mg tablet", "unit": "tablet" }, { "cost": "0.59", "description": "Jantoven 5 mg tablet", "unit": "tablet" }, { "cost": "0.61", "description": "Warfarin sodium 1 mg tablet", "unit": "tablet" }, { "cost": "0.63", 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[]

[ "Apo-warfarin", "Apo-warfarin", "Apo-warfarin", "Apo-warfarin", "Apo-warfarin", "Apo-warfarin", "Apo-warfarin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin", "Coumadin Tab 10mg", "Coumadin Tab 1mg", "Coumadin Tab 2.5mg", "Coumadin Tab 2mg", "Coumadin Tab 3mg", "Coumadin Tab 4mg", "Coumadin Tab 5mg", "Coumadin Tab 6 mg", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Jantoven", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Mylan-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Novo-warfarin", "Nu-warfarin", "Nu-warfarin", "Nu-warfarin", "Nu-warfarin", "Nu-warfarin", "Nu-warfarin", "Nu-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Taro-warfarin", "Warfarin", "Warfarin", 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"Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfarin Sodium", "Warfilone Tab 5mg" ]

[ "Lawarin", "Marevan", "Waran", "Warfant" ]

[]

[ "Q9BQB6", "O75469" ]

[ "P11712", "P05177", "P33261", "P08684", "P10632", "P33260" ]

[ "P02768", "P02763" ]

[]

DB00683

Midazolam

Midazolam is a short-acting hypnotic-sedative drug with anxiolytic, muscle relaxant, anticonvulsant, sedative, hypnotic, and amnesic properties.[A173842] It belongs to a class of drugs called _benzodiazepines_. This drug is unique from others in this class due to its rapid onset of effects and short duration of action.[A173842] Midazolam is available by oral, rectal, intranasal, intramuscular (IM), and intravenous (IV) routes and has been used in various biomedical applications, including dentistry, cardiac surgery, and endoscopic procedures as pre-anesthetic medication, and as an adjunct to local anesthesia.[F2977] This drug was initially approved by the US FDA in 1985, and has been approved for various indications since.[L45098] In late 2018, the intramuscular preparation was approved by the FDA for the treatment of status epilepticus in adults.[L45098] In May 2019, the nasal spray of midazolam was approved for the acute treatment of distinctive intermittent, stereotypic seizure episodes in patients 12 years of age and older.[A257153] Midazolam is considered a schedule IV drug in the United States due to the low potential for abuse and low risk of dependence.[L5074]

solid

Midazolam has different indications depending on its formulation by the FDA. **Nasal** For the nasal spray formulation, midazolam is indicated for the acute treatment of intermittent, stereotypic episodes of frequent seizure activity (i.e., seizure clusters, acute repetitive seizures) that are distinct from a patient’s usual seizure pattern in patients with epilepsy 12 years of age and older.[L44773] **Intravenous** For the intravenous injection formulation, midazolam is indicated as an agent for sedation/anxiolysis/amnesia and prior to or during diagnostic, therapeutic or endoscopic procedures, such as bronchoscopy, gastroscopy, cystoscopy, coronary angiography, cardiac catheterization, oncology procedures, radiologic procedures, suture of lacerations and other procedures either alone or in combination with other CNS depressants.[L12981] The sedative, anxiolytic and amnestic use of midazolam can also be employed pre-operatively.[L12981] It can also be indicated for induction of general anesthesia, before administration of other anesthetic agents or as a component of intravenous supplementation of nitrous oxide and oxygen for a balanced anesthesia.[L12981] A relatively narrower dose range of midazolam and a shorter period of induction can be achieved if midazolam is combined with narcotic premedication.[L12981] Finally, midazolam can be indicated as a continous intravenous infusion for sedation of intubated and mechanically ventilated patients as a component of anesthesia or during treatment in a critical care setting.[L12981] **Intramuscular** For the intramusuclar injection formulation, midazolam is indicated for preoperative sedation/anxiolysis/amnesia or for treatment of status epilepticus in adults.[L12981,L45048] **Oral** Midazolam syrup is indicated for use in pediatric patients for sedation, anxiolysis and amnesia prior to diagnostic, therapeutic or endoscopic procedures or before induction of anesthesia. It is only approved in monitored settings only and not for chronic or home use.[L5092] In Europe, a buccal formulation of midazolam is also approved for the treatment of prolonged, acute, convulsive seizures in infants, toddlers, children and adolescents (from 3 months to < 18 years). For infants between 3-6 months of age treatment should be in a hospital setting where monitoring is possible and resuscitation equipment is available.[L45053]

**General effects** Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepine drugs, include sedative, anxiolytic, amnestic, muscle relaxant, as well as hypnotic activities.[F2434] Benzodiazepines enhance the inhibitory action of the amino acid neurotransmitter gamma-aminobutyric acid (GABA). Receptors for GABA are targeted by many important drugs that affect GABA function and are commonly used in the treatment of anxiety disorder, epilepsy, insomnia, spasticity, and aggressive behavior.[A173854] **Sedation and memory** The onset of sedation after intramuscular administration in adults is 15 minutes, with maximal sedation occurring 30-60 minutes after injection.[FDA label] In one study of adults, when tested the following day, 73% of the patients who were administered midazolam intramuscularly had no recollection of memory cards shown 30 minutes following drug administration; 40% had no recollection of the memory cards shown 60 minutes after drug administration. Onset time of sedative effects in pediatric patients begins within 5 minutes and peaks at 15-30 minutes depending upon the dose administered. In the pediatric population, up to 85% had no memory of pictures shown after receiving intramuscular midazolam compared to 5% of the placebo control group.[F2434] Sedation in both adult and pediatric patients is reached within 3 to 5 minutes post intravenous (IV) injection. The time of onset is affected by the dose administered and the simultaneous administration of narcotic pre-medication. Seventy-one (71%) percent of the adult patients in clinical endoscopy studies had no memory of insertion of the endoscope; 82% of the patients had no memory of withdrawal of the endoscope.[L12981] **Anesthesia induction** When midazolam is administered intravenously (IV) for anesthetic induction, induction of anesthesia occurs in about 1.5 minutes when narcotic pre-medication has been given and in 2 to 2.5 minutes without narcotic pre-medication/ other sedative pre-medication. Impairment in a memory test was observed in 90% of the patients.[L12981]

The actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the central nervous system. Benzodiazepines increase the activity of GABA, thereby producing a sedating effect, relaxing skeletal muscles, and inducing sleep, anesthesia, and amnesia. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening.[F2434] These receptors have been identified in different body tissues including the heart and skeletal muscle, although mainly appear to be present in the central nervous system.[A173842]

**Intramuscular** Following IM administration of a single 10 mg midazolam dose to healthy subjects, midazolam was absorbed with median Tmax (range) of 0.5 (0.25 to 0.5) hours; midazolam's mean (±SD) Cmax and AUC0-∞ were 113.9 (±30.9) ng/mL and 402.7 (±97.0) ng∙h/mL, respectively.[L45048] **Rectal** After rectal administration midazolam is absorbed rapidly. Maximum plasma concentration is reached within 30 minutes. The absolute bioavailability is approximately 50%.[F2977] **Intranasal Administration** Following the nasal administration of a single 5 mg midazolam dose to healthy adults, midazolam was absorbed with a median Tmax (range) of 17.3 (7.8 to 28.2) minutes; midazolam's mean (±SD) Cmax and AUC0-∞ were 54.7 (±30.4) ng/mL and 126.2 (±59) ng∙h/mL, respectively. The mean absolute bioavailability is approximately 44%.[L44773] **Oral** In pediatric patients from 6 months to <16 years old, the mean Tmax values across dose groups (0.25, 0.5, and 1.0 mg/kg) range from 0.17 to 2.65 hours. Midazolam also exhibits linear pharmacokinetics within this dose range (up to a maximum dose of 40 mg). Linearity was also demonstrated across the doses within the age group of 2 years to <12 years having 18 patients at each of the three doses. Due to first-pass metabolism, only 40-50% of the administered oral dose reaches the circulation.[A173842] The absolute bioavailability of midazolam is about 36%, which is not affected by pediatric age or weight. Cmax and AUC0-∞ were also calculated to range from 28 to 201 ng/mL and 67.6 to 821 ng∙h/mL respectively.[L5092] **Buccal** After oromucosal administration midazolam is absorbed rapidly. Maximum plasma concentration is reached within 30 minutes in children. The absolute bioavailability of oromucosal midazolam is about 75% in adults. The bioavailability of oromucosal midazolam has been estimated at 87% in children with severe malaria and convulsions. Cmax and AUC0-∞ were also calculated to range from 87 to 148 ng/mL and 168 to 254 ng∙h/mL respectively.[L45053]

In vitro studies with human liver microsomes indicate that the biotransformation of midazolam is mediated by the cytochrome P450-3A4 (CYP3A4). This enzyme is present in gastrointestinal tract mucosa, as well as in the liver. The 1-hydroxy-midazolam (also termed alpha-hydroxymidazolam) metabolite comprises 60% to 70% of the biotransformation products of midazolam, while 4-hydroxy-midazolam constitutes 5% or less. Small amounts of a dihydroxy derivative have also been detected, but not quantified.[L45048] Midazolam also undergoes N-glucuronidation via UGT1A4 after the process of hepatic oxidation by cytochrome enzymes.[A173842] Studies of the intravenous administration of 1-hydroxy-midazolam in humans suggest that 1-hydroxymidazolam is at least as potent as the parent compound, and may contribute to the net pharmacologic activity of midazolam. In vitro studies have demonstrated that the affinities of 1- and 4-hydroxy-midazolam for the benzodiazepine receptor are approximately 20% and 7%, respectively, relative to midazolam.[L45048]

LD50=215 mg/kg, in rats.[MSDS] **Overdose** Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs. Serious cardiorespiratory adverse reactions have occurred, sometimes ending in death or permanent neurologic effects, after the administration of midazolam.[FDA label] **A note on cardiac and respiratory depression** After administration of midazolam, continuous monitoring of respiratory and cardiac function is recommended until the patient is in stable condition. Serious and life-threatening cardiorespiratory adverse reactions, including hypoventilation, airway obstruction, apnea, and hypotension have been reported with the use of midazolam. Patients should be monitored in a setting with immediate access to resuscitative drugs if they are required. Resuscitation equipment and personnel trained in their use and skilled in airway management should be available when midazolam is administered.[FDA label] The usual recommended intramuscular pre-medicating doses of midazolam do not depress the ventilatory response to carbon dioxide stimulation to a clinically significant extent in adults. Intravenous induction doses of midazolam depress the ventilatory response to carbon dioxide stimulation for at least 15 minutes longer than the duration of ventilatory depression following administration of thiopental in adults. Impairment of ventilatory response to carbon dioxide is more severe in adult patients diagnosed with chronic obstructive pulmonary disease (COPD).[F2434] **A note on dependence** When midazolam is used in long-term sedation in the ICU (intensive care unit) or other settings, physical dependence on midazolam may develop. The risk of dependence increases with dose and duration of treatment; this risk is also greater in patients with a medical history of substance abuse.[L5074] **Special caution should be exercised when administering midazolam in the following populations** High-risk patients include adults over 60 years of age, chronically ill or debilitated patients, which may include patients with chronic respiratory insufficiency, patients with chronic renal failure, impaired hepatic function or with impaired cardiac function, pediatric patients (especially those with cardiovascular instability). These high-risk patients require lower dosages and should be monitored on a continuous basis for early signs of alterations of vital functions, so that appropriate management may be administered.[L5074] **Mutagenesis** Midazolam was negative for genotoxicity during in vitro and in vivo assays.[FDA label] **Impairment of Fertility** When midazolam (0, 1, 4, or 16 mg/kg) was given orally to male and female rats before and during mating and continuing in females throughout gestation and lactation, no adverse effects on male or female fertility were observed. Midazolam plasma exposures (AUC) at the highest dose tested were approximately 6 times that in humans at the recomended human dose.[FDA label]

**Intravenous**: Six single-dose pharmacokinetic studies involving healthy adults yield an elimination half-life of 1.8 to 6.4 hours (mean of approximately 3 hours).[L12981] **Intramuscular** Following IM administration of 10 mg midazolam, the mean (±SD) elimination half-life of midazolam was 4.2 (±1.87) hours.[L45048] **Intranasal** Following the administration of NAYZILAM in clinical trials, median midazolam and 1-hydroxy-midazolam elimination half-lives ranged from 2.1 to 6.2 hours and 2.7 to 7.2 hours, respectively, independent of dose.[L44773] **Oral** The mean elimination half-life of midazolam ranged from 2.2 to 6.8 hours following single oral doses of 0.25, 0.5, and 1.0 mg/kg of midazolam HCl syrup.[L5092] **Buccal* The initial and terminal elimination half-lives are 27 and 204 minutes, respectively.[L45053]

In adults and pediatric patients, midazolam is approximately 97% bound to plasma protein, principally albumin. In healthy volunteers, 1-hydroxy midazolam is bound to the extent of 89%.[L44773]

The _α-hydroxymidazolam_ glucuronide conjugate of midazolam is excreted in the urine. No significant amount of parent drug or metabolites is found in urine before beta-glucuronidase and sulfatase deconjugation, suggesting that the urinary metabolites are excreted mainly as conjugates. The amount of midazolam excreted unchanged in the urine when given intravenously is less than 0.5%. 45% to 57% of the dose was excreted in the urine as 1-hydroxymethyl midazolam conjugate.[L45048] The principal urinary excretion products are glucuronide conjugates of hydroxylated derivatives.[L45048] Plasma clearance of midazolam is higher in patients that remain in the supine position, because of a 40-60 percent increase in hepatic blood flow during supination. Pregnancy may also increase the metabolism of midazolam.[A173842]

Female gender, old age, and obesity may increase the volume of distribution. Midazolam may also cross the placenta and has been detected in human milk and cerebrospinal fluid.[FDA label,F2434] **Intravenous administration** In pediatric patients (6 months to <16 years) receiving 0.15 mg/kg IV midazolam, the mean steady-state volume of distribution ranged from 1.24 to 2.02 L/kg.[L5092] For healthy adult patients, the volume of distribution determined from six single-dose pharmacokinetic studies ranged from 1.0 to 3.1 L/kg.[L12981] **Intramuscular administration** The mean (±SD) apparent volume of distribution (Vz/F) of midazolam following a single IM dose of 10 mg midazolam was 2117 (±845.1) mL/kg in healthy subjects.[L45048] **Intranasal** The estimated total volume of distribution of midazolam is 226.5 L.[L44773] **Buccal** The steady-state volume of distribution following oromucosal administration is estimated to be 5.3 l/kg.[L45053]

**Intramuscular** Following IM administration of 10 mg midazolam, the apparent total body clearance (CL/F) of midazolam was 367.3 (±73.5) mL/hr/kg.[L45048] **Intravenous**: Six single-dose pharmacokinetic studies involving healthy adults yield a total clearance (Cl) of 0.25 to 0.54 L/hr/kg.[L12981] **Intranasal** Midazolam clearance was calculated to be 1.9 mL/min/kg **Oral** Following a group of patients receiving the 0.15 mg/kg IV dose, the mean total clearance ranged from 9.3 to 11.0 mL/min/kg.[L5092] **Buccal* Plasma clearance of midazolam in children following oromucosal administration is 30 ml/kg/min.[L45053]

Organic compounds

Organoheterocyclic compounds

Benzodiazepines

1,4-benzodiazepines

[ "approved", "illicit" ]

[ "N05CD", "N05C", "N05", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.08", "description": "Midazolam hcl 2 mg/ml syrup", "unit": "ml" }, { "cost": "1.13", "description": "Midazolam-nacl 1 mg/ml inj", "unit": "ml" }, { "cost": "1.18", "description": "Midazolam hcl 5 mg/ml vial", "unit": "ml" }, { "cost": "2.31", "description": "Midazolam-nacl 2 mg/ml inj", "unit": "ml" }, { "cost": "3.9", "description": "Midazolam 5 mg/ml", "unit": "ml" }, { "cost": "0.26", "description": "Midazolam hcl 1 mg/ml vial", "unit": "ml" }, { "cost": "0.73", "description": "Midazolam 1 mg/ml isecure syr", "unit": "ml" } ]

[ { "approved": "2016-03-22", "country": "United States", "expires": "2028-01-18", "number": "9289432" }, { "approved": "2017-06-27", "country": "United States", "expires": "2028-01-18", "number": "9687495" }, { "approved": "2012-07-10", "country": "United States", "expires": "2028-01-18", "number": "8217033" }, { "approved": "2014-08-19", "country": "United States", "expires": "2028-01-18", "number": "8809322" }, { "approved": "2021-04-06", "country": "United States", "expires": "2038-06-20", "number": "10966990" } ]

[ "Apo-midazolam Injectable 1 mg/ml", "Apo-midazolam Injectable 5 mg/ml", "Buccolam", "Buccolam", "Buccolam", "Buccolam", "Buccolam", "Buccolam", "Buccolam", "Buccolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam", "Midazolam HCl", "Midazolam HCl", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam hydrochloride", "Midazolam hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam Hydrochloride", "Midazolam in Sodium Chloride", "Midazolam in Sodium Chloride", "Midazolam in Sodium Chloride", "Midazolam in Sodium Chloride", "Midazolam in Sodium Chloride", "Midazolam in Sodium Chloride", "Midazolam In Sodium Chloride", "Midazolam In Sodium Chloride", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection", "Midazolam Injection BP", "Midazolam Injection BP", "Midazolam Injection Sdz", "Midazolam Injection Sdz", "Midazolam Injection USP", "Midazolam Injection USP", "Midazolam Injection USP", "Midazolam Injection USP", "Midazolam Injection USP", "Midazolam Injection USP", "Midazolam Injection, USP", "Midazolam Injection, USP", "MKH Dose Pack", "MKO Melt", "MKO Melt Dose Pack", "N/a", "Nayzilam", "PMS-midazolam", "PMS-midazolam", "Seizalam", "Versed Inj 1mg/ml", "Versed Inj 5mg/ml" ]

[ "Anquil", "Benzosed", "Dalam", "Damizol", "Demizolam", "Doricum", "Dormicum", "Dormid", "Dormipron", "Dormire", "Dormitol", "Dormixal", "Dormonid", "Drimnorth", "Epistatus", "Flormidal", "Fulsed", "Fulsed Injection", "Garen", "Gobbizolam", "Hipnazolam", "Hipnoz", "Hypnofast", "Hypnovel", "Ipnovel", "Nocturna", "Setam", "Talentum", "Terap", "Versed" ]

[ "MKH Dose Pack", "MKO Melt Dose Pack", "MKO Melt" ]

[ "P30536", "P14867", "P47869", "P34903", "P48169", "P31644", "Q16445", "P18505", "P47870", "P28472", "O14764", "P78334", "Q8N1C3", "P18507", "Q99928", "O00591", "Q9UN88", "P14867", "P47869", "P34903", "P31644", "Q8N1C3", "P18507", "Q99928", "P29274" ]

[ "P08684", "P22310", "P20815", "P24462", "P16662", "P06133" ]

[ "P02768", "P02763" ]

[ "P08183", "P43004" ]

DB00685

Trovafloxacin

Trovafloxacin is a broad spectrum antibiotic that has been commonly marketed under the brand name Trovan by Pfizer. It exerts its antibacterial activity by inhibiting the uncoiling of supercoiled DNA in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It was shown to be more effective against Gram-positive bacteria than Gram-negative bacteria when compared to previous fluoroquinolones. Due to its hepatotoxic potential, trovafloxacin was withdrawn from the market.

solid

For treatment of infections caused by susceptible strains of the designated microorganisms in uncomplicated urethral gonorrhea in males and endocervical and rectal gonorrhea in females caused by Neisseria gonorrhoeae as well as non gonoccocal urethritis and cervicitis due to Chlamydia trachomatis.

Trovafloxacin is a broad spectrum antibiotic that inhibits DNA supercoiling in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It is not used widely due to the risk of hepatotoxicity. It tends to have better gram-positive bacterial coverage and less gram-negative coverage than the previous fluoroquinolones. Mechanism of action of fluoroquinolones including trovafloxacin is different from that of penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines. Therefore fluoroquinolones may be active against pathogens that are resistant to these antibiotics. There is no cross-resistance between trovafloxacin and the mentioned classes of antibiotics. The overall results obtained from in vitro synergy studies, testing combinations of trovafloxacin with beta-lactams and aminoglycosides, indicate that synergy is strain specific and not commonly encountered. This agrees with results obtained previously with other fluoroquinolones. Resistance to trovafloxacin in vitro develops slowly via multiple-step mutation in a manner similar to other fluoroquinolones. Resistance to trovafloxacin in vitro occurs at a general frequency of between 1x10-7 to 10-10. Although cross-resistance has been observed between trovafloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to trovafloxacin.

Trovafloxacin is a fluoronaphthyridone related to the fluoroquinolones with in vitro activity against a wide range of gram-negative and gram-positive aerobic and anaerobic microorganisms. The bactericidal action of trovafloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

Well-absorbed from the gastrointestinal tract after oral administration and does not depend on concomitant food intake. The absolute bioavailability is approximately 88%.

Metabolism Trovafloxacin is metabolized by conjugation (the role of cytochrome P450 oxidative metabolism of trovafloxacin is minimal). The major metabolites include the ester glucuronide, which appears in the urine (13% of the administered dose); and the N -acetyl metabolite, which appears in the feces and serum (9% and 2.5% of the administered dose, respectively). Other minor metabolites include diacid, hydroxycarboxylic acid, and sulfamate, which have been identified in both the feces and the urine in small amounts (< 4% of the administered dose).

Symptoms of overdose include convulsions, decreased activity, diarrhea, sleepiness, tremors, and/or vomiting.

Following oral administration, half-life ranged from 9.1 hours to 12.2 hours over the dosage range of 100 to 200 mg tablets. Following intravenous infusion, half-life ranged from 9.4 to 12.7 hours over a dosage range of 100 to 300 mg.

The mean plasma protein bound fraction is approximately 76%, and is concentration-independent.

Approximately 50% of an oral dose is excreted unchanged (43% in the feces and 6% in the urine).

null

Organic compounds

Organoheterocyclic compounds

Diazanaphthalenes

Naphthyridines

[ "approved", "investigational", "withdrawn" ]

[ "J01MA", "J01M", "J01", "J" ]

[ "Enteric bacteria and other eubacteria" ]

[]

[ { "approved": "1992-11-17", "country": "United States", "expires": "2009-11-17", "number": "5164402" }, { "approved": "1996-12-10", "country": "Canada", "expires": "2010-08-14", "number": "2023217" }, { "approved": "2001-02-13", "country": "United States", "expires": "2019-01-20", "number": "6187341" } ]

Trovafloxacin | trovafloxacino | 5.99.1.3 | 5.99.1.3 | 5.99.1.3 | 5.99.1.3 | Topoisomerase IV subunit A | 5.6.2.2 | DNA topoisomerase II, alpha isozyme | TOP2 | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3 | Hydroperoxy icosatetraenoate dehydratase

[ "Trovan", "Trovan", "Trovan", "Trovan", "Trovan Tablets 100mg", "Trovan Tablets 200mg" ]

[ "Trovan" ]

[]

[ "P11388" ]

[ "P05177" ]

[]

DB00686

Pentosan polysulfate

Pentosan polysulfate is a sulfated pentosyl polysaccharide with heparin-like properties.

solid

For the relief of bladder pain or discomfort associated with interstitial cystitis.

Pentosan polysulfate sodium is a low molecular weight heparin-like compound. It has anticoagulant and fibrinolytic effects.

Pentosan polysulfate is a polymer of xylose hydrogen sulfate and contains two sulfate groups per carbohydrate monomer. It binds Fibroblast growth factors (FGFs) as well as other heparin-binding growth factors. It has been shown to interact also with the heparin-binding site of FGFR-1. It inhibits the growth of SW13 adrenocortical cells transfected with FGF-4 and tumorigenicity of MCF-7 breast carcinoma cells transfected with FGF-1 or FGF-4.

Slow

null

4.8 hours

null

Organic compounds

Organic oxygen compounds

Organooxygen compounds

Carbohydrates and carbohydrate conjugates

[ "approved" ]

[ "C05BA", "C05B", "C05", "C", "G04BX", "G04B", "G04", "G" ]

[ "Humans and other mammals" ]

[ { "cost": "3.32", "description": "Elmiron 100 mg capsule", "unit": "capsule" } ]

[ { "approved": "1993-01-19", "country": "United States", "expires": "2010-01-19", "number": "5180715" } ]

[ "Elmiron", "Elmiron", "Elmiron", "Elmiron", "Elmiron", "Elmiron", "Elmiron", "Elmiron", "Elmiron" ]

[ "Comfora", "Fibrase", "Fibrezym", "Hemoclar", "Hémoclar", "Tavan-SP", "Thrombocid" ]

[]

[ "P09038", "P05230", "P08620" ]

[]

DB00687

Fludrocortisone

Fludrocortisone is a synthetic mineralocorticoid used in conjunction with [hydrocortisone] to replace missing endogenous corticosteroids in patients with adrenal insufficiency.[A187169,A187187] It is functionally similar to [aldosterone], the body's primary endogenous mineralocorticoid, and is structurally analogous to [cortisol], differing only by a fluorine atom at the 9-position of the steroid structure - this fluorination is thought to be crucial to fludrocortisone's significant mineralocorticoid potency.[A5423]

solid

Fludrocortisone is indicated as partial replacement therapy for primary or secondary adrenocortical insufficiency in Addison's disease. It is also indicated for the treatment of salt-losing androgenital syndrome.[L8971]

Fludrocortisone is a synthetic mineralocorticoid used to replace endogenous [aldosterone] in conditions resulting in missing or inadequate endogenous synthesis.[L8971,L8974] It acts on the kidneys to increase both sodium reabsorption and potassium excretion.[T28,A187187] As its effects are exerted at the transcriptional level, a single dose of fludrocortisone may work over the course of 1-2 days[L8974] despite a relatively short plasma half-life.[A187159,A187169,A187181] Like other systemic corticosteroids, fludrocortisone may mask signs of infection by depressing the normal immune response - infections occurring during fludrocortisone therapy should be promptly treated with appropriate antimicrobial therapy.[L8971]

The main endogenous mineralocorticoid, aldosterone, is produced in the zona glomerulosa of the adrenal cortex - it acts on mineralocorticoid receptors in the kidneys to increase sodium reabsorption and potassium excretion, which in turn helps to regulate plasma electrolyte composition and blood pressure.[T28] In conditions of adrenal insufficiency, such as Addison’s disease, aldosterone is not produced (or is produced in insufficient quantities) and must be replaced by exogenous mineralocorticoids such as fludrocortisone.[A187187] Fludrocortisone binding to mineralocorticoid receptors causes alterations to DNA transcription and translation of proteins that result in an increased density of sodium channels on the apical side of renal tubule cells and an increased density of Na+-K+-ATPase on the basolateral side.[T28] These increases in receptor density result in increased plasma sodium concentrations, and thus increased blood pressure, as well as a decreased plasma potassium concentration. Fludrocortisone may also exert a direct effect on plasma sodium levels via action at the Na+-H+ exchanger found in the apical membrane of renal tubule cells.[T28] Fludrocortisone also acts on glucocorticoid receptors, albeit with a much lower affinity - the glucocorticoid potency of fludrocortisone is approximately 5-10 times that of endogenous cortisol, whereas its mineralocorticoid potency is 200-400 times greater.[A5423]

Absorption of fludrocortisone following oral administration is rapid and complete.[L8977,A187169,A187181,A187159] Pharmacokinetic studies have estimated the Cmax to be 0.0012 to 0.20 μg/L with a Tmax between 0.5 and 2 hours.[A187169,A187181] The AUC0-∞ of fludrocortisone after oral administration has been variably estimated to be between 1.22 to 3.07 μg.h/L.[A187169,A187181]

There exists is a paucity of information regarding the specific metabolic pathway _in vivo_ of fludrocortisone. The 9α-fluorination of fludrocortisone appears to greatly simplify its metabolism as compared to other corticosteroids[A187162] - while oxidation via 11-hydroxysteroid dehydrogenases has been observed,[A187144] this reaction is greatly impaired as the fluorine moiety appears to confer "protection" from 11β-oxidation by these enzymes. The reduction in 11β-oxidation is thought to be one of the reasons behind fludrocortisone's profound mineralocorticoid potency.[A5423] An _in vitro_ study generated only two metabolites following incubation in human liver microsomes and cytosol, namely 20β-dihydrofluorocortisol and 6β-hydroxyfluorocortisol, and did not explore in detail the potential enzymes responsible for this reaction.[A187162] Given that fludrocortisone is a corticosteroid, a class of medications known to be metabolized by the CYP3A family,[A14813] and is not recommended to be given with strong inhibitors/inducers of CYP3A,[L8974] it is likely that the CYP3A family of enzymes contributes in some way to its metabolism (though this information does not appear to have been specifically elucidated for fludrocortisone).

The oral LD50 of fludrocortisone in rats is >1g/kg.[L9055] Acute overdosage of fludrocortisone is likely to result in symptoms consistent with its adverse effect profile. Patients receiving a single large dose should be treated with plenty of water by mouth and should undergo monitoring of serum electrolytes, particularly potassium and sodium, and be treated appropriately for any developing imbalances.[L8974,L8977]

The plasma half-life of fludrocortisone has been variably reported to be between 1-3.5 hours,[A187159,A187169,A187181] though prescribing information gives an approximate half-life of 18-36 hours.[L8974]

Fludrocortisone is 70-80% protein bound in plasma, mostly to albumin and corticosteroid-binding globulin.[L8977,A187181]

Approximately 80% of an administered dose of fludrocortisone shows up in the urine, with the other 20% likely eliminated via fecal or biliary route.[L8977,A187181]

The apparent volume of distribution of fludrocortisone is 80-85 L.[A187169,A187159] Distribution into CSF appears minimal - the observed ratio of CSF drug concentration versus plasma drug concentration is 1:6.[L8977]

Population pharmacokinetics have estimated the plasma clearance of fludrocortisone to be 40.8 L/h.[A187169]

Organic compounds

Lipids and lipid-like molecules

Steroids and steroid derivatives

Hydroxysteroids

[ "approved", "investigational" ]

[ "S02CA", "S02C", "S02", "S", "S01CA", "S01C", "S01", "S", "H02AA", "H02A", "H02", "H", "S03CA", "S03C", "S03", "S" ]

[ "Humans and other mammals" ]

[ { "cost": "1.49", "description": "Florinef acetate 0.1 mg tablet", "unit": "tablet" }, { "cost": "73.14", "description": "Fludrocortisone acetate powder", "unit": "g" }, { "cost": "0.25", "description": "Florinef 0.1 mg Tablet", "unit": "tablet" }, { "cost": "0.75", "description": "Fludrocortisone 0.1 mg tablet", "unit": "tablet" }, { "cost": "0.81", "description": "Fludrocortisone Acetate 0.1 mg tablet", "unit": "tablet" } ]

[]

[ "Florinef", "Florinef Acetate", "Florinef Acetate", "Florinef Acetate 0.1mg", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone Acetate", "Fludrocortisone acetate", "Fludrocortisone acetate", "Jamp Fludrocortisone", "Truemed Group LLC" ]

[ "Adixone", "Astonin", "Cortineff", "Florinef Acetaat", "Florinefe", "Fludrocortison", "Lonikan" ]

[]

[ "P10275", "P08235", "P04150" ]

[ "P08684", "P80365", "P28845" ]

[ "P02768", "P08185" ]

[]

DB00688

Mycophenolate mofetil

Mycophenolate mofetil, also known as MMF or CellCept, is a prodrug of mycophenolic acid, and classified as a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH).[A180805] This drug is an immunosuppressant combined with drugs such as [Cyclosporine] and corticosteroids to prevent organ rejection after hepatic, renal, and cardiac transplants.[L7363] It is marketed by Roche Pharmaceuticals and was granted FDA approval for the prophylaxis of transplant rejection in 1995.[A180826] In addition to the above uses, mycophenolate mofetil has also been studied for the treatment of nephritis and other complications of autoimmune diseases. Unlike another immunosuppressant class, the calcineurin inhibitors, MMF generally does not cause nephrotoxicity or fibrosis.[A180799,A180805] Previously, mycophenolic acid (MPA) was administered to individuals with autoimmune diseases beginning in the 1970s, but was discontinued due to gastrointestinal effects and concerns over carcinogenicity.[A180826] The new semi-synthetic 2-morpholinoethyl ester of MPA was synthesized to avoid the gastrointestinal effects associated with the administration of MPA. It demonstrates an increased bioavailability, a higher efficacy, and reduced gastrointestinal effects when compared to MPA.[A180826]

solid

Mycophenolate mofetil is indicated in combination with other immunosuppressants to prevent the rejection of kidney, heart, or liver transplants in adult and pediatric patients ≥3 months old.[L42020] Mycophenolate mofetil may also be used off-label as a second-line treatment for autoimmune hepatitis that has not responded adequately to first-line therapy.[A180814] Other off-label uses of this drug include lupus-associated nephritis and dermatitis in children.[A180817]

Mycophenolate mofetil is a prodrug of mycophenolic acid (MPA). The active form of mycophenolate, MPA, prevents the proliferation of immune cells and the formation of antibodies that cause transplant rejection.[A180805] The above effects lead to higher rates of successful transplantation, avoiding the devastating effects of graft rejection.

The active metabolite of mycophenolate, mycophenolic acid, prevents T-cell and B-cell proliferation and the production of cytotoxic T-cells and antibodies. Lymphocyte and monocyte adhesion to endothelial cells of blood vessels that normally part of inflammation is prevented via the glycosylation of cell adhesion molecules by MPA.[A180892] MPA inhibits de novo purine biosynthesis (that promotes immune cell proliferation) by inhibiting inosine 5’-monophosphate dehydrogenase enzyme (IMPDH), with a preferential inhibition of IMPDH II.[A180826] IMPDH normally transforms inosine monophosphate (IMP) to xanthine monophosphate (XMP), a metabolite contributing to the production of guanosine triphosphate (GTP).[A180799,A180805,A180817] GTP is an important molecule for the synthesis of ribonucleic acid (RNA), deoxyribonucleic acid (DNA), and protein. As a result of the above cascade of effects, mycophenolate mofetil reduces de-novo production of guanosine nucleotides, interfering with the synthesis of DNA, RNA, and protein required for immune cell production.[A180826] Further contributing to the above anti-inflammatory effects, MMF depletes tetrahydrobiopterin, causing the decreased function of inducible nitric oxide synthase enzyme, in turn decreasing the production of peroxynitrite, a molecule that promotes inflammation.[A180907]

Mycophenolate mofetil is rapidly absorbed in the small intestine.[L7363,A180898] The maximum concentration of its active metabolite, MPA, is attained 60 to 90 minutes following an oral dose.[A180826] The average bioavailability of orally administered mycophenolate mofetil in a pharmacokinetic study of 12 healthy patients was 94%. In healthy volunteers, the Cmax of mycophenolate mofetil was 24.5 (±9.5)μg/mL.[L7363] In renal transplant patients 5 days post-transplant, Cmax was 12.0 (±3.82) μg/mL, increasing to 24.1 (±12.1)μg/mL 3 months after transplantation. AUC values were 63.9 (±16.2) μg•h/mL in healthy volunteers after one dose, and 40.8 (±11.4) μg•h/mL, and 65.3 (±35.4)μg•h/mL 5 days and 3 months after a renal transplant, respectively.[L7363] The absorption of mycophenolate mofetil is not affected by food.[A180826]

After both oral and intravenous administration mycophenolate mofetil is entirely metabolized by liver carboxylesterases 1 and 2 to mycophenolic acid (MPA), the active parent drug. It is then metabolized by the enzyme glucuronyl transferase, producing the inactive phenolic glucuronide of MPA (MPAG).[L7363] The glucuronide metabolite is important, as it is then converted to MPA through enterohepatic recirculation. Mycophenolate mofetil that escapes metabolism in the intestine enters the liver via the portal vein and is transformed to pharmacologically active MPA in the liver cells.[A180898]N-(2-carboxymethyl)-morpholine, N-(2-hydroxyethyl)-morpholine, and the N-oxide portion of N-(2-hydroxyethyl)-morpholine are additional metabolites of MMF occurring in the intestine as a result of liver carboxylesterase 2 activity.[A180898,L7363] UGT1A9 and UGT2B7 in the liver are the major enzymes contributing to the metabolism of MPA in addition to other UGT enzymes, which also play a role in MPA metabolism. The four major metabolites of MPA are 7-O-MPA-β-glucuronide (MPAG, inactive), MPA acyl-glucuronide (AcMPAG), produced by uridine 5ʹ-diphosphate glucuronosyltransferases (UGT) activities, 7-O-MPA glucoside produced via UGT, and small amounts 6-O-des-methyl-MPA (DM-MPA) via CYP3A4/5 and CYP2C8 enzymes.[A180826]

LD50 The LD50 of oral mycophenolate mofetil in rats is 250 mg/kg and >4000 mg/kg in mice.[L7366] **Overdose information** Possible signs and symptoms of acute overdose may consist of hematological abnormalities including leukopenia and neutropenia, and gastrointestinal symptoms.[A180826,A180829,A180832]

The average apparent half-life of mycophenolate mofetil is 17.9 (±6.5) hours after oral administration and 16.6 (±5.8) hours after intravenous administration.[L7363]

The protein binding of mycophenolic acid, the metabolite of mycophenolate mofetil, is 97%[L7363] and it is mainly bound to albumin.[A180826] MPAG, the inactive metabolite, is 82% bound to plasma albumin at normal therapeutic concentrations. At elevated MPAG concentrations due to various reasons, including renal impairment, the binding of MPA may be decreased due to competition for binding.[L7363]

A small amount of drug is excreted as MPA in the urine (less than 1%). When mycophenolate mofetil was given orally in a pharmacokinetic study, it was found to be 93% excreted in urine and 6% excreted in feces. Approximately 87% of the entire administered dose is found to be excreted in the urine as MPAG, an inactive metabolite.[A180826,L7363]

The volume of distribution of mycophenolate mofetil is 3.6 (±1.5) to 4.0 (±1.2) L/kg.[L7363]

Plasma clearance of mycophenolate mofetil is 193 mL/min after an oral dose and 177 (±31) mL/min after an intravenous dose.[L7363]

Organic compounds

Organoheterocyclic compounds

Isocoumarans

Isobenzofuranones

[ "approved", "investigational" ]

[]

[ "Humans and other mammals" ]

[ { "cost": "4.13", "description": "Mycophenolate Mofetil 250 mg capsule", "unit": "capsule" }, { "cost": "5.21", "description": "CellCept 250 mg capsule", "unit": "capsule" }, { "cost": "7.93", "description": "Mycophenolate 500 mg tablet", "unit": "tablet" }, { "cost": "8.25", "description": "Mycophenolate Mofetil 500 mg tablet", "unit": "tablet" }, { "cost": "10.43", "description": "Cellcept 500 mg tablet", "unit": "tablet" }, { "cost": "65.03", "description": "Cellcept 500 mg vial", "unit": "vial" }, { "cost": "875.84", "description": "CellCept 200 mg/ml Suspension 175ml Bottle", "unit": "bottle" } ]

[ { "approved": "1997-11-18", "country": "United States", "expires": "2014-11-18", "number": "5688529" }, { "approved": "1996-08-06", "country": "United States", "expires": "2013-09-15", "number": "5543408" }, { "approved": "2007-07-17", "country": "Canada", "expires": "2014-09-27", "number": "2172506" }, { "approved": "1994-11-29", "country": "Canada", "expires": "2011-11-29", "number": "1333285" }, { "approved": "2019-08-16", "country": "United States", "expires": "2039-08-16", "number": "11931455" }, { "approved": "2019-08-16", "country": "United States", "expires": "2039-08-16", "number": "12097285" }, { "approved": "2019-08-16", "country": "United States", "expires": "2039-08-16", "number": "12097284" } ]

[ "Accel-mycophenolate Mofetil Capsules", "Accel-mycophenolate Mofetil Tablets", "Ach-mycophenolate", "Ach-mycophenolate", "Ach-mycophenolate", "Ag-mycophenolate", "Apo-mycophenolate", "Apo-mycophenolate", "Apo-mycophenolate Mofetil", "Apo-mycophenolate Mofetil", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "CellCept", "Cellcept", "Cellcept", "Cellcept", "Cellcept", "Cellcept", "Cellcept", "Cellcept", "Cellcept I.V.", "Co Mycophenolate", "Jamp-mycophenolate", "Jamp-mycophenolate Capsules", "Mar-mycophenolate Mofetil", "Myclausen", "Myclausen", "Myclausen", "Myclausen", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil", "Mycophenolate Mofetil for Injection USP", "Mycophenolate Mofetil for Injection, USP", "Mycophenolate Mofetil Teva", "Mycophenolate Mofetil Teva", "Mycophenolate Mofetil Teva", "Mycophenolate Mofetil Teva", "Mycophenolate Mofetil Teva", "Mycophenolate Mofetil Teva", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myfenax", "Myhibbin", "Mylan-mycophenolate", "Mylan-mycophenolate", "Sandoz Mycophenolate Mofetil", "Sandoz Mycophenolate Mofetil", "Taro-mycophenolate", "Teva-mycophenolate", "Teva-mycophenolate", "Van-mycophenolate", "Van-mycophenolate" ]

[ "CellCept Oral Suspension", "CellCept Intravenous" ]

[]

[ "P43116", "P20839", "P12268", "Q03393" ]

[ "Q9HAW7", "P19224", "O60656", "P16662", "Q9HAW9", "Q9HAW8", "P23141", "P08684", "P20815", "P10632", "Q6IPK9", "P22309" ]

[]

[ "Q9Y6L6", "Q9NPD5", "Q9UNQ0", "P08183", "Q92887" ]

DB01024

Mycophenolic acid

Mycophenolic acid is a potent immunosuppressant agent that inhibits _de novo_ purine biosynthesis.[L42165] It was derived from _Penicillium stoloniferum_, and has also shown antibacterial, antifungal and antiviral properties.[A249170]. Mycophenolic acid is used in immunosuppressive regimens as part of a triple therapy that includes a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone.[A249175] This regimen can be used in place of the older anti-proliferative [azathioprine] due to its stronger immunosuppressive potency.[A249180] However, mycophenolic acid treatment is more expensive and requires therapeutic drug monitoring to optimize efficacy and minimize toxicity.[A249180,A249185] Mycophenolic acid is available as enteric-coated tablets of delayed-release, in an effort to improve upper gastrointestinal adverse events by delaying mycophenolic acid release until it reaches the small intestine.[A249190] [Mycophenolate mofetil], a prodrug of mycophenolic acid, is also prescribed to transplant recipients to prevent organ rejection.[L42020]

solid

Mycophenolic acid is an antimetabolite immunosuppressant indicated for prophylaxis of organ rejection in adult patients receiving kidney transplants and in pediatric patients at least 5 years of age and older who are at least 6 months post kidney transplant. Mycophenolic acid is used in combination with cyclosporine and corticosteroids.[L42165]

Mycophenolic acid is a potent inhibitor of inosine monophosphate dehydrogenase (IMPDH) that blocks _de novo_ biosynthesis of purine nucleotides. This affects lymphocytes primarily and leads to the suppression of DNA synthesis in T- and B-cells.[A249175,L42165] Mycophenolic acid arrests the T-lymphocyte cell cycle at the G1/S interface and inhibits the proliferation of lymphocytes.[A249175] Also, it has been suggested that mycophenolic acid suppresses cytokine production by limiting the number of cytokine-producing cells.[A249175] The enteric-coating of mycophenolic acid tablets prevents the development of upper gastrointestinal adverse events by delaying drug release until it reaches the small intestine.[A249190] Patients treated with mycophenolic acid have a higher risk of developing new or reactivated viral infections, serious infections, blood dyscrasias (including pure red cell aplasia), serious gastrointestinal tract complications, acute inflammatory syndrome associated with mycophenolate products, lymphoma, and other malignancies.[L42165] The use of mycophenolic acid is also associated with an increased risk of first-trimester pregnancy loss and congenital malformations. Mycophenolic acid should be avoided in patients with rare hereditary deficiency of hypoxanthine-guanine phosphoribosyl-transferase (HGPRT). Patients treated with mycophenolic acid should not receive live attenuated vaccines or donate blood or semen.[L42165]

Mycophenolic acid is a selective noncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), that blocks the conversion of inosine-5-phosphate and xanthine-5-phosphate to guanosine-5-phosphate.[A249170,L42165] By inhibiting IMPDH, mycophenolic acid interferes with the _de novo_ pathway of guanosine nucleotide synthesis without incorporation into DNA. While other cell types are able to use salvage pathways, T- and B-lymphocyte proliferation is a mechanism heavily dependent on the _de novo_ synthesis of purines. Therefore, mycophenolic acid has potent cytostatic effects on T- and B- and lymphocytes.[A249170,L42165] Mycophenolic acid also suppresses antibody formation by B-lymphocytes and prevents the glycosylation of lymphocyte and monocyte glycoproteins involved in intercellular adhesion to endothelial cells.[L42020]

Between 360 mg and 2,160 mg, mycophenolic acid follows a linear and dose-proportional pharmacokinetic profile. The enteric-coating of mycophenolic acid tablets prevents release under acidic conditions (stomach, pH < 5). However, enteric-coated mycophenolic acid tablets are highly soluble in neutral pH conditions such as those in the intestine.[L42165] In renal transplant patients, the median delay (Tlag) in the rise of mycophenolic acid concentration ranged between 0.25 and 1.25 hours, and the Tmax ranged between 1.5 and 2.75 hours. Adult renal transplant patients on cyclosporine given mycophenolic acid had a Tmax of 2 h, a Cmax of 26.1 μg/mL, and an AUC0-12 of 66.5 μg⋅h/mL. Stable pediatric (5-16 years old) renal transplant patients had a Cmax and AUC 33% and 18% higher than the ones detected in adults.[L42165] In stable renal transplant patients treated with cyclosporine, the gastrointestinal absorption and absolute bioavailability of delayed-release tablets of mycophenolic acid were 93% and 72%, respectively.[L42165] Following the administration of a high-fat meal (55 g fat, 1000 calories), the AUC of mycophenolic acid (enteric-coated tablets, 720 mg) was comparable to the one detected during fasting. However, a high-fat meal can lead to a 33% decrease of the Cmax, a 3.5-hour delay in the Tlag (range of -6 to 18 hours), and a 5.0-hour delay in the Tmax (range of -9 to 20 hours). To avoid variability in the absorption of mycophenolic acid, this drug should be taken on an empty stomach.[L42165]

Mycophenolic acid is mainly metabolized by glucuronyl transferase to form glucuronidated metabolites. Mycophenolic acid glucuronide (MPAG), the major metabolite of mycophenolic acid, does not display pharmacological activity. However, the acyl glucuronide minor metabolite has a pharmacological activity similar to mycophenolic acid. The AUC ratio of mycophenolic acid:MPAG:acyl glucuronide is approximately 1:24:0.28 at a steady state.[L42165]

There are anecdotal reports of deliberate or accidental overdoses with mycophenolic acid; however, not all patients have experienced related adverse reactions. In those cases where adverse reactions have been reported, reactions fall within the safety profile of its class of drugs. A mycophenolic acid overdose could lead to the oversuppression of the immune system and increase the susceptibility to infection.[L42165] It may be appropriate to interrupt or discontinue mycophenolic acid if blood dyscrasias occur. Some of the signs and symptoms associated with mycophenolic acid overdose are hematological abnormalities, such as leukopenia and neutropenia, and gastrointestinal symptoms, such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia.[L42165] Carcinogenicity studies of 104 weeks done in rats and mice, suggest that mycophenolate sodium does not induce the formation of tumours. Rats were given up to 9 mg/kg of mycophenolate sodium, which corresponded to 0.6-1.2 times the systemic exposure observed in renal transplant patients, while mice were given 180 mg/kg, an equivalent of 0.6 times the mycophenolate sodium therapeutic dose.[L42165] The genotoxicity of mycophenolate sodium was confirmed by the mouse lymphoma/thymidine kinase assay, the micronucleus test in V79 Chinese hamster cells, and the _in vivo_ mouse micronucleus assay. Mycophenolate mofetil, a prodrug of mycophenolic acid, had a similar genotoxic profile. At daily oral doses as high as 18 mg/kg and 20 mg/kg, mycophenolate sodium had no effect on male and female rat fertility, respectively.[L42165] The oral LD50 of mycophenolic acid is 352 mg/kg in rats and 1000 mg/kg in mice.[L42180]

The mean elimination half-life of mycophenolic acid ranges between 8 and 16 hours, while the mean elimination half-life of mycophenolic acid glucuronide, its major metabolite, ranges between 13 and 17 hours.[L42165]

Mycophenolic acid is highly protein-bound, and more than 98% of it is bound to albumin.[L42165]

In stable renal transplant patients, approximately 60% of mycophenolic acid is eliminated in the urine as mycophenolic acid glucuronide (MPAG), while 3% is eliminated unchanged.[L42165] MPAG is also secreted in the bile and is available for deconjugation by gut flora. The mycophenolic acid that results from MPAG deconjugation may be reabsorbed and produce a second peak 6-8 hours after administration.[L42165]

At steady state, the volume of distribution of mycophenolic acid is 54 L. At the elimination phase, the volume of distribution of mycophenolic acid is 112 L.[L42165]

The mean clearance of mycophenolic acid is 140 mL/min. The mean renal clearance of its metabolite, mycophenolic acid glucuronide, is 15.5 mL/min.[L42165]

Organic compounds

Organoheterocyclic compounds

Isocoumarans

Isobenzofuranones

[ "approved", "investigational" ]

[ "L04AA", "L04A", "L04", "L" ]

[ "Humans and other mammals" ]

[ { "cost": "3.85", "description": "Myfortic 180 mg tablet", "unit": "tablet" }, { "cost": "7.69", "description": "Myfortic 360 mg tablet", "unit": "tablet" }, { "cost": "8.0", "description": "Myfortic 360 mg Enteric Coated Tabs", "unit": "tab" } ]

[ { "approved": "2006-10-03", "country": "Canada", "expires": "2017-04-10", "number": "2250906" }, { "approved": "2000-02-15", "country": "United States", "expires": "2017-04-10", "number": "6025391" }, { "approved": "2001-01-09", "country": "United States", "expires": "2017-04-10", "number": "6172107" }, { "approved": "2001-10-23", "country": "United States", "expires": "2018-02-27", "number": "6306900" } ]

[ "Apo-mycophenolic Acid", "Apo-mycophenolic Acid", "Jamp Mycophenolic Acid", "Jamp Mycophenolic Acid", "Mar-mycophenolic Acid", "Mar-mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Mycophenolic Acid", "Myfortic", "Myfortic", "Myfortic", "Myfortic", "Myfortic", "Sandoz Mycophenolic Acid", "Sandoz Mycophenolic Acid" ]

[ "Melbex", "Myfortic" ]

[]

[ "P12268", "P20839" ]

[ "P16662", "Q9HAW9", "O60656", "P22309", "Q9HAW7", "Q9HAW8", "P19224", "P08684", "P20815", "P10632" ]

[ "P02768" ]

[]

DB00689

Cephaloglycin

A cephalorsporin antibiotic that is no longer commonly used.

solid

For treatment of severe infections caused by susceptible bacteria.

Cephaloglycin is an antibiotic related to cephalosporin but no longer in common use. It is an orally absorbed derivative of cephalosporin C.

The bactericidal activity of cephaloglycin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).

Well absorbed following oral administration.

null

Adverse effects following overdosage include nausea, vomiting, epigastric distress, diarrhea, and convulsions.

null

Organic compounds

Organoheterocyclic compounds

Lactams

Beta lactams

[ "approved" ]

[]

[ "Enteric bacteria and other eubacteria" ]

[]

[]

[ "Kafocin" ]

[]

[ "O76082" ]

DB00690

Flurazepam

A benzodiazepine derivative used mainly as a hypnotic.

solid

For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits

Flurazepam, a benzodiazepine derivative, is a hypnotic agent which does not appear to decrease dream time as measured by rapid eye movements (REM). Furthermore, it decreases sleep latency and number of awakenings for a consequent increase in total sleep time.

Flurazepam binds to an allosteric site on GABA-A receptors. Binding potentiates the action of GABA on GABA-A receptors by opening the chloride channel within the receptor, causing chloride influx and hyperpolarization.

Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form

Coma, confusion, low blood pressure, sleepiness

The mean apparent half-life of flurazepam is 2.3 hours. The half life of elimination of N1-des-alkyl- flurazepam ranged from 47 to 100 hours

83%

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Less than 1% of the dose is excreted in the urine as N1-desalkyl-flurazepam.

null

Organic compounds

Organoheterocyclic compounds

Benzodiazepines

1,4-benzodiazepines

[ "approved", "illicit", "investigational" ]

[ "N05CD", "N05C", "N05", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.79", "description": "Dalmane 15 mg capsule", "unit": "capsule" }, { "cost": "2.01", "description": "Dalmane 30 mg capsule", "unit": "capsule" }, { "cost": "0.08", "description": "Apo-Flurazepam 15 mg Capsule", "unit": "capsule" }, { "cost": "0.1", "description": "Apo-Flurazepam 30 mg Capsule", "unit": "capsule" }, { "cost": "0.28", "description": "Flurazepam 15 mg capsule", "unit": "capsule" }, { "cost": "0.34", "description": "Flurazepam 30 mg capsule", "unit": "capsule" }, { "cost": "0.4", "description": "Flurazepam HCl 30 mg capsule", "unit": "capsule" }, { "cost": "0.43", "description": "Flurazepam HCl 15 mg capsule", "unit": "capsule" } ]

[]

[ "Bio-flurazepam", "Bio-flurazepam", "Dalmane", "Dalmane", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam", "Flurazepam 15", "Flurazepam 15mg Capsule", "Flurazepam 30", "Flurazepam 30mg Capsule", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Flurazepam Hydrochloride", "Novo-flupam Cap 15mg", "Novo-flupam Cap 30mg", "PMS-flurazepam Cap 15mg", "PMS-flurazepam Cap 30mg", "Riva-flurazepam 15mg Capsules", "Riva-flurazepam 30mg Capsules", "Som-pam", "Som-pam", "Somnol 15mg", "Somnol 30mg" ]

[ "Dalmadorm", "Dalmadorm medium", "Felison", "Flunox", "Insumin", "Sompan", "Valdorm" ]

[]

[ "P30536", "P14867", "P47869", "P34903", "P48169", "P31644", "Q16445", "P18505", "P47870", "P28472", "O14764", "P78334", "Q8N1C3", "P18507", "Q99928", "O00591", "Q9UN88", "P14867", "P47869", "P34903", "P31644", "Q8N1C3", "P18507", "Q99928" ]

[ "P08684", "P05181", "P11509" ]

[]

[ "P08183", "O15244" ]

DB00691

Moexipril

Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.

solid

For the treatment of hypertension.

Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.

Moexipril is a prodrug for moexiprilat, which inhibits ACE in humans and animals. The mechanism through which moexiprilat lowers blood pressure is believed to be primarily inhibition of ACE activity. ACE is a peptidyl dipeptidase that catalyzes the conversion of the inactive decapeptide angiotensin I to the vasoconstrictor substance angiotensin II. Angiotensin II is a potent peripheral vasoconstrictor that also stimulates aldosterone secretion by the adrenal cortex and provides negative feedback on renin secretion. ACE is identical to kininase II, an enzyme that degrades bradykinin, an endothelium-dependent vasodilator. Moexiprilat is about 1000 times as potent as moexipril in inhibiting ACE and kininase II. Inhibition of ACE results in decreased angiotensin II formation, leading to decreased vasoconstriction, increased plasma renin activity, and decreased aldosterone secretion. The latter results in diuresis and natriuresis and a small increase in serum potassium concentration (mean increases of about 0.25 mEq/L were seen when moexipril was used alone). Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of moexipril remains to be elucidated. Although the principal mechanism of moexipril in blood pressure reduction is believed to be through the renin-angiotensin-aldosterone system, ACE inhibitors have some effect on blood pressure even in apparent low-renin hypertension.

Moexipril is incompletely absorbed, with bioavailability as moexiprilat of about 13% compared to intravenous (I.V.) moexipril (both measuring the metabolite moexiprilat), and is markedly affected by food, which reduces Cmax and AUC by about 70% and 40%, respectively, after the ingestion of a low-fat breakfast or by 80% and 50%, respectively, after the ingestion of a high-fat breakfast.

Rapidly converted to moexiprilat, the active metabolite. Conversion to the active metabolite is thought to require carboxyesterases and is likely to occur in organs or tissues, other than the gastrointestinal tract, in which carboxyesterases occur. The liver is thought to be one site of conversion, but not the primary site.

Human overdoses of moexipril have not been reported. In case reports of overdoses with other ACE inhibitors, hypotension has been the principal adverse effect noted. Single oral doses of 2 g/kg moexipril were associated with significant lethality in mice. Rats, however, tolerated single oral doses of up to 3 g/kg. Common adverse effects include cough, dizziness, diarrhea, flu syndrome, fatigue, pharyngitis, flushing, rash, and myalgia

Moexipril elimination half-life is approximately 1 hour. Moexiprilat elimination half-life is 2 to 9 hours.

Moexiprilat is approxomately 50% protein bound.

Moexiprilat undergoes renal elimination.

* 183 L

* 441 mL/min

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved" ]

[ "C09AA", "C09A", "C09", "C", "C09BA", "C09B", "C09", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "1.41", "description": "Moexipril hcl 7.5 mg tablet", "unit": "tablet" }, { "cost": "1.48", "description": "Moexipril hcl 15 mg tablet", "unit": "tablet" }, { "cost": "2.13", "description": "Univasc 7.5 mg tablet", "unit": "tablet" }, { "cost": "2.44", "description": "Univasc 15 mg tablet", "unit": "tablet" } ]

[]

[ "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril hydrochloride", "Moexipril hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril hydrochloride/hydrochlorothiazide", "Moexipril hydrochloride/hydrochlorothiazide", "Moexipril hydrochloride/hydrochlorothiazide", "Uniretic", "Uniretic", "Uniretic", "Uniretic", "Univasc", "Univasc", "Univasc", "Univasc" ]

[]

[ "Uniretic", "Moexipril hydrochloride/hydrochlorothiazide", "Moexipril hydrochloride/hydrochlorothiazide", "Moexipril hydrochloride/hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Uniretic", "Uniretic", "Uniretic", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide", "Moexipril Hydrochloride and Hydrochlorothiazide" ]

[ "P12821" ]

[]

[ "P46059", "Q16348" ]

DB00692

Phentolamine

Phentolamine is a reversible, non-selective alpha-adrenergic blocker that induces vasodilation. While initially introduced to the market for the treatment of hypertension, this clinical use was halted due to cardiovascular and gastrointestinal adverse effects with the prolonged use of large oral doses of phentolamine.[A261781, A261786] It has several therapeutic uses, including the treatment of hypertensive episodes, prevention of norepinephrine-induced extravasation, diagnosis of pheochromocytoma, reversal of soft-tissue anesthesia, and treatment of pharmacologically-induced mydriasis.[L48420, L48415, L48390] Phentolamine is administered intravenously, intramuscularly, submucosally, and topically.

solid

When used intravenously or intramuscularly, phentolamine is used to prevent or control hypertensive episodes that may occur in a patient with pheochromocytoma due to stress or manipulation during preoperative preparation and surgical excision. It is also used to prevent or treat dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine. It may be used to diagnose pheochromocytoma by the phentolamine-blocking test.[L48420] Submucosal injection of phentolamine is indicated for the reversal of soft-tissue anesthesia (e.g. anesthesia of the lip and tongue) and the associated functional deficits resulting from an intraoral submucosal injection of a local anesthetic containing a vasoconstrictor in patients three years old and older.[L48415] Phentolamine ophthalmic solution is used to treat pharmacologically-induced mydriasis produced by adrenergic agonists (e.g., phenylephrine) or parasympatholytic (e.g., tropicamide) agents.[L48390]

Phentolamine produces an alpha-adrenergic block of a relatively short duration.[L48415] Phentolamine induces vasodilatation of vascular smooth muscle and pupils.[L48415, L48390] When used in an ophthalmic solution, the onset of pupil dilation generally occurred in 30 minutes, with the maximal effect seen in 60 to 90 minutes. Pupil dilation lasted for at least 24 hours.[L48390] Phentolamine also has direct but less marked positive inotropic and chronotropic effects on cardiac muscle and vasodilator effects on vascular smooth muscle;[L48420] however, phentolamine is not believed to affect contractile or adenyl cyclase function.[A261781] Large doses can lead to a mild sympatholytic action.[A261781] Some evidence suggests that phentolamine also stimulates beta-adrenergic receptors, thereby causing peripheral vasodilation.[A261781] Phentolamine was shown to stimulate insulin secretion, possibly related to its blocking actions on ATP-sensitive K+ channels.[A261781, A261761]

Phentolamine is a reversible, competitive antagonist at alpha-1 and alpha-2 adrenergic receptors.[A261766, L48390] It causes vasodilation of vascular smooth muscles.[L48415] Pupil dilation is primarily controlled by the radial iris dilator muscles surrounding the pupil, which are activated by the alpha-1 adrenergic receptors. Phentolamine reversibly binds to these receptors and reduces pupil diameter. By blocking alpha-1 adrenergic receptors, phentolamine can also be used to reverse mydriasis induced by muscarinic antagonists.[L48390]

The peak concentrations of phentolamine are achieved within 10 to 20 minutes following submucosal administration. The Cmax was higher in children with greater weights.[L48415] Following topical ocular administration of phentolamine ophthalmic solution 0.75%, the peak concentration levels were achieved between 15 minutes and one hour after dosing with the median value of 0.45 ng/mL.[L48390]

null

The oral LD50 of phentolamine mesylate, a salt of phentolamine, was 1250 mg/kg in rats and 1000-1100 mg/kg in mice.[L48410, L48420] No deaths due to acute poisoning with phentolamine have been reported. Overdosage with phentolamine is characterized chiefly by cardiovascular disturbances, such as arrhythmias, tachycardia, hypotension, and possibly shock. Other possible signs and symptoms include excitation, headache, sweating, pupillary contraction, visual disturbances, nausea, vomiting, diarrhea, and hypoglycemia. There is no specific antidote: Treatment consists of appropriate monitoring and supportive care. A plasma expander and norepinephrine may be administered to manage decreased blood pressure.[L48415, L48420]

Phentolamine has a half-life of 19 minutes following intravenous administration.[L48420] The terminal elimination half-life of phentolamine was approximately two to three hours following submucosal administration.[L48415]

null

Approximately 13% of a single intravenous dose appears in the urine as unchanged drug.[L48420]

While there is limited information on phentolamine distribution, the drug is reported to cross the blood-brain barrier.[A261766]

null

Organic compounds

Organic nitrogen compounds

Organonitrogen compounds

Amines

[ "approved" ]

[ "V03AB", "V03A", "V03", "V", "C04AB", "C04A", "C04", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "84.0", "description": "Phentolamine 5 mg vial", "unit": "vial" } ]

[ { "approved": "2004-07-20", "country": "United States", "expires": "2021-05-11", "number": "6764678" }, { "approved": "2009-08-04", "country": "United States", "expires": "2023-10-17", "number": "7569230" }, { "approved": "2005-03-29", "country": "United States", "expires": "2021-05-11", "number": "6872390" }, { "approved": "2007-06-12", "country": "United States", "expires": "2023-06-20", "number": "7229630" }, { "approved": "2009-08-18", "country": "United States", "expires": "2025-04-21", "number": "7575757" }, { "approved": "2014-01-31", "country": "United States", "expires": "2034-01-31", "number": "11844858" }, { "approved": "2014-01-31", "country": "United States", "expires": "2034-01-31", "number": "9795560" }, { "approved": "2014-01-31", "country": "United States", "expires": "2034-01-31", "number": "11090261" }, { "approved": "2014-01-31", "country": "United States", "expires": "2034-01-31", "number": "10278918" }, { "approved": "2014-01-31", "country": "United States", "expires": "2034-01-31", "number": "10772829" }, { "approved": "2019-10-25", "country": "United States", "expires": "2039-10-25", "number": "11400077" } ]

[ "OraVerse", "Oraverse", "Oraverse", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate", "Phentolamine Mesylate Injection Sandoz Standard", "Regitine", "Rogitine", "Rogitine 5mg/vial", "Ryzumvi" ]

[ "Regitin", "Regitina", "Vigamed" ]

[]

[ "P35348", "P35368", "P25100", "P14416", "P08913", "P18089", "P18825", "Q14654" ]

[]

DB00693

Fluorescein

A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium, such as the aqueous humor, and is used therapeutically as a diagnostic aid in corneal injuries and corneal trauma. It has been approved by FDA for use in externally applied drugs and cosmetics. (From Merck Index, 12th ed; American Medical Association Drug Evaluations; 1995, p2275)

solid

For diagnostic imaging. Primarily indicated in diagnostic fluorescein angiography or angioscopy of the fundus and of the iris vasculature.

null

Fluorescein sodium is used extensively as a diagnostic tool in the field of ophthalmology. Fluorescein is a fluorescent compound or fluorophore having a maximum absorbance of 494 m and an emission maximum of 521 nm. The yellowish-green fluorescence of the compound can be used to demarcate the vascular area under observation, distinguishing it from adjacent areas. It is applied topically in the form of a drop or it can be injected intravenously to produce a fluorescein angiogram. Topical fluorescein is a useful tool in the diagnosis of corneal abrasions, corneal ulcers, herpetic corneal infections, and dry eye. Fluorescein angiography is used to diagnose and categorize macular degeneration, diabetic retinopathy, inflammatory intraocular conditions, and intraocular tumors.

Rapidly distributed

null

85%

Fluorescein and its metabolites are mainly eliminated via renal excretion.

* 0.5 L/kg

* renal cl=1.75 mL/min/kg [After IV administration] * hepatic cl=1.50 mL/min/kg [After IV administration]

Organic compounds

Organoheterocyclic compounds

Benzopyrans

1-benzopyrans

[ "approved" ]

[ "S01JA", "S01J", "S01", "S", "S01JA", "S01J", "S01", "S" ]

[ "Humans and other mammals" ]

[ { "cost": "1.56", "description": "Ak-fluor 10% vial", "unit": "ml" }, { "cost": "1.72", "description": "Fluorescein lite 10% vial", "unit": "ml" }, { "cost": "2.4", "description": "Fluorescein sodium 25% vial", "unit": "ml" }, { "cost": "3.9", "description": "Ak-fluor 25% vial", "unit": "ml" }, { "cost": "4.29", "description": "Fluorescein lite 25% vial", "unit": "ml" }, { "cost": "5.99", "description": "Fluorescite 10% ampul", "unit": "ml" }, { "cost": "12.0", "description": "Fluorescein 2% droptainer", "unit": "ml" }, { "cost": "0.08", "description": "Fluorescein powder", "unit": "g" }, { "cost": "0.96", "description": "Fluorescein sodium 10% vial", "unit": "ml" } ]

[ { "approved": "2019-05-21", "country": "United States", "expires": "2037-11-15", "number": "10293047" }, { "approved": "2020-04-28", "country": "United States", "expires": "2037-11-15", "number": "10632197" }, { "approved": "2020-11-24", "country": "United States", "expires": "2037-11-15", "number": "10842872" } ]

[ "Ak-fluor", "Ak-fluor", "Ak-fluor", "Ak-fluor", "Altafluor", "Altafluor", "Angiofluor", "Angiofluor Lite", "Angiofluor Lite", "Bio Glo", "BioGlo", "BioGlo", "C20H10Na2O5 Fluorescein Sodium Ophthalmic Strips", "Diofluor Strips", "Dry Eye Test", "Flucaine", "Fluorescein", "Fluorescein", "Fluorescein", "Fluorescein", "Fluorescein", "Fluorescein Lite", "Fluorescein Lite", "Fluorescein Sodium", "Fluorescein Sodium", "Fluorescein Sodium & Benoxinate Hydrochloride Ophthalmic Solution, USP", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluorescein Sodium and Proparacaine Hydrochloride", "Fluorescite", "Fluorescite", "Fluorescite Inj 25%", "Fluorets - Stp Oph 1mg", "Fluorets (fluorescein Ophthalmic Strips)", "Fluorox", "Fluress", "Fluress", "Fluress Liq Oph", "Flurox", "Flurox", "Ful-glo", "Ful-glo", "Ful-glo", "Funduscein 25% Inj", "GloStrips", "GloStrips", "Minims Fluorescein Sodium", "Minims Lidocaine and Fluorescein", "Odan-fluoracaine", "Odan-fluorescein", "Odan-fluorescein", "Odan-fluorets" ]

[]

[ "Flurox", "Flurox", "Fluress", "Altafluor", "Fluorescein Sodium and Proparacaine Hydrochloride", "Fluorescein Sodium and Benoxinate Hydrochloride", "Flucaine", "Altafluor", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluorescein Sodium and Benoxinate Hydrochloride", "Fluress Liq Oph", "Minims Lidocaine and Fluorescein", "Fluorox", "Odan-fluoracaine", "Fluorescein Sodium & Benoxinate Hydrochloride Ophthalmic Solution, USP", "Fluress", "Fluorescein Sodium and Benoxinate Hydrochloride" ]

[ "Q8TCC7", "P06310" ]

[]

[ "Q4U2R8", "O95342", "P33527" ]

DB00694

Daunorubicin

A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of leukemia and other neoplasms.

solid

For remission induction in acute nonlymphocytic leukemia (myelogenous, monocytic, erythroid) of adults and for remission induction in acute lymphocytic leukemia of children and adults. Daunorubicin is indicated in combination with [cytarabine] for the treatment of newly-diagnosed therapy-related acute myeloid leukemia (t-AML) or AML with myelodysplasia-related changes (AML-MRC) in adults and pediatric patients 1 year and older.[L32843]

Daunorubicin is an anthracycline antibiotic and antineoplastic agent.[L32843] It acts by inhibiting cellular reproduction through interference with DNA replication although it may contribute to the induction of cell death by increasing oxidative stress through the generation of reactive oxygen species and free radicals. As an antineoplastic agent, daunorubicin carries significant toxicities including cytopenias, hepatotoxicity, and extravasation reactions. Like other anthracyclines, daunorubicin also exhibits cardiotoxicity in proportion with the cumulative dose received over time.

Daunorubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Daunorubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.

Daunorubicin was found to have a tmax of 2 h and a cmax of 24.8 μg/mL after a 90 min infusion of the liposomal formulation at a dose of 44 mg/m2. [A237405]

null

Daunorubicin has been determined to have a terminal half-life of 18.5 h (+/- 4.9).[A237395] Daunorubicinol, the primary active metabolite has been determined to have a terminal half-life of 26.7 h (+/- 12.8). The mean half-life of elimination of liposomal daunorubicin has been reported to be 22.1 h in pharmacokinetic studies and 31.5 h in official FDA labeling.[A237405 ,L32843]

null

Daunorubicin is eliminated hepatically. 40% of daunorubicin is excreted in the bile while 25% is excreted in an active form (daunorubicin or daunorubicinol) in the urine.[L35460] In the liposomal formulation, only 9% of active molecules are excreted in the urine.[L32843]

Daunorubicin has a steady-state volume of distribution of 1.91 L/m2 reported with the liposomal formulation.[A237395] The average volume of distribution reported for the liposomal formulation is 6.6 L. [L32843]

Daunorubicin has a clearance of 68.4 mL/h/m2 determined using the liposomal formulation.[A237405]

Organic compounds

Phenylpropanoids and polyketides

Anthracyclines

null

[ "approved" ]

[ "L01DB", "L01D", "L01", "L", "L01XY", "L01X", "L01", "L" ]

[ "Humans and other mammals" ]

[ { "cost": "13.06", "description": "Daunoxome 2 mg/ml vial", "unit": "ml" }, { "cost": "42.45", "description": "Daunorubicin 50 mg/10 ml vial", "unit": "ml" }, { "cost": "50.4", "description": "Cerubidine 20 mg vial", "unit": "vial" }, { "cost": "163.01", "description": "Daunorubicin 20 mg/4 ml vial", "unit": "ml" } ]

[ { "approved": "2010-12-14", "country": "United States", "expires": "2027-01-23", "number": "7850990" }, { "approved": "2011-09-20", "country": "United States", "expires": "2027-09-14", "number": "8022279" }, { "approved": "2013-04-30", "country": "United States", "expires": "2025-04-22", "number": "8431806" }, { "approved": "2012-01-10", "country": "United States", "expires": "2029-04-01", "number": "8092828" }, { "approved": "2013-08-27", "country": "United States", "expires": "2026-06-07", "number": "8518437" }, { "approved": "2016-03-01", "country": "United States", "expires": "2027-01-23", "number": "9271931" }, { "approved": "2018-07-24", "country": "United States", "expires": "2034-09-29", "number": "10028912" }, { "approved": "2019-01-01", "country": "United States", "expires": "2032-10-15", "number": "10166184" }, { "approved": "2020-11-17", "country": "United States", "expires": "2032-10-15", "number": "10835492" } ]

[ "Cerubidine", "Cerubidine", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride", "Daunorubicin Hydrochloride for Injection", "Daunorubicin Hydrochloride Injection", "Daunorubicin Injectable Solution", "Daunorubicin Injectable Solution", "DaunoXome", "DaunoXome", "Daunoxome Liposomal - IV 2mg/ml, 50mg/vial", "Vyxeos", "Vyxeos", "Vyxeos Liposomal", "Vyxeos Liposomal", "Vyxeos Liposomal" ]

[ "Cerubidin", "Cérubidine", "Daunoblastin", "Daunoblastina", "Daunorrubicina", "Maxidauno" ]

[ "Vyxeos", "Vyxeos", "Vyxeos Liposomal", "Vyxeos Liposomal", "Vyxeos Liposomal" ]

[ "P11388", "Q02880" ]

[ "P08684", "P20815", "P16435", "Q16678", "P15121", "P16152", "O75828" ]

[]

[ "P08183", "P33527", "Q5T3U5", "Q9UNQ0", "O95255" ]

DB00695

Furosemide

Furosemide is a potent loop diuretic that acts on the kidneys to ultimately increase water loss from the body. It is an anthranilic acid derivative.[L7958] Furosemide is used for edema secondary to various clinical conditions, such as congestive heart failure exacerbation, liver failure, renal failure, and high blood pressure.[L7961] It mainly works by inhibiting electrolyte reabsorption from the kidneys and enhancing the excretion of water from the body. Furosemide has a fast onset and short duration of action and has been used safely and effectively in both pediatric and adult patients.[A182495] The use of furosemide is particularly beneficial in clinical settings that require a drug with a higher diuretic potential. In addition to oral formulations, the solution for intravenous and intramuscular administration is also available, which is typically limited to patients who are unable to take oral medication or for patients in emergency clinical situations.[L7958]

solid

Furosemide is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome, in adults and pediatric patients.[L7958] Oral furosemide is indicated alone for the management of mild to moderate hypertension or severe hypertension in combination with other antihypertensive medications.[L9659] Intravenous furosemide is indicated as adjunctive therapy in acute pulmonary edema when a rapid onset of diuresis is desired.[L7958] Subcutaneous furosemide is indicated for the treatment of congestion due to fluid overload in adults with NYHA Class II/III chronic heart failure. This drug formulation is not indicated for emergency situations or in patients with acute pulmonary edema.[L43408]

Furosemide manages hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome. Furosemide is a potent loop diuretic that works to increase the excretion of Na+ and water by the kidneys by inhibiting their reabsorption from the proximal and distal tubules, as well as the loop of Henle.[L7958] It works directly acts on the cells of the nephron and indirectly modifies the content of the renal filtrate.[T28] Ultimately, furosemide increases the urine output by the kidney. Protein-bound furosemide is delivered to its site of action in the kidneys and secreted via active secretion by nonspecific organic transporters expressed at the luminal site of action.[A31831,L7958] Following oral administration, the onset of the diuretic effect is about 1 and 1.5 hours [L7958], and the peak effect is reached within the first 2 hours.[L7961] The duration of effect following oral administration is about 4-6 hours but may last up to 8 hours.[L9659] Following intravenous administration, the onset of effect is within 5 minutes, and the peak effect is reached within 30 minutes. The duration of action following intravenous administration is approximately 2 hours. Following intramuscular administration, the onset of action is somewhat delayed.[L7958]

Furosemide promotes diuresis by blocking tubular reabsorption of sodium and chloride in the proximal and distal tubules, as well as in the thick ascending loop of Henle. This diuretic effect is achieved through the competitive inhibition of sodium-potassium-chloride cotransporters (NKCC2) expressed along these tubules in the nephron, preventing the transport of sodium ions from the lumenal side into the basolateral side for reabsorption. This inhibition results in increased excretion of water along with sodium, chloride, magnesium, calcium, hydrogen, and potassium ions.[L7961] As with other loop diuretics, furosemide decreases the excretion of uric acid.[T28] Furosemide exerts direct vasodilatory effects, which results in its therapeutic effectiveness in the treatment of acute pulmonary edema. Vasodilation leads to reduced responsiveness to vasoconstrictors, such as angiotensin II and noradrenaline, and decreased production of endogenous natriuretic hormones with vasoconstricting properties. It also leads to increased production of prostaglandins with vasodilating properties. Furosemide may also open potassium channels in resistance arteries.[T28] The main mechanism of action of furosemide is independent of its inhibitory effect on carbonic anhydrase and aldosterone.[L7958]

Following oral administration, furosemide is absorbed from the gastrointestinal tract.[L9659] It displays variable bioavailability from oral dosage forms, ranging from 10 to 90%.[A31831] The oral bioavailability of furosemide from oral tablets or oral solution is about 64% and 60%, respectively, of that from an intravenous injection of the drug.[L7958]

The metabolism of furosemide occurs mainly in the kidneys and the liver, to a smaller extent. The kidneys are responsible for about 85% of total furosemide total clearance, where about 40% involves biotransformation.[A183563] Two major metabolites of furosemide are furosemide glucuronide, which is pharmacologically active, and saluamine (CSA) or 4-chloro-5-sulfamoylanthranilic acid.[A183281]

Clinical consequences from overdose depend on the extent of electrolyte and fluid loss and include dehydration, blood volume reduction, hypotension, electrolyte imbalance, hypokalemia, hypochloremic alkalosis,[L7958] hemoconcentration, cardiac arrhythmias (including A-V block and ventricular fibrillation).[L9659] Symptoms of overdose include acute renal failure, thrombosis, delirious states, flaccid paralysis, apathy and confusion. In cirrhotic patients, overdosage might precipitate hepatic coma.[L9659] In rats, the oral LD50, intraperitoneal LD50, and subcutaneous LD50 is 2600 mg/kg, 800 mg/kg, and 4600 mg/kg, respectively. The Lowest published toxic dose (TDLo) in a female is 6250 μg/kg.[L7964]

The half-life from the dose of 40 mg furosemide was 4 hours following oral administration and 4.5 hours following intravenous administration. The terminal half-life of furosemide is approximately 2 hours following parenteral administration.[L7958] The terminal half-life may be increased up to 24 hours in patients with severe renal failure.[L9659]

Plasma concentrations ranging from 1 to 400 mcg/mL are about 91-99% bound in healthy individuals. The unbound fraction is about 2.3-4.1% at therapeutic concentrations.[L9659] Furosemide mainly binds to serum albumin.[L7958]

The kidneys are responsible for 85% of total furosemide total clearance, where about 43% of the drug undergoes renal excretion.[A183563] Significantly more furosemide is excreted in urine following the I.V. injection than after the tablet or oral solution. Approximately 50% of the furosemide load is excreted unchanged in urine, and the rest is metabolized into glucuronide in the kidney.[A31831]

The volume of distribution following intravenous administration of 40 mg furosemide were 0.181 L/kg in healthy subjects and 0.140 L/kg in patients with heart failure.[A188838]

Following intravenous administration of 400 mg furosemide, the plasma clearance was 1.23 mL/kg/min in patients with heart failure and 2.34 mL/kg/min in healthy subjects, respectively.[A188838]

Organic compounds

Benzenoids

Benzene and substituted derivatives

Benzenesulfonamides

[ "approved", "vet_approved" ]

[ "C03EB", "C03E", "C03", "C", "C03CA", "C03C", "C03", "C", "G01AE", "G01A", "G01", "G", "C03CB", "C03C", "C03", "C" ]

[ "Humans and other mammals" ]

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[ { "approved": "2014-04-03", "country": "United States", "expires": "2034-04-03", "number": "11433044" }, { "approved": "2018-02-06", "country": "United States", "expires": "2034-04-03", "number": "9884039" }, { "approved": "2019-04-30", "country": "United States", "expires": "2034-04-03", "number": "10272064" } ]

[ "14-Panel Toxicology Medicated Collection System", "Active-Medicated specimen collection kit", "Apo-furosemide", "Apo-furosemide", "Apo-furosemide", "Ava-furosemide", "Ava-furosemide", "Ava-furosemide", "Bio-furosemide", "Bio-furosemide", "Diascreen 12-Panel Medicated Collection System", "Diuscreen Medicated Collection Kit", "Diuscreen Multi-Drug Medicated Test Kit", "Dom-furosemide", "Dom-furosemide", "Fuosemide", "Furoscix", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", 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"Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide", "Furosemide 20mg Tablets", "Furosemide 40mg Tab", "Furosemide 40mg Tablets", "Furosemide Inj 10mg/ml", "Furosemide Inj USP", "Furosemide Injection", "Furosemide Injection Sdz", "Furosemide Injection USP", "Furosemide Injection USP", "Furosemide Injection USP", "Furosemide Injection USP", "Furosemide Injection USP", "Furosemide Injection USP", "Furosemide Injection, USP", "Furosemide Injection, USP", "Furosemide Injection, USP", "Furosemide Special", "Furosemide Special Injection", "Furosemide Special Injection", "Furosemide Special Sdz", "Furoside Tab 20mg", "Furoside Tab 40mg", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix", "Lasix - Tab 80mg", "Lasix 40mg Tablets", "Lasix 80mg Tablets", "Lasix Injection 10mg/ml", "Lasix Injection 10mg/ml - Im IV", "Lasix Oral Soln 10mg/ml", "Lasix Oral Solution", "Lasix Oral Solution 10mg/ml", "Lasix Parenteral Inj", "Lasix Parenteral Injection 10mg/ml", "Lasix Special", "Lasix Special Inj 10mg/ml", "Lasix Special Tab 500mg", "Lasix Special Tablets 500mg", "Lasix Tab 20mg", "Lasix Tab 20mg", "Lasix Tab 80mg", "Lasix Tabs 40 mg", "Mint-furosemide", "Mint-furosemide", "Mint-furosemide", "Ntp-furosemide", "Ntp-furosemide", "Ntp-furosemide", "Nu-furosemide Tablets", "Nu-furosemide Tablets", "Nu-furosemide Tablets", "PMS-furosemide", "PMS-furosemide", "Pro-furosemide", "Pro-furosemide", "Pro-furosemide", "Rx-Specimen Collection Kit", "Specimen Collection Kit", "Teva-furosemide", "Teva-furosemide", "Teva-furosemide", "Toxicology Medicated Collection System", "TOXYCOLOGY Medicated Collection System", "UDSx Medicated System", "UDSxMP Medicated System", "Urinx Medicated Specimen Collection", "Uritol Tab" ]

[ "Diurapid", "Diurin", "Diurmessel", "Eutensin", "Frumex", "Frusenex", "Frusol", "Furo-Puren", "Seguril" ]

[ "Active-Medicated specimen collection kit", "Urinx Medicated Specimen Collection", "Diuscreen Medicated Collection Kit", "Diuscreen Multi-Drug Medicated Test Kit", "Rx-Specimen Collection Kit", "Diascreen 12-Panel Medicated Collection System", "TOXYCOLOGY Medicated Collection System", "Specimen Collection Kit", "Toxicology Medicated Collection System", "14-Panel Toxicology Medicated Collection System", "UDSxMP Medicated System", "UDSx Medicated System" ]

[ "Q13621", "P00918", "Q9HC97" ]

[ "P52209", "P22309" ]

[ "P02768", "P05543" ]

[ "Q4U2R8", "O76082", "Q8TCC7", "Q92887", "Q92959", "Q9NSA0" ]

DB00696

Ergotamine

A vasoconstrictor found in ergot of Central Europe. It is an alpha-1 selective adrenergic agonist and is commonly used in the treatment of migraine disorders.

solid

For use as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia".

Ergotamine is a vasoconstrictor and alpha adrenoreceptor antagonist. The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow.

Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

The bioavailability of sublingually administered ergotamine has not been determined.

Hepatic. Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile.

Signs of overexposure include irritation, nausea, vomiting, headache, diarrhea, thirst, coldness of skin, pruritus, weak pulse, numbness, tingling of extremities, and confusion.

2 hours

null

Organic compounds

Alkaloids and derivatives

Ergoline and derivatives

Lysergic acids and derivatives

[ "approved" ]

[ "N02CA", "N02C", "N02", "N", "N02CA", "N02C", "N02", "N", "N02CA", "N02C", "N02", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.14", "description": "Ergotamine-caffeine tablet", "unit": "tablet" }, { "cost": "1.89", "description": "Cafergot tablet", "unit": "tablet" }, { "cost": "7.39", "description": "Migergot suppository", "unit": "suppository" }, { "cost": "8.97", "description": "Ergomar 2 mg tablet sl", "unit": "tablet" }, { "cost": "224.35", "description": "Ergotamine tartrate powder", "unit": "powder" } ]

[]

[ "Bellergal Spacetabs", "Bellergal Tab", "Cafergot", "Cafergot", "Cafergot", "Cafergot Pb Sup", "Cafergot Pb Tab", "Cafergot Sup", "Cafergot Tab", "Ercaf", "Ergodryl Cap", "Ergomar", "Ergomar Slt 2mg", "Ergomar Sublingual", "Ergotamine", "Ergotamine Tartrate and Caffeine", "Ergotamine Tartrate and Caffeine", "Ergotamine Tartrate and Caffeine", "Ergotamine Tartrate, Caffeine", "Gravergol Capsules", "Medihaler-Ergotamine", "Megral Tabs", "Migergot", "Migergot", "Migergot", "Truemed Group LLC", "Wigraine Suppositories", "Wigraine Tab" ]

[ "Anervan", "Antimigraine", "Enxak", "Ergam", "Ergo-Kranit", "Gynaemine", "Gynergen", "Wigrettes" ]

[ "Ercaf", "Cafergot", "Ergotamine", "Migergot", "Ergotamine Tartrate and Caffeine", "Migergot", "Migergot", "Cafergot", "Ergotamine Tartrate and Caffeine", "Ergotamine Tartrate and Caffeine", "Cafergot", "Megral Tabs", "Cafergot Sup", "Cafergot Tab", "Wigraine Tab", "Wigraine Suppositories", "Ergodryl Cap", "Bellergal Spacetabs", "Gravergol Capsules", "Bellergal Tab", "Cafergot Pb Tab", "Cafergot Pb Sup", "Ergotamine Tartrate, Caffeine", "Truemed Group LLC" ]

[ "P28221", "P28222", "P28223", "P35348", "P35368", "P25100", "P14416", "P08913", "P21728", "P21918", "P08908", "P30939", "P28335", "P41595", "P18825" ]

[ "P08684" ]

[]

[ "P08183" ]

DB00697

Tizanidine

Tizanidine is a fast-acting drug used for the management of muscle spasm, which may result from the effects of multiple sclerosis, stroke, an acquired brain injury, or a spinal cord injury [T574]. It may also be caused by musculoskeletal injury [A177583]. Regardless of the cause, muscle spasticity can be an extremely painful and debilitating condition. Initially approved by the FDA in 1996, tizanidine is an Alpha-2 adrenergic receptor agonist reducing spasticity by the presynaptic inhibition of excitatory neurotransmitters that cause firing of neurons promoting muscle spasm [FDA label].

solid

Tizanidine is indicated for the relief of muscle spasticity, which can interfere with daily activities. The general recommendation is to reserve tizanidine use for periods of time when there is a particular need for relief, as it has a short duration of action [FDA label, F4471].

**A note on spasticity** Spasticity is an increase in muscle accompanied by uncontrolled, repetitive contractions of skeletal muscles which are involuntary. The patient suffering from muscle spasticity may have reduced mobility and high levels of pain, contributing to poor quality of life and problems performing activities of personal hygiene and care [A177640]. **General effects** Tizanidine is a rapidly acting drug used for the relief of muscle spasticity when it is required for performing specific activities. It acts as an agonist at Alpha-2 adrenergic receptor sites and relieves symptoms of muscle spasticity, allowing the continuation of normal daily activities. In animal models, tizanidine has not been shown to exert direct effects on skeletal muscle fibers or the neuromuscular junction, and has shown no significant effect on monosynaptic spinal reflexes (consisting of the communication between only 1 sensory neuron and 1 motor neuron) [L6064]. The frequency of muscle spasm and clonus are shown to be decreased by tizanidine [T574]. Tizanidine shows a stronger action on polysynaptic reflexes, which involve several interneurons (relay neurons) communicating with motor neurons stimulating muscle movement [L6064]. **Effects on blood pressure and heart rate** This drug decreases heart rate and blood pressure in humans [A177559, A177589]. Despite this, rebound hypertension and tachycardia along with increased spasticity can occur when tizanidine is abruptly discontinued [A177643].

Tizanidine reduces spasticity by causing presynaptic inhibition of motor neurons via agonist actions at Alpha-2 adrenergic receptor sites. This drug is centrally acting and leads to a reduction in the release of excitatory amino acids like glutamate and aspartate, which cause neuronal firing that leads to muscle spasm. The above reduction and excitatory neurotransmitter release results in presynaptic inhibition of motor neurons. The strongest effect of tizanidine has been shown to occur on spinal polysynaptic pathways. The anti-nociceptive and anticonvulsant activities of tizanidine may also be attributed to agonist action on Alpha-2 receptors. Tizanidine also binds with weaker affinity to the Alpha-1 receptors, explaining its slight and temporary effect on the cardiovascular system [T574].

This drug undergoes significant first-pass metabolism. After the administration of an oral dose, tizanidine is mostly absorbed. The absolute oral bioavailability of tizanidine is measured to be about 40% [FDA label]. **Effect of food on absorption** Food has been shown to increase absorption for both the tablets and capsules. The increase in absorption with the tablet (about 30%) was noticeably higher than the capsule (~10%). When the capsule and tablet were administered with food, the amount absorbed from the capsule was about 80% of the amount absorbed from the tablet [FDA label]. It is therefore advisable to take this drug with food for increased absorption, especially in tablet form.

About 95% of the ingested dose of tizanidine is metabolized. The main enzyme involved in the hepatic metabolism of tizanidine is CYP1A2 [FDA label].

**LD50 information** Oral LD50 (rat): 414 mg/kg; Subcutaneous LD50 (rat): 282 mg/kg; Oral LD50 (mouse): 235 mg/kg [MSDS] **Use in pregnancy** Animal studies have determined that this drug causes fetal harm [FDA label]. Studies have not been performed in humans, and it is advisable to ensure that tizanidine use in pregnant women should be reserved for cases in which possible benefit clearly outweighs the possible risk to mother and unborn child [F4471]. **Use in breastfeeding** In studies of rat models, this tizanidine was found excreted in the breastmilk with a milk-to-blood ratio of 1.8:1 [FDA label]. In young nursing rats, abnormal results were obtained in tests indicative of central nervous system function. Various developmental changes that may have been attributable to the drug were observed. It is unknown whether tizanidine is excreted in human milk. It is a lipid-soluble drug, however, and likely to be excreted into breast milk [F4471]. **Carcinogenesis and mutagenesis** No signs of carcinogenicity were observed in two dietary studies performed in rodent models. Tizanidine was given to mice for 78 weeks at doses reaching a maximum 16 mg/kg (equivalent to twice the maximum recommended human dose). In addition, the drug was given to rats for 104 weeks at doses reaching 9 mg/kg (equivalent to 2.5 times the maximum recommended human dose). There was a lack of a statistically significant increase in the occurrence of tumors in either study group [F4471]. Tizanidine was not found to be mutagenic or clastogenic in several laboratory essays, including the bacterial Ames test, the mammalian gene mutation test, in addition to the chromosomal aberration test in Chinese hamster cells and several other assays [F4471].

Approximately 2.5 hours [FDA label].

About 30% bound to plasma proteins [FDA label].

This drug is mainly eliminated by the kidney [FDA label].

Extensively distributed throughout the body. The average steady-state volume of distribution is 2.4 L/kg [FDA label].

**A note on renal impairment** Tizanidine clearance is found to be decreased by more than 50% in elderly patients with renal insufficiency (creatinine clearance < 25 mL/min) compared to healthy elderly subjects; this would be expected to lead to a longer duration of clinical effect. This drug should be used with caution in patients with renal impairment [FDA label].

Organic compounds

Organoheterocyclic compounds

Benzothiadiazoles

null

[ "approved", "investigational" ]

[ "M03BX", "M03B", "M03", "M" ]

[ "Humans and other mammals" ]

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[ { "approved": "2002-09-24", "country": "United States", "expires": "2021-11-28", "number": "6455557" } ]

[ "Apo-tizanidine", "Apo-tizanidine", "Comfort Pac with Tizanidine", "Mint-tizanidine", "Mylan-tizanidine", "Pal-tizanidine", "Tizandine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine", "Tizanidine HCl", "Tizanidine HCl", "Tizanidine HCL", "Tizanidine HCL", "Tizanidine HCL", "Tizanidine HCL", "Tizanidine HCl", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine hydrochloride", "Tizanidine hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine hydrochloride", "Tizanidine hydrochloride", "Tizanidine hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine hydrochloride", "Tizanidine hydrochloride", "Tizanidine hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidine Hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Tizanidne hydrochloride", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex", "Zanaflex" ]

[ "Cimbrar", "Musant", "Myores", "Navizan", "Relaxkov", "Sirdalid", "Sirdalud", "Sirdalud MR", "Sizolan", "Spaslax", "Telzanine", "Ternelin", "Tizadin", "Tizaflex", "Tizalud", "Tizan", "Zanpeak", "Zitanid" ]

[]

[ "P35348", "P35368", "P25100", "P08913", "P18089", "P18825", "Q9Y2I1" ]

[ "P05177" ]

[]

DB00698

Nitrofurantoin

Nitrofurantoin is a nitrofuran antibiotic used to treat uncomplicated urinary tract infections.[L6856,L6859,L6862] Nitrofurantoin is converted by bacterial nitroreductases to electrophilic intermediates which inhibit the citric acid cycle as well as synthesis of DNA, RNA, and protein.[A179824] This drug is more resistant to the development of bacterial resistance because it acts on many targets at once.[A179824] Nitrofurantoin is a second line treatment to [trimethoprim]/[sulfamethoxazole].[A179830] Nitrofurantoin was granted FDA approval on 6 February 1953.[L6895]

solid

Nitrofurantoin is indicated to treat acute uncomplicated urinary tract infections.[L6856,L6859,L6862]

Nitrofurantoin interferes with vital processes in bacteria, which leads to their death.[A179824] Nitrofurantoin rapidly reaches therapeutic concentrations in the urine and is also cleared rapidly.[A179830]

Nitrofurantoin is converted by bacterial nitroreductases to electrophilic intermediates which inhibit the citric acid cycle as well as synthesis of DNA, RNA, and protein.[A179824]

Nitrofurantoin reaches a Cmax of 0.875-0.963mg/L with an AUC of 2.21-2.42mg\*h/L.[A179830] It is 38.8-44.3% bioavailable.[A179830] Taking nitrofurantoin with food increases the absorption and duration of therapeutic concentrations in the urine.[A179854]

0.8-1.8% of a dose is metabolized to aminofurantoin, and ≤0.9% of a dose is metabolized to other metabolites.[A179860]

Symptoms of overdose include vomiting.[L6856,L6859,L6862] In case of overdose, induce vomiting if it has not already occurred and increase fluid intake to promote urination.[L6856,L6859,L6862] In extreme cases, nitrofurantoin can be removed from circulation by dialysis.[L6856,L6859,L6862]

The half life of nitrofurantoin is 0.72-0.78h.[A179830]

Nitrofurantoin could be up to 90% protein bound in plasma.[A179806]

27-50% of an oral dose is excreted in the urine as unchanged nitrofurantoin.[A179830] 90% of the total dose is eliminated in the urine.[A179836]

Data regarding the volume of distribution in humans is scarce but it has been reported as 0.46L/kg in dogs.[A179857]

The clearance of nitrofurantoin is 16.7-19.4L/h.[A179830]

Organic compounds

Organoheterocyclic compounds

Azolidines

Imidazolidines

[ "approved", "vet_approved" ]

[ "J01XE", "J01X", "J01", "J", "J01XE", "J01X", "J01", "J" ]

[ "Gram negative and gram positive bacteria" ]

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[]

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Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantion Macrocrystals", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", 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(monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin 50 Tab 50mg", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin macrocrystals", "Nitrofurantoin macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin macrocrystals", "Nitrofurantoin macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Macrocrystals", "Nitrofurantoin Mono", "Nitrofurantoin Mono", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystal", "Nitrofurantoin Monohydrate/Macrocrystal", "Nitrofurantoin Monohydrate/Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin monohydrate/macrocrystals (monohydrate/macrocrystals)", "Nitrofurantoin monohydrate/macrocrystals (monohydrate/macrocrystals)", "Nitrofurantoin Oral Suspension", "Nitrofurantoine 100 Tab 100mg", "Novo-furan 100mg", "Novo-furan Sus 25mg/5ml", "Novo-furan Tab 50mg", "Nu-nitrofurantoin Tablets", "Nu-nitrofurantoin Tablets", "PMS-nitrofurantoin Bid", "Teva-nitrofurantoin", "Teva-nitrofurantoin" ]

[ "Furabid", "Niftran", "Siraliden", "Urantoin", "Urolong" ]

[ "Macrobid", "Macrobid", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Macrobid", "Macrobid", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Macrobid", "Macrobid", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Macrobid", "Macrobid", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin monohydrate/macrocrystals (monohydrate/macrocrystals)", "Nitrofurantoin monohydrate/macrocrystals (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Mono", "Nitrofurantoin Mono", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Macrobid", "Macrobid", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Macrobid", "Macrobid", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin Monohydrate Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin monohydrate macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin Monohydrate/Macrocrystals", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin Monohydrate/Macrocrystal", "Nitrofurantoin Monohydrate/Macrocrystal", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin Monohydrate/ Macrocrystalline", "Nitrofurantoin Monohydrate/ Macrocrystalline", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin", "Nitrofurantoin", "Nitrofurantoin (monohydrate/macrocrystals)", "Nitrofurantoin (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)", "NITROFURANTOIN (monohydrate/macrocrystals)" ]

[]

[ "P16435" ]

[]

[ "Q9UNQ0", "O95342", "P08183", "Q92887" ]

DB00699

Nicergoline

An ergot derivative that has been used as a cerebral vasodilator and in peripheral vascular disease. It has been suggested to ameliorate cognitive deficits in cerebrovascular disease.

solid

For the treatment of senile dementia, migraines of vascular origin, transient ischemia, platelet hyper-aggregability, and macular degeneration.

Nicergoline is a potent vasodilator (improves brain blood flow). On the cerebral level it prompts a lowering of vascular resistance, an increase in arterial flow and stimulates the use of oxygen and glucose. Nicergoline also improves blood circulation in the lungs and limbs and has been shown to inhibit blood platelet aggregation.

Nicergoline acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. Therefore the mechanism of Nicergoline is to increase vascular circulation in the brain, thereby enhancing the transmission of nerve signals across the nerve fibres, which secrete acetylcholine as a neural transmitter.

null

Organic compounds

Organoheterocyclic compounds

Quinolines and derivatives

Indoloquinolines

[ "approved", "investigational" ]

[ "C04AE", "C04A", "C04", "C" ]

[ "Humans and other mammals" ]

[]

[]

[ "Sermion" ]

[]

[ "P35348" ]

[ "P10635" ]

[]

DB00701

Amprenavir

Amprenavir is a protease inhibitor used to treat HIV infection.

solid

For the treatment of HIV-1 infection in combination with other antiretroviral agents.

Amprenavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Amprenavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.

Amprenavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Rapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax) typically between 1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established.

Hepatic. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system. The 2 major metabolites result from oxidation of the tetrahydrofuran and aniline moieties. Glucuronide conjugates of oxidized metabolites have been identified as minor metabolites in urine and feces.

null

7.1-10.6 hours

Very high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein.

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Benzenesulfonamides

[ "approved", "investigational" ]

[ "J05AE", "J05A", "J05", "J" ]

[ "Human Immunodeficiency Virus" ]

[ { "cost": "0.21", "description": "Agenerase 15 mg/ml Solution", "unit": "ml" }, { "cost": "0.65", "description": "Agenerase 50 mg capsule", "unit": "capsule" } ]

[ { "approved": "1996-12-17", "country": "United States", "expires": "2013-12-17", "number": "5585397" }, { "approved": "2004-05-04", "country": "United States", "expires": "2017-11-11", "number": "6730679" } ]

[ "Agenerase", "Agenerase", "Agenerase", "Agenerase", "Agenerase", "Agenerase", "Agenerase", "Agenerase", "Agenerase" ]

[ "Agemerase", "Prozei" ]

[]

[ "P03366" ]

[ "P20813", "P33261", "P11712", "P10635", "P20815", "P08684" ]

[]

[ "P08183", "P33527", "Q9Y6L6" ]

DB00702

Icodextrin

Icodextrin is an iso-osmotic peritoneal dialysis solution containing glucose polymers. It is used primarily for ambulatory peritoneal dialysis (CAPD) of diabetic patients and automated peritoneal dialysis (APD) for patients with end-stage renal disease. It is injected as a solution into the peritoneal cavity. The drug is absorbed via convective transport via peritoneal lymphatic pathways.

solid

Used for continuous ambulatory peritoneal dialysis (CAPD) of diabetic patients or automated peritoneal dialysis (APD) for the management of end-stage renal disease.

Icodextrin is an iso-osmotic peritoneal dialysis solution containing glucose polymers. It is used primarily for ambulatory peritoneal dialysis (CAPD) of diabetic patients and automated peritoneal dialysis (APD) for patients with end-stage renal disease. It is injected as a solution into the peritoneal cavity. The drug is absorbed via convective transport via peritoneal lymphatic pathways.

Icodextrin is a starch-derived, water-soluble glucose polymer linked by alpha (1-4) and alpha (1-6) glycosidic bonds with an average molecular weight between 13,000 and 19,000 daltons. It functions as a colloid osmotic agent to achieve ultrafiltration during long (12-16 hour) peritoneal dialysis dwells. In other words it helps clean waste out of the body when the kidneys are not functioning properly. Icodectrin acts in the peritoneal cavity by exerting osmotic pressure across small intercellular pores resulting in transcapillary ultrafiltration through the dwell. This is due to the fact that the polymer is minimially absorbed across the peritoneal membrane. Icodextrin achieves superior fluid removal compared with glucose-based dialysates.

40% of instilled icodextrin was absorbed from the peritoneal solution during a 12-hour dwell.

Icodextrin is metabolized by alpha-amylase into oligosaccharides with a lower degree of polymerization), including maltose, maltotriose, maltotetraose, and higher molecular weight species.

null

[ "approved", "investigational" ]

[]

[ "Humans and other mammals" ]

[ { "cost": "0.05", "description": "Extraneal icodextrin dial soln", "unit": "ml" } ]

[ { "approved": "1988-08-02", "country": "United States", "expires": "2009-08-09", "number": "4761237" }, { "approved": "2000-06-20", "country": "United States", "expires": "2017-06-20", "number": "6077836" }, { "approved": "2001-06-19", "country": "United States", "expires": "2018-06-19", "number": "6248726" } ]

[ "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal" ]

[ "Adept", "Dextrin, Caloreen", "Icodial" ]

[ "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal", "Extraneal" ]

[]

[ "P04746" ]

[]

DB00703

Methazolamide

A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.

solid

For treatment of chronic open-angle glaucoma and acute angle-closure glaucoma

Methazolamide is topical carbonic anhydrase inhibitor. Methazolamide is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Methazolamide is a sulfonamide derivative; however, it does not have any clinically significant antimicrobial properties. Although methazolamide achieves a high concentration in the cerebrospinal fluid, it is not-considered an effective anticonvulsant. Methazolamide has a weak and transient diuretic effect, therefore use results in an increase in urinary volume, with excretion of sodium, potassium and chloride.

Methazolamide is a potent inhibitor of carbonic anhydrase. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport.

Methazolamide is well absorbed from the gastrointestinal tract.

null

Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur in the case of an overdose.

14 hours

55%

null

* 17 to 23 L

null

[ "approved" ]

[ "G01AE", "G01A", "G01", "G", "S01EC", "S01E", "S01", "S" ]

[ "Humans and other mammals" ]

[ { "cost": "27.0", "description": "Methazolamide powder", "unit": "g" }, { "cost": "0.49", "description": "Methazolamide 25 mg tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Apo-Methazolamide 50 mg Tablet", "unit": "tablet" }, { "cost": "0.6", "description": "Neptazane 25 mg tablet", "unit": "tablet" }, { "cost": "0.77", "description": "Methazolamide 50 mg tablet", "unit": "tablet" } ]

[]

[ "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Methazolamide", "Neptazane", "Neptazane", "Neptazane", "Neptazane", "Neptazane Tablets 25mg", "Neptazane Tablets 25mg USP", "Neptazane Tablets 50mg", "Neptazane Tablets 50mg" ]

[ "Naptazane" ]

[]

[ "P00915", "P22748", "P00918", "P43166", "P07451" ]

[]

[ "Q4U2R8" ]

DB00704

Naltrexone

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

solid

Used as an adjunct to a medically supervised behaviour modification program in the maintenance of opiate cessation in individuals who were formerly physically dependent on opiates and who have successfully undergone detoxification. Also used for the management of alcohol dependence in conjunction with a behavioural modification program.

Naltrexone, a pure opioid antagonist, is a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. It markedly attenuates or completely blocks, reversibly, the subjective effects of intravenously administered opioids. When co-administered with morphine, on a chronic basis, naltrexone blocks the physical dependence to morphine, heroin and other opioids. In subjects physically dependent on opioids, naltrexone will precipitate withdrawal symptomatology.

Naltrexone is a pure opiate antagonist and has little or no agonist activity. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone is thought to act as a competitive antagonist at mc, κ, and δ receptors in the CNS, with the highest affintiy for the μ receptor. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. This leads to the antagonization of most of the subjective and objective effects of opiates, including respiratory depression, miosis, euphoria, and drug craving. The major metabolite of naltrexone, 6-β-naltrexol, is also an opiate antagonist and may contribute to the antagonistic activity of the drug.

Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.

Hepatic. When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol (which may contribute to the therapeutic effect) and other minor metabolites.

In the mouse, rat and guinea pig, the oral LD50s were 1,100-1,550 mg/kg; 1,450 mg/kg; and 1,490 mg/kg; respectively. High doses of naltrexone (generally >1,000 mg/kg) produce salivation, depression/reduced activity, tremors, and convulsions.

4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol.

21% bound to plasma proteins over the therapeutic dose range.

Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration.

* 1350 L [intravenous administration]

* ~ 3.5 L/min [after IV administration]

Organic compounds

Benzenoids

Phenanthrenes and derivatives

null

[ "approved", "investigational", "vet_approved" ]

[ "N02AA", "N02A", "N02", "N", "N07BB", "N07B", "N07", "N", "A08AA", "A08A", "A08", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "4.28", "description": "Depade 50 mg tablet", "unit": "tablet" }, { "cost": "4.45", "description": "Naltrexone HCl 50 mg tablet", "unit": "tablet" }, { "cost": "4.57", "description": "Naltrexone 50 mg tablet", "unit": "tablet" }, { "cost": "9.35", "description": "Revia 50 mg tablet", "unit": "tablet" }, { "cost": "69.0", "description": "Naltrexone powder", "unit": "g" }, { "cost": "172.54", "description": "Naltrexone hcl powder", "unit": "g" }, { "cost": "291.73", "description": "ReVia 30 50 mg tablet Bottle", "unit": "bottle" }, { "cost": "960.0", "description": "Vivitrol injectable suspension", "unit": "each" } ]

[ { "approved": "2011-04-05", "country": "United States", "expires": "2029-10-15", "number": "7919499" }, { "approved": "2003-03-25", "country": "United States", "expires": "2019-11-12", "number": "6537586" }, { "approved": "2001-12-18", "country": "United States", "expires": "2019-11-12", "number": "6331317" }, { "approved": "2003-12-23", "country": "United States", "expires": "2020-11-25", "number": "6667061" }, { "approved": "1998-08-11", "country": "United States", "expires": "2017-11-02", "number": "5792477" }, { "approved": "2002-05-28", "country": "United States", "expires": "2019-11-12", "number": "6395304" }, { "approved": "2010-09-21", "country": "United States", "expires": "2020-05-25", "number": "7799345" }, { "approved": "1999-06-29", "country": "United States", "expires": "2017-11-02", "number": "5916598" }, { "approved": "2002-04-30", "country": "United States", "expires": "2019-06-30", "number": "6379703" }, { "approved": "2002-12-17", "country": "United States", "expires": "2020-05-25", "number": "6495164" }, { "approved": "2002-06-11", "country": "United States", "expires": "2017-11-02", "number": "6403114" }, { "approved": "2002-04-30", "country": "United States", "expires": "2020-05-19", "number": "6379704" }, { "approved": "2003-07-22", "country": "United States", "expires": "2019-06-30", "number": "6596316" }, { "approved": "2004-03-30", "country": "United States", "expires": "2019-11-12", "number": "6713090" }, { "approved": "2001-02-27", "country": "United States", "expires": "2019-06-30", "number": "6194006" }, { "approved": "2001-07-24", "country": "United States", "expires": "2020-05-19", "number": "6264987" }, { "approved": "2002-12-17", "country": "United States", "expires": "2019-11-12", "number": "6495166" }, { "approved": "2003-03-18", "country": "United States", "expires": "2020-05-19", "number": "6534092" }, { "approved": "2005-09-06", "country": "United States", "expires": "2019-11-12", "number": "6939033" }, { "approved": "2014-04-01", "country": "United States", "expires": "2025-07-03", "number": "8685443" }, { "approved": "2012-04-17", "country": "United States", "expires": "2027-06-19", "number": "8158156" }, { "approved": "2010-03-23", "country": "United States", "expires": "2027-06-19", "number": "7682633" }, { "approved": "2014-01-07", "country": "United States", "expires": "2029-11-07", "number": "8623418" }, { "approved": "2014-04-01", "country": "United States", "expires": "2025-07-03", "number": "8685444" }, { "approved": "2014-09-30", "country": "United States", "expires": "2027-06-19", "number": "8846104" }, { "approved": "2010-10-19", "country": "United States", "expires": "2027-12-12", "number": "7815934" }, { "approved": "2010-03-23", "country": "United States", "expires": "2027-06-19", "number": "7682634" }, { "approved": "2014-11-04", "country": "United States", "expires": "2027-06-19", "number": "8877247" }, { "approved": "2014-05-13", "country": "United States", "expires": "2027-11-08", "number": "8722085" }, { "approved": "2012-11-27", "country": "United States", "expires": "2027-11-08", "number": "8318788" }, { "approved": "2008-12-09", "country": "United States", "expires": "2024-07-20", "number": "7462626" }, { "approved": "2014-08-26", "country": "United States", "expires": "2024-07-20", "number": "8815889" }, { "approved": "2015-08-18", "country": "United States", "expires": "2027-06-04", "number": "9107837" }, { "approved": "2015-09-08", "country": "United States", "expires": "2027-11-08", "number": "9125868" }, { "approved": "2014-12-23", "country": "United States", "expires": "2030-02-02", "number": "8916195" }, { "approved": "2016-02-02", "country": "United States", "expires": "2032-01-13", "number": "9248123" }, { "approved": "2012-01-03", "country": "United States", "expires": "2029-02-03", "number": "8088786" }, { "approved": "2008-05-20", "country": "United States", "expires": "2025-03-26", "number": "7375111" }, { "approved": "2019-03-19", "country": "United States", "expires": "2034-07-02", "number": "10231964" }, { "approved": "2019-06-04", "country": "United States", "expires": "2027-11-08", "number": "10307376" }, { "approved": "2020-11-17", "country": "United States", "expires": "2034-07-02", "number": "10835527" }, { "approved": "2020-11-10", "country": "United States", "expires": "2034-07-02", "number": "10828294" }, { "approved": "2021-10-05", "country": "United States", "expires": "2033-06-05", "number": "11139056" }, { "approved": "2019-09-03", "country": "United States", "expires": "2033-06-05", "number": "10403170" }, { "approved": "2017-04-25", "country": "United States", "expires": "2033-06-25", "number": "9633575" }, { "approved": "2021-06-15", "country": "United States", "expires": "2031-01-10", "number": "11033543" }, { "approved": "2004-04-21", "country": "United States", "expires": "2024-04-21", "number": "11278544" }, { "approved": "2009-05-29", "country": "United States", "expires": "2029-05-29", "number": "11324741" }, { "approved": "2014-07-02", "country": "United States", "expires": "2034-07-02", "number": "11998542" }, { "approved": "2007-11-08", "country": "United States", "expires": "2027-11-08", "number": "12048769" } ]

[ "Addex-1000", "Apo-naltrexone", "Contrave", "Contrave", "Contrave", "Contrave Extended-Release", "Contrave Extended-Release", "Contrave Extended-Release", "Embeda", "Embeda", "Embeda", "Embeda", "Embeda", "Embeda", "Embeda", "Mysimba", "Mysimba", "Naltrexone", "Naltrexone Hcl", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride", "Naltrexone Hydrochloride and Bupropion Hydrochloride Extended-Release", "Naltrexone Hydrochloride Tablets USP", "Revia", "Revia", "Revia - Tab 50mg", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Vivitrol", "Vivitrol", "Vivitrol" ]

[ "Abernil", "Adepend", "Antaxon", "Antaxone", "Arrop", "Celupan", "Depade", "Dependex", "Nalerona", "Nalorex", "Naltax", "Naltrekson", "Narcoral", "Neksi", "Nemexin", "Opizone", "Revez", "Trexan", "Vivitrex" ]

[ "Embeda", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Troxyca ER", "Naltrexone Hydrochloride and Bupropion Hydrochloride Extended-Release", "Naltrexone", "Contrave Extended-Release", "Contrave Extended-Release", "Embeda", "Embeda", "Embeda", "Embeda", "Embeda", "Embeda", "Contrave Extended-Release", "Contrave", "Contrave", "Contrave", "Mysimba", "Mysimba" ]

[ "P35372", "P41145", "P41143", "Q99720" ]

[ "P22309" ]

[]

DB00705

Delavirdine

A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.

solid

For the treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Delavirdine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of Delavirdine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdine.

Delavirdine binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.

Rapidly absorbed

Hepatic

Major toxicity of delavirdine is rash and should be advised to promptly notify their physician should rash occur. The majority of rashes associated with delavirdine occur within 1 to 3 weeks after initiating treatment with delavirdine. The rash normally resolves in 3 to 14 days and may be treated symptomatically while therapy with delavirdine is continued. Any patient experiencing severe rash or rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches should discontinue medication and consult a physician.

5.8 hours

98%

Delavirdine is extensively converted to several inactive metabolites by cytochrome P450 3A (CYP3A). Delavirdine was excreted in the milk of lactating rats at a concentration three to five times that of rat plasma.

null

Organic compounds

Organoheterocyclic compounds

Diazinanes

Piperazines

[ "approved" ]

[ "J05AG", "J05A", "J05", "J" ]

[ "Human Immunodeficiency Virus" ]

[ { "cost": "1.92", "description": "Rescriptor 200 mg tablet", "unit": "tablet" } ]

[ { "approved": "1996-10-08", "country": "United States", "expires": "2013-10-08", "number": "5563142" }, { "approved": "2005-05-03", "country": "Canada", "expires": "2015-03-01", "number": "2184598" }, { "approved": "2001-03-20", "country": "Canada", "expires": "2010-12-24", "number": "2071529" }, { "approved": "2001-01-23", "country": "United States", "expires": "2019-06-07", "number": "6177101" } ]

(N-[2-[4-[3-(1-methylethylamino)pyridin-2-yl]piperazin-1-yl]carbonyl-1H-indol-5-yl] methanesulfonamide) | 1-(3-((1-methylethyl)amino)-2-pyridinyl)-4-((5-((methylsulfonyl)amino)-1H-indol-2-yl)carbonyl)piperazine | 2-(4-(5-methanesulfonamido-1H-indol-2-ylcarbonyl)-1-piperazinyl)-N-(1-methylethyl)-3-pyridinamine | Delavirdin | Delavirdina | Delavirdine | Delavirdinum | N-(2-(1-(3-(isopropylamino)pyridin-2-yl)piperazine-4-carbonyl)-1H-indol-5-yl)methanesulfonamide | N-{2-[4-(3-Isopropylamino-pyridin-2-yl)-piperazine-1-carbonyl]-1H-indol-5-yl}-methanesulfonamide | Pr160Gag-Pol | 1,4-cineole 2-exo-monooxygenase | 1,8-cineole 2-exo-monooxygenase | 1.14.14.1 | Albendazole monooxygenase (sulfoxide-forming) | Albendazole sulfoxidase | Cholesterol 25-hydroxylase | CYP3A3 | CYPIIIA3 | CYPIIIA4 | Cytochrome P450 3A3 | Cytochrome P450 HLp | Cytochrome P450 NF-25 | Cytochrome P450-PCN1 | Nifedipine oxidase | Quinine 3-monooxygenase | 1.14.14.- | Cholesterol 25-hydroxylase | CYP2DL1 | CYPIID6 | Cytochrome P450-DB1 | Debrisoquine 4-hydroxylase | 1.14.14.1 | CYPIIIA5 | Cytochrome P450-PCN3 | 1.14.14.1 | CYPIIIA7 | Cytochrome P450-HFLA | P450HLp2 | (R)-limonene 6-monooxygenase | (S)-limonene 6-monooxygenase | (S)-limonene 7-monooxygenase | 1.14.14.1 | Cholesterol 25-hydroxylase | CYP2C10 | CYPIIC9 | Cytochrome P-450MP | Cytochrome P450 MP-4 | Cytochrome P450 MP-8 | Cytochrome P450 PB-1 | S-mephenytoin 4-hydroxylase | (R)-limonene 6-monooxygenase | (S)-limonene 6-monooxygenase | (S)-limonene 7-monooxygenase | 1.14.14.1 | CYPIIC17 | CYPIIC19 | Cytochrome P450-11A | Cytochrome P450-254C | Fenbendazole monooxygenase (4'-hydroxylating) | Mephenytoin 4-hydroxylase

[ "Rescriptor", "Rescriptor", "Rescriptor", "Rescriptor", "Rescriptor", "Rescriptor", "Rescriptor" ]

[]

[ "P03366" ]

[ "P08684", "P10635", "P20815", "P24462", "P11712", "P33261" ]

[]

DB00706

Tamsulosin

Tamsulosin is a selective alpha-1A and alpha-1B adrenoceptor antagonist that exerts its greatest effect in the prostate and bladder, where these receptors are most common.[Label] It is indicated for the treatment of signs and symptoms of benign prostatic hypertrophy.[Label] Antagonism of these receptors leads to relaxation of smooth muscle in the prostate and detrusor muscles in the bladder, allowing for better urinary flow.[Label] Other alpha-1 adrenoceptor antagonists developed in the 1980s were less selective and more likely to act on the smooth muscle of blood vessels, resulting in hypotension.[A178351] Tamsulosin was first approved by the FDA on April 15, 1997.[L6238]

solid

Tamsulosin is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia.[Label] Tamsulosin is also used off label for the treatment of ureteral stones, prostatitis, and female voiding dysfunction.[A178339,L6259]

Tamsulosin is an alpha adrenoceptor blocker with specificity for the alpha-1A and alpha-1D subtypes, which are more common in the prostate and submaxillary tissue.[A1078] The final subtype, alpha-1B, are most common in the aorta and spleen.[A1078] Tamsulosin binds to alpha-1A receptors 3.9-38 times more selectively than alpha-1B and 3-20 times more selectively than alpha-1D.[A1078] This selectivity allows for a significant effect on urinary flow with a reduced incidence of adverse reactions like orthostatic hypotension.[A1078]

Tamsulosin is a blocker of alpha-1A and alpha-1D adrenoceptors.[Label,A1078] About 70% of the alpha-1 adrenoceptors in the prostate are of the alpha-1A subtype.[Label] By blocking these adrenoceptors, smooth muscle in the prostate is relaxed and urinary flow is improved.[Label] The blocking of alpha-1D adrenoceptors relaxes the detrusor muscles of the bladder which prevents storage symptoms.[A1078] The specificity of tamsulosin focuses the effects to the target area while minimizing effects in other areas.[Label]

Oral tamsulosin is 90% absorbed in fasted patients.[Label] The area under the curve is 151-199ng/mL\*hr for a 0.4mg oral dose and 440-557ng/mL*hr for a 0.8mg oral dose.[Label] The maximum plasma concentration is 3.1-5.3ng/mL for a 0.4mg oral dose and 2.5-3.6ng/mL for a 0.8mg oral dose.[Label] Taking tamsulosin with food increases the time to maximum concentration from 4-5 hours to 6-7 hours but increases bioavailability by 30% and maximum plasma concentration by 40-70%.[Label]

Tamsulosin is mostly metabolized in the liver by cytochrome P450 (CYP) 3A4 and 2D6, with some metabolism by other CYPs.[Label,A1078] CYP3A4 is responsible for the deethylation of tamsulosin to the M-1 metabolite and the oxidative deamination to the AM-1 metabolite,[A178276,A178321] while CYP2D6 is responsible for the hydroxylation of tamsulosin to the M-3 metabolite and the demethylation of tamsulosin to the M-4 metabolite.[A178276] In addition, tamsulosin can be hydroxylated at a different position by an unknown enzyme to form the M-2 metabolite.[A178276] The M-1, M-2, M-3, and M-4 metabolites can be glucuronidated, and the M-1 and M-3 metabolites can undergo sulfate conjugation to form other metabolites before excretion.[A178321]

In the event of overdose, patients may experience hypotension and should lie down in a supine position to maintain blood pressure and heart rate.[Label] If further measures are required intravenous fluids should be considered.[Label] If further progression is required, vasopressors may be used and renal function should be monitored.[Label] Dialysis is unlikely to assist in treating overdose because tamsulosin is extensively protein bound.[Label] The oral LD50 in rats is 650mg/kg.[MSDS] Tamsulosin is not indicated for use in women and no studies have been performed in pregnancy, though animal studies have not shown fetal harm.[Label] Tamsulosin is excreted in the milk of rats but there is no available data on what the effect of this tamsulosin exposure may be.[Label] Animal studies have shown male and female rat fertility is affected by tamsulosin due to impairment of ejaculation and fertilization.[Label] In men, tamsulosin is associated with abnormal ejaculation.[Label] Tamsulosin is not mutagenic but may be carcinogenic at levels above the maximum recommended human dose.[Label] Female rats experience a slight increase in the rates of mammary gland fibroadenomas and adenocarcinomas.[Label]

The half life in fasted patients is 14.9±3.9 hours.[Label] The elimination half life is 5-7 hours and the apparent half life is 9 to 13 hours in healthy subjects.[Label] In patients who require tamsulosin, the apparent half life is 14-15 hours.[Label]

Tamsulosin is 94%-99% protein bound, mostly to alpha-1-acid glycoprotein.[Label]

97% of an orally administered does is recovered in studies, which 76% in the urine and 21% in the feces after 168 hours.[Label] 8.7% of the dose is excreted as unmetabolized tamsulosin.[Label,A1078]

16L after intravenous administration.[Label]

2.88L/h.[Label]

Organic compounds

Benzenoids

Benzene and substituted derivatives

Phenethylamines

[ "approved", "investigational" ]

[ "G04CA", "G04C", "G04", "G", "G04CA", "G04C", "G04", "G", "G01AE", "G01A", "G01", "G", "G04CA", "G04C", "G04", "G", "G04CA", "G04C", "G04", "G" ]

[ "Humans and other mammals" ]

[ { "cost": "4.3", "description": "Tamsulosin hcl 0.4 mg capsule", "unit": "capsule" }, { "cost": "4.71", "description": "Flomax 0.4 mg capsule", "unit": "capsule" }, { "cost": "0.57", "description": "Novo-Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.57", "description": "Ran-Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.57", "description": "Ratio-Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.57", "description": "Sandoz Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.57", "description": "Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.63", "description": "Flomax Cr 0.4 mg Extended-Release Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Mylan-Tamsulosin 0.4 mg Sustained-Release Capsule", "unit": "capsule" } ]

[ { "approved": "1987-10-27", "country": "United States", "expires": "2010-04-27", "number": "4703063" }, { "approved": "2008-08-26", "country": "Canada", "expires": "2023-12-24", "number": "2490299" }, { "approved": "2005-05-24", "country": "Canada", "expires": "2013-09-10", "number": "2144077" }, { "approved": "1996-10-15", "country": "United States", "expires": "2015-11-20", "number": "5565467" } ]

[ "Apo-tamsulosin CR", "Auro-tamsulosin CR", "Ava-tamsulosin CR", "Dutasteride and tamsulosin hydrochloride", "Dutasteride and Tamsulosin Hydrochloride", "Dutasteride and tamsulosin hydrochloride", "Dutasteride and tamsulosin hydrochloride", "Dutasteride and Tamsulosin Hydrochloride", "Dutasteride and Tamsulosin Hydrochloride", "Dutasteride and Tamsulosin Hydrochloride", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax", "Flomax CR", "Jalyn", "Jalyn", "Jalyn", "Jalyn", "Jamp Tamsulosin", "Mylan-tamsulosin", "Ran-tamsulosin", "Ratio-tamsulosin", "Sandoz Tamsulosin", "Sandoz Tamsulosin", "Sandoz Tamsulosin CR", "Tamsulosin CR", "Tamsulosin CR", "Tamsulosin CR", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Tamsulosin Hydrochloride", "Teva-tamsulosin", "Teva-tamsulosin CR", "Uflo" ]

[ "Betamsal", "Contiflo XL", "Flomaxtra", "Harnal D", "Maxrin", "Mecir", "Omexel", "Omipro", "Omix", "Omnic", "Pradif", "Ranomax", "Salover", "Secotex", "Stronazon", "Tamsact", "Tamsol", "Tamsul", "Urimax" ]

[ "Jalyn", "Dutasteride and tamsulosin hydrochloride", "Jalyn", "Dutasteride and Tamsulosin Hydrochloride", "Dutasteride and tamsulosin hydrochloride", "Dutasteride and tamsulosin hydrochloride", "Dutasteride and Tamsulosin Hydrochloride", "Jalyn", "Dutasteride and Tamsulosin Hydrochloride", "Jalyn", "Dutasteride and Tamsulosin Hydrochloride" ]

[ "P35348", "P25100", "P35368" ]

[ "P10635", "P08684" ]

[ "P02763" ]

[]

DB00707

Porfimer sodium

The purified component of hematoporphyrin derivative, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (hematoporphyrin photoradiation); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of photodynamic therapy in the United States.

solid

Indicated in the treatment of esophageal cancer.

Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer is indicated for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who cannot be satisfactorily treated with Nd:YAG laser therapy, reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC), and the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. The cytotoxic and antitumor actions of porfimer are light and oxygen dependent. Tumor selectivity in treatment occurs through a combination of selective retention of porfimer and selective delivery of light.

Cellular damage caused by porfimer is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Spin transfer from porfimer to molecular oxygen may then generate singlet oxygen. Subsequent radical reactions can form superoxide and hydroxyl radicals. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release.

null

10-452 hours

~90%

null

* 0.49 ± 0.28 L/kg [2 mg/kg dose of porfimer sodium to 4 male cancer patients]

* Renal cl=199.7 +/- 56.9 mL/min [Healthy subjects receiving a single 300-mg oral dose]

null

[ "approved", "investigational" ]

[ "L01XD", "L01X", "L01", "L" ]

[ "Humans and other mammals" ]

[ { "cost": "3317.04", "description": "Photofrin 75 mg vial", "unit": "vial" } ]

[ { "approved": "1992-09-08", "country": "United States", "expires": "2009-12-15", "number": "5145863" }, { "approved": "1996-10-22", "country": "Canada", "expires": "2013-04-27", "number": "2094974" } ]

[ "Photofrin", "Photofrin", "Photofrin", "Photofrin" ]

[ "PhotoBarr", "Photofrin II" ]

[]

[ "P01130", "P12314" ]

[]

DB00709

Lamivudine

A reverse transcriptase inhibitor and zalcitabine analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV).

solid

Lamivudine is indicated in combination with other antiretrovirals the treatment of HIV infection and chronic hepatitis B (HBV).[L51474] In combination with [dolutegravir], lamivudine is indicated for the treatment of HIV-1 in patients ≥12 years of age and weighing ≥25 kg.[L51469]

Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV) to disrupt viral DNA synthesis. When phosphorylated, lamivudine can form active metabolites that compete for incorporation into viral DNA. Via DNA incorporation, lamivudine metabolites competitively inhibit the activity of the HIV reverse transcriptase enzyme and act as a chain terminator of DNA synthesis. Due to the lack of a 3'-OH group, incorporated nucleoside analogues prevent the formation of a 5' to 3' phosphodiester linkage that is essential for DNA chain elongation.

Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination.

Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in 12 adult patients was 86% ± 16% (mean ± SD) for the 150-mg tablet and 87% ± 13% for the oral solution. The peak serum lamivudine concentration (Cmax) was 1.5 ± 0.5 mcg/mL when an oral dose of 2 mg/kg twice a day was given to HIV-1 patients. When given with food, absorption is slower, compared to the fasted state.

Metabolism of lamivudine is a minor route of elimination. In man, the only known metabolite of lamivudine is the trans-sulfoxide metabolite. This biotransformation is catalyzed by sulfotransferases.

The most common reported adverse reactions (incidence ≥15%) in adults were headache, nausea, malaise and fatigue, nasal signs and symptoms, diarrhea, and cough.

5 to 7 hours (healthy or HBV-infected patients)

<36% bound to plasma protein.

The majority of lamivudine is eliminated unchanged in urine by active organic cationic secretion. 5.2% ± 1.4% (mean ± SD) of the dose was excreted as the trans-sulfoxide metabolite in the urine. Lamivudine is excreted in human breast milk and into the milk of lactating rats.

Apparent volume of distribution, IV administration = 1.3 ± 0.4 L/kg. Volume of distribution was independent of dose and did not correlate with body weight.

* Renal clearance = 199.7 ± 56.9 mL/min [300 mg oral dose, healthy subjects] * Renal clearance = 280.4 ± 75.2 mL/min [single IV dose, HIV-1-infected patients] * Total clearance = 398.5 ± 69.1 mL/min [HIV-1-infected patients]

Organic compounds

Nucleosides, nucleotides, and analogues

Nucleoside and nucleotide analogues

3'-thia pyrimidine nucleosides

[ "approved", "investigational" ]

[ "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AR", "J05A", "J05", "J", "J05AF", "J05A", "J05", "J" ]

[ "Human Immunodeficiency Virus", "Hepatitis B virus" ]

[ { "cost": "7.79", "description": "Epivir 150 mg tablet", "unit": "tablet" }, { "cost": "13.94", "description": "Epivir hbv 100 mg tablet", "unit": "tablet" }, { "cost": "15.57", "description": "Epivir 300 mg tablet", "unit": "tablet" }, { "cost": "35.78", "description": "Epzicom tablet", "unit": "tablet" }, { "cost": "37.21", "description": "Epzicom 600-300 mg tablet", "unit": "tablet" }, { "cost": "0.53", "description": "Epivir 10 mg/ml Solution", "unit": "ml" } ]

[ { "approved": "2006-10-10", "country": "United States", "expires": "2009-08-08", "number": "7119202" }, { "approved": "2004-08-03", "country": "Canada", "expires": "2012-06-02", "number": "2070230" }, { "approved": "1999-02-23", "country": "Canada", "expires": "2012-01-03", "number": "2100269" }, { "approved": "2016-01-26", "country": "United States", "expires": "2030-06-08", "number": "9242986" }, { "approved": "1999-05-18", "country": "United States", "expires": "2016-11-18", "number": "5905082" }, { "approved": "1999-12-21", "country": "United States", "expires": "2018-09-20", "number": "6004968" }, { "approved": "2007-05-15", "country": "United States", "expires": "2023-04-21", "number": "7217713" }, { "approved": "2008-10-14", "country": "United States", "expires": "2023-04-21", "number": "7435734" }, { "approved": "2010-07-13", "country": "United States", "expires": "2029-09-11", "number": "7754731" }, { "approved": "2007-01-30", "country": "United States", "expires": "2024-04-03", "number": "7169780" }, { "approved": "2002-07-09", "country": "United States", "expires": "2016-09-28", "number": "6417191" }, { "approved": "2012-03-06", "country": "United States", "expires": "2028-04-05", "number": "8129385" }, { "approved": "2010-10-26", "country": "United States", "expires": "2023-04-25", "number": "7820660" }, { "approved": "2001-09-25", "country": "United States", "expires": "2018-11-14", "number": "6294540" }, { "approved": "2013-07-16", "country": "United States", "expires": "2031-10-07", "number": "8486975" }, { "approved": "2020-03-31", "country": "United States", "expires": "2036-11-29", "number": "10603282" }, { "approved": "2020-11-24", "country": "United States", "expires": "2036-11-29", "number": "10842751" }, { "approved": "2011-01-24", "country": "United States", "expires": "2031-01-24", "number": "11234985" } ]

[ "3tc", "3tc", "3tc", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and lamivudine", "Abacavir and lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir and Lamivudine", "Abacavir Sulfate, Lamivudine and Zidovudine", "Abacavir, Lamivudine and Zidovudine", "Apo-abacavir-lamivudine", "Apo-abacavir-lamivudine Tablets", "Apo-abacavir-lamivudine-zidovudine", "Apo-lamivudine", "Apo-lamivudine", "Apo-lamivudine Hbv", "Apo-lamivudine-zidovudine", "Apo-zidovudine-lamivudine-nevirapine", "Auro-abacavir/lamivudine", "Auro-lamivudine", "Auro-lamivudine", "Auro-lamivudine/zidovudine", "Cimduo", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Combivir", "Delstrigo", "Delstrigo", "Delstrigo", "Delstrigo", "Dovato", "Dovato", "Dovato", "Dovato", "Dovato", "Dovato", "Dutrebis", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir", "Epivir Hbv", "Epivir Hbv", "Epivir Hbv", "Epzicom", "Epzicom", "Epzicom", "Epzicom", "Epzicom", "Epzicom", "Epzicom", "Heptovir", "Heptovir", "Jamp Abacavir / Lamivudine", "Jamp Lamivudine", "Jamp Lamivudine", "Jamp Lamivudine / Zidovudine", "Jamp Lamivudine Hbv", "Kivexa", "Kivexa", "Kivexa", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "Lamivudine Oral Solution", "Lamivudine Teva", "Lamivudine Teva", "Lamivudine Teva", "Lamivudine Teva", "Lamivudine Teva", "Lamivudine Teva", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Teva Pharma B.V.", "Lamivudine Zidovudine", "Lamivudine, Nevirapine, and Zidovudine", "Lamivudine/zidovudine Teva", "Lamivudine/zidovudine Teva", "Mint-abacavir/lamivudine", "Mylan-abacavir/lamivudine", "PMS-abacavir-lamivudine", "Symfi", "Symfi Lo", "Symfi Lo", "Temixys", "Temixys", "Teva-abacavir/lamivudine", "Teva-lamivudine/zidovudine", "Triumeq", "Triumeq", "Triumeq", "Triumeq", "Triumeq", "Triumeq", "Triumeq", "Triumeq", "Triumeq PD", "Trizivir", "Trizivir", "Trizivir", "Trizivir", "Trizivir", "Trizivir", "Trizivir", "Zeffix", "Zeffix", "Zeffix" ]

[ "Amilitrap", "Antiheb", "Avilam", "Avolam", "Epivir-HBV", "Flamivud", "Ganvirel", "Hepavir", "Hepitec", "Heptavir", "Heptodin", "Heptodine", "Lamda", "Lamibergen", "Lamidac", "Lamitec", "Lamivir", "Zeffix" ]

[ "Epzicom", "Combivir", "Epzicom", "Combivir", "Trizivir", "Combivir", "Epzicom", "Combivir", "Combivir", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Combivir", "Lamivudine and Zidovudine", "Combivir", "Trizivir", "Triumeq", "Epzicom", "Lamivudine and Zidovudine", "Abacavir Sulfate, Lamivudine and Zidovudine", "Combivir", "Lamivudine Zidovudine", "Combivir", "Triumeq", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Symfi Lo", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Abacavir and Lamivudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "Cimduo", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Combivir", "Lamivudine and Zidovudine", "Abacavir, Lamivudine and Zidovudine", "Abacavir and Lamivudine", "Abacavir and lamivudine", "Abacavir and lamivudine", "Abacavir and Lamivudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Abacavir and Lamivudine", "Delstrigo", "Lamivudine and Zidovudine", "Temixys", "Abacavir and Lamivudine", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine, Nevirapine, and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Symfi Lo", "Dovato", "Triumeq", "Lamivudine and Zidovudine", "Abacavir and Lamivudine", "LAMIVUDINE and ZIDOVUDINE", "Symfi", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Epzicom", "Abacavir and Lamivudine", "Epzicom", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Temixys", "LAMIVUDINE and ZIDOVUDINE", "Epzicom", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Lamivudine and Zidovudine", "Abacavir and Lamivudine", "Lamivudine and Zidovudine", "Combivir", "Triumeq", "Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate", "Lamivudine and Zidovudine", "LAMIVUDINE and ZIDOVUDINE", "Abacavir and Lamivudine", "Trizivir", "Abacavir and Lamivudine", "Lamivudine and Zidovudine", "Combivir", "Teva-lamivudine/zidovudine", "Apo-lamivudine-zidovudine", "Auro-lamivudine/zidovudine", "Apo-zidovudine-lamivudine-nevirapine", "Delstrigo", "Jamp Lamivudine / Zidovudine", "Trizivir", "Kivexa", "Apo-abacavir-lamivudine-zidovudine", "Apo-abacavir-lamivudine", "Teva-abacavir/lamivudine", "Mylan-abacavir/lamivudine", "Auro-abacavir/lamivudine", "PMS-abacavir-lamivudine", "Triumeq", "Dovato", "Jamp Abacavir / Lamivudine", "Mint-abacavir/lamivudine", "Apo-abacavir-lamivudine Tablets", "Triumeq PD", "Abacavir and Lamivudine", "Lamivudine/zidovudine Teva", "Lamivudine/zidovudine Teva", "Dutrebis", "Trizivir", "Trizivir", "Trizivir", "Combivir", "Combivir", "Delstrigo", "Delstrigo", "Dovato", "Dovato", "Dovato", "Dovato", "Triumeq", "Triumeq", "Triumeq", "Kivexa", "Kivexa" ]

[ "P03366" ]

[ "P27707", "P30085", "P00558", "P15531", "P22392", "P49585", "Q99447", "Q8TCD5" ]

[ "P02768" ]

[ "P33527", "Q4U2R8", "Q9UNQ0", "O15245", "O15244", "O75751", "P08183", "O15439", "O15438", "Q92887" ]

DB00711

Diethylcarbamazine

An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa.

solid

Used for the treatment of certain filarial diseases, including tropical pulmonary eosinophilia, loiasis, and lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori.

Diethylcarbamazine is an anthelmintic drug that does not resemble other antiparasitic compounds. It is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements.

The mechanism of action of diethylcarbamazine is thought to involve sensitizing the microfilariae to phagocytosis. One study showed that diethylcarbamazine's activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway. It confirmed the important role of the arachidonic acid metabolic pathway in diethylcarbamazine's mechanism of action in vivo and showes that in addition to its effects on the 5-lipoxygenase pathway, it targets the cyclooxygenase pathway and COX-1.

Readily absorbed following oral administration.

Partially metabolized to diethylcarbamazine N-oxide.

Oral LD50 in rat and mouse is 1400 mg/kg and 660 mg/kg, respectively.

Approximately 8 hours.

null

Organic compounds

Organoheterocyclic compounds

Diazinanes

Piperazines

[ "approved", "investigational", "vet_approved" ]

[ "P02CB", "P02C", "P02", "P" ]

[ "Humans and other mammals", "Parasitic nematodes and other roundworms" ]

[]

[ "Hetrazan Tab 50mg" ]

[ "Banocide", "Banocide Forte", "Camin", "Carbilazine", "Caricide", "Cypip", "Decet", "Dicarb", "Diethizine", "Eofil", "Ethodryl", "Hetrazan", "Notezine", "Spatonin", "Supatonin" ]

[]

[ "P09917", "P23219" ]

[ "P06276" ]

[]

DB00713

Oxacillin

An antibiotic similar to [flucloxacillin] used in resistant staphylococci infections.

solid

Used in the treatment of resistant staphylococci infections.

Oxacillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Oxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Oxacillin results from the inhibition of cell wall synthesis and is mediated through Oxacillin binding to penicillin binding proteins (PBPs). Oxacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Oxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Oxacillin interferes with an autolysin inhibitor.

null

20 to 30 minutes

94.2 +/- 2.1% (binds to serum protein, mainly albumin)

Oxacillin Sodium is rapidly excreted as unchanged drug in the urine by glomerular filtration and active tubular secretion.

null

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved", "investigational" ]

[ "J01CR", "J01C", "J01", "J", "J01CF", "J01C", "J01", "J" ]

[ "Enteric bacteria and other eubacteria", "Staphylococcus aureus" ]

[ { "cost": "12.41", "description": "Oxacillin 1 gm vial", "unit": "each" }, { "cost": "24.08", "description": "Oxacillin 2 gm vial", "unit": "each" }, { "cost": "118.01", "description": "Oxacillin 10 gm vial", "unit": "each" }, { "cost": "0.43", "description": "Oxacillin 1 gm/ 50 ml inj", "unit": "ml" }, { "cost": "0.62", "description": "Oxacillin 2 gm/ 50 ml inj", "unit": "ml" } ]

[]

(2S,5R,6R)-3,3-dimethyl-6-{[(5-methyl-3-phenylisoxazol-4-yl)carbonyl]amino}-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid | (5-methyl-3-phenyl-4-isoxazolyl)penicillin | 5-methyl-3-phenyl-4-isoxazolyl-penicillin | 6β-(5-methyl-3-phenylisoxazol-4-yl)penicillanic acid | Ossacillina | Oxacilina | Oxacillin | Oxacilline | Oxacillinum | Oxazocillin | Oxazocilline | Putative D-alanyl-D-alanine carboxypeptidase | exp2 | Exported protein 2 | PBP-1A | pbp2b | PBP1 | Intestinal H(+)/peptide cotransporter | Oligopeptide transporter, small intestine isoform | PEPT1 | Peptide transporter 1 | Kidney H(+)/peptide cotransporter | Oligopeptide transporter, kidney isoform | PEPT2 | Peptide transporter 2 | 3.5.2.6 | Intestinal H(+)/peptide cotransporter | Oligopeptide transporter, small intestine isoform | PEPT1 | Peptide transporter 1 | Kidney H(+)/peptide cotransporter | Oligopeptide transporter, kidney isoform | PEPT2 | Peptide transporter 2

[ "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin", "Oxacillin" ]

[ "Bactocill", "Biocilina", "Bristopen", "Dicloxal Ox", "InfectoStaph", "Ocillina", "Oxacil", "Oxacilina", "Oxacilinã", "Oxagram", "Oxal", "Oxamicin", "Oxapen", "Oxipen", "Panadox", "Penstapho", "Prostafilina", "Prostaphlin", "Stafcil", "Staficilin-N", "Wydox" ]

[]

[ "P46059", "Q16348" ]

[]

[ "P46059", "Q16348" ]

DB00714

Apomorphine

Apomorphine is a non-ergoline dopamine D2 agonist indicated to treat hypomobility associated with Parkinson's. It was first synthesized in 1845 and first used in Parkinson's disease in 1884.[A203618] Apomorphine has also been investigated as an emetic, a sedative, a treatment for alcoholism, and a treatment of other movement disorders.[A203597,A203618] Apomorphine was granted FDA approval on 20 April 2004.[L13919]

solid

Apomorphine is indicated to treat acute, intermittent treatment of hypomobility, off episodes associated with advanced Parkinson's disease.[L13919,L13922]

Apomorphine is a dopaminergic agonist that may stimulate regions of the brain involved in motor control.[A203594,L13919,L13922] It has a short duration of action and a wide therapeutic index as large overdoses are necessary for significant toxicity.[L13919,L13922] Patients should be counselled regarding the risk of nausea, vomiting, daytime somnolence, hypotension, oral mucosal irritation, falls, hallucinations, psychotic-like behaviour, impulsive behaviour, withdrawal hyperpyrexia, and prolongation of the QT interval.[L13919,L13922] Given the incidence of nausea and vomiting in patients taking apomorphine, treatment with [trimethobenzamide] may be recommended prior to or during therapy. Antiemetic pretreatment may be started three days prior to beginning therapy with apomorphine - it should only be continued as long as is necessary and generally for no longer than two months.[L41915]

Apomorphine is a non-ergoline dopamine agonist with high binding affinity to dopamine D2, D3, and D5 receptors.[L13919,L13922] Stimulation of D2 receptors in the caudate-putamen, a region of the brain responsible for locomotor control, may be responsible for apomorphine's action.[A203594] However, the means by which the cellular effects of apomorphine treat hypomobility of Parkinson's remain unknown.[L13919,L13922]

Apomorphine has a plasma Tmax of 10-20 minutes and a cerebrospinal fluid Tmax.[A203549] The Cmax and AUC of apomorphine vary significantly between patients, with 5- to 10-fold differences being reported.[A203549,A203405]

Apomorphine is N-demethylated by CYP2B6, 2C8, 3A4, and 3A5.[L13919] It can be glucuronidated by various UGTs,[L13919] or sulfated by SULTs 1A1, 1A2, 1A3, 1E1, and 1B1.[A203447] Approximately 60% of sublingual apomorphine is eliminated as a sulfate conjugate, though the structure of these sulfate conjugates are not readily available.[A203447,L13919] The remainder of an apomorphine dose is eliminated as apomorphine glucuronide and norapomorphine glucuronide.[L13919] Only 0.3% of subcutaneous apomorphine is recovered as the unchanged parent drug.[A203402]

Patients experiencing an overdose of apomorphine may present with nausea, hypotension, and loss of consciousness.[L13919] Treat patients with symptomatic and supportive measures. The intraperitoneal LD50 in mice is 145µg/kg.[L14012]

The terminal elimination half life of a 15mg sublingual dose of apomorphine is 1.7h,[L13919] while the terminal elimination half life of an intravenous dose is 50 minutes.[L13922]

Apomorphine is expected to be 99.9% bound to human serum albumin, as no unbound apomorphine is detected.[A177817,A203405]

Data regarding apomorphine's route of elimination is not readily available.[L13919,L13922] A study in rats has shown apomorphine is predominantly eliminated in the urine.[A203579]

The apparent volume of distribution of subcutaneous apomorphine is 123-404L with an average of 218L.[L13919] The apparent volume of distribution of sublingual apomorphine is 3630L.[L13922]

The clearance of a 15mg sublingual dose of apomorphine is 1440L/h,[L13919] while the clearance of an intravenous dose is 223L/h.[L13922]

Organic compounds

Alkaloids and derivatives

Aporphines

null

[ "approved", "investigational" ]

[ "G04BE", "G04B", "G04", "G", "N04BC", "N04B", "N04", "N" ]

[ "Humans and other mammals" ]

[]

[ { "approved": "2013-12-10", "country": "United States", "expires": "2024-04-03", "number": "8603514" }, { "approved": "2018-01-02", "country": "United States", "expires": "2022-02-14", "number": "9855221" }, { "approved": "2018-04-03", "country": "United States", "expires": "2022-02-14", "number": "9931305" }, { "approved": "2014-07-01", "country": "United States", "expires": "2024-02-20", "number": "8765167" }, { "approved": "2013-04-09", "country": "United States", "expires": "2031-12-16", "number": "8414922" }, { "approved": "2017-06-06", "country": "United States", "expires": "2030-06-11", "number": "9669021" }, { "approved": "2017-06-06", "country": "United States", "expires": "2030-06-11", "number": "9669019" }, { "approved": "2014-09-30", "country": "United States", "expires": "2031-12-16", "number": "8846074" }, { "approved": "2016-03-15", "country": "United States", "expires": "2030-06-11", "number": "9283219" }, { "approved": "2019-09-24", "country": "United States", "expires": "2030-06-11", "number": "10420763" }, { "approved": "2016-05-03", "country": "United States", "expires": "2030-06-11", "number": "9326981" }, { "approved": "2019-10-22", "country": "United States", "expires": "2036-04-19", "number": "10449146" }, { "approved": "2014-03-04", "country": "United States", "expires": "2023-02-02", "number": "8663687" }, { "approved": "2015-06-02", "country": "United States", "expires": "2030-06-11", "number": "9044475" }, { "approved": "2020-11-03", "country": "United States", "expires": "2029-08-07", "number": "10821074" }, { "approved": "2021-01-12", "country": "United States", "expires": "2022-02-14", "number": "10888499" }, { "approved": "2021-03-30", "country": "United States", "expires": "2036-04-19", "number": "10959943" }, { "approved": "2021-08-03", "country": "United States", "expires": "2022-02-14", "number": "11077068" }, { "approved": "2011-12-16", "country": "United States", "expires": "2031-12-16", "number": "11419769" } ]

[ "Apokyn", "Apokyn", "Apokyn", "Apomorphine Hydrocloride", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Movapo", "Movapo" ]

[ "Ixense", "Spontane", "Uprima" ]

[ "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi", "Kynmobi" ]

[ "P21917", "P14416", "P35462", "P21918", "P21728", "P18825", "P18089", "P08908", "P28223", "P41595", "P28335", "P08913", "P28221", "P28222" ]

[ "P21964", "P50225", "P50226", "P0DMM9", "P49888", "O43704", "P20813", "P10632", "P08684", "P20815", "P19224", "P22309", "Q9HAW8", "P35503", "P22310", "Q9HAW7", "Q9HAW9", "O60656", "P54855", "P06133", "P16662" ]

[ "P02768" ]

[ "Q05940" ]

DB00715

Paroxetine

Paroxetine is a selective serotonin reuptake inhibitor (SSRI) drug commonly known as Paxil. It has a variety of uses, including the treatment of anxiety disorders, major depression, posttraumatic stress disorder, and symptoms of menopause, among others.[T653] It was approved by the FDA in the early 1990s and marketed by SmithKline Beecham.[L7712,L7715] A unique feature of this drug is that it is highly potent and selective in its inhibition of serotonin reuptake and has little effect on other neurotransmitters.[A31914] Because of its potent inhibition of serotonin reuptake, paroxetine is more likely to cause withdrawal effects upon cessation. Paroxetine is well tolerated in most patients with a similar adverse effect profile to other members of its drug class.[A31914] The controlled release formulation was designed to decrease the likelihood of nausea that is sometimes associated with paroxetine.[L7700,L7742]

solid

Paroxetine is indicated for the management of depression, obsessive-compulsive disorder, panic disorder, social anxiety disorder, generalized anxiety disorder, posttraumatic stress disorder.[L3358] One form of paroxetine, commercially known as Brisdelle, is used to manage mild to moderate vasomotor symptoms of menopause.[L7703] Off-label, paroxetine may be used for the treatment of premature ejaculation or irritable bowel syndrome (IBS).[A1093,A181754,A181904]

Paroxetine treats the symptoms of depression, various anxiety disorders, posttraumatic stress disorder, obsessive-compulsive disorder, and the vasomotor symptoms of menopause via the inhibition of serotonin reuptake.[T653,L3358,L7703] The onset of action of paroxetine is reported to be approximately 6 weeks.[A181874] Due its serotonergic activity, paroxetine, like other SSRI drugs, may potentiate serotonin syndrome. This risk is especially high when monoamine oxidase (MAO) inhibitors are given within 2 weeks of paroxetine administration. Upon cessation of MAO inhibitors, a 2-week interval before paroxetine administration is recommended. Do not coadminister these agents.[T656]

Paroxetine enhances serotonergic activity via the inhibition presynaptic reuptake of serotonin by the serotonin (SERT) receptor.[A5492,A181772] This inhibition raises the level of serotonin in the synaptic cleft, relieving various symptoms. This drug has been demonstrated to be a stronger inhibitor of serotonin reuptake than other members of the same drug class, including [Citalopram], [Fluoxetine], and [Fluvoxamine].[A31914] The mechanism of action of paroxetine in relieving the vasomotor symptoms of menopause is unknown, according to the Brisdelle prescribing information[L7703], but may occur due to its effects on thermoregulation.[A181973] Paroxetine shows a clinically insignificant affinity for adrenergic alpha-1 and alpha-2 receptors and β-adrenergic receptors, dopamine D1 and D2 receptors, histamine H1 receptors and serotonin 5-HT1A, 5-HT2A and 5-HT2C receptors.[A31914] This drug shows some affinity for muscarinic cholinergic receptors and 5-H2B receptors.[A181829,A181847] The delayed onset of paroxetine therapeutic effects may be explained by the initial paroxetine actions on the 5-HT neurons. In rats, paroxetine activates 5-HT1A receptors when it is first administered, inhibiting the stimulation of the 5-HT neurons and subsequent release of serotonin at the synaptic cleft.[A31914]

Paroxetine is readily absorbed from the gastrointestinal tract. Due to the first-pass metabolism, the bioavailability ranges from 30-60%. Cmax is attained 2 to 8 hours after an oral dose.[A181760] Mean Tmax is 4.3 hours in healthy patients.[L7706] The steady-state concentration of paroxetine is achieved within 7 to 14 days of oral therapy.[A31914] In a pharmacokinetic study, AUC in healthy patients was 574 ng·h/mL and 1053 ng·h/mL in those with moderate renal impairment.[L7706]

Paroxetine metabolism occurs in the liver and is largely mediated by cytochrome CYP2D6 with contributions from CYP3A4 and possibly other cytochrome enzymes.[A415,T656] Genetic polymorphisms of the CYP2D6 enzyme may alter the pharmacokinetics of this drug. Poor metabolizers may demonstrate increased adverse effects while rapid metabolizers may experience decreased therapeutic effects.[A31914,A181769,L7718] The majority of a paroxetine dose is oxidized to a catechol metabolite that is subsequently converted to both glucuronide and sulfate metabolites via methylation and conjugation. In rat synaptosomes, the glucuronide and sulfate conjugates have been shown to thousands of times less potent than paroxetine itself.[L7706] The metabolites of paroxetine are considered inactive.[A181883,A31914,T656]

The acute LD50 in mice and rats is 350 mg/kg.[L7733] Overdose information The lowest dose of paroxetine reported to lead to a fatal outcome is approximately 400 mg. The largest reported paroxetine overdose from which a patient has survived and recovered is a dose of 2000 mg. Common manifestations in a paroxetine overdose include fatigue, fever, insomnia hypertension, tachycardia, nausea, vomiting, somnolence, tremor, dizziness, agitation, confusion, anxious symptoms, headache, insomnia, hyperhidrosis, dilated pupils, seizures, paresthesia, serotonin syndrome, involuntary muscle contraction, and change in mental status. It should be noted that in some cases, patients may have consumed alcohol in addition to taking an overdose of paroxetine.[L7706] Some of these symptoms may also be seen with clinical use. There is no specific antidote to an overdose of paroxetine.[A181775]

The mean elimination half-life of paroxetine is about 21 hours.[L3358] In healthy young subjects, mean elimination half-life was found to be 17.3 hours.[L7706]

Paroxetine is 95% bound to plasma proteins.[A181760,A181799,L3358]

About 2/3 of a single paroxetine dose is found to be excreted in the urine and the remainder is found to be excreted in feces. Almost all of the dose is eliminated as metabolites; 3% is found to be excreted as unchanged paroxetine.[A31914] About 64% of a 30 mg oral dose was found excreted in the urine, with 2% as the parent drug and 62% appearing as metabolites. Approximately 36% of the dose was found to be eliminated in the feces primarily as metabolites and less than 1% as the parent compound.[L3358]

Paroxetine has a large volume of distribution and is found throughout the body, including in the central nervous system. Only 1% of the drug is found in the plasma.[L3358] Paroxetine is found in the breast milk at concentrations similar to the concentrations found in plasma.[A31914]

The apparent oral clearance of paroxetine is 167 L/h.[A181799] The clearance of paroxetine in patients with renal failure is significantly lower and dose adjustment may be required, despite the fact that it is mainly cleared by the liver. Dose adjustments may be required in hepatic impairment.[A181799,L3358,L7706]

Organic compounds

Organoheterocyclic compounds

Piperidines

Phenylpiperidines

[ "approved", "investigational" ]

[ "N06AB", "N06A", "N06", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.05", "description": "Apo-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Co Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Mylan-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Novo-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Phl-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Pms-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Ratio-Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Sandoz Paroxetine 20 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Apo-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Co Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Mylan-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Novo-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Phl-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Pms-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Ratio-Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "1.12", "description": "Sandoz Paroxetine 30 mg Tablet", "unit": "tablet" }, { "cost": "2.03", "description": "Paxil 20 mg Tablet", "unit": "tablet" }, { "cost": "2.1", "description": "Pms-Paroxetine 40 mg Tablet", "unit": "tablet" }, { "cost": "2.16", "description": "Paxil 30 mg Tablet", "unit": "tablet" }, { "cost": "2.58", "description": "Paroxetine hcl 10 mg tablet", "unit": "tablet" }, { "cost": "2.7", "description": "Paroxetine hcl 20 mg tablet", "unit": "tablet" }, { "cost": "2.78", "description": "Paroxetine hcl 30 mg tablet", "unit": "tablet" }, { "cost": "2.93", "description": "Paroxetine hcl 40 mg tablet", "unit": "tablet" }, { "cost": "3.76", "description": "PARoxetine HCl 12.5 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "3.91", "description": "Paxil 10 mg tablet", "unit": "tablet" }, { "cost": "3.93", "description": "PARoxetine HCl 25 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "4.02", "description": "Paxil cr 12.5 mg tablet", "unit": "tablet" }, { "cost": "4.04", "description": "PARoxetine HCl 37.5 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "4.16", "description": "Paxil 20 mg tablet", "unit": "tablet" }, { "cost": "4.18", "description": "Paxil CR 12.5 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "4.2", "description": "Paxil 30 mg tablet", "unit": "tablet" }, { "cost": "4.2", "description": "Paxil cr 25 mg tablet", "unit": "tablet" }, { "cost": "4.32", "description": "Paxil cr 37.5 mg tablet", "unit": "tablet" }, { "cost": "4.37", "description": "Paxil CR 25 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "4.44", "description": "Paxil 40 mg tablet", "unit": "tablet" }, { "cost": "4.5", "description": "Paxil CR 37.5 mg 24 Hour tablet", "unit": "tablet" }, { "cost": "5.6", "description": "Pexeva 10 mg tablet", "unit": "tablet" }, { "cost": "5.84", "description": "Pexeva 20 mg tablet", "unit": "tablet" }, { "cost": "6.11", "description": "Pexeva 30 mg tablet", "unit": "tablet" }, { "cost": "6.29", "description": "Pexeva 40 mg tablet", "unit": "tablet" }, { "cost": "121.87", "description": "Paxil 30 10 mg tablet Bottle", "unit": "bottle" }, { "cost": "131.0", "description": "Paxil 30 30 mg tablet Bottle", "unit": "bottle" }, { "cost": "138.39", "description": "Paxil 30 40 mg tablet Bottle", "unit": "bottle" }, { "cost": "0.85", "description": "Paxil 10 mg/5ml Suspension", "unit": "ml" } ]

[ { "approved": "2004-03-09", "country": "United States", "expires": "2022-10-21", "number": "6703408" }, { "approved": "1998-08-04", "country": "United States", "expires": "2009-07-06", "number": "5789449" }, { "approved": "2009-11-24", "country": "Canada", "expires": "2016-07-19", "number": "2445678" }, { "approved": "1997-12-16", "country": "Canada", "expires": "2016-02-05", "number": "2168829" }, { "approved": "2009-10-06", "country": "United States", "expires": "2023-02-12", "number": "7598271" }, { "approved": "2000-09-19", "country": "United States", "expires": "2017-09-17", "number": "6121291" }, { "approved": "1998-09-22", "country": "United States", "expires": "2016-03-22", "number": "5811436" }, { "approved": "2000-05-16", "country": "United States", "expires": "2019-10-23", "number": "6063927" }, { "approved": "2001-01-09", "country": "United States", "expires": "2018-07-15", "number": "6172233" }, { "approved": "2007-06-12", "country": "United States", "expires": "2017-01-19", "number": "7229640" }, { "approved": "2003-04-15", "country": "United States", "expires": "2017-01-19", "number": "6548084" }, { "approved": "1999-02-23", "country": "United States", "expires": "2017-06-10", "number": "5874447" }, { "approved": "2014-02-25", "country": "United States", "expires": "2029-04-06", "number": "8658663" }, { "approved": "2015-02-03", "country": "United States", "expires": "2026-08-04", "number": "8946251" }, { "approved": "2000-10-17", "country": "United States", "expires": "2015-11-19", "number": "6133289" }, { "approved": "1999-05-04", "country": "United States", "expires": "2015-11-19", "number": "5900423" }, { "approved": "1999-02-16", "country": "United States", "expires": "2015-11-19", "number": "5872132" }, { "approved": "2000-06-27", "country": "United States", "expires": "2015-11-19", "number": "6080759" }, { "approved": "2016-07-19", "country": "United States", "expires": "2026-08-04", "number": "9393237" } ]

[ "Act Paroxetine", "Act Paroxetine", "Act Paroxetine", "Ag-paroxetine", "Ag-paroxetine", "Ag-paroxetine", "Ag-paroxetine Tablets", "Ag-paroxetine Tablets", "Ag-paroxetine Tablets", "Apo-paroxetine", "Apo-paroxetine", "Apo-paroxetine", "Auro-paroxetine", "Auro-paroxetine", "Auro-paroxetine", "Bio-paroxetine", "Bio-paroxetine", "Bio-paroxetine", "Brisdelle", "Brisdelle", "Dom-paroxetine", "Dom-paroxetine", "Dom-paroxetine", "Dom-paroxetine", "Ipg-paroxetine", "Ipg-paroxetine", "Ipg-paroxetine", "Jamp Paroxetine Tablets", "Jamp Paroxetine Tablets", "Jamp Paroxetine Tablets", "Jamp-paroxetine", "Jamp-paroxetine", "Jamp-paroxetine", "M-paroxetine", "M-paroxetine", "M-paroxetine", "Mar-paroxetine", "Mar-paroxetine", "Mar-paroxetine", "Mint-paroxetine", "Mint-paroxetine", "Mint-paroxetine", "Mylan-paroxetine", "Mylan-paroxetine", "Mylan-paroxetine", "Nra-paroxetine", "Nra-paroxetine", "Nra-paroxetine", "Ntp-paroxetine", "Ntp-paroxetine", "Ntp-paroxetine", "Nu-paroxetine", "Nu-paroxetine", "Nu-paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride", "Paroxetine Hydrochloride Anhydrous", "PAROXETINE HYDROCHLORIDE Controlled-Release", "Paroxetine Hydrochloride CR", "Paroxetine-10", "Paroxetine-20", "Paroxetine-30", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil CR", "Paxil Tab 10mg", "Paxil Tab 20mg", "Paxil Tab 30mg", "Paxilcr CR", "Paxilcr CR", "Paxilcr CR", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "Pexeva", "PMS-paroxetine", "PMS-paroxetine", "PMS-paroxetine", "PMS-paroxetine", "Priva-paroxetine", "Priva-paroxetine", "Priva-paroxetine", "Q-paroxetine", "Q-paroxetine", "Q-paroxetine", "Ratio-paroxetine", "Ratio-paroxetine", "Ratio-paroxetine", "Riva-paroxetine", "Riva-paroxetine", "Riva-paroxetine", "Sandoz Paroxetine", "Sandoz Paroxetine", "Sandoz Paroxetine", "Sandoz Paroxetine", "Sandoz Paroxetine", "Sandoz Paroxetine Tablets", "Sandoz Paroxetine Tablets", "Sandoz Paroxetine Tablets", "Teva-paroxetine", "Teva-paroxetine", "Teva-paroxetine" ]

[ "Aropax", "PAXILCR", "Sereupin", "Seroxat", "Seroxat CR" ]

[]

[ "P31645", "P23975", "P28223", "P35348", "P35368", "P25100", "P08913", "P18089", "P18825", "P08588", "P07550", "P13945", "P14416", "P35367", "P08908", "P28222", "P28221", "P28566", "P30939", "P28223", "P41595", "P28335", "P46098", "O95264", "Q8WXA8", "Q70Z44", "A5X5Y0", "Q13639", "P50406", "P34969", "P11229", "P08172", "P20309", "P08173", "P08912", "P41595", "P21728", "P21918" ]

[ "P20813", "P05177", "P08684", "P33261", "P10635", "P11712" ]

[]

[ "P08183" ]

DB00716

Nedocromil

A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets.

solid

For the treatment of mild to moderate asthma

Nedocromil is a anti-inflammatory agent and can be administered directly to the bronchial mucosa. It has significant inhibitory effect on allergen-induced early and late asthmatic reactions and on bronchial hyperresponsiveness.

Nedocromil has been shown to inhibit the in vitro activation of, and mediator release from, a variety of inflammatory cell types associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits activation and release of inflammatory mediators such as histamine, prostaglandin D2 and leukotrienes c4 from different types of cells in the lumen and mucosa of the bronchial tree. These mediators are derived from arachidonic acid metabolism through the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of nedocromil may be due partly to inhibition of axon reflexes and release of sensory neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil does not posess any bronchodilator, antihistamine, or corticosteroid activity.

Low

Nedocromil is not metabolized after IV administration and is excreted unchanged.

Side effects include headache, nasal congestion, ocular burning, irritation and stinging, unpleasant taste, cough, difficulty breathing, noisy breathing, shortness of breath, tightness in chest, wheezing, conjunctivitis, blurred vision, change in color vision, difficulty seeing at night, increased sensitivity of eyes to sunlight.

~3.3 hours

approximately 89% protein bound in human plasma over a concentration range of 0.5 to 50 µg/mL

It is not metabolized and is eliminated primarily unchanged in urine (70%) and feces (30%).

null

Organic compounds

Organoheterocyclic compounds

Benzopyrans

1-benzopyrans

[ "approved", "investigational" ]

[ "R03BC", "R03B", "R03", "R", "R01AC", "R01A", "R01", "R", "S01GX", "S01G", "S01", "S" ]

[ "Humans and other mammals" ]

[ { "cost": "19.34", "description": "Alocril 2% eye drops", "unit": "ml" }, { "cost": "100.57", "description": "Alocril 2% Solution 5ml Bottle", "unit": "bottle" } ]

[ { "approved": "2004-10-19", "country": "United States", "expires": "2012-08-22", "number": "RE38628" } ]

[ "Alocril", "Alocril", "Mireze", "Nedocromil Sodium", "Tilade", "Tilade", "Tilade Inhaler 2mg/aem" ]

[]

[ "Q9Y271", "Q9NS75", "P21462", "Q13258", "P07900" ]

[]

DB00717

Norethisterone

Norethisterone, also known as norethindrone, is a synthetic progestational hormone belonging to the 19-nortestosterone-derived class of progestins.[A10367] It is further classified as a second-generation progestin, along with [levonorgestrel] and its derivatives, and is the active form of several other progestins including [norethynodrel] and [lynestrenol].[A10367] Norethisterone mimics the actions of endogenous [progesterone], albeit with a greater potency,[A188075] and is used on its own or in combination with estrogen derivatives in a variety of applications including contraception and hormone replacement therapy.[L9527,L10301,L10304,L10307] First derived in 1951 in Mexico City, norethisterone was originally intended for use as a remedy for irregular menstruation and endometriosis, and was not marketed for use as an oral contraceptive until 1962.[L10439]

solid

Norethisterone is indicated as an oral contraceptive when given as monotherapy[L9527] or in combination with an estrogen component, such as [ethinylestradiol] or [estradiol].[L10313,L10307] In combination with an estrogen component, oral norethisterone is also indicated as a hormone replacement therapy in the treatment of postmenopausal osteoporosis and moderate-to-severe vasomotor symptoms arising from menopause.[L10304] When applied via transdermal patch, the combination of norethisterone and estradiol is indicated for the treatment of hypoestrogenism, vulvovaginal atrophy, and moderate-severe vasomotor symptoms.[L10301] Norethisterone, taken in combination with intramuscular [leuprolide], is also indicated for the symptomatic treatment of endometriosis-related pain.[L10310]

Norethisterone is a synthetic oral progestin used for contraception or to treat other hormone-related conditions such as menopausal symptoms and endometriosis. As a synthetic progestin, norethisterone acts similarly to endogenous progesterone but with a much higher potency - it acts at the pelvic level to alter cervical and endometrial function, as well as via the inhibition of pituitary hormones that play a role in follicular maturation and ovulation.[L9527] A small increase in the risk of developing breast cancer has been observed in patients using combined oral contraceptives, with some evidence also implicating progestin-only pills - patients starting hormonal contraception should be advised of this risk and should employ routine breast self-examinations to check for evidence of any developing masses.[L9527]

On a molecular level, progestins like norethisterone exert their effects on target cells via binding to progesterone receptors that result in downstream changes to target genes.[L10304] Target cells are found in the reproductive tract, breast, pituitary, hypothalamus, skeletal tissue, and central nervous system.[L10304] Contraceptive efficacy is derived mainly from changes to the cervical mucus, wherein norethisterone increases the cell content and viscosity of the mucous to impede sperm transport and migration.[L9527] Norethisterone also induces a variety of changes to the endometrium - including atrophy, irregular secretion, and suppressed proliferation - that make it inhospitable for implantation.[L9527,A37129] Working via a negative feedback loop, norethisterone also acts on both the hypothalamus and anterior pituitary to suppress the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. Suppression of these hormones prevents follicular development, ovulation, and corpus luteum development.[A37129] When used as a component of hormone replacement therapy in menopausal women, norethisterone’s value is mainly in suppressing the growth of the endometrium.[A188156] As estrogen stimulates endometrial growth, the unopposed use of estrogen in postmenopausal women with an intact uterus can lead to endometrial hyperplasia which can increase the risk of endometrial cancer. The addition of a progestin to a hormone replacement therapy in this population protects against this endometrial hyperplasia and, therefore, lowers the risk associated with the use of hormone replacement therapies. Norethisterone, along with other progestins and endogenous progesterone, has a low affinity for other steroid receptors, such as the androgen receptor and glucocorticoid receptor.[A10367,A188075] While affinity and agonistic activity at these receptors is minimal, it is thought that androgen receptor agonism is responsible for some of the adverse effects observed with progestin use (e.g. acne, serum lipid changes).[A10367]

The Cmax of norethisterone following oral administration of a single dose ranges from 5.39 to 7.36 ng/mL with a Tmax of 1-2 hours.[L9527,L10304,L10307] AUC0-24 values following single oral doses range from approximately 30 to 37 ng*hr/mL.[L9527,L10304,L10307] The oral bioavailability of norethisterone is approximately 64%.[L10307] When applied transdermally, norethisterone is well-absorbed through the skin, reaches steady-state concentrations within 24 hours, and has a Cmax ranging from 617 to 1060 pg/mL at steady state.[L10301] Norethisterone is often formulated as norethisterone acetate, which is completely and rapidly deacetylated to norethisterone following oral administration - the disposition of norethisterone acetate is indistinguishable from that of orally administered norethisterone.[L10307]

Norethisterone is extensively metabolized, primarily in the liver, to a number of metabolites via partial and total reduction of its A-ring.[A188078] The enzymes predominantly involved are 3α- and 3β-hydroxysteroid dehydrogenase (HSD) as well as 5α- and 5β-reductase.[A188078,A188075] The 5α-reduced metabolites, including 5α-dihydronorethisterone and its derivatives, appear to carry biological activity while the 5β-reduced metabolites appear inactive.[A188075] Norethisterone and its metabolites are also extensively conjugated - most of the plasmatic metabolites are sulfate conjugates, while most of the urinary metabolites are glucuronide conjugates.[A188072,L10307] The major metabolites in plasma are a disulfate conjugate of 3α,5α-tetrahydronorethisterone and a monosulfate conjugate of 3α,5β-tetrahydronorethisterone, while the major metabolite(s) in the urine are comprised of glucuronide and/or sulfate conjugates of 3α,5β-tetrahydronorethisterone.[A188150] Norethisterone has also been observed to undergo some degree of metabolism via the cytochrome P450 enzyme system, predominantly by CYP3A4 and, to a much lesser extent, by CYP2C19, CYP1A2, and CYP2A6.[A35871] The metabolites generated by these reactions have not been fully characterized.

The oral LD50 in mice 6 g/kg and the TDLo in human women is 42 mg/kg.[L10433] There have been no reports of serious ill effects following overdose of oral contraceptives, including following ingestion by children.[L10307,L10313] Symptoms of overdosage are likely to be consistent with the adverse effect profile of the contraceptive and may, therefore, include significant nausea and/or vomiting.

The half-life of norethisterone has been variably estimated as 8-10 hours.[A188072,A188069,A10367,L9527,L10313]

Norethisterone is 38% bound to sex hormone-binding globulin and 61% bound to albumin.[A188072,L10307]

Following administration of radio-labeled norethisterone, slightly more than 50% of the administered dose was eliminated in the urine and 20-40% was eliminated in the feces.[A182033]

The volume of distribution of norethisterone is approximately 4 L/kg.[A188072,L10307] Sulfated metabolites of norethisterone, as well as small quantities of parent drug, have been shown to distribute into breast milk.[A188153]

The plasma clearance of norethisterone has been estimated as 0.4 L/hr/kg,[A188072,L10307] and the intrinsic clearance is approximately 73-81 L/h.[A188147]

Organic compounds

Lipids and lipid-like molecules

Steroids and steroid derivatives

Estrane steroids

[ "approved" ]

[ "H01CC", "H01C", "H01", "H", "H01CC", "H01C", "H01", "H", "G03AA", "G03A", "G03", "G", "G03DC", "G03D", "G03", "G", "G03AB", "G03A", "G03", "G", "G03AC", "G03A", "G03", "G", "G03FA", "G03F", "G03", "G", "G03FB", "G03F", "G03", "G" ]

[ "Humans and other mammals" ]

[ { "cost": "1.02", "description": "Ortho-novum 7-7-7-28 tablet", "unit": "tablet" }, { "cost": "1.05", "description": "Necon 1-50-28 tablet", "unit": "tablet" }, { "cost": "1.15", "description": "Necon 0.5-35-28 tablet", "unit": "tablet" }, { "cost": "1.15", "description": "Necon 7-7-7-28 tablet", "unit": "tablet" }, { "cost": "1.23", "description": "Ortho micronor tablet", "unit": "tablet" }, { "cost": "1.29", "description": "Demulen 1-50-28 tablet", "unit": "tablet" }, { "cost": "1.32", "description": "Camila tablet", "unit": "tablet" }, { "cost": "1.32", "description": "Jolivette tablet", "unit": "tablet" }, { "cost": "1.32", "description": "Nora-be tablet", "unit": "tablet" }, { "cost": "1.32", "description": "Norethindrone 0.35 mg tablet", "unit": "tablet" }, { "cost": "1.33", "description": "Ortho-novum 7/7/7-28 tablet", "unit": "tablet" }, { "cost": "1.34", "description": "Errin 0.35 mg tablet", "unit": "tablet" }, { "cost": "1.4", "description": "Ortho-novum 7-7-7-21 tablet", "unit": "tablet" }, { "cost": "1.67", "description": "Demulen 1-50-21 tablet", "unit": "tablet" }, { "cost": "1.73", "description": "Norinyl 1+35-28 tablet", "unit": "tablet" }, { "cost": "1.73", "description": "Norinyl 1+50-28 tablet", "unit": "tablet" }, { "cost": "1.8", "description": "Brevicon 28 tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Ortho-novum 1-35-28 tablet", "unit": "tablet" }, { "cost": "2.01", "description": "Tri-norinyl 28 tablet", "unit": "tablet" }, { "cost": "2.07", "description": "Modicon 28 tablet", "unit": "tablet" }, { "cost": "2.11", "description": "Necon 1-35-28 tablet", "unit": "tablet" }, { "cost": "2.24", "description": "Nor-q-d tablet", "unit": "tablet" }, { "cost": "2.44", "description": "Micronor tablet", "unit": "tablet" }, { "cost": "2.62", "description": "Ovcon-50 28 tablet", "unit": "tablet" }, { "cost": "2.65", "description": "Norethindrone 5 mg tablet", "unit": "tablet" }, { "cost": "2.75", "description": "Loestrin fe 1.5-30 tablet", "unit": "tablet" }, { "cost": "2.75", "description": "Norethindrone Acetate 5 mg tablet", "unit": "tablet" }, { "cost": "3.06", "description": "Ovcon-35 28 tablet", "unit": "tablet" }, { "cost": "3.27", "description": "Aygestin 5 mg tablet", "unit": "tablet" }, { "cost": "3.66", "description": "Loestrin 21 1.5-30 tablet", "unit": "tablet" }, { "cost": "3.66", "description": "Loestrin 21 1-20 tablet", "unit": "tablet" }, { "cost": "5.23", "description": "Loestrin fe 1-20 tablet", "unit": "tablet" }, { "cost": "31.99", "description": "Necon 1/35 (28) 28 1-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "32.99", "description": "Necon 0.5/35 (28) 28 0.5-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "33.99", "description": "Ortho-Novum 7/7/7 (28) 28 0.5/0.75/1-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "35.99", "description": "Necon 10/11 (28) 28 35 mcg tablet Disp Pack", "unit": "disp" }, { "cost": "52.99", "description": "Norinyl 1+50 (28) 28 1-50 mg-mcg tablet 1 Disp Pack = 28 Pills", "unit": "disp" }, { "cost": "53.0", "description": "Brevicon (28) 28 0.5-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "55.99", "description": "Norinyl 1+35 (28) 28 1-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "55.99", "description": "Ortho-Novum 1/35 (28) 28 1-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "59.99", "description": "Modicon (28) 28 0.5-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "60.25", "description": "Ortho-Novum 10/11 (28) 28 35 mcg tablet Disp Pack", "unit": "disp" }, { "cost": "62.63", "description": "Tri-Norinyl (28) 28 0.5/1/0.5-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "65.87", "description": "Nor-QD 28 0.35 mg tablet Disp Pack", "unit": "disp" }, { "cost": "75.15", "description": "Loestrin 24 Fe 28 1-20 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "77.1", "description": "Loestrin Fe 1.5/30 28 1.5-30 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "79.32", "description": "Loestrin 1.5/30 (21) 21 1.5-30 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "79.32", "description": "Loestrin 1/20 (21) 21 1-20 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "79.32", "description": "Loestrin Fe 1/20 28 1-20 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "89.09", "description": "Ovcon-35 (28) 28 0.4-35 mg-mcg tablet Disp Pack", "unit": "disp" }, { "cost": "89.09", "description": "Ovcon-50 28 50-1 mcg-mg tablet Disp Pack", "unit": "disp" }, { "cost": "0.66", "description": "Micronor (28 Day) 0.35 mg Tablet", "unit": "tablet" } ]

[ { "approved": "2000-03-14", "country": "United States", "expires": "2016-12-13", "number": "6036976" }, { "approved": "2003-12-23", "country": "United States", "expires": "2019-04-06", "number": "6667050" }, { "approved": "2010-04-27", "country": "United States", "expires": "2029-02-02", "number": "7704984" }, { "approved": "2003-11-25", "country": "United States", "expires": "2020-03-29", "number": "6652880" }, { "approved": "2008-12-09", "country": "United States", "expires": "2021-01-25", "number": "7462625" }, { "approved": "2007-02-20", "country": "United States", "expires": "2021-03-07", "number": "7179815" }, { "approved": "2008-09-02", "country": "United States", "expires": "2024-07-06", "number": "7419983" }, { "approved": "2006-06-06", "country": "United States", "expires": "2024-09-10", "number": "7056927" }, { "approved": "2005-03-29", "country": "United States", "expires": "2021-01-25", "number": "6872728" }, { "approved": "2021-01-05", "country": "United States", "expires": "2034-03-14", "number": "10881659" }, { "approved": "2011-11-15", "country": "United States", "expires": "2024-01-28", "number": "8058280" }, { "approved": "2007-11-27", "country": "United States", "expires": "2024-01-28", "number": "7300935" }, { "approved": "2016-05-24", "country": "United States", "expires": "2024-02-17", "number": "9346822" }, { "approved": "2021-06-15", "country": "United States", "expires": "2037-09-29", "number": "11033551" }, { "approved": "2021-06-29", "country": "United States", "expires": "2034-03-14", "number": "11045470" }, { "approved": "2008-11-07", "country": "United States", "expires": "2028-11-07", "number": "11459305" }, { "approved": "2019-07-23", "country": "United States", "expires": "2039-07-23", "number": "11542239" }, { "approved": "2020-08-27", "country": "United States", "expires": "2040-08-27", "number": "11690845" }, { "approved": "2018-05-03", "country": "United States", "expires": "2038-05-03", "number": "11793812" }, { "approved": "2013-09-27", "country": "United States", "expires": "2033-09-27", "number": "11795178" }, { "approved": "2017-09-29", "country": "United States", "expires": "2037-09-29", "number": "11957684" }, { "approved": "2018-08-20", "country": "United States", "expires": "2038-08-20", "number": "12083227" } ]

[ "Activella", "Activella", "Activella", "Activella", "Activella", "Activella", "Activelle", "Activelle Ld", "Affodel", "Alyacen 1/35", "Alyacen 1/35", "Alyacen 1/35", "Alyacen 1/35", "Alyacen 1/35", "Alyacen 7/7/7", "Alyacen 7/7/7", "Alyacen 7/7/7", "Alyacen 7/7/7", "Alyacen 7/7/7", "Amabelz", "Amabelz", "Aranelle", "Aranelle", "Aurovela 1.5/30", "Aurovela 1/20", "Aurovela 24 Fe", "AUROVELA Fe", "Aurovela Fe 1/20", "Aygestin", "Balziva", "Balziva", "Blisovi 24 Fe", "Blisovi Fe 1.5/30", "Blisovi Fe 1/20", "Brevicon", "Brevicon 0.5/35 21 Tab", "Brevicon 0.5/35 28 Tab", "Brevicon 0.5/35 Tablets (21-day Pack)", "Brevicon 0.5/35 Tablets (28-day Pack)", "Brevicon 1/35 21 Tab", "Brevicon 1/35 28 Tab", "Brevicon 1/35 Tablets (21-day Pack)", "Brevicon 1/35 Tablets (28-day Pack)", "Briellyn", "Camila", "Camila", "Camila", "Camila", "Camila", "Charlotte 24Fe", "CombiPatch", "CombiPatch", "CombiPatch", "CombiPatch (estradiol/norethindrone acetate transdermal system)", "CombiPatch (estradiol/norethindrone acetate transdermal system)", "Cyclafem 1/35", "Cyclafem 1/35", "Cyclafem 1/35", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyonanz", "Dasetta 1/35", "Dasetta 7/7/7", "Dasetta 7/7/7", "Dasetta 7/7/7", "Deblitane", "Emzahh", "Errin", "Errin", "Errin", "Errin", "Errin", "Estalis 140/50 Mcg", "Estalis 250/50 Mcg", "Estalis Sequi", "Estalis Sequi", "Estracomb", "Estradiol / Norethindrone Acetate", "Estradiol / Norethindrone Acetate", "Estradiol / Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "Etyqa", "Etyqa", "FEMCON Fe", "FEMCON Fe", "FEMCON Fe", "FEMCON Fe", "Femhrt", "Femhrt", "Femhrt", "Femhrt", "Femlyv", "Finzala", "Fyavolv", "Fyavolv", "Gallifrey", "Gemmily", "Generess", "GENERESS Fe", "GENERESS Fe", "Gildagia", "Gildess 1.5/30", "Gildess 1/20", "Gildess 24 Fe", "Gildess Fe 1.5/30", "Gildess Fe 1/20", "Hailey 1.5/30", "Hailey 24 Fe", "Hailey Fe 1.5/30", "Hailey Fe 1.5/30", "HAILEY Fe 1/20", "Heather", "Heather", "Incassia", "Jencycla", "Jencycla", "Jencycla", "Jevantique", "Jevantique Lo", "Jinteli", "Jinteli", "Jolivette", "Junel 1.5/30", "Junel 21 Day", "Junel 21 Day", "Junel 21 Day", "Junel 21 Day", "Junel FE", "Junel Fe 1.5/30", "Junel Fe 1.5/30", "Junel Fe 1.5/30", "Junel Fe 1/20", "Junel Fe 1/20", "Junel Fe 24", "Junel Fe 28 Day", "Junel Fe 28 Day", "Junel Fe 28 Day", "Junel Fe 28 Day", "Junel Fe 28 Day", "Junel Fe 28 Day", "Kaitlib Fe", "Kaitlib Fe", "Larin 1.5/30", "Larin 1/20", "Larin 24 Fe", "Larin Fe 1.5/30", "Larin Fe 1.5/30", "Larin Fe 1/20", "Larin Fe 1/20", "Layolis Fe", "Leena", "Leena", "Leena", "Leena", "Lo Loestrin Fe", "Lo Loestrin Fe", "Lo Minastrin Fe", "Loestrin 1.5/30", "Loestrin 1.5/30", "LOESTRIN 1.5/30 21 Day", "LOESTRIN 1/20 21 Day", "Loestrin 21 1.5/30", "Loestrin 21 1/20", "Loestrin 21 Day", "Loestrin 21 Day", "Loestrin 24 Fe", "Loestrin 24 Fe", "LOESTRIN Fe 1.5/30", "LOESTRIN Fe 1.5/30 28 Day", "LOESTRIN Fe 1.5/30 28 Day", "LOESTRIN Fe 1.5/30 28 Day", "LOESTRIN Fe 1/20", "LOESTRIN Fe 1/20 28 Day", "LOESTRIN Fe 1/20 28 Day", "LOESTRIN Fe 1/20 28 Day", "Loestrin Fe 28 Day", "Loestrin Fe 28 Day", "Loestrin Fe 28 Day", "Loestrin Fe 28 Day", "Lolo", "Lomedia 24 Fe", "Lopreeza", "Lopreeza", "Lopreeza", "Lopreeza", "Lupaneta Pack", "Lupaneta Pack", "Lyleq", "Lyleq", "Lyza", "Lyza", "Maeve", "Melodetta 24 Fe", "Merzee", "Merzee", "Mibelas 24 Fe", "Microgestin", "Microgestin", "Microgestin", "Microgestin", "Microgestin", "Microgestin", "Microgestin", "Microgestin 1.5/30", "Microgestin 1.5/30", "Microgestin 1.5/30", "Microgestin 1/20", "Microgestin 1/20", "Microgestin 1/20", "Microgestin 1/20", "Microgestin 24 Fe", "Microgestin 24 Fe", "Microgestin Fe", "Microgestin Fe", "Microgestin Fe", "MICROGESTIN Fe 1.5/30", "MICROGESTIN Fe 1.5/30", "Microgestin Fe 1.5/30", "Microgestin Fe 1.5/30", "Microgestin Fe 1.5/30", "Microgestin Fe 1.5/30", "MICROGESTIN Fe 1/20", "MICROGESTIN Fe 1/20", "Microgestin Fe 1/20", "Microgestin Fe 1/20", "Microgestin Fe 1/20", "Micronor", "Micronor Tablets 28-day", "Mimvey", "Mimvey Lo", "Minastrin 24 Fe", "Minastrin 24 Fe", "Minestrin 1/20", "Minestrin 1/20", "Modicon", "Modicon", "Modicon", "Movisse", "Myfembree", "Myfembree", "Necon", "Necon", "Necon", "Necon", "Necon (28 Day Regimen)", "Necon 0.5/35", "Necon 0.5/35", "Necon 1/35", "Necon 1/35", "Necon 1/35 (28 Day Regimen)", "Necon 10/11", "Necon 10/11", "Necon 777", "Necon 777", "Necon 777", "Necon 777", "Necon 777", "Necon 777", "Necon 777 777", "Necon 777 777", "Necon 777 777", "Nexesta Fe", "Nor QD", "Nor QD", "Nora BE", "Nora BE", "Nora-BE", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone", "Norethindrone Acetate", "Norethindrone acetate", "Norethindrone Acetate", "Norethindrone Acetate", "Norethindrone Acetate", "Norethindrone Acetate", "Norethindrone acetate", "Norethindrone Acetate", "Norethindrone Acetate", "Norethindrone acetate", "Norethindrone Acetate", "Norethindrone Acetate", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol, and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol, and Ferrous Fumarate", "Norethindrone acetate and ethinyl estradiol, and ferrous fumarate", "Norethindrone and ethinyl estradiol", "Norethindrone and ethinyl estradiol", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone and ethinyl estradiol and ferrous fumarate", "Norethindrone and Ethinyl Estradiol, and Ferrous Fumarate", "Norinyl", "Norinyl", "Norinyl 1/50 -(21-day Regimen)", "Norinyl 1/50 -(28-day Regimen)", "Norinyl 1/50 21 Tab", "Norinyl 1/50 28 Tab", "Norlutate", "Norlyda", "Norlyda", "Norlyroc", "Nortrel (21 Day Regimen)", "Nortrel 21 Day", "Nortrel 28 Day", "Nortrel 28 Day", "Nortrel 28 Day", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nylia 1/35", "Nylia 7/7/7", "Nylia 7/7/7", "Nylia 7/7/7", "Nylia 7/7/7", "Oriahnn", "Ortho 0.5/35 Tablets (21 Day)", "Ortho 0.5/35 Tablets (28 Day)", "Ortho 1/35 Tablets (21 Day)", "Ortho 1/35 Tablets (28 Day)", "Ortho 10/11 Tablets (21 Day)", "Ortho 10/11 Tablets (21 Day)", "Ortho 10/11 Tablets (28 Day)", "Ortho 10/11 Tablets (28 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Ortho Micronor", "Ortho Micronor", "Ortho Novum 1/35", "Ortho Novum 135", "Ortho-novum", "Ortho-novum 1/50 Tablets (21 Day)", "Ortho-novum 1/50 Tablets (28 Day)", "Ortho-novum 10/11", "Ortho-novum 10/11", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Oshih", "Ovcon 35", "Ovcon 35", "Ovcon 35", "Ovcon 35", "Ovcon 50", "Ovcon 50", "Philith", "Pirmella 1/35", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Rhuzdah", "Ryeqo", "Ryeqo", "Ryeqo", "Ryeqo", "Select 1/35 (21-day)", "Select 1/35 (28-day)", "Sharobel", "Synphasic 21 Tablets", "Synphasic 21 Tablets", "Synphasic 21 Tablets", "Synphasic 21 Tablets", "Synphasic 28 Tablets", "Synphasic 28 Tablets", "Synphasic-28 Tablets", "Synphasic-28 Tablets", "Tarina 24 Fe", "Tarina 24 Fe", "TARINA Fe 1/20", "TARINA Fe 1/20", "Tarina Fe 1/20 EQ", "Tarina Fe 1/20 EQ", "Taysofy", "Taytulla", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tri-Legest Fe 28 Day", "Tri-Legest Fe 28 Day", "Tri-Legest Fe 28 Day", "Tri-Norinyl", "Tri-Norinyl", "Tri-Norinyl", "Tri-Norinyl", "Tulana", "Tulana", "Vyfemla", "Vyfemla", "Wera", "Wera", "Wymzya Fe", "Wymzya Fe", "WYMZYA Fe", "Zenchent", "Zenchent", "Zenchent", "Zenchent 0.4/35", "Zenchent FE", "Zenchent FE", "Zenchent FE", "Zeosa" ]

[ "Conludag", "Micronovum", "Mini-PE", "Mini-pill", "Norcolut", "Noriday", "Norluten", "Norlutin", "Primolut-N", "Utovlan" ]

[ "Loestrin 24 Fe", "Femhrt", "Jinteli", "Zenchent", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Necon 1/35", "Necon", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Necon 777 777", "Necon 777 777", "Necon 777 777", "FEMCON Fe", "Wymzya Fe", "Microgestin Fe", "Microgestin", "Estradiol / Norethindrone Acetate", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho Novum 1/35", "Modicon", "Junel 1.5/30", "Junel Fe 1/20", "Junel Fe 1.5/30", "Ovcon 50", "Ovcon 35", "LOESTRIN Fe 1/20 28 Day", "LOESTRIN Fe 1.5/30 28 Day", "Ovcon 50", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Junel Fe 1.5/30", "Necon 0.5/35", "Modicon", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "Jevantique", "CombiPatch", "Microgestin", "Microgestin Fe", "Microgestin Fe", "Microgestin", "Zenchent FE", "Wymzya Fe", "LOESTRIN 1/20 21 Day", "LOESTRIN Fe 1/20 28 Day", "LOESTRIN 1.5/30 21 Day", "LOESTRIN Fe 1.5/30 28 Day", "LOESTRIN Fe 1/20 28 Day", "LOESTRIN Fe 1.5/30 28 Day", "Lomedia 24 Fe", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Cyclafem 1/35", "Zeosa", "Kaitlib Fe", "Vyfemla", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "FEMCON Fe", "Kaitlib Fe", "FEMCON Fe", "Alyacen 7/7/7", "Alyacen 7/7/7", "Alyacen 7/7/7", "Alyacen 1/35", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Ovcon 35", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Zenchent", "Briellyn", "Norethindrone Acetate and Ethinyl Estradiol", "CombiPatch", "CombiPatch", "Gildess 1/20", "Gildess Fe 1.5/30", "Gildess Fe 1/20", "Gildess 1.5/30", "Gildess 24 Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Zenchent FE", "Necon 777", "Necon 777", "Necon 777", "WYMZYA Fe", "Loestrin 21 1/20", "LOESTRIN Fe 1/20", "Loestrin 21 1.5/30", "LOESTRIN Fe 1.5/30", "Vyfemla", "Hailey 24 Fe", "Norethindrone and ethinyl estradiol", "Norethindrone and Ethinyl Estradiol, and Ferrous Fumarate", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Loestrin 24 Fe", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Hailey 1.5/30", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "Microgestin 24 Fe", "Necon", "Activella", "Activella", "Ovcon 35", "Ovcon 35", "Ortho-novum", "Ortho-novum 10/11", "Ortho-novum 10/11", "Nortrel (21 Day Regimen)", "Modicon", "Femhrt", "Alyacen 7/7/7", "MICROGESTIN Fe 1/20", "TARINA Fe 1/20", "Cyclafem 1/35", "Microgestin 1/20", "MICROGESTIN Fe 1.5/30", "Jevantique Lo", "Hailey Fe 1.5/30", "Zenchent 0.4/35", "Wera", "Dasetta 1/35", "Larin Fe 1.5/30", "Leena", "Leena", "Dasetta 7/7/7", "Dasetta 7/7/7", "Dasetta 7/7/7", "Larin 1.5/30", "Larin 24 Fe", "Larin 1/20", "Norethindrone and Ethinyl Estradiol and Ferrous Fumarate", "Philith", "Tri-Norinyl", "Tri-Norinyl", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Femhrt", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Necon 777", "Necon 777", "Necon 777", "Activella", "Activella", "Larin Fe 1/20", "Jinteli", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Blisovi Fe 1/20", "Melodetta 24 Fe", "Lopreeza", "Lopreeza", "Lopreeza", "Loestrin 21 Day", "Loestrin Fe 28 Day", "Loestrin 21 Day", "Loestrin Fe 28 Day", "Loestrin Fe 28 Day", "Loestrin Fe 28 Day", "Estradiol and Norethindrone Acetate", "Estradiol and Norethindrone Acetate", "TARINA Fe 1/20", "Aurovela 24 Fe", "Balziva", "Aranelle", "Aranelle", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Minastrin 24 Fe", "GENERESS Fe", "GENERESS Fe", "Necon (28 Day Regimen)", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Layolis Fe", "Lo Loestrin Fe", "Cyonanz", "Aurovela Fe 1/20", "Aurovela 1.5/30", "Aurovela 1/20", "Norethindrone Acetate and Ethinyl Estradiol", "Norethindrone Acetate and Ethinyl Estradiol", "Nexesta Fe", "Estradiol / Norethindrone Acetate", "Estradiol / Norethindrone Acetate", "Nylia 1/35", "Taytulla", "Tarina Fe 1/20 EQ", "Tarina 24 Fe", "Cyclafem 1/35", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Cyclafem 7/7/7", "Norethindrone Acetate and Ethinyl Estradiol", "Mimvey Lo", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 7/7/7", "Pirmella 1/35", "Norethindrone Acetate and Ethinyl Estradiol", "Mimvey", "Junel 21 Day", "Junel Fe 28 Day", "Junel 21 Day", "Junel Fe 28 Day", "Blisovi Fe 1.5/30", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Tri-Legest Fe 28 Day", "Tri-Legest Fe 28 Day", "Tri-Legest Fe 28 Day", "Blisovi 24 Fe", "MICROGESTIN Fe 1/20", "Microgestin 1/20", "Microgestin 1.5/30", "MICROGESTIN Fe 1.5/30", "CombiPatch (estradiol/norethindrone acetate transdermal system)", "CombiPatch (estradiol/norethindrone acetate transdermal system)", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Nortrel 21 Day", "Nortrel 28 Day", "Nortrel 28 Day", "Fyavolv", "Fyavolv", "AUROVELA Fe", "Amabelz", "Amabelz", "Norethindrone Acetate and Ethinyl Estradiol", "Junel Fe 24", "Lopreeza", "Nylia 7/7/7", "Nylia 7/7/7", "Nylia 7/7/7", "Lupaneta Pack", "Lupaneta Pack", "Alyacen 1/35", "Charlotte 24Fe", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Junel Fe 1.5/30", "Activella", "Activella", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho-Novum 777", "Ortho Novum 135", "Mibelas 24 Fe", "HAILEY Fe 1/20", "Oriahnn", "Alyacen 7/7/7", "Tri-Norinyl", "Tri-Norinyl", "Alyacen 1/35", "Leena", "Leena", "Brevicon", "Norinyl", "Norinyl", "Zenchent", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Cyclafem 7/7/7", "Gildagia", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "FEMCON Fe", "Minastrin 24 Fe", "Wera", "Lo Minastrin Fe", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Larin Fe 1/20", "Lo Loestrin Fe", "Necon 1/35", "Necon 0.5/35", "Necon 10/11", "Necon 10/11", "Norethindrone Acetate and Ethinyl Estradiol", "ESTROSTEP Fe", "ESTROSTEP Fe", "ESTROSTEP Fe", "Necon 1/35 (28 Day Regimen)", "Larin Fe 1.5/30", "Microgestin", "Microgestin", "Microgestin", "Microgestin", "Junel Fe 1/20", "Microgestin Fe 1/20", "Microgestin 1/20", "Microgestin Fe 1.5/30", "Necon", "Gemmily", "Microgestin 24 Fe", "Microgestin 1.5/30", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Alyacen 1/35", "Tarina Fe 1/20 EQ", "Tarina 24 Fe", "Merzee", "Balziva", "Nortrel 28 Day", "Alyacen 1/35", "Norethindrone Acetate and Ethinyl Estradiol, and Ferrous Fumarate", "Myfembree", "Norethindrone Acetate and Ethinyl Estradiol, and Ferrous Fumarate", "Taysofy", "Norethindrone Acetate and Ethinyl Estradiol", "Loestrin 1.5/30", "Brevicon 0.5/35 Tablets (21-day Pack)", "Minestrin 1/20", "Minestrin 1/20", "Loestrin 1.5/30", "Brevicon 0.5/35 Tablets (28-day Pack)", "Synphasic 21 Tablets", "Synphasic 21 Tablets", "Synphasic 28 Tablets", "Synphasic 28 Tablets", "Brevicon 1/35 Tablets (21-day Pack)", "Brevicon 1/35 Tablets (28-day Pack)", "Select 1/35 (21-day)", "Select 1/35 (28-day)", "Activelle", "Activelle Ld", "Estracomb", "Ortho-novum 1/50 Tablets (21 Day)", "Ortho-novum 1/50 Tablets (28 Day)", "Norinyl 1/50 28 Tab", "Brevicon 0.5/35 21 Tab", "Brevicon 0.5/35 28 Tab", "Norinyl 1/50 -(21-day Regimen)", "Norinyl 1/50 -(28-day Regimen)", "Ortho 10/11 Tablets (21 Day)", "Ortho 10/11 Tablets (21 Day)", "Ortho 10/11 Tablets (28 Day)", "Ortho 10/11 Tablets (28 Day)", "Brevicon 1/35 28 Tab", "Brevicon 1/35 21 Tab", "Norinyl 1/50 21 Tab", "Estalis Sequi", "Estalis Sequi", "Synphasic 21 Tablets", "Synphasic 21 Tablets", "Synphasic-28 Tablets", "Synphasic-28 Tablets", "Generess", "Femhrt", "Estalis 140/50 Mcg", "Estalis 250/50 Mcg", "Ortho 1/35 Tablets (21 Day)", "Ortho 0.5/35 Tablets (21 Day)", "Ortho 1/35 Tablets (28 Day)", "Ortho 0.5/35 Tablets (28 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (21 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Ortho 7/7/7 Tablets (28 Day)", "Lolo", "Junel Fe 28 Day", "Junel Fe 28 Day", "Merzee", "Microgestin Fe 1/20", "Zenchent FE", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Norethindrone Acetate and Ethinyl Estradiol and Ferrous Fumarate", "Finzala", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Nortrel 7/7/7 (28 Day Regimen)", "Junel FE", "Rhuzdah", "Norethindrone and ethinyl estradiol and ferrous fumarate", "Norethindrone and ethinyl estradiol", "Norethindrone acetate and ethinyl estradiol, and ferrous fumarate", "Pirmella 7/7/7", "Etyqa", "Etyqa", "Microgestin Fe 1.5/30", "Hailey Fe 1.5/30", "Nylia 7/7/7", "Myfembree", "Norethindrone Acetate and Ethinyl Estradiol", "Oshih", "Microgestin Fe 1/20", "Microgestin 1.5/30", "Microgestin Fe 1.5/30", "Tilia Fe", "Tilia Fe", "Tilia Fe", "Necon", "Microgestin 1/20", "Microgestin Fe 1.5/30", "Estradiol and Norethindrone Acetate", "Junel Fe 28 Day", "Junel 21 Day", "Femlyv", "Junel Fe 28 Day", "Junel 21 Day", "Ryeqo", "Ryeqo", "Ryeqo", "Ryeqo" ]

[ "P06401", "P10275", "P04150" ]

[ "P08684", "P17516", "P26439", "P18405", "P31213", "Q9H8P0", "P51857", "P33261", "P05177", "P11509" ]

[ "P02768", "P04278" ]

[ "P08183" ]

DB00718

Adefovir dipivoxil

Adefovir dipivoxil, previously called bis-POM PMEA, with trade names Preveon and Hepsera, is an orally-administered acyclic nucleotide analog reverse transcriptase inhibitor (ntRTI) used for treatment of hepatitis B. It is ineffective against HIV-1. Adefovir dipivoxil is the diester prodrug of adefovir.

solid

Indicated for the treatment of chronic hepatitis B in adult patients with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease; this is based on histological, virological, biochemical, and serological responses in adult patients with HBeAg+ and HBeAg- chronic hepatitis B with compensated liver function, and in adult patients with clinical evidence of lamivudine-resistant hepatitis B virus with either compensated or decompensated liver function.

Adefovir dipivoxil a diester prodrug of adefovir. Adefovir is an acyclic nucleotide analog with activity against human hepatitis B virus (HBV). The concentration of adefovir that inhibited 50% of viral DNA synthesis (IC50) in vitro ranged from 0.2 to 2.5 μM in HBV transfected human hepatoma cell lines. The combination of adefovir with lamivudine showed additive anti-HBV activity.

Adefovir dipivoxil is a prodrug of adefovir. Adefovir is an acyclic nucleotide analog of adenosine monophosphate which is phosphorylated to the active metabolite adefovir diphosphate by cellular kinases. Adefovir diphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate deoxyadenosine triphosphate and by causing DNA chain termination after its incorporation into viral DNA. The inhibition constant (Ki) for adefovir diphosphate for HBV DNA polymerase was 0.1 μM. Adefovir diphosphate is a weak inhibitor of human DNA polymerases α and γ with Ki values of 1.18 μM and 0.97μM, respectively.

The approximate oral bioavailability of adefovir from HEPSERA is 59%. When a single oral 10 mg dose is given to chronic hepatitis B patients, the peak plasma concentration (Cmax) of adefovir was 18.4 ± 6.26 ng/mL. This occurred between 0.58 - 4 hours post dose (Tmax). The adefovir area under the plasma concentration-time curve (AUC0–∞) was 220 ± 70.0 ng∙h/mL. Food does not affect the exposure of adeforvir.

Following oral administration, adefovir dipivoxil is rapidly converted to adefovir. 45% of the dose is recovered as adefovir in the urine over 24 hours at steady state following 10 mg oral doses. Adefovir is not a substrate of the cytochrome P450 enzymes.

Renal tubular nephropathy characterized by histological alterations and/or increases in BUN and serum creatinine was the primary dose-limiting toxicity associated with administration of adefovir dipivoxil in animals. Nephrotoxicity was observed in animals at systemic exposures approximately 3–10 times higher than those in humans at the recommended therapeutic dose of 10 mg/day.

Plasma adefovir concentrations declined in a biexponential manner with a terminal elimination half-life of 7.48 ± 1.65 hours.

≤4% over the adefovir concentration range of 0.1 to 25 μg/mL

Adefovir is renally excreted by a combination of glomerular filtration and active tubular secretion.

* 392 ± 75 mL/kg [Vd at steady state, intravenous administration of 1.0 mg/kg/day] * 352 ± 9 mL/kg [Vd at steady state, intravenous administration of 3.0 mg/kg/day]

* 469 ± 99.0 mL/min [Patients with Unimpaired renal Function receiving a 10 mg single dose] * 356 ± 85.6 mL/min [Patients with mild renal impairement receiving a 10 mg single dose] * 237 ± 118 mL/min [Patients with moderate renal impairement receiving a 10 mg single dose] * 91.7 ± 51.3 mL/min [Patients with severe renal impairement receiving a 10 mg single dose]

Organic compounds

Organoheterocyclic compounds

Imidazopyrimidines

Purines and purine derivatives

[ "approved", "investigational" ]

[ "J05AF", "J05A", "J05", "J" ]

[ "Hepatitis B virus" ]

[ { "cost": "30.32", "description": "Hepsera 10 mg tablet", "unit": "tablet" } ]

[ { "approved": "1997-09-02", "country": "United States", "expires": "2014-09-02", "number": "5663159" }, { "approved": "2008-11-18", "country": "Canada", "expires": "2018-07-23", "number": "2298057" }, { "approved": "2003-03-25", "country": "Canada", "expires": "2011-09-12", "number": "2051239" }, { "approved": "2002-09-17", "country": "United States", "expires": "2018-07-23", "number": "6451340" } ]

[ "Aa-adefovir", "Adefovir Dipivoxil", "Adefovir dipivoxil", "Hepsera", "Hepsera", "Hepsera", "Hepsera", "Hepsera" ]

[ "A Di Xian", "A Gan Ding", "Adesera", "Adfovir", "Ailuwei", "Antiva", "Biovir", "Dai Ding", "Dinghe", "Infovir", "Jiule", "Lifuzhi", "Ming Zheng", "Nafasera", "Preveon", "Pymefovir", "Xinfunuo", "Yilaifen" ]

[]

[ "P54819", "P27144", "P15531", "P22392" ]

[]

[ "Q4U2R8", "O15439", "O15440", "O75751" ]

DB00719

Azatadine

Antihistamines such as azatadine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.

solid

For the relief of the symptoms of upper respiratory mucosal congestion in perennial and allergic rhinitis, and for the relief of nasal congestion and eustachian t.b. congestion.

Azatadine is an antihistamine, related to cyproheptadine, with anti-serotonin, anticholinergic (drying), and sedative effects. Azatadine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, azatadine is not used clinically as an anti-psychotic. Antihistamines antagonize the vasodilator effect of endogenously released histamine, especially in small vessels, and mitigate the effect of histamine which results in increased capillary permeability and edema formation. As consequences of these actions, antihistamines antagonize the physiological manifestations of histamine release in the nose following antigen-antibody interaction, such as congestion related to vascular engorgement, mucosal edema, and profuse, watery secretion, and irritation and sneezing resulting from histamine action on afferent nerve terminals.

Antihistamines such as azatadine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.

Well absorbed after oral administration.

Hepatic.

The oral LD50 in mature rats and mice was greater than 1700 mg/kg and 600 mg/kg, respectively. Symptoms of overdose include clumsiness or unsteadiness, seizures, severe drowsiness, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath, shuffling walk, tic-like (jerky) movements of head and face, trembling and shaking of hands, and insomnia.

null

Organic compounds

Organoheterocyclic compounds

Benzocycloheptapyridines

null

[ "approved" ]

[ "R06AX", "R06A", "R06", "R" ]

[ "Humans and other mammals" ]

[]

[ "Optimine Tab 1mg", "Trinalin Repetabs" ]

[ "Idumed", "Optimine", "Zadine" ]

[ "Trinalin Repetabs" ]

[ "P35367" ]

[]

DB00720

Clodronic acid

Clodronic acid is a first generation bisphosphonate similar to [etidronic acid] and [tiludronic acid].[A203111] These drugs were developed to mimic the action of pyrophosphate, a regulator of calcification and decalcification.[A1923] clodronate’s use has decreased over the years in favor of the third generation, nitrogen containing bisphosphonate [zoledronic acid], [ibandronic acid], [minodronic acid], and [risedronic acid].[A203111] Clodronic acid is not FDA approved, but is approved in Canada.[L13910]

solid

Clodronic acid is indicated as an adjunct in the management of osteolysis from bone metastases of malignant tumors and for management of hypercalcemia of malignancy.[L13910]

Clodronic acid is a first generation bisphosphonate that inhibits osteoclast mediated bone resorption.[L13910] It has a wide therapeutic index as a large overdose is required for significant toxicity and a long duration of action due to the slow release from bone.[L13910] Patients should be counselled regarding the risk of hypocalcemia, hypovolemia, renal insufficiency, transient hyperphosphatemia, and transient hyperparathyroidism.[L13910]

Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis.[A959] Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.[A959] Osteoclasts mediate resorption of bone.[A6366] When osteoclasts bind to bone they form podosomes, ring structures of F-actin.[A6366] Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.[A6366] First generation bisphosphonates closely mimic the structure of pyrophosphate, which can be incorporated into ATP anologues that cannot be hydrolyzed, disrupting all ATP mediated actions of osteoclasts.[A203360]

Oral clodronic acid has a bioavailability of 1-2%.[A203378] A 200mg intravenous dose reaches a Cmax of 16.1mg/L with an AUC of 44.2mg\*h/L.[A203378] A 200mg intramuscular dose reaches a Cmax of 12.8mg/L with an AUC of 47.5mg\*h/L.[A203378] Further pharmacokinetic data for clodronic acid are not readily available.[L13910]

Clodronate is not metabolized in humans.[L13910]

Patients experiencing an overdose may present with hypocalcemia, while severe overdoses can present with kidney failure, liver damage, and unconsciousness.[L13910] Overdose can be managed through symptomatic and supportive care, including monitoring and administration of electrolytes including calcium.[L13910] Gastric lavage may remove unabsorbed drug in the gastrointestinal tract.[L13910]

The mean plasma half life of clodronate is 5.6h.[L13910]

Clodronic acid is 36% protein bound in plasma.[A203375]

Clodronate is eliminated unchanged in the urine.[L13910]

null

The renal clearance of clodronate is approximately 90mL/min.[L13910]

Organic compounds

Organic acids and derivatives

Organic phosphonic acids and derivatives

Bisphosphonates

[ "approved", "investigational", "vet_approved" ]

[ "M05BA", "M05B", "M05", "M" ]

[ "Humans and other mammals" ]

[ { "cost": "1.36", "description": "Clasteon 400 mg Capsule", "unit": "capsule" }, { "cost": "2.04", "description": "Bonefos 400 mg Capsule", "unit": "capsule" }, { "cost": "13.69", "description": "Bonefos 60 mg/ml", "unit": "ml" } ]

[]

[ "Bonefos", "Bonefos", "Clasteon", "Ostac Cap 400mg" ]

[ "Lodronat", "Loron", "Lytos", "Ostac", "Sindronat" ]

[]

[ "P12235", "P05141", "P12236" ]

[ "P35354" ]

[]

DB00721

Procaine

A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). Procaine has also been investigated as an oral entry inhibitor in treatment-experienced HIV patients [L1215].

solid

Used as a local anesthetic primarily in oral surgery

Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine.

Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.

null

Hydrolysis by plasma esterases to PABA

null

7.7 minutes

null

With normal kidney function, the drug is excreted rapidly by tubular excretion.

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Benzoic acids and derivatives

[ "approved", "investigational", "vet_approved" ]

[ "N01BA", "N01B", "N01", "N", "C05AD", "C05A", "C05", "C", "S01HA", "S01H", "S01", "S", "N01BA", "N01B", "N01", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.28", "description": "Nesacaine-mpf 2% vial", "unit": "ml" }, { "cost": "1.34", "description": "Nesacaine-mpf 3% vial", "unit": "ml" }, { "cost": "1.76", "description": "Procaine hcl crystals", "unit": "g" }, { "cost": "1.79", "description": "Novocain 1% ampul", "unit": "ml" }, { "cost": "2.4", "description": "Novocain 10% ampul", "unit": "ml" }, { "cost": "0.15", "description": "Procaine hcl 2% vial", "unit": "ml" }, { "cost": "0.26", "description": "Chloroprocaine 2% vial", "unit": "ml" }, { "cost": "0.33", "description": "Chloroprocaine 3% vial", "unit": "ml" }, { "cost": "0.72", "description": "Nesacaine 1% vial", "unit": "ml" }, { "cost": "0.74", "description": "Nesacaine 2% vial", "unit": "ml" } ]

[]

[ "Novocain", "Novocain", "Novocain", "Novocain 20 mg/ml", "Novocain Liq 2%", "Novocaine", "Procaine Hydrochloride" ]

[]

[ "Q9Y5Y9", "Q8TCU5", "P46098", "Q01959", "Q15822", "Q12791", "Q16558", "Q9Y691", "Q9NPA1", "Q86W47", "O15554", "Q92952", "Q9H2S1", "Q9UGI6", "P47712", "Q86U10", "P21397", "P27338", "P26358", "Q9Y6K1" ]

[ "P06276" ]

[]

[ "Q01959", "P23975", "P31645" ]

DB00722

Lisinopril

Lisinopril is an angiotensin converting enzyme inhibitor (ACEI) used to treat hypertension, heart failure, and myocardial infarction.[L8384,L8387,L8390] Lisinopril and [captopril] are the only ACEIs that are not prodrugs.[A184853] It functions by inhibition of angiotensin converting enzyme as well as the renin angiotensin aldosterone system.[A184781,A184808,A184817] ACEIs are commonly used as a first line therapy in the treatment of hypertension, along with thiazide diuretics or beta blockers.[A184844] Lisinopril was granted FDA approval on 29 December 1987.[L8384]

solid

Lisinopril is indicated for the treatment of acute myocardial infarction, hypertension in patients ≥6 years, and as an adjunct therapy for heart failure.[L8384,L8387] A combination product with hydrochlorothiazide is indicated for the treatment of hypertension.[L8390]

Lisinopril is an angiotensin converting enzyme inhibitor used to treat hypertension, heart failure, and myocardial infarction.[L8384,L8387,L8390] Lisinopril is not a prodrug, and functions by inhibition of angiotensin converting enzyme as well as the renin angiotensin aldosterone system.[A184781,A184808,A184817] It has a wide therapeutic index and a long duration of action as patients are generally given 10-80mg daily.[L8384,L8387,L8390]

Angiotensin II constricts coronary blood vessels and is positively inotropic, which under normal circumstances, would increase vascular resistance and oxygen consumption.[A184781] This action can eventually lead to myocyte hypertrophy and vascular smooth muscle cell proliferation.[A184781] Lisinopril is an angiotensin converting enzyme inhibitor (ACEI), preventing the conversion of angiotensin I to angiotensin II.[A184781,A184808] This action prevents myocyte hypertrophy and vascular smooth muscle cell proliferation seen in untreated patients.[A184808] Increased levels of bradykinin also exhibit vasodilating effects for patients taking ACEIs.[A184808] Lisinopril also inhibits renin's conversion of angiotensin to angiotensin I.[A184817]

Lisinopril is 6-60% orally bioavailable with an average of 25% bioavailability.[A184754,L8384,L8387,L8390] Lisinopril reaches a Cmax of 58ng/mL with a Tmax of 6-8h.[A184754] Lisinopril's absorption is not affected by food.[A184754]

Lisinopril is not metabolized and is excreted as the unchanged drug.[L8384,L8387,L8390]

The oral and subcutaneous LD50 in rats is >8500mg/kg and in mice is >9100mg/kg.[L8399] The oral LDLO in women is 1200µg/kg/16D and in men is 43mg/kg/43W.[L8399] Patients experiencing an overdose of lisinopril may present with hypotension.[L8384,L8387,L8390] Patients should be treated with intravenous saline to restore blood pressure.[L8384,L8387,L8390] Lisinopril can be removed from the blood by hemodialysis due to it not being protein bound.[L8384,L8387,L8390]

Lisinopril has an effective half life of accumulation of 12.6h[A184754,L8384,L8387,L8390] and a terminal half life of 46.7h.[A184754]

Lisinopril has not been demonstrated to bind to serum proteins.[L8384,L8387,L8390]

Lisinopril is entirely eliminated exclusively in the urine.[L8384,L8387,L8390]

The apparent volume of distribution of lisinopril is 124L.[A184781]

A 30kg child has a typical clearance of 10L/h, which increases with renal function.[L8384,L8387] The mean renal clearance of lisinopril in healthy adult males is 121mL/min.[A184754]

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved", "investigational" ]

[ "C09BA", "C09B", "C09", "C", "C10BX", "C10B", "C10", "C", "C09AA", "C09A", "C09", "C", "C09BB", "C09B", "C09", "C" ]

[ "Humans and other mammals" ]

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Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorthiazide", "Lisinopril Tablets", "Lisinopril Tablets", "Lisinopril Tablets", "Lisinopril Tablets USP", "Lisinopril Tablets USP", "Lisinopril Tablets USP", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril/HCTZ", "Lisinopril/hctz (type Z)", "Lisinopril/hctz (type Z)", "Lisinopril/hctz (type Z)", "Lisinoril", "Lisnopril/hctz (type P)", "Lisnopril/hctz (type P)", "Lisnopril/hctz (type P)", "Lytensopril", "Lytensopril-90", "Mar-lisinopril", "Mar-lisinopril", "Mar-lisinopril", "Mint-lisinopril", "Mint-lisinopril", "Mint-lisinopril", "Mylan-lisinopril", "Mylan-lisinopril", "Mylan-lisinopril", "Mylan-lisinopril Hctz", "Mylan-lisinopril Hctz", "Mylan-lisinopril Hctz", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type Z)", "Ntp-lisinopril/hctz (type Z)", "Ntp-lisinopril/hctz (type Z)", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril", "Nu-lisinopril/hctz", "Nu-lisinopril/hctz", "Nu-lisinopril/hctz", "PMS-lisinopril", "PMS-lisinopril", "PMS-lisinopril", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinivil", "Prinzide", "Prinzide", "Prinzide", "Prinzide", "Prinzide", "Prinzide", "Pro-lisinopril - 10", "Pro-lisinopril - 20", "Pro-lisinopril - 5", "Qbrelis", "Ratio-lisinopril P", "Ratio-lisinopril P", "Ratio-lisinopril P", "Ratio-lisinopril Z", "Ratio-lisinopril Z", "Ratio-lisinopril Z", "Riva-lisinopril", "Riva-lisinopril", "Riva-lisinopril", "Sandoz Lisinopril", "Sandoz Lisinopril", "Sandoz Lisinopril", "Sandoz Lisinopril HCT", "Sandoz Lisinopril HCT", "Sandoz Lisinopril HCT", "Taro-lisinopril", "Taro-lisinopril", "Taro-lisinopril", "Teva-lisinopril (type P)", "Teva-lisinopril (type P)", "Teva-lisinopril (type P)", "Teva-lisinopril (type Z)", "Teva-lisinopril (type Z)", "Teva-lisinopril (type Z)", "Teva-lisinopril/hctz (type P)", "Teva-lisinopril/hctz (type P)", "Teva-lisinopril/hctz (type P)", "Teva-lisinopril/hctz (type Z)", "Teva-lisinopril/hctz (type Z)", "Teva-lisinopril/hctz (type Z)", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestoretic", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril", "Zestril" ]

[ "Acebitor", "Acemin", "Acerbon", "Acinopril", "Bellisin", "Biopril", "Dapril", "Fibsol", "Fisopril", "Hipril", "Linopril", "Lisipril", "Noperten", "Presiten", "Ranolip", "Ranopril", "Rantex", "Sinopren", "Sinopril", "Tensopril" ]

[ "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lytensopril", "Lytensopril-90", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Prinzide", "Prinzide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorthiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Zestoretic", "Zestoretic", "Zestoretic", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Prinzide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril/HCTZ", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Zestoretic", "Zestoretic", "Zestoretic", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril with Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Prinzide", "Prinzide", "Prinzide", "Zestoretic", "Zestoretic", "Zestoretic", "Apo-lisinopril/hctz", "Apo-lisinopril/hctz", "Apo-lisinopril/hctz", "Nu-lisinopril/hctz", "Nu-lisinopril/hctz", "Nu-lisinopril/hctz", "Teva-lisinopril/hctz (type Z)", "Teva-lisinopril/hctz (type Z)", "Teva-lisinopril/hctz (type Z)", "Teva-lisinopril/hctz (type P)", "Teva-lisinopril/hctz (type P)", "Teva-lisinopril/hctz (type P)", "Sandoz Lisinopril HCT", "Sandoz Lisinopril HCT", "Sandoz Lisinopril HCT", "Ava-lisinopril HCT", "Ava-lisinopril HCT", "Ava-lisinopril HCT", "Lisnopril/hctz (type P)", "Lisnopril/hctz (type P)", "Lisnopril/hctz (type P)", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type P)", "Ntp-lisinopril/hctz (type Z)", "Ntp-lisinopril/hctz (type Z)", "Ntp-lisinopril/hctz (type Z)", "Lisinopril/hctz (type Z)", "Lisinopril/hctz (type Z)", "Lisinopril/hctz (type Z)", "Mylan-lisinopril Hctz", "Mylan-lisinopril Hctz", "Mylan-lisinopril Hctz", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide", "Lisinopril and Hydrochlorothiazide" ]

[ "P12821", "P00797" ]

[]

[ "P46059", "Q16348" ]

DB00723

Methoxamine

An alpha-adrenergic agonist that causes prolonged peripheral vasoconstriction. It has little if any direct effect on the central nervous system.

solid

Indicated for the treatment and management of hypotension.

Methoxamine is a potent sympathomimetic amine that increases both systolic and diastolic blood pressure. Methoxamine is indicated for prevention and treatment of the acute hypotensive state occurring with spinal anesthesia. It is also indicated as adjunctive treatment of hypotension due to hemorrhage, reactions to medications, surgical complications, and shock associated with brain damage due to trauma or tumor. Methoxamine acts on both α1-adrenergic receptors but appears to have no effect on β-adrenergic receptors. It acts by increasing the force of the heart's pumping action as well as constricting peripheral blood vessels.

Methoxamine acts through peripheral vasoconstriction by acting as a pure alpha-1 adrenergic receptor agonist, consequently increasing systemic blood pressure (both systolic and diastolic).

null

Low

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Methoxybenzenes

[ "approved", "investigational" ]

[ "C01CA", "C01C", "C01", "C" ]

[ "Humans and other mammals" ]

[]

[ "Vasoxyl Inj 20mg/ml" ]

[ "Mexan", "Vasoxine", "Vasoxyl" ]

[]

[ "P35348", "P25100", "P35368" ]

[]

DB00724

Imiquimod

Imiquimod is an immune response modifier that acts as a toll-like receptor 7 agonist. Imiquimod is commonly used topically to treat warts on the skin of the genital and anal areas. Imiquimod does not cure warts, and new warts may appear during treatment. Imiquimod does not fight the viruses that cause warts directly, however, it does help to relieve and control wart production. Miquimod is also used to treat a skin condition of the face and scalp called actinic keratoses and certain types of skin cancer called superficial basal cell carcinoma.

solid

For the topical treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adults. Also indicated for the treatment of external genital and perianal warts/condyloma acuminata in individuals 12 years old and above.

Imiquimod is an immune response modifier that acts as a toll-like receptor 7 agonist. Imiquimod is commonly used topically to treat warts on the skin of the genital and anal areas. Imiquimod does not cure warts, and new warts may appear during treatment. Imiquimod does not fight the viruses that cause warts directly, however, it does help to relieve and control wart production. It is not used on warts inside the vagina, penis, or rectum. Imiquimod is also used to treat a skin condition of the face and scalp called actinic keratoses. Imiquimod can also be used to treat certain types of skin cancer called superficial basal cell carcinoma. Imiquimod is particularly useful on areas where surgery or other treatments may be difficult, complicated or otherwise undesirable, especially the face and lower legs.

Imiquimod's mechanism of action is via stimulation of innate and acquired immune responses, which ultimately leads to inflammatory cell infiltration within the field of drug application followed by apoptosis of diseased tissue. Imiquimod does not have direct antiviral activity. Studies of mice show that imiquimod may induce cytokines, including interferon-alpha (IFNA) as well as several IFNA genes (IFNA1, IFNA2, IFNA5, IFNA6, and IFNA8) as well as the IFNB gene. Imiquimod also induced the expression of interleukin (IL)-6, IL-8, and tumor necrosis factor alpha genes. In the treatment of basal cell carcinoma, Imiquimod appears to act as a toll-like receptor-7 agonist, and is thought to exert its anti-tumor effect via modification of the immune response and stimulation of apoptosis in BCC cells. In treating basal cell carcinoma it may increase the infiltration of lymphocytes, dendritic cells, and macrophages into the tumor lesion.

Well absorbed through skin (as a cream)

null

Symptoms of overdose include flu-like symptoms, such as fever, fatigue, headache, nausea, diarrhoea and muscle pain.

20 hours (topical dose), 2 hours (subcutaneous dose)

null

Organic compounds

Organoheterocyclic compounds

Quinolines and derivatives

Imidazoquinolines

[ "approved", "investigational" ]

[ "D06BB", "D06B", "D06", "D" ]

[ "Humans and other mammals" ]

[ { "cost": "24.43", "description": "Zyclara 3.75% cream", "unit": "each" }, { "cost": "26.04", "description": "Aldara 5% cream", "unit": "each" }, { "cost": "33.17", "description": "Imiquimod 5% cream", "unit": "each" }, { "cost": "42.89", "description": "Imiquimod 5% Cream Packet", "unit": "packet" }, { "cost": "46.99", "description": "Aldara 5% Cream Pack", "unit": "pack" } ]

[ { "approved": "1987-08-25", "country": "United States", "expires": "2009-08-25", "number": "4689338" }, { "approved": "2010-04-13", "country": "United States", "expires": "2024-10-01", "number": "7696159" }, { "approved": "2012-07-17", "country": "United States", "expires": "2029-12-11", "number": "8222270" }, { "approved": "2012-08-07", "country": "United States", "expires": "2029-12-11", "number": "8236816" }, { "approved": "2012-10-30", "country": "United States", "expires": "2029-12-11", "number": "8299109" }, { "approved": "2013-12-03", "country": "United States", "expires": "2029-08-18", "number": "8598196" }, { "approved": "2019-03-26", "country": "United States", "expires": "2029-08-18", "number": "10238645" }, { "approved": "2019-03-26", "country": "United States", "expires": "2029-12-11", "number": "10238644" }, { "approved": "2021-02-16", "country": "United States", "expires": "2030-04-30", "number": "10918635" }, { "approved": "2021-12-21", "country": "United States", "expires": "2030-04-30", "number": "11202752" }, { "approved": "2009-12-11", "country": "United States", "expires": "2029-12-11", "number": "11318130" }, { "approved": "2010-04-30", "country": "United States", "expires": "2030-04-30", "number": "11850245" } ]

[ "Aldara", "Aldara", "Aldara", "Aldara", "Aldara", "Aldara", "Aldara P", "Apo-imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod", "Imiquimod 5% / Levocetirizine Dihydrochloride 1% / Niacinamide 2%", "Imiquimod 5% / Levocetirizine Dihydrochloride 1% / Tretinoin 0.05%", "Imiquimod 5% / Niacinamide 4%", "Imiquimod 5% / Salicylic Acid 30% / Tretinoin 0.1%", "Imiquimod 5% / Tretinoin 0.025%", "Taro-imiquimod", "Taro-imiquimod Pump", "Truemed Group LLC", "Vyloma", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara", "Zyclara" ]

[ "Beselna", "Imimore", "Imiquad", "Labimiq", "Li Di", "Miquimod", "Nan Bo", "Nilwart", "Omiquidar", "Tian Rui", "Vetland", "You Care", "Youbiqing" ]

[ "Imiquimod 5% / Levocetirizine Dihydrochloride 1% / Niacinamide 2%", "Imiquimod 5% / Levocetirizine Dihydrochloride 1% / Tretinoin 0.05%", "Imiquimod 5% / Niacinamide 4%", "Imiquimod 5% / Tretinoin 0.025%", "Imiquimod 5% / Salicylic Acid 30% / Tretinoin 0.1%" ]

[ "Q9NYK1", "Q9NR97" ]

[ "P08684" ]

[]

DB00725

Homatropine methylbromide

Homatropine methylbromide is a quaternary ammonium muscarinic acetylcholine receptor antagonist belonging to the group of medicines called anti-muscarinics. Homatropine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.

solid

Used in conjunction with antacids or histamine H2-receptor antagonists in the treatment of peptic ulcers, gastric ulcers and duodenal ulcers, to reduce further gastric acid secretion and delay gastric emptying.

Homatropine methylbromide belongs to the group of medicines called anti-muscarinics. Homatropine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness.

Homatropine is a quaternary ammonium muscarinic acetylcholine receptor antagonist. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Homatropine methylbromide inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These postganglionic receptor sites are present in the autonomic effector cells of the smooth muscle, cardiac muscle, sinoatrial and atrioventricular nodes, and exocrine glands. Depending on the dose, anticholinergics may reduce the motility and secretory activity of the gastrointestinal system, and the tone of the ureter and urinary bladder and may have a slight relaxant action on the bile ducts and gallbladder.

null

Organic compounds

Alkaloids and derivatives

Tropane alkaloids

null

[ "approved" ]

[ "A03CB", "A03C", "A03", "A", "A03BB", "A03B", "A03", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "1.4", "description": "Hycodan tablet", "unit": "each" }, { "cost": "2.69", "description": "Homatropine hbr crystals", "unit": "g" }, { "cost": "3.82", "description": "Homatropaire 5% eye drops", "unit": "ml" }, { "cost": "5.57", "description": "Isopto homatropine 2% drops", "unit": "ml" }, { "cost": "6.06", "description": "Homatropine hbr 5% eye drop", "unit": "ml" }, { "cost": "6.41", "description": "Isopto homatropine 5% drops", "unit": "ml" } ]

[]

[ "Acidobyl", "Antitussive hydrocodone bitartrate and homatropine methylbromide", "Debiline H", "Hycodan", "Hycodan", "Hycodan", "Hycodan", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydromet", "Hydromet", "Tussigon", "Tussigon" ]

[]

[ "Antitussive hydrocodone bitartrate and homatropine methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Tussigon", "Tussigon", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydromet", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hycodan", "Hydromet", "Hycodan", "Hycodan", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hycodan", "Acidobyl", "Debiline H", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide", "Hydrocodone Bitartrate and Homatropine Methylbromide" ]

[ "P08172", "P11229", "P08173", "P08912", "P20309" ]

[]

DB00726

Trimipramine

Tricyclic antidepressant similar to imipramine, but with more antihistaminic and sedative properties.

solid

For the treatment of depression and depression accompanied by anxiety, agitation or sleep disturbance

Trimipramine is a tricyclic antidepressant. It was thought that tricyclic antidepressants work by inhibiting the re-uptake of the neurotransmitters norepinephrine and serotonin by nerve cells. However, this response occurs immediately, yet mood does not lift for around two weeks. It is now thought that changes occur in receptor sensitivity in the cerebral cortex and hippocampus. The hippocampus is part of the limbic system, a part of the brain involved in emotions. Presynaptic receptors are affected: a1 and b1 receptors are sensitized, a2 receptors are desensitised (leading to increased noradrenaline production). Tricyclics are also known as effective analgesics for different types of pain, especially neuropathic or neuralgic pain. A precise mechanism for their analgesic action is unknown, but it is thought that they modulate anti-pain opioid systems in the CNS via an indirect serotonergic route. They are also effective in migraine prophylaxis, but not in abortion of acute migraine attack. The mechanism of their anti-migraine action is also thought to be serotonergic.

Trimipramine's mechanism of action differs from other tricyclic antidepressants. Trimipramine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).

Rapid absorption

Hepatic

Side effects include agitation, coma, confusion, convulsions, dilated pupils, disturbed concentration, drowsiness, hallucinations, high fever, irregular heart rate, low body temperature, muscle rigidity, overactive reflexes, severely low blood pressure, stupor, vomiting

11-18 hrs

93%-96% (to plasma proteins)

null

Organic compounds

Organoheterocyclic compounds

Benzazepines

Dibenzazepines

[ "approved" ]

[ "N06AA", "N06A", "N06", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.92", "description": "Trimipramine 25 mg capsule", "unit": "capsule" }, { "cost": "2.49", "description": "Surmontil 25 mg capsule", "unit": "capsule" }, { "cost": "3.14", "description": "Trimipramine 50 mg capsule", "unit": "capsule" }, { "cost": "3.27", "description": "Trimipramine Maleate 50 mg capsule", "unit": "capsule" }, { "cost": "4.15", "description": "Surmontil 50 mg capsule", "unit": "capsule" }, { "cost": "5.92", "description": "Surmontil 100 mg capsule", "unit": "capsule" }, { "cost": "51.0", "description": "Trimipramine maleate powder", "unit": "g" } ]

[]

[ "Apo-trimipramine", "Apo-trimipramine", "Apo-trimipramine", "Apo-trimipramine", "Apo-trimipramine", "Novo-tripramine Tab 100mg BP", "Novo-tripramine Tab 25mg BP", "Novo-tripramine Tab 50mg BP", "Nu-trimipramine Tab 100mg", "Nu-trimipramine Tab 12.5mg", "Nu-trimipramine Tab 25mg", "Nu-trimipramine Tab 50mg", "Rhotrimine", "Rhotrimine", "Rhotrimine", "Rhotrimine", "Rhotrimine", "Surmontil", "Surmontil", "Surmontil", "Surmontil", "Surmontil", "Surmontil 100", "Surmontil 12.5", "Surmontil 75", "Trimipramine", "Trimipramine", "Trimipramine", "Trimipramine", "Trimipramine", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Maleate", "Trimipramine Tab 100mg", "Trimipramine Tab 12.5mg", "Trimipramine Tab 25mg", "Trimipramine Tab 50mg", "Trimipramine-75 - Cap 75mg" ]

[ "Herphonal", "Sapilent", "Stangyl", "Trimidura", "Trimineurin", "Tripress", "Tydamine" ]

[]

[ "P31645", "P23975", "Q01959", "P28223", "P08908", "P35348", "P35368", "P14416", "P18089", "P35367", "P28335", "P46098", "P28221", "P08913", "P21728", "P21918", "P08588", "P07550", "P13945", "P11229", "P08172", "P20309", "P08173", "P08912" ]

[ "P11712", "P10635", "P33261" ]

[]

[ "P08183" ]

DB00727

Nitroglycerin

Nitroglycerin, also known as glyceryl trinitrate,[A180169] is an organic nitrate and a vasodilating agent [L38369] that was first discovered in 1847.[A249965] Originally used to dynamite, its antianginal effects were identified in the late 1860s after it produced headaches in factory workers while workers with angina pectoris or heart failure experienced relief from chest pain.[A180166,A180172] Its use as a treatment for angina dates back to 1879 and is still used to treat and prevent angina.[A249970] Nitroglycerin causes vasodilation in both arteries and veins.[A180172] Nitroglycerin is used in a variety of different conditions, including angina pectoris due to coronary artery disease,[L7102,L7141,L38369,L42320] peri-operative hypertension, congestive heart failure,[L7099] and chronic anal fissure.[L42445] It is also used to induce intraoperative hypotension.[L7099]

liquid

Sublingual nitroglycerin is indicated for the acute relief of an attack or acute prophylaxis of angina pectoris due to coronary artery disease.[L7102,L38369,L42320] Transdermal nitroglycerin is indicated for the prevention of angina pectoris due to coronary artery disease.[L7141] Intravenous nitroglycerin is indicated for the treatment of peri-operative hypertension; for control of congestive heart failure in the setting of acute myocardial infarction; for treatment of angina pectoris in patients who have not responded to sublingual nitroglycerin and beta (β)-blockers; and for induction of intraoperative hypotension.[L7099] Topical nitroglycerin ointment is used to treat moderate to severe pain associated with chronic anal fissure.[L42445]

Nitroglycerin causes the relaxation of vascular smooth muscles, causing arteriolar and venous dilatation.[L38369] It increases blood flow to the myocardium and reduces cardiac preload and afterload, decreasing myocardial wall stress and ameliorating anginal symptoms.[A180172,A249970,L7102] Nitroglycerin also reduces coronary artery spasm, decreasing systemic vascular resistance as well as systolic and diastolic blood pressure.[L38369] Like other organic nitrates, repeated and prolonged administration of nitroglycerin can lead to the development of tolerance or desensitization of vascular smooth muscle to further nitroglycerin-induced vasorelaxation. This loss of efficacy may be associated with the inhibition of mitochondrial aldehyde dehydrogenase, which is an important enzyme involved in the bioactivation of nitroglycerin.[A180166,A180169,A180172] Nitroglycerin tolerance may be accompanied by pro-oxidant effects, endothelial dysfunction, and increased sensitivity to vasoconstrictors.[A180172]

Nitroglycerin is converted by mitochondrial aldehyde dehydrogenase in smooth muscle cells to nitric oxide (NO), a potent vasodilator. NO activates the enzyme guanylate cyclase, which converts guanosine triphosphate (GTP) to cyclic guanosine 3',5'-monophosphate (cGMP) in vascular smooth muscle and other tissues.[A180166,A180169,A249970] cGMP is an endogenous vasodilator of vascular smooth muscle:[A180172] it causes protein kinase-dependent phosphorylation and activates downstream cascades that promote relaxation and increased blood flow in veins, arteries and cardiac tissue.[A180172,A249970] An _in vitro_ study using mouse aorta suggests that nitric oxide, an active metabolite of nitroglycerin, targets the natriuretic peptide receptors.[A5526]

Nitroglycerin is rapidly absorbed and is often used in emergency situations for this reason.[A249970] After a sublingual dose of 0.5 mg of nitroglycerin in patients with ischemic heart disease, the peak concentration (Cmax) was 2.56 ng/mL and the mean Tmax was 4.4 minutes.[A180175] The Cmax following a 0.6mg dose of sublingual nitroglycerin was 2.1 ng/mL and the Tmax was 7.2 minutes.[L38369] The absolute bioavailability following sublingual administration was about 40%. The bioavailability of nitroglycerin depends on several factors, such as mucosal metabolism and hydration status, which both affect the absorption of sublingual drugs.[L38369]

Mitochondrial aldehyde dehydrogenase 2 (ALDH2) promotes the bioactivation of nitroglycerin. Nitroglycerin is metabolized to nitrite; 1,2-glyceryl dinitrate; and 1,3 glyceryl dinitrate.[A180166,A180265,L7099] Nitrite is further metabolized to nitric oxide. 1,2- and 1,3-dinitroglycerols are less biologically active than nitroglycerin but they have longer half-lives, which explains some prolonged effects of nitrates. Both dinitrates are finally metabolized to glycerol, carbon dioxide, and mononitrates that do not have vasodilatory actions.[A180184,L7099] Nitroglycerin can also chemically react with a thiol to generate an intermediate S-nitrosothiol, which resulted in further production of nitric oxide.[A180166,A180172,A180265]

The oral LD50 of nitroglycerin in rats is 105 mg/kg and the LD50 of the intravenous form in rats is 23.2 mg/kg.[L7105] Nitrate overdosage can result in following conditions: severe hypotension, persistent throbbing headache, vertigo, palpitation, visual disturbance, flushing and perspiring skin (later becoming cold and cyanotic), nausea and vomiting (possibly with colic and even bloody diarrhea), syncope (especially in the upright posture), methemoglobinemia with cyanosis and anorexia, initial hyperpnea, dyspnea and slow breathing, slow pulse (dicrotic and intermittent), heart block, increased intracranial pressure with cerebral symptoms of confusion and moderate fever, paralysis and coma followed by clonic convulsions, and possibly death due to circulatory collapse.[L38369] Methemoglobinemia can rarely occur at conventional doses of organic nitrates. This condition is dose-related and it can be even more pronounced in patients with genetic abnormalities of hemoglobin that favor methemoglobin formation. Methemoglobinemia can be managed with the administration of methylene blue unless the patient has a known G-6-PD deficiency.[L38369] There are no known antidotes to an overdose of nitroglycerin, and it is not known whether its metabolites can be removed from the circulation.[L38369,L7099] Hypotension associated with nitroglycerin overdose can be managed with different symptomatic and supportive measures, including the elevation of the lower limbs, administration of intravenous saline or other fluids to maintain central fluid volume, and administration of oxygen and artificial ventilation. Gastric lavage may be used in case of ingestion of excess nitroglycerin.[L38369]

Following intravenous administration, the plasma half-life is about three minutes.[A180178,L7099] The estimated plasma half-life following sublingual administration is approximately six minutes.[A180175] The elimination half-lives of metabolites 1,2-dinitroglycerin and 1,3-dinitroglycerin range between 32 to 26 minutes.[L38369]

After a sublingual dose of nitroglycerin, at concentrations in the plasma ranging from 50 to 500 ng/mL, plasma protein binding of nitroglycerin is about 60%. The plasma protein binding of the metabolites 1,2-dinitroglycerin is 60% and that of 1,3-dinitroglycerin is 30%.[L38369]

Metabolism is the main route by which nitroglycerin is eliminated from the body.[L38369]

The volume of distribution of nitroglycerin is 3 L/kg.[L7099]

The estimated clearance following intravenous administration is 1 L/kg/min.[L7099] The apparent clearance after a sublingual dose was 21.9 L/min in a pharmacokinetic study of patients with ischemic heart disease and angina.[A180175]

Organic compounds

Organic oxygen compounds

Organic oxoanionic compounds

Organic nitrates

[ "approved", "investigational" ]

[ "C01DA", "C01D", "C01", "C", "C01DA", "C01D", "C01", "C", "C05AE", "C05A", "C05", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "1.0", "description": "Nitroglycerin er 9 mg capsule", "unit": "capsule" }, { "cost": "1.16", "description": "Nitro-Dur 0.8 0.8 mg/hr Patch", "unit": "patch" }, { "cost": "1.27", "description": "Nitroglycerin CR 9 mg capsule", "unit": "capsule" }, { "cost": "1.64", "description": "Nitroglycerin 0.1 mg/hr Patches", "unit": "patch" }, { "cost": "1.66", "description": "Nitroglycerin CR 6.5 mg capsule", "unit": "capsule" }, { "cost": "2.84", "description": "Minitran 0.1 mg/hr patch", "unit": "patch" }, { "cost": "2.89", "description": "Minitran 0.2 mg/hr patch", "unit": "patch" }, { "cost": "3.24", "description": "Minitran 0.4 mg/hr patch", "unit": "patch" }, { "cost": "3.4", "description": "Nitro-dur 0.1 mg/hr patch", "unit": "patch" }, { "cost": "3.45", "description": "Nitro-dur 0.2 mg/hr patch", "unit": "patch" }, { "cost": "3.51", "description": "Minitran 0.6 mg/hr patch", "unit": "patch" }, { "cost": "3.87", "description": "Nitro-dur 0.3 mg/hr patch", "unit": "patch" }, { "cost": "3.87", "description": "Nitro-dur 0.4 mg/hr patch", "unit": "patch" }, { "cost": "4.19", "description": "Nitro-dur 0.6 mg/hr patch", "unit": "patch" }, { "cost": "4.19", "description": "Nitro-dur 0.8 mg/hr patch", "unit": "patch" }, { "cost": "9.5", "description": "Nitroglycerin 25 0.4 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "19.31", "description": "Nitrostat 25 0.4 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "22.99", "description": "Nitroglycerin 100 0.3 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "23.99", "description": "Nitroglycerin 100 0.6 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "24.99", "description": "Nitrostat 100 0.6 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "27.75", "description": "Nitrostat 100 0.3 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "28.5", "description": "Nitromist 400 mcg spray", "unit": "g" }, { "cost": "29.88", "description": "Nitrostat 100 0.4 mg Sublingual Tabs Bottle", "unit": "bottle" }, { "cost": "50.44", "description": "Nitroglycerin 30 0.2 mg/hr Patches Box", "unit": "box" }, { "cost": "57.62", "description": "Nitroglycerin 30 0.4 mg/hr Patches Box", "unit": "box" }, { "cost": "62.38", "description": "Nitroglycerin 5 mg/ml kit", "unit": "kit" }, { "cost": "63.55", "description": "Nitroglycerin 30 0.6 mg/hr Patches Box", "unit": "box" }, { "cost": "92.36", "description": "Minitran 30 0.1 mg/hr Patches Box", "unit": "box" }, { "cost": "93.86", "description": "Minitran 30 0.2 mg/hr Patches Box", "unit": "box" }, { "cost": "105.18", "description": "Minitran 30 0.4 mg/hr Patches Box", "unit": "box" }, { "cost": "105.6", "description": "Nitro-Dur 30 0.2 mg/hr Patches Box", "unit": "box" }, { "cost": "106.09", "description": "Nitro-Dur 30 0.1 mg/hr Patches Box", "unit": "box" }, { "cost": "114.01", "description": "Minitran 30 0.6 mg/hr Patches Box", "unit": "box" }, { "cost": "117.1", "description": "Nitro-Dur 30 0.4 mg/hr Patches Box", "unit": "box" }, { "cost": "120.68", "description": "Nitro-Dur 30 0.3 mg/hr Patches Box", "unit": "box" }, { "cost": "130.86", "description": "Nitro-Dur 30 0.6 mg/hr Patches Box", "unit": "box" }, { "cost": "130.86", "description": "Nitro-Dur 30 0.8 mg/hr Patches Box", "unit": "box" }, { "cost": "141.43", "description": "Nitrolingual 0.4 mg/spray Solution 4.9 gm Bottle", "unit": "bottle" }, { "cost": "242.83", "description": "Nitrolingual 0.4 mg/spray Solution 12 gm Bottle", "unit": "bottle" }, { "cost": "0.02", "description": "Ntg 50 mg/500 ml in d5w", "unit": "ml" }, { "cost": "0.04", "description": "Mylan-Nitro 0.4 mg/dose Metered Dose Spray", "unit": "dose" }, { "cost": "0.04", "description": "Ntg 25 mg/250 ml in d5w", "unit": "ml" }, { "cost": "0.04", "description": "Rho-Nitro Pumpspray 0.4 mg/dose Metered Dose Spray", "unit": "dose" }, { "cost": "0.07", "description": "Nitrostat 0.3 mg tablet sl", "unit": "tablet" }, { "cost": "0.08", "description": "Nitrolingual Pumpspray 0.4 mg/dose Metered Dose Spray", "unit": "dose" }, { "cost": "0.08", "description": "Nitroquick 0.4 mg tablet sl", "unit": "tablet" }, { "cost": "0.08", "description": "Nitroquick 0.6 mg tablet sl", "unit": "tablet" }, { "cost": "0.13", "description": "Nitrostat 0.3 mg Sublingual Tablet", "unit": "tablet" }, { "cost": "0.13", "description": "Nitrostat 0.6 mg Sublingual Tablet", "unit": "tablet" }, { "cost": "0.14", "description": "Nitroglycerin 0.3 mg tablet sl", "unit": "tablet" }, { "cost": "0.14", "description": "Nitroglycerin 0.6 mg tablet sl", "unit": "tablet" }, { "cost": "0.16", "description": "Nitrostat 0.6 mg tablet sl", "unit": "tablet" }, { "cost": "0.17", "description": "Nitroglycerin 2% ointment", "unit": "g" }, { "cost": "0.18", "description": "Nitroglycerin 2.5 mg capsule sa", "unit": "capsule" }, { "cost": "0.19", "description": "Nitroquick 0.3 mg tablet sl", "unit": "tablet" }, { "cost": "0.22", "description": "Nitroglycerin 6.5 mg capsule sa", "unit": "capsule" }, { "cost": "0.28", "description": "Nitroglycerin er 2.5 mg capsule", "unit": "capsule" }, { "cost": "0.29", "description": "Nitro-time er 2.5 mg capsule", "unit": "capsule" }, { "cost": "0.33", "description": "Nitro-time er 6.5 mg capsule", "unit": "capsule" }, { "cost": "0.35", "description": "Nitrostat 0.4 mg tablet sl", "unit": "tablet" }, { "cost": "0.36", "description": "Nitroglycerin 0.4 mg tablet sl", "unit": "tablet" }, { "cost": "0.37", "description": "Nitro-time er 9 mg capsule", "unit": "capsule" }, { "cost": "0.47", "description": "Nitroglycerin CR 2.5 mg capsule", "unit": "capsule" }, { "cost": "0.48", "description": "Nitro-bid 2% ointment", "unit": "g" }, { "cost": "0.53", "description": "Nitroglycerin 9 mg capsule sa", "unit": "capsule" }, { "cost": "0.59", "description": "Nitro-Dur 0.2 0.2 mg/hr Patch", "unit": "patch" }, { "cost": "0.59", "description": "Trinipatch 0.2 0.2 mg/hr Patch", "unit": "patch" }, { "cost": "0.64", "description": "Nitrol 2 % Ointment", "unit": "g" }, { "cost": "0.66", "description": "Minitran 0.2 0.2 mg/hr Patch", "unit": "patch" }, { "cost": "0.67", "description": "Nitro-Dur 0.4 0.4 mg/hr Patch", "unit": "patch" }, { "cost": "0.67", "description": "Nitro-Dur 0.6 0.6 mg/hr Patch", "unit": "patch" }, { "cost": "0.67", "description": "Trinipatch 0.4 0.4 mg/hr Patch", "unit": "patch" }, { "cost": "0.67", "description": "Trinipatch 0.6 0.6 mg/hr Patch", "unit": "patch" }, { "cost": "0.71", "description": "Transderm-Nitro 0.2 0.2 mg/hr Patch", "unit": "patch" }, { "cost": "0.72", "description": "Nitroglycerin er 6.5 mg capsule", "unit": "capsule" }, { "cost": "0.74", "description": "Minitran 0.4 0.4 mg/hr Patch", "unit": "patch" }, { "cost": "0.74", "description": "Minitran 0.6 0.6 mg/hr Patch", "unit": "patch" }, { "cost": "0.81", "description": "Transderm-Nitro 0.4 0.4 mg/hr Patch", "unit": "patch" }, { "cost": "0.81", "description": "Transderm-Nitro 0.6 0.6 mg/hr Patch", "unit": "patch" } ]

[ { "approved": "1993-02-16", "country": "United States", "expires": "2010-02-16", "number": "5186938" }, { "approved": "2011-01-18", "country": "United States", "expires": "2028-03-14", "number": "7872049" }, { "approved": "2002-12-31", "country": "United States", "expires": "2018-09-16", "number": "6500456" }, { "approved": "1999-02-09", "country": "United States", "expires": "2016-04-16", "number": "5869082" }, { "approved": "2015-08-11", "country": "United States", "expires": "2032-03-11", "number": "9101592" } ]

[ "Apo-nitroglycerin", "Basic Dental Emergency Kit", "Deluxe Dental Emergency Kit", "Gonitro", "Gonitro", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran", "Minitran - Patch Trd 72mg/26.6 Sq Cm", "Mylan-nitro Patch 0.2", "Mylan-nitro Patch 0.4", "Mylan-nitro Patch 0.6", "Mylan-nitro Patch 0.8", "Mylan-nitro Sublingual Spray", "Nitro-bid", "Nitro-bid", "Nitro-bid", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur", "Nitro-dur 0.2", "Nitro-dur 0.3 - 60mg/15 Sq Cm, 0.3mg/hr", "Nitro-dur 0.4", "Nitro-dur 0.6", "Nitro-dur 0.8", "Nitro-Time", "Nitro-Time", "Nitro-time", "Nitro-time", "Nitro-time", "Nitro-Time", "Nitro-Time", "Nitro-Time", "Nitro-Time", "Nitrogard-SR Tab 1mg", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin", "Nitroglycerin ER", "Nitroglycerin ER", "Nitroglycerin ER", "Nitroglycerin ER", "Nitroglycerin ER", "Nitroglycerin In 5% Dextrose Inj.-100mcg/ml", "Nitroglycerin In 5% Dextrose Inj.-200mcg/ml", "Nitroglycerin In 5% Dextrose Inj.-400mcg/ml", "Nitroglycerin in Dextrose", "Nitroglycerin in Dextrose", "Nitroglycerin in Dextrose", "Nitroglycerin In Dextrose", "Nitroglycerin In Dextrose", "Nitroglycerin In Dextrose", "Nitroglycerin In Dextrose", "Nitroglycerin Inj 5mg/ml", "Nitroglycerin Injection USP", "Nitroglycerin Injection USP", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Lingual", "Nitroglycerin Slocaps", "Nitroglycerin Slocaps", "Nitroglycerin Slocaps", "Nitroglycerin Slocaps", "Nitroglycerin Slocaps", "Nitroglycerin SR", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Delivery System", "Nitroglycerin Transdermal Infusion System", "Nitroglycerin Transdermal Infusion System", "Nitroglycerin Transdermal Infusion System", "Nitroglycerin Transdermal Infusion System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroglycerin Transdermal System", "Nitroject", "Nitroject Inj 1mg/ml", "Nitrol", "Nitrolingual", "Nitrolingual", "Nitrolingual", "Nitrolingual", "Nitrolingual", "Nitrolingual", "Nitrolingual Pumpspray", "Nitrolingual Pumpspray", "Nitrolingual Spray 0.4mg/eam", "NitroMist", "NitroMist", "NitroMist", "NitroMist", "Nitronal", "Nitrong SR Srt 2.6mg", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Nitrostat", "Rectiv", "Rectiv", "Rho-nitro Pumpspray", "Transderm Nitro", "Transderm Nitro", "Transderm Nitro", "Transderm Nitro", "Transderm-nitro 0.2", "Transderm-nitro 0.4", "Transderm-nitro 0.6", "Transderm-nitro 0.8", "Tridil Injection 5mg/ml", "Trinipatch 0.2", "Trinipatch 0.4", "Trinipatch 0.6" ]

[ "Deponit", "Dermatrans", "Gen-Nitro", "Glytrin", "Glytrin Spray", "Natispray", "Nitrocap", "Nitroderm TTS", "Nitrolingual Pump Spray", "Rectogesic", "Stangyl", "Transderm-Nitro", "Tridil", "Trimonit", "Trinipatch", "Triniplas", "Trinispray", "Trinitrin Simplex Laleuf", "Trinitron", "Trinitrosan", "Trintek", "Trocer", "Trocer SR", "Vasolator", "Vasovin", "Venitrin", "Vernies", "Willlong" ]

[ "Nitroglycerin In 5% Dextrose Inj.-400mcg/ml", "Nitroglycerin In 5% Dextrose Inj.-200mcg/ml", "Nitroglycerin In 5% Dextrose Inj.-100mcg/ml", "Basic Dental Emergency Kit", "Deluxe Dental Emergency Kit" ]

[ "P00533", "Q02108", "Q02153", "P16066" ]

[ "P05091" ]

[]

DB00728

Rocuronium

Rocuronium (rapid onset-curonium) is a desacetoxy analogue of vecuronium with a more rapid onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Introduced in 1994, rocuronium has rapid onset, and intermediate duration of action. It is commonly marketed under the trade names Zemuron and Esmeron. The drug is associated with the risk of developing allergic reactions in some high-risk patients, such as those with asthma. However, there was a similar incidence of allergic reactions associated with other non-depolarizing neuromuscular blocking agents. [Sugammadex] is a γ-cyclodextrin derivative that has been introduced as a novel agent to reverse the action of rocuronium.

solid

For inpatients and outpatients as an adjunct to general anesthesia to facilitate both rapid sequence and routine tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation.

Neuromuscular blocking agents are drugs that cause skeletal muscle relaxation primarily by causing a decreased response to the neurotransmitter acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle. At that site, ACh normally produces electrical depolarization of the postjunctional membrane of motor end-plate, which leads to conduction of muscle action potential and subsequently induces skeletal muscle contraction. Neuromuscular agents are classified as depolarizing or nondepolarizing. Rocuronium is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. Rocuronium, like vecuronium is longer acting in infants than in children. However, unlike vecuronium, rocuronium retains the characteristics of an intermediate-acting NMBD in infants.

Rocuronium acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. Rocuronium acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Evidence also suggests that nondepolarizing agents can affect ACh release. It has been hypothesized that nondepolarzing agents bind to postjunctional ("curare") receptors and may therefore interfere with the sodium and potassium flux, which is responsible for depolarization and repolarization of the membranes involved in muscle contraction.

Poorly absorbed from the GI tract.

Rocuronium is metabolized to a less active metabolite, 17-desacetyl-rocuronium, and is eliminated primarily by the liver.

No cases of significant accidental or intentional overdose have been reported. Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.

The rapid distribution half-life is 1-2 minutes and the slower distribution half-life is 14-18 minutes. Renal impairment has no net effect on half-life, however, half-life is almost doubled in patients with impaired liver function.

Approximately 30% bound to human plasma proteins.

Studies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.

* 0.3 L/kg [3 to <12 mos] * 0.26 L/kg [1 to <3 yrs] * 0.21 L/kg [3 to <8 yrs]

* 0.25 L/kg/hr [Adults (Ages 27 to 58 years)] * 0.21 L/kg/hr [Geriatrics (>=65 yrs)] * 0.16 L/kg/hr [Normal ewnal and hepatice function] * 0.13 L/kg/hr [Renal transplant patients] * 0.13 L/kg/hr [Hepatic dysfunction patients] * 0.35 +/- 0.08 L/kg/hr [Pediatric Patients 3 to <12 mos] * 0.32 +/- 0.07 L/kg/hr [Pediatric Patients 1 to 3 yrs] * 0.44 +/- 0.16 L/kg/hr [Pediatric Patients 3 to 8 yrs]

Organic compounds

Lipids and lipid-like molecules

Steroids and steroid derivatives

Steroid esters

[ "approved" ]

[ "M03AC", "M03A", "M03", "M" ]

[ "Humans and other mammals" ]

[ { "cost": "1.08", "description": "Rocuronium 50 mg/5 ml vial", "unit": "ml" }, { "cost": "2.66", "description": "Rocuronium 100 mg/10 ml vial", "unit": "ml" }, { "cost": "4.62", "description": "Zemuron 10 mg/ml vial", "unit": "ml" } ]

[]

[ "Injectable Rocuronium Bromide", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium bromide", "Rocuronium bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection", "Rocuronium Bromide Injection Sdz", "Zemuron", "Zemuron" ]

[ "Esmeron" ]

[]

[ "Q15822", "P08172", "P46098" ]

[]

[ "O15245", "P46721" ]

DB00730

Thiabendazole

2-Substituted benzimidazole first introduced in 1962. It is active against a variety of nematodes and is the drug of choice for strongyloidiasis. It has CNS side effects and hepatototoxic potential. (From Smith and Reynard, Textbook of Pharmacology, 1992, p919)

solid

For the treatment of strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, and trichinosis.

Thiabendazole is a fungicide and parasiticide. Thiabendazole is also a chelating agent, which means that it is used medicinally to bind metals in cases of metal poisoning, such as lead poisoning, mercury poisoning or antimony poisoning. Thiabendazole is vermicidal and/or vermifugal against Ascaris lumbricoides ("common roundworm"), Strongyloides stercoralis (threadworm), Necator americanus, Ancylostoma duodenale (hookworm), Trichuris trichiura (whipworm), Ancylostoma braziliense (dog and cat hookworm), Toxocara canis, Toxocara cati (ascarids), and Enterobius vermicularis (pinworm). Thiabendazole also suppresses egg and/or larval production and may inhibit the subsequent development of those eggs or larvae which are passed in the feces.

The precise mode of action of thiabendazole on the parasite is unknown, but it most likely inhibits the helminth-specific enzyme fumarate reductase.

Rapidly absorbed and peak plasma concentration is reached within 1 to 2 hours after the oral administration of a suspension. Some systemic absorption may occur from topical preparations applied to the skin.

Hepatic. Metabolized almost completely to the 5-hydroxy form which appears in the urine as glucuronide or sulfate conjugates.

Overdosage may be associated with transient disturbances of vision and psychic alterations. The oral LD 50 is 3.6 g/kg, 3.1 g/kg and 3.8 g/kg in the mouse, rat, and rabbit respectively.

The half-life for thiabendazole in both normal and anephric patients is 1.2 hours (range 0.9 to 2 hours). The half-life for the 5-hydroxythiabendazole metabolite in both normal and anephric patients is 1.7 hours (range 1.4 to 2 hours).

null

It is metabolized almost completely to the 5-hydroxy form which appears in the urine as glucuronide or sulfate conjugates.

null

Organic compounds

Organoheterocyclic compounds

Benzimidazoles

null

[ "approved", "vet_approved" ]

[ "D01AC", "D01A", "D01", "D", "P02CA", "P02C", "P02", "P" ]

[ "Roundworms, hookworms, and other helminth species" ]

[ { "cost": "1.27", "description": "Thiabendazole powder", "unit": "g" } ]

[]

[ "Mintezol", "Mintezol", "Mintezol Chewable Tab 500mg" ]

[ "Equizole", "Thibenzole" ]

[]

[ "P05177", "P04798" ]

[]

DB00731

Nateglinide

Nateglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Nateglinide is an amino acid derivative that induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those naïve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Nateglinide is extensively metabolized in the liver and excreted in urine (83%) and feces (10%). The major metabolites possess less activity than the parent compound. One minor metabolite, the isoprene, has the same potency as its parent compound.

solid

For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.

Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporters. Once inside the cell, glucose is metabolized to produce ATP. High concentrations of ATP inhibit ATP-sensitive potassium channels causing membrane depolarization. When extracellular glucose concentrations are low, ATP-sensitive potassium channels open causing membrane repolarization. High glucose concentrations cause ATP-sensitive potassium channels to close resulting in membrane depolarization and opening of L-type calcium channels. The influx of calcium ions stimulates calcium-dependent exocytosis of insulin granules. Nateglinide increases insulin release by inhibiting ATP-sensitive potassium channels in a glucose-dependent manner.

Nateglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, nateglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, nateglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of nateglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Nateglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

Rapidly absorbed following oral administration prior to a meal, absolute bioavailability is estimated to be approximately 73%. Peak plasma concentrations generally occur within 1 hour of oral administration. Onset of action is <20 minutes and the duration of action is approximately 4 hours.

Hepatic, via cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%). Metabolism is via hydroxylation followed by glucuronidation. The major metabolites have less antidiabetic activity than nateglinide, but the isoprene minor metabolite has antidiabetic activity comparable to that of nateglinide.

An overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms.

1.5 hours

98% bound to serum proteins, primarily serum albumin and to a lesser extent α1 acid glycoprotein

Urine (83%) and feces (10%)

10 liters in healthy subjects

null

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved", "investigational" ]

[ "A10BX", "A10B", "A10", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "1.66", "description": "Nateglinide 60 mg tablet", "unit": "tablet" }, { "cost": "1.73", "description": "Nateglinide 120 mg tablet", "unit": "tablet" }, { "cost": "2.01", "description": "Starlix 60 mg tablet", "unit": "tablet" }, { "cost": "2.12", "description": "Starlix 120 mg tablet", "unit": "tablet" } ]

[ { "approved": "1995-03-14", "country": "United States", "expires": "2009-09-08", "number": "RE34878" }, { "approved": "2003-10-14", "country": "Canada", "expires": "2017-11-14", "number": "2271865" }, { "approved": "1999-04-27", "country": "Canada", "expires": "2014-02-01", "number": "2114678" }, { "approved": "2003-05-06", "country": "United States", "expires": "2020-09-15", "number": "6559188" }, { "approved": "2003-11-04", "country": "United States", "expires": "2017-11-14", "number": "6641841" }, { "approved": "2005-01-18", "country": "United States", "expires": "2017-11-14", "number": "6844008" }, { "approved": "2005-04-12", "country": "United States", "expires": "2020-09-15", "number": "6878749" } ]

[ "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Nateglinide", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix", "Starlix 120mg", "Starlix 180mg", "Starlix 60mg", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec", "Trazec" ]

[ "Fastic", "Starsis" ]

[]

[ "Q09428", "P37231" ]

[ "P11712", "P08684", "P20815", "P24462", "P23219", "O60656", "P10635" ]

[ "P02768", "P02763" ]

[ "O15439", "P53985", "P46059", "Q16348", "Q4U2R8" ]

DB00732

Atracurium besylate

A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

solid

For use, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.

Atracurium is a nondepolarizing skeletal muscle relaxant. Atracurium can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. The duration of neuromuscular block produced by Atracurium is approximately one third to one half the duration of block by d-tubocurarine, metocurine, and pancuronium at initially equipotent doses. As with other nondepolarizing neuromuscular blockers, the time to onset of paralysis decreases and the duration of maximum effect increases with increasing doses of Atracurium. Repeated administration of maintenance doses of Atracurium has no cumulative effect on the duration of neuromuscular block if recovery is allowed to begin prior to repeat dosing. Moreover, the time needed to recover from repeat doses does not change with additional doses. Repeat doses can therefore be administered at relatively regular intervals with predictable results.

Atracurium antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.

null

Excessive doses can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension.

The elimination half-life is approximately 20 minutes.

null

Organic compounds

Organoheterocyclic compounds

Isoquinolines and derivatives

Benzylisoquinolines

[ "approved" ]

[]

[ "Humans and other mammals" ]

[ { "cost": "0.96", "description": "Atracurium 10 mg/ml vial", "unit": "ml" } ]

[]

Atracurium besilate | Atracurium besylate | Atracurium dibesylate | Besilate d'atracurium | Besilato de atracurio

[ "Atracurium - (for Multiple Dose Vial - With Preservative)", "Atracurium - (for Single Dose )", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate", "Atracurium Besylate Injection", "Atracurium Besylate Injection", "Atracurium Besylate Injection", "Tracrium" ]

[]

[ "Q15822" ]

[]

DB00733

Pralidoxime

Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. If given within 24 hours,after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase.

solid

For the treatment of poisoning due to those pesticides and chemicals of the organophosphate class which have anticholinesterase activity and in the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis.

Pralidoxime is to reactivate cholinesterase (mainly outside of the central nervous system) which has been inactivated by phosphorylation due to an organophosphate pesticide or related compound. The destruction of accumulated acetylcholine can then proceed, and neuromuscular junctions will again function normally. Pralidoxime also slows the process of "aging" of phosphorylated cholinesterase to a nonreactivatable form, and detoxifies certain organophosphates by direct chemical reaction. The drug has its most critical effect in relieving paralysis of the muscles of respiration. Because pralidoxime is less effective in relieving depression of the respiratory center, atropine is always required concomitantly to block the effect of accumulated acetylcholine at this site. Pralidoxime relieves muscarinic signs and symptoms, salivation, bronchospasm, etc., but this action is relatively unimportant since atropine is adequate for this purpose.

Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. Acetylcholinesterase inhibition causes acetylcholine to accumulate in synapses, producing continuous stimulation of cholinergic fibers throughout the nervous systems. If given within 24 hours after organophosphate exposure, pralidoxime reactivates the acetylcholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase.

null

Hepatic

null

74-77 minutes

No binding to plasma proteins

The drug is rapidly excreted in the urine partly unchanged, and partly as a metabolite produced by the liver.

null

Organic compounds

Organoheterocyclic compounds

Pyridines and derivatives

Methylpyridines

[ "approved", "vet_approved" ]

[ "V03AB", "V03A", "V03", "V", "V03AB", "V03A", "V03", "V" ]

[ "Humans and other mammals" ]

[ { "cost": "104.04", "description": "Protopam chloride 1 gm vial", "unit": "tablet" } ]

[]

[ "ATNAA atropine and pralidoxime chloride Auto-Injector", "DuoDote", "Pralidoxime Chloride", "Protopam Chloride", "Protopam Chloride", "Protopam Chloride - (pws 1g/vial)", "Protopam Chloride Inj 1gm" ]

[ "ComboPen", "Contrathion", "Nispam", "Pamcl", "Pampara", "Pamu", "Protopam" ]

[ "ATNAA atropine and pralidoxime chloride Auto-Injector", "DuoDote" ]

[ "P22303", "P06276" ]

[]

DB00734

Risperidone

Risperidone is a second-generation antipsychotic (SGA) medication used in the treatment of a number of mood and mental health conditions including schizophrenia and bipolar disorder.[L12885] It is one of the most widely used SGAs. [Paliperidone], another commonly used SGA, is the primary active metabolite of risperidone (i.e. 9-hydroxyrisperidone).[L12885] Schizophrenia and various mood disorders are thought to be caused by an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively. Risperidone is thought to reduce this overactivity through inhibition of dopaminergic D2 receptors and serotonergic 5-HT2A receptors in the brain.[L12885] Risperidone binds with a very high affinity to 5-HT2A receptors, approximately 10-20 fold greater than the drug's binding affinity to D2 receptors, and carries lesser activity at several off-targets which may responsible for some of its undesirable effects.[L12885]

solid

Risperidone is indicated for the treatment of schizophrenia [L12885,L44692,L46297] and irritability associated with autistic disorder.[L12885] It is also indicated as monotherapy, or adjunctly with lithium or valproic acid, for the treatment of acute mania or mixed episodes associated with bipolar I disorder.[L12885,L44692] Risperidone is additionally indicated in Canada for the short-term symptomatic management of aggression or psychotic symptoms in patients with severe dementia of the Alzheimer type unresponsive to nonpharmacological approaches.[L12906] Risperidone is also used off-label for a number of conditions including as an adjunct to antidepressants in treatment-resistant depression.[A177226]

The primary action of risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders.[A1115,A1116] Risperidone has a high binding affinity for serotonergic 5-HT2A receptors when compared to dopaminergic D2 receptors in the brain.[A1114,A1115] Risperidone binds to D2 receptors with a lower affinity than first-generation antipsychotic drugs, which bind with very high affinity. A reduction in extrapyramidal symptoms with risperidone, when compared to its predecessors, is likely a result of its moderate affinity for dopaminergic D2 receptors.[A1119,A1117]

Though its precise mechanism of action is not fully understood, current focus is on the ability of risperidone to inhibit the D2 dopaminergic receptors and 5-HT2A serotonergic receptors in the brain. Schizophrenia is thought to result from an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively.[A1115, A1116, A1117] D2 dopaminergic receptors are transiently inhibited by risperidone, reducing dopaminergic neurotransmission, therefore decreasing positive symptoms of schizophrenia, such as delusions and hallucinations.[A251765] Risperidone binds transiently and with loose affinity to the dopaminergic D2 receptor, with an ideal receptor occupancy of 60-70% for optimal effect.[A1119,A31773] Rapid dissociation of risperidone from the D2 receptors contributes to decreased risk of extrapyramidal symptoms (EPS), which occur with permanent and high occupancy blockade of D2 dopaminergic receptors.[A1118,A1119] Low-affinity binding and rapid dissociation from the D2 receptor distinguish risperidone from the traditional antipsychotic drugs. A higher occupancy rate of D2 receptors is said to increase the risk of extrapyramidal symptoms and is therefore to be avoided.[A1118,A1119,A31771] Increased serotonergic mesocortical activity in schizophrenia results in negative symptoms, such as depression and decreased motivation. The high-affinity binding of risperidone to 5-HT2A receptors leads to a decrease in serotonergic activity. In addition, 5-HT2A receptor blockade results in decreased risk of extrapyramidal symptoms, likely by increasing dopamine release from the frontal cortex, and not the nigrostriatal tract. Dopamine level is therefore not completely inhibited.[A1117,A1119] Through the above mechanisms, both serotonergic and D2 blockade by risperidone are thought to synergistically work to decrease the risk of extrapyramidal symptoms. Risperidone has also been said to be an antagonist of alpha-1 (α1), alpha-2 (α2), and histamine (H1) receptors.[A37034] Blockade of these receptors is thought to improve symptoms of schizophrenia, however the exact mechanism of action on these receptors is not fully understood at this time.[L12885]

Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.[L12885]

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone (i.e. [paliperidone]), which has approximately the same receptor binding affinity as risperidone.[A1118,A31772] Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase.[A1119,A31772] Risperidone also undergoes N-dealkylation to a lesser extent.[A1119,A31772]

Symptoms of overdose include lethargy, dystonia/spasm, tachycardia, bradycardia, and seizures. LD50=57.7 mg/kg (rat, oral) and 34 mg/kg (rat, intravenous).[A1117,A1118,A1119]

3 hours in extensive metabolizers[A31772] Up to 20 hours in poor metabolizers[A31772]

Risperidone and its active metabolite, 9-hydroxyrisperidone, are ~88% and ~77% protein-bound in human plasma, respectively.[A31772,L12885] They each bind to both serum albumin and alpha-1-acid glycoprotein.[L12885]

Risperidone is extensively metabolized in the liver. In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives are prolonged compared to young healthy subjects.[A31772,L1214]

The volume of distribution of risperidone is approximately 1 to 2 L/kg.[L12885]

Risperidone is cleared by the kidneys. Clearance is decreased in the elderly and those with a creatinine clearance (ClCr) between 15-59 mL/min, in whom clearance is decreased by approximately 60%.[L1214]

Organic compounds

Organoheterocyclic compounds

Pyridopyrimidines

null

[ "approved", "investigational" ]

[ "N05AX", "N05A", "N05", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.16", "description": "Risperdal M-Tab 1 mg Disintegrating Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Apo-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Co Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Mylan-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Novo-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Phl-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Pms-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Ran-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Ratio-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Rbx-Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.26", "description": "Sandoz Risperidone 2 mg Tablet", "unit": "tablet" }, { "cost": "1.88", "description": "Risperidone 0.25 mg tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Apo-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Co Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Mylan-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Novo-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Phl-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Pms-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Ran-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Ratio-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Rbx-Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Sandoz Risperidone 3 mg Tablet", "unit": "tablet" }, { "cost": "2.29", "description": "Risperdal M-Tab 2 mg Disintegrating Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Apo-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Co Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Mylan-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Novo-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Phl-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Pms-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Ran-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Ratio-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Rbx-Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "2.53", "description": "Sandoz Risperidone 4 mg Tablet", "unit": "tablet" }, { "cost": "3.03", "description": "Risperidone 0.5 mg tablet", "unit": "tablet" }, { "cost": "3.27", "description": "Risperidone 1 mg tablet", "unit": "tablet" }, { "cost": "3.44", "description": "Risperdal M-Tab 3 mg Disintegrating Tablet", "unit": "tablet" }, { "cost": "3.62", "description": "Risperdal 0.5 mg tablet", "unit": "tablet" }, { "cost": "4.48", "description": "Risperidone 0.25 mg odt", "unit": "tablet" }, { "cost": "4.56", "description": "Risperdal 0.25 mg tablet", "unit": "tablet" }, { "cost": "4.6", "description": "Risperdal M-Tab 4 mg Disintegrating Tablet", "unit": "tablet" }, { "cost": "4.71", "description": "Risperidone m-tab 0.5 mg odt", "unit": "tablet" }, { "cost": "4.9", "description": "Risperidone M-TAB 0.5 mg Dispersible Tablet", "unit": "dispersible tablet" }, { "cost": "5.5", "description": "Risperidone m-tab 1 mg odt", "unit": "tablet" }, { "cost": "5.59", "description": "Risperidone 2 mg tablet", "unit": "tablet" }, { "cost": "5.76", "description": "Risperdal m-tab 0.5 mg odt", "unit": "tablet" }, { "cost": "6.12", "description": "Risperdal 1 mg tablet", "unit": "tablet" }, { "cost": "6.63", "description": "Risperidone 3 mg tablet", "unit": "tablet" }, { "cost": "6.73", "description": "Risperdal m-tab 1 mg odt", "unit": "tablet" }, { "cost": "6.94", "description": "Risperdal 2 mg tablet", "unit": "tablet" }, { "cost": "8.95", "description": "Risperidone m-tab 2 mg odt", "unit": "tablet" }, { "cost": "9.0", "description": "Risperidone 4 mg tablet", "unit": "tablet" }, { "cost": "10.95", "description": "Risperdal m-tab 2 mg odt", "unit": "tablet" }, { "cost": "11.29", "description": "Risperidone m-tab 3 mg odt", "unit": "tablet" }, { "cost": "11.45", "description": "Risperdal 3 mg tablet", "unit": "tablet" }, { "cost": "13.81", "description": "Risperdal m-tab 3 mg odt", "unit": "tablet" }, { "cost": "15.16", "description": "Risperidone m-tab 4 mg odt", "unit": "tablet" }, { "cost": "16.47", "description": "Risperdal 4 mg tablet", "unit": "tablet" }, { "cost": "18.55", "description": "Risperdal m-tab 4 mg odt", "unit": "tablet" }, { "cost": "148.22", "description": "Risperdal consta 12.5 mg syr", "unit": "syringe" }, { "cost": "158.66", "description": "Risperidone 1 mg/ml Solution 30ml Bottle", "unit": "bottle" }, { "cost": "167.82", "description": "Risperdal M-TAB 28 0.5 mg Dispersible Tablet Bottle", "unit": "bottle" }, { "cost": "196.08", "description": "Risperdal M-TAB 28 1 mg Dispersible Tablet Box", "unit": "box" }, { "cost": "204.42", "description": "Risperdal 1 mg/ml Solution 30ml Bottle", "unit": "bottle" }, { "cost": "296.46", "description": "Risperdal consta 25 mg syr", "unit": "syringe" }, { "cost": "444.68", "description": "Risperdal consta 37.5 mg syr", "unit": "syringe" }, { "cost": "592.93", "description": "Risperdal consta 50 mg syr", "unit": "syringe" }, { "cost": "0.27", "description": "Apo-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Co Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Mylan-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Novo-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Phl-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Pms-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Ran-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Ratio-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Rbx-Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Sandoz Risperidone 0.25 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Apo-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Co Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Mylan-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Novo-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Phl-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Pms-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Ran-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Ratio-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Rbx-Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.46", "description": "Sandoz Risperidone 0.5 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Apo-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Co Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Mylan-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Novo-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Phl-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Pms-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Ran-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Ratio-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Rbx-Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.63", "description": "Sandoz Risperidone 1 mg Tablet", "unit": "tablet" }, { "cost": "0.84", "description": "Risperdal M-Tab 0.5 mg Disintegrating Tablet", "unit": "tablet" } ]

[ { "approved": "2000-08-29", "country": "United States", "expires": "2013-11-19", "number": "6110921" }, { "approved": "2009-12-22", "country": "Canada", "expires": "2021-04-19", "number": "2406536" }, { "approved": "1998-01-27", "country": "Canada", "expires": "2015-07-04", "number": "2194564" }, { "approved": "2003-12-23", "country": "United States", "expires": "2020-11-25", "number": "6667061" }, { "approved": "1998-08-11", "country": "United States", "expires": "2017-11-02", "number": "5792477" }, { "approved": "1999-06-29", "country": "United States", "expires": "2017-11-02", "number": "5916598" }, { "approved": "2002-04-30", "country": "United States", "expires": "2019-06-30", "number": "6379703" }, { "approved": "2002-06-11", "country": "United States", "expires": "2017-11-02", "number": "6403114" }, { "approved": "2003-07-22", "country": "United States", "expires": "2019-06-30", "number": "6596316" }, { "approved": "2001-02-27", "country": "United States", "expires": "2019-06-30", "number": "6194006" }, { "approved": "2001-05-01", "country": "United States", "expires": "2017-12-10", "number": "6224905" }, { "approved": "2015-11-17", "country": "United States", "expires": "2028-02-13", "number": "9186413" }, { "approved": "2018-07-03", "country": "United States", "expires": "2028-02-13", "number": "10010612" }, { "approved": "2015-11-10", "country": "United States", "expires": "2028-02-13", "number": "9180197" }, { "approved": "2017-03-21", "country": "United States", "expires": "2026-09-26", "number": "9597402" }, { "approved": "2018-08-28", "country": "United States", "expires": "2026-09-26", "number": "10058554" }, { "approved": "2019-09-10", "country": "United States", "expires": "2026-06-26", "number": "10406160" }, { "approved": "2019-08-13", "country": "United States", "expires": "2028-02-13", "number": "10376590" }, { "approved": "2021-05-25", "country": "United States", "expires": "2028-02-13", "number": "11013809" }, { "approved": "2021-09-07", "country": "United States", "expires": "2026-11-05", "number": "11110093" }, { "approved": "2019-09-10", "country": "United States", "expires": "2032-04-10", "number": "10406161" }, { "approved": "2018-10-16", "country": "United States", "expires": "2032-04-10", "number": "10098882" }, { "approved": "2017-01-03", "country": "United States", "expires": "2032-04-10", "number": "9532991" }, { "approved": "2016-09-20", "country": "United States", "expires": "2032-04-10", "number": "9446135" }, { "approved": "2021-09-07", "country": "United States", "expires": "2032-04-10", "number": "11110094" }, { "approved": "2016-09-13", "country": "United States", "expires": "2025-01-12", "number": "9439905" }, { "approved": "2012-07-17", "country": "United States", "expires": "2027-11-12", "number": "8221778" }, { "approved": "2014-06-03", "country": "United States", "expires": "2027-11-12", "number": "8741327" }, { "approved": "2018-03-27", "country": "United States", "expires": "2025-01-12", "number": "9925268" }, { "approved": "2020-08-11", "country": "United States", "expires": "2025-01-12", "number": "10736965" }, { "approved": "2014-08-12", "country": "United States", "expires": "2025-01-12", "number": "8802127" }, { "approved": "2017-08-01", "country": "United States", "expires": "2025-01-12", "number": "9717799" }, { "approved": "2015-05-05", "country": "United States", "expires": "2033-04-05", "number": "9023897" }, { "approved": "2018-02-20", "country": "United States", "expires": "2025-01-12", "number": "9895447" }, { "approved": "2008-02-13", "country": "United States", "expires": "2028-02-13", "number": "11712475" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11752092" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11241377" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11173110" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11007139" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10195138" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10182982" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11759416" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11752094" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10085936" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10881605" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10058504" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10463607" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "11752093" }, { "approved": "2011-05-31", "country": "United States", "expires": "2031-05-31", "number": "10335366" } ]

[ "Act Risperidone", "Act Risperidone", "Act Risperidone", "Act Risperidone", "Act Risperidone", "Act Risperidone", "Ag-risperidone", "Ag-risperidone", "Ag-risperidone", "Ag-risperidone", "Ag-risperidone", "Ag-risperidone", "Apo-risperidone", "Apo-risperidone", "Apo-risperidone", "Apo-risperidone", "Apo-risperidone", "Apo-risperidone", "Apo-risperidone", "Ava-risperidone", "Ava-risperidone", "Ava-risperidone", "Ava-risperidone", "Ava-risperidone", "Ava-risperidone", "Ava-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone", "Dom-risperidone ODT", "Dom-risperidone ODT", "Dom-risperidone ODT", "Ipg-risperidone", "Ipg-risperidone", "Ipg-risperidone", "Ipg-risperidone", "Ipg-risperidone", "Ipg-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Jamp-risperidone", "Mar-risperidone", "Mar-risperidone", "Mar-risperidone", "Mar-risperidone", "Mar-risperidone", "Mar-risperidone", "Mint-risperidon", "Mint-risperidon", "Mint-risperidon", "Mint-risperidon", "Mint-risperidon", "Mint-risperidon", "Mylan-risperidone", "Mylan-risperidone", "Mylan-risperidone", "Mylan-risperidone", "Mylan-risperidone", "Mylan-risperidone", "Mylan-risperidone ODT", "Mylan-risperidone ODT", "Mylan-risperidone ODT", "Mylan-risperidone ODT", "Mylan-risperidone ODT", "Nu-risperidone", "Nu-risperidone", "Nu-risperidone", "Nu-risperidone", "Nu-risperidone", "Nu-risperidone", "Okedi", "Okedi", "Okedi", "Okedi", "Perseris", "Perseris", "Perseris", "Perseris", "PHL-risperidone", "PHL-risperidone", "PHL-risperidone", "PHL-risperidone", "PHL-risperidone", "PHL-risperidone", "PHL-risperidone ODT", "PHL-risperidone ODT", "PHL-risperidone ODT", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone", "PMS-risperidone ODT", "PMS-risperidone ODT", "PMS-risperidone ODT", "PMS-risperidone ODT", "PMS-risperidone ODT", "Pro-risperidone", "Pro-risperidone", "Pro-risperidone", "Pro-risperidone", "Pro-risperidone", "Pro-risperidone", "Q-risperidone", "Q-risperidone", "Q-risperidone", "Q-risperidone", "Q-risperidone", "Q-risperidone", "Ran-risperidone", "Ran-risperidone", "Ran-risperidone", "Ran-risperidone", "Ran-risperidone", "Ran-risperidone", "Ratio-risperidone", "Ratio-risperidone", "Ratio-risperidone", "Ratio-risperidone", "Ratio-risperidone", "Ratio-risperidone", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal Consta", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal M-tab", "Risperdal Oral Solution", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", 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"Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone", "Risperidone - 0.25", "Risperidone - 0.5", "Risperidone - 1", "Risperidone - 2", "Risperidone - 3", "Risperidone - 4", "Risperidone M-TAB", "Risperidone M-TAB", "Risperidone M-TAB", "Risperidone M-TAB", "Risperidone M-TAB", "Risperidone Tablets", "Risperidone Tablets", "Risperidone Tablets", "Risperidone Tablets", "Risperidone Tablets", "Risperidone Tablets", "Risvan", "Risvan", "Riva-risperidone", "Riva-risperidone", "Riva-risperidone", "Riva-risperidone", "Riva-risperidone", "Riva-risperidone", "Rykindo extended-release microspheres", "Rykindo extended-release microspheres", "Rykindo extended-release microspheres", "Rykindo extended-release microspheres", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Sandoz Risperidone", "Taro-risperidone", "Taro-risperidone", "Taro-risperidone", "Taro-risperidone", "Taro-risperidone", "Taro-risperidone", "Teva-risperidone", "Teva-risperidone", "Teva-risperidone", "Teva-risperidone", "Teva-risperidone", "Teva-risperidone", "Truemed Group LLC", "Uzedy", "Uzedy", "Uzedy", "Uzedy", "Uzedy", "Uzedy", "Uzedy" ]

[ "Risperidal M-Tab", "Risperin", "Rispolept", "Rispolin", "Sequinan" ]

[]

[ "P28223", "P14416", "P35368", "P18089", "P35348", "P18825", "P35367", "P28335", "P28221", "P08908", "P34969", "P21728" ]

[ "P10635", "P08684" ]

[ "P02768", "P02763" ]

[ "P08183" ]

DB00735

Naftifine

Naftifine is a synthetic, broad spectrum, antifungal agent and allylamine derivative for the topical treatment of tinea pedis, tinea cruris, and tinea corporis caused by the organisms Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans and Epidermophyton floccosum.

solid

For the topical treatment of tinea pedis, tinea cruris, and tinea corporis caused by the organisms Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans and Epidermophyton floccosum.

Naftifine is a synthetic, broad spectrum, antifungal agent and allylamine derivative. The following in vitro data are available, but their clinical significance is unknown. Naftifine has been shown to exhibit fungicidal activity in vitro against a broad spectrum of organisms including Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Epidermophyton floccosum, and Microsporum canis, Microsporum audouini, and Microsporum gypseum; and fungistatic activity against Candida species including Candida albicans. However it is only used to treat the organisms listed in the indications.

Although the exact mechanism of action against fungi is not known, naftifine appears to interfere with sterol biosynthesis by inhibiting the enzyme squalene 2,3-epoxidase. This inhibition of enzyme activity results in decreased amounts of sterols, especially ergosterol, and a corresponding accumulation of squalene in the cells.

Following single topical applications of 3H-labeled naftifine gel 1% to the skin of healthy subjects, up to 4.2% of the applied dose was absorbed.

null

Approximately 2 to 3 days following topical administration.

null

Naftifine and/or its metabolites are excreted via the urine and feces with a half-life of approximately two to three days.

null

Organic compounds

Benzenoids

Naphthalenes

null

[ "approved" ]

[ "D01AE", "D01A", "D01", "D" ]

[ "Yeast and other fungi" ]

[ { "cost": "2.45", "description": "Naftin 1% cream", "unit": "g" }, { "cost": "3.2", "description": "Naftin pump 1% cream", "unit": "g" }, { "cost": "101.62", "description": "Naftin 1% Cream 30 gm Tube", "unit": "tube" }, { "cost": "147.0", "description": "Naftin 1% Gel 40 gm Tube", "unit": "tube" }, { "cost": "183.77", "description": "Naftin 1% Cream 60 gm Tube", "unit": "tube" }, { "cost": "208.5", "description": "Naftin 1% Gel 60 gm Tube", "unit": "tube" }, { "cost": "248.26", "description": "Naftin 1% Cream 90 gm Tube", "unit": "tube" }, { "cost": "290.08", "description": "Naftin 1% Gel 90 gm Tube", "unit": "tube" } ]

[ { "approved": "2015-10-20", "country": "United States", "expires": "2033-01-31", "number": "9161914" }, { "approved": "2014-07-15", "country": "United States", "expires": "2033-01-31", "number": "8778365" }, { "approved": "2019-01-01", "country": "United States", "expires": "2033-01-31", "number": "10166206" }, { "approved": "2019-01-01", "country": "United States", "expires": "2033-01-31", "number": "10166205" }, { "approved": "2020-06-30", "country": "United States", "expires": "2033-01-31", "number": "10695303" }, { "approved": "2020-08-04", "country": "United States", "expires": "2033-01-31", "number": "10729667" } ]

[ "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine Hydrochloride", "Naftifine hydrochloride", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin", "Naftin Crm 1%", "Naftin Gel 1%" ]

[ "A Mei", "Ancent", "Exoderil", "Micosona", "Naftifina", "Suadian" ]

[]

[ "Q14534" ]

[]

DB00736

Esomeprazole

Esomeprazole, sold under the brand name Nexium, is a proton pump inhibitor (PPI) medication used for the management of gastroesophageal reflux disease (GERD), for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, and for the treatment of pathological hypersecretory conditions including Zollinger-Ellison (ZE) Syndrome. It can also be found in quadruple regimens for the treatment of _H. pylori_ infections along with other antibiotics including [DB01060], [DB01211], and [DB00916], for example.[A177271, F4498] Its efficacy is considered similar to other medications within the PPI class including [DB00338], [DB00213], [DB00448], [DB05351], and [DB01129]. Esomeprazole is the s-isomer of [DB00338], which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as [DB00338], without any significant differences between the two compounds _in vitro_. Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect persists longer than 24 hours.[FDA Label] PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes.[A177577, A177580] Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients such as iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life.[A177571] Rapid discontinuation of PPIs such as esomeprazole may cause a rebound effect and a short term increase in hypersecretion.[A177574] Esomeprazole doses should be slowly lowered, or tapered, before discontinuing to prevent this rebound effect.

solid

Esomeprazole is indicated for the treatment of acid-reflux disorders including healing and maintenance of erosive esophagitis, and symptomatic gastroesophageal reflux disease (GERD), peptic ulcer disease, H. pylori eradication, prevention of gastrointestinal bleeds with NSAID use, and for the long-term treatment of pathological hypersecretory conditions including Zollinger-Ellison Syndrome.

Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. Esomeprazole is the s-isomer of [DB00338], which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as [DB00338], without any significant differences between the two compounds _in vitro_. PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes.[A177577, A177580] Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life.[A177571]

Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect that persists longer than 24 hours.[FDA Label]

After oral administration, peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 90% compared to 64% after a single dose of 40 mg. The mean exposure (AUC) to esomeprazole increases from 4.32 μmol*hr/L on Day 1 to 11.2 μmol*hr/L on Day 5 after 40 mg once daily dosing. The AUC after administration of a single 40 mg dose of Esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.[FDA Label] _Combination Therapy with Antimicrobials:_ Esomeprazole magnesium 40 mg once daily was given in combination with [DB01211] 500 mg twice daily and [DB01060] 1000 mg twice daily for 7 days to 17 healthy male and female subjects. The mean steady state AUC and Cmax of esomeprazole increased by 70% and 18%, respectively during triple combination therapy compared to treatment with esomeprazole alone. The observed increase in esomeprazole exposure during co-administration with clarithromycin and amoxicillin is not expected to produce significant safety concerns.

Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack antisecretory activity. The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite. CYP2C19 isoenzyme exhibits polymorphism in the metabolism of esomeprazole, since some 3% of Caucasians and 15 to 20% of Asians lack CYP2C19 and are termed Poor Metabolizers.[FDA Label] However, the influence of CYP 2C19 polymorphism is less pronounced for esomeprazole than for omeprazole.[F4495] At steady state, the ratio of AUC in Poor Metabolizers to AUC in the rest of the population (Extensive Metabolizers) is approximately 2. Following administration of equimolar doses, the S- and R-isomers are metabolized differently by the liver, resulting in higher plasma levels of the S- than of the R-isomer.[FDA Label] Nine major urinary metabolites have been detected. The two main metabolites have been identified as hydroxyesomeprazole and the corresponding carboxylic acid. Three major metabolites have been identified in plasma: the 5-O-desmethyl- and sulphone derivatives and hydroxyesomeprazole. The major metabolites of esomeprazole have no effect on gastric acid secretion.[F4495]

Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating

1-1.5 hours

Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 to 20 µmol/L.[FDA Label]

The plasma elimination half-life of esomeprazole is approximately 1 to 1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the feces.

The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.[FDA Label]

null

Organic compounds

Organoheterocyclic compounds

Benzimidazoles

Sulfinylbenzimidazoles

[ "approved", "investigational" ]

[ "A02BD", "A02B", "A02", "A", "A02BC", "A02B", "A02", "A", "M01AE", "M01A", "M01", "M" ]

[ "Humans and other mammals" ]

[ { "cost": "6.5", "description": "Nexium 10 mg packet", "unit": "each" }, { "cost": "6.5", "description": "Nexium 20 mg capsule", "unit": "capsule" }, { "cost": "6.5", "description": "Nexium 20 mg packet", "unit": "each" }, { "cost": "6.5", "description": "Nexium 40 mg capsule", "unit": "capsule" }, { "cost": "6.5", "description": "Nexium 40 mg packet", "unit": "each" }, { "cost": "6.76", "description": "NexIUM 20 mg Delayed Release Capsule", "unit": "capsule" }, { "cost": "6.76", "description": "NexIUM 40 mg Delayed Release Capsule", "unit": "capsule" }, { "cost": "33.91", "description": "Nexium i.v. 20 mg vial", "unit": "vial" }, { "cost": "33.91", "description": "Nexium i.v. 40 mg vial", "unit": "vial" } ]

[ { "approved": "1999-03-02", "country": "United States", "expires": "2014-05-27", "number": "5877192" }, { "approved": "2009-02-10", "country": "Canada", "expires": "2019-11-03", "number": "2346988" }, { "approved": "1996-06-11", "country": "Canada", "expires": "2013-06-11", "number": "1338377" }, { "approved": "2000-11-14", "country": "United States", "expires": "2019-04-09", "number": "6147103" }, { "approved": "1999-05-04", "country": "United States", "expires": "2016-11-04", "number": "5900424" }, { "approved": "2002-04-09", "country": "United States", "expires": "2018-11-25", "number": "6369085" }, { "approved": "2002-08-06", "country": "United States", "expires": "2020-05-03", "number": "6428810" }, { "approved": "2008-08-12", "country": "United States", "expires": "2018-11-25", "number": "7411070" }, { "approved": "2013-06-18", "country": "United States", "expires": "2018-11-25", "number": "8466175" }, { "approved": "2014-10-07", "country": "United States", "expires": "2022-05-31", "number": "8852636" }, { "approved": "2014-10-14", "country": "United States", "expires": "2022-05-31", "number": "8858996" }, { "approved": "2005-08-09", "country": "United States", "expires": "2023-02-28", "number": "6926907" }, { "approved": "2010-06-29", "country": "United States", "expires": "2018-10-13", "number": "7745466" }, { "approved": "2015-10-20", "country": "United States", "expires": "2022-05-31", "number": "9161920" }, { "approved": "2015-12-01", "country": "United States", "expires": "2022-05-31", "number": "9198888" }, { "approved": "2015-02-03", "country": "United States", "expires": "2031-10-17", "number": "8945621" }, { "approved": "2013-10-15", "country": "United States", "expires": "2022-05-31", "number": "8557285" }, { "approved": "2015-12-29", "country": "United States", "expires": "2031-03-10", "number": "9220698" }, { "approved": "1998-02-03", "country": "United States", "expires": "2015-08-03", "number": "5714504" }, { "approved": "2016-05-24", "country": "United States", "expires": "2022-05-31", "number": "9345695" }, { "approved": "2016-07-19", "country": "United States", "expires": "2029-09-03", "number": "9393208" }, { "approved": "2001-02-20", "country": "United States", "expires": "2019-04-09", "number": "6191148" }, { "approved": "2000-12-26", "country": "United States", "expires": "2019-04-09", "number": "6166213" }, { "approved": "2017-07-18", "country": "United States", "expires": "2022-05-31", "number": "9707181" }, { "approved": "2018-09-18", "country": "United States", "expires": "2036-12-08", "number": "10076494" }, { "approved": "2020-11-17", "country": "United States", "expires": "2036-12-08", "number": "10835488" } ]

[ "Acid Reducer", "Acid Reducer", "Acid Reducer", "Acid Reducer", "Acid Reducer", "Acid Reducer", "Anodyne Ile", "Apo-esomeprazole", "Apo-esomeprazole", "Basic Care Esomeprazole Magnesium", "Basic Care Esomeprazole Magnesium", "Basic Care Esomeprazole Magnesium", "Berkley and Jensen Heartburn Treatment", "Careone Esomeprazole Magnesium", "DG Health Esomeprazole Magnesium", "Dg Health Esomeprazole Magnesium", "Dg Health Esomeprazole Magnesium", "Equaline Esomeprazole Magnesium", "Equate Esomeprazole Magnesium", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole", "Esomeprazole DR", "Esomeprazole DR", "Esomeprazole DR", "Esomeprazole Magneisum D/r", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium", "Esomeprazole Magnesium D/r", "Esomeprazole Magnesium Delayed-Release 20 mg mini", "Esomeprazole Magnesium Delayed-Release Capsules, 20 mg", "Esomeprazole Magnesium Dr", "Esomeprazole Magnesium DR", "Esomeprazole Magnesium DR", "Esomeprazole Magnesium DR", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole sodium", "Esomeprazole sodium", "Esomeprazole Sodium", "Esomeprazole sodium", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole Sodium", "Esomeprazole sodium", "Esomeprazole sodium", "Esomeprazole Strontium", "Esomeprazole Strontium", "Esomeprazole strontium", "Esomeprazole strontium", "Esomeprazole strontium", "Esomeprazole strontium", "Esomeprazole Strontium", "Esomeprazole Strontium", "Esomeprazole strontium", "Exchange Select Esomeprazole Magnesium", "Family Wellness Esomeprazole Magnesium", "Foster and Thrive Acid Reducer", "Genozol", "Good Neighbor Pharmacy Esomeprazole Magnesium", "Good Neighbor Pharmacy Esomeprazole Magnesium", "Good Neighbor Pharmacy Esomeprazole Magnesium", "Good Sense Esomeprazole Magnesium", "Good Sense Esomeprazole Magnesium", "Good Sense Esomeprazole Magnesium", "Harris Teeter Acid Reducer", "Health Mart Esomeprazole Magnesium", "Healthy Accents Esomeprazole Magnesium", "Kirkland Signature Esomeprazole Magnesium", "Leader Heartburn Treatment", "M-esomeprazole", "M-esomeprazole", "Members Mark Esomeprazole Magnesium", "Myl-esomeprazole", "Myl-esomeprazole", "Mylan-esomeprazole", "Mylan-esomeprazole", "Mylan-esomeprazole", "Mylan-esomeprazole", "Mylan-naproxen/esomeprazole Mr", "Mylan-naproxen/esomeprazole Mr", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium", "Nexium - 20mg", "Nexium - 40mg", "Nexium 24HR", "Nexium 24HR", "Nexium 24HR", "Nexium 24HR", "Nexium 24HR", "Nexium 24HR", "Nexium 24HR ClearMinis", "Nexium Control", "Nexium Control", "Nexium Control", "Nexium Control", "Nexium Control", "Nexium I.V.", "Nexium I.V.", "Nexium I.V.", "PharmapureRx ESOMEP-EZS", "PMS-esomeprazole Dr", "PMS-esomeprazole Dr", "Pmsc-esomeprazole Dr", "Pmsc-esomeprazole Dr", "Riva-esomeprazole Dr", "Riva-esomeprazole Dr", "Rugby Esomeprazole Magnesium", "Sandoz Esomeprazole", "Sandoz Esomeprazole", "Shoprite Esomeprazole Magnesium", "Signature Care Esomeprazole Magnesium", "Signature Care Esomeprazole Magnesium", "Smart Sense Esomeprazole Magnesium", "Sound Body Esomeprazole Magnesium", "Sunmark Esomeprazole Magnesium", "Taro-esomeprazole", "Taro-esomeprazole", "Teva-esomeprazole", "Teva-esomeprazole", "Topcare Esomeprazole Magnesium", "Topcare Esomeprazole Magnesium", "Up and Up Esomeprazole Magnesium", "Up and Up Esomeprazole Magnesium", "Vimovo", "Vimovo", "Vimovo", "Vimovo", "Vimovo", "Vimovo", "Vimovo" ]

[ "Alenia", "Awa-Block", "Axagon", "Cor", "Cronopep", "Emanera", "Emep", "Emozul", "ES-OD", "Esmep", "Eso", "Esofag", "Esolok", "Esomarfan", "Esomenta", "Esomep", "Esomeprazol Genfar", "Esopral", "Esorest", "Inexium paranova", "Lucen", "Nexiam" ]

[ "Vimovo", "Anodyne Ile", "Vimovo", "Vimovo", "Vimovo", "Vimovo", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and Esomeprazole Magnesium", "Vimovo", "Vimovo", "Mylan-naproxen/esomeprazole Mr", "Mylan-naproxen/esomeprazole Mr", "Naproxen and Esomeprazole Magnesium", "Naproxen and Esomeprazole Magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium", "Naproxen and esomeprazole magnesium" ]

[ "P20648", "P51164", "O94760" ]

[ "P33261", "P08684" ]

[]

[ "P08183", "Q8TCC7" ]

DB00737

Meclizine

Meclizine is a histamine H1 antagonist with antiemetic and antivertigo properties. It is used in the symptomatic treatment of motion sickness and control of vertigo associated with vestibular system diseases. It also exhibits anticholinergic, central nervous system depressant, and local anesthetic effects.[L6760] Commonly marketed under the brand name Antivert in the U.S., meclizine is available as oral tablets.

solid

Indicated for the symptomatic treatment of nausea, vomiting, and dizziness associated with motion sickness,[L6772] and management of vertigo due to various causes, including radiation sickness, Meniere’s syndrome, labyrinthitis and other vestibular disturbances.[L6766]

Meclizine works on the higher centres of the brain to reduce nausea, vomiting, or vertigo. It is effective against nausea and vomiting arising from many causes, including motion sickness and disorders affecting the vestibular system. The onset of action of meclizine is about 1 hour, with effects lasting between 8 to 24 hours.[L6760] Meclizine is reported to cause drowsiness due to its anticholinergic actions.[L6766]

Vomiting is a centrally regulated reflex mechanism that initiates from the vomiting center and the chemoreceptor trigger zone (CTZ) located in the medulla. Motion sickness is also regulated by CTZ. The blood-brain barrier near the CTZ is relatively permeable to circulating mediators and CTZ can transmit impulses to vomiting center located in the brainstem. Different receptors responding to different factors, including histamine, 5-HT, enkephalins, substance P, and dopamine, are expressed along the brainstem to activate respective pathways and contribute to the control of vomiting. Histamine H1 receptors are expressed on the vestibular nuclei and nucleus of the solitary tract (NTS) that are activated by motion sickness and stimuli from the pharynx and stomach. When activated, H1 receptor signaling from these nuclei is transmitted to the CTZ and vomiting centre.[T28] Through its antagonistic action on the H1 receptors, meclizine primarily works by inhibiting signaling pathway transduction through histaminergic neurotransmission from the vestibular nuclei and NTS to the CTZ and medullary vomiting center.[A179581] Meclizine may also decrease the labyrinth excitability and vestibular stimulation.[L6760]

Most histamine H1 antagonists are reported to be readily absorbed following oral administration.[L6760] Upon oral administration, the time to reach peak plasma concentrations (Cmax) of meclizine is about 3 hours post-dose, with the value ranging from 1.5 to 6 hours.[L6772]

There is limited human data on meclizine metabolism. According to the findings of _in vitro_ studies, meclizine may undergo aromatic hydroxylation or benzylic oxidation mediated by the hepatic CYP2D6 enzyme.[A179584]

The oral and intraperitoneal LD50 in mouse are 1600 mg/kg and 625 mg/kg, respectively. The lowest published toxic dose (TDLo) in rats via the oral route is 800 mg/kg.[MSDS] Symptoms of overdose mainly involve CNS depression with drowsiness, coma, and convulsions. Hypotension may also occur, particularly in the elderly. In children, anticholinergic effects and CNS stimulation, characterized by hallucinations, seizures, trouble sleeping, are more likely to occur. In case of overdose, symptomatic and supportive treatment is recommended. In case of recent ingestion, induction of emesis or gastric lavage should be initiated to limit further drug absorption. Although there is no known antidote to meclizine, physostigmine may be useful to counteract the CNS anticholinergic effects of meclizine.[L6766]

Meclizine has a plasma elimination half-life of about 5-6 hours in humans.[L6772]

There is limited data on the protein binding profile of meclizine.

Meclizine is excreted in the urine as metabolites and in the feces as unchanged drug.[L6760]

The volume of distribution of meclizine in humans has not been fully studied. It is proposed that meclizine may be excreted into breast milk.[L6760]

There is limited data on the clearance of meclizine.

Organic compounds

Benzenoids

Benzene and substituted derivatives

Diphenylmethanes

[ "approved" ]

[ "R06AE", "R06A", "R06", "R", "R06AE", "R06A", "R06", "R" ]

[ "Humans and other mammals" ]

[ { "cost": "1.04", "description": "Meclizine hcl powder", "unit": "g" }, { "cost": "1.23", "description": "Antivert 25 mg tablet", "unit": "tablet" }, { "cost": "2.12", "description": "Antivert 50 mg tablet", "unit": "tablet" }, { "cost": "89.97", "description": "Meclizine HCl 100 25 mg tablet Box", "unit": "box" }, { "cost": "0.06", "description": "Medi-meclizine 25 mg tablet", "unit": "tablet" }, { "cost": "0.07", "description": "Meclizine 25 mg tablet", "unit": "tablet" }, { "cost": "0.28", "description": "Dramamine 50 mg tablet", "unit": "tablet" }, { "cost": "0.33", "description": "Bonamine 25 mg Chewable Tablet", "unit": "tablet" }, { "cost": "0.42", "description": "Dramamine less drowsy tablet", "unit": "tablet" }, { "cost": "0.43", "description": "Meclizine HCl 12.5 mg tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Sm motion sicknes 25 mg tablet", "unit": "tablet" }, { "cost": "0.62", "description": "Meclizine 12.5 mg tablet", "unit": "tablet" }, { "cost": "0.67", "description": "Meclizine HCl 25 mg tablet", "unit": "tablet" }, { "cost": "0.82", "description": "Antivert 12.5 mg tablet", "unit": "tablet" }, { "cost": "0.9", "description": "Vertin-32 tablet", "unit": "tablet" } ]

[]

[ "Antivert", "Antivert", "Antivert", "Antivert", "Antivert", "Antivert", "Antivert", "Antivert", "Antivert Tab", "Bonamine", "Bonamine Tab 25mg Chewable", "Bonine", "Bonine", "Bonine", "Bonine Max", "CVS Motion Sickness Fast Melting", "CVS Motion Sickness Strips", "Diphen", "Dramamine", "Dramamine - N", "Dramamine Less Drowsy", "Dramamine Less Drowsy Formula", "Jet-Avert Motion Sickness Aid", "Less Drowsy Formula Motion Sickness Relief", "Less Drowsy Motion Sickness Relief", "Less Drowsy Motion Sickness Relief", "Less Drowsy Motion Sickness Relief", "Less Drowsy Motion Sickness Relief", "Meclinzine Hydorchloride", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine", "Meclizine 25", "Meclizine 25", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCL", "Meclizine HCl", "Meclizine HCL", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCL", "Meclizine HCl", "Meclizine HCl", "Meclizine HCL", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCl", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCL 12.5 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCl 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCL 25 mg", "Meclizine HCl 25 mg", "Meclizine HCL 25 mg", "Meclizine HCL 25 mg", "Meclizine HCL 25 mg", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine hydrochloride", "Meclizine hydrochloride", "Meclizine hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrochloride", "Meclizine Hydrocloride", "Medique Medi-Meclizine", "Medique Medi-Meclizine", "Medique Medi-Meclizine", "Medique Medi-Meclizine", "Motion Relief - Less Drowsy Formula", "Motion sickness", "Motion Sickness", "Motion Sickness", "Motion Sickness", "Motion Sickness", "Motion Sickness", "Motion Sickness All Day Less Drowsy", "Motion Sickness II", "Motion Sickness II", "Motion Sickness II", "Motion Sickness II", "Motion Sickness II", "Motion Sickness Less Drowsy", "Motion sickness less drowsy formula", "Motion Sickness Less Drowsy Formula", "Motion sickness less drowsy formula", "Motion Sickness Less Drowsy Formula", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief", "Motion Sickness Relief Less Drowsy", "Motion Sickness Relief Less Drowsy", "Motion-Time Chewable", "Motion-Time Chewable", "Motion-Time Chewable", "Motion-Time Chewable", "Naus-ease", "Naus-ease", "Nausea Relief", "Nausea Relief", "Novominsyrup", "PhysiciansCare Motion Sickness", "Rugby", "Rugby Meclizine HCl", "Rugby Meclizine HCl", "Rugby Meclizine HCl, 12.5 mg Each Antiemetic", "Rugby Meclizine HCl, 12.5 mg Each Antiemetic", "Rugby Meclizine HCl, 12.5 mg Each Antiemetic", "Rugby Meclizine HCl, 12.5 mg Each Antiemetic", "RUGBY Meclizine HCl, 12.5 mg Each Antiemetic", "Rugby Travel Sickness", "Rugby Travel Sickness Meclizine HCl 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (ANTIEMETIC)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (ANTIEMETIC)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel Sickness Meclizine HCl, 25 mg Each (Antiemetic)", "Rugby Travel SicknessMeclizine HCl, 25 mg Each (ANTIEMETIC)", "RugbyMeclizine HCl, 12.5 mg Each ANTIEMETIC Meclizine HCl, 12.5 mg Each ANTIEMETIC", "Sea-calm", "Trav-L-tabs", "Travel Ease", "Travel Sickness Meclizine HCl", "Travel Time", "Travel-Ease", "Travel-Ease", "Travel-Ease", "Verticalm", "Wal Dram", "Wal-Dram 2 Quick-Dissolving", "Welly Travel Medicine Kit", "Zentrip", "ZenTrip Motion Sickness" ]

[ "Chiclida", "Meclicot", "Navicalm", "Nevidoxine", "Postafen", "Sea-Legs" ]

[ "Welly Travel Medicine Kit", "Antivert Tab", "Diphen", "Novominsyrup" ]

[ "P35367", "Q14994" ]

[ "P10635" ]

[ "P02768" ]

[]

DB00738

Pentamidine

Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of pneumocystis pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.

solid

For the treatment of pneumonia due to Pneumocystis carinii.

Pentamidine is an antiprotozoal agent. It is an aromatic diamidine, and is known to have activity against Pneumocystis carinii. The exact nature of its antiprotozoal action is unknown. in vitro studies with mammalian tissues and the protozoan Crithidia oncopelti indicate that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids and proteins. Little is known about the drug's pharmacokinetics. The medication is also useful in Leishmaniasis and in prophylaxis against sleeping sickness caused by Trypanosoma brucei gambiense. Hydration before treatment lessens the incidence and severity of side effects, which include liver or kidney dysfunction, hypertension, hypotension, hypoglycemia, hypocalemia, leukopenia, thrombcytopenia, anemia, and allergic reaction. It is generally well-tolerated.

The mode of action of pentamidine is not fully understood. It is thought that the drug interferes with nuclear metabolism producing inhibition of the synthesis of DNA, RNA, phospholipids, and proteins.

Absorbed poorly through the gastrointestinal tract and is usually administered parenterally.

Hepatic.

Symptoms of overdose include pain, nausea, anorexia, hypotension, fever, rash, bad taste in mouth, confusion/hallucinations, dizziness, and diarrhea.

9.1-13.2 hours

69%

null

Organic compounds

Benzenoids

Phenol ethers

null

[ "approved", "investigational" ]

[ "P01CX", "P01C", "P01", "P" ]

[ "Pneumocystis carinii" ]

[ { "cost": "45.31", "description": "Pentamidine 300 mg vial", "unit": "vial" }, { "cost": "94.8", "description": "Pentam 300 vial", "unit": "vial" }, { "cost": "122.84", "description": "Nebupent 300 mg inhal powder", "unit": "each" } ]

[]

[ "NebuPent", "NebuPent", "Pentacarinat 300 Inj Pws 300mg/vial", "Pentam 300", "Pentamidine Isethionate", "Pentamidine Isethionate", "Pentamidine Isethionate", "Pentamidine Isethionate", "Pentamidine Isethionate", "Pentamidine Isethionate Inj 300mg/vial BP", "Pentamidine Isetionate for Injection BP", "Pentamidine Isetionate for Injection BP" ]

[ "Pentacarinat", "Pentacrinat", "Pentam", "Pneumopent" ]

[]

[ "Q15661", "O14717" ]

[ "P33261", "P04798", "P10635", "P20815", "Q02928" ]

[]

DB00739

Hetacillin

Hetacillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Hetacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Hetacillin results from the inhibition of cell wall synthesis and is mediated through Hetacillin binding to penicillin binding proteins (PBPs). Hetacillin has been withdrawn from the market since it has been discovered that it has no therapeutic advantage compared to non-ester derivatives like ampicillin.

solid

Hetacillin is a beta-lactam antibiotic prodrug used to treat bacterial infections. In the body it gets converted to ampicillin.

Hetacillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Hetacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Hetacillin results from the inhibition of cell wall synthesis and is mediated through Hetacillin binding to penicillin binding proteins (PBPs).

Hetacillin is a semisynthetic penicillin prodrug which itself has no antibacterial activity, but is converted in the body to ampicillin and has actions and uses similar to those of ampicillin. Hetacillin is prepared by reacting ampicillin with acetone. Ampicillin rapidly decomposes because of the intramolecular attack of the side chain amino group on the lactam ring. _In vitro_ studies have shown that hetacillin is resistant to beta lactamase activity.[A216921] However, this effect is transient, as the hydrolysis product, ampicillin, is readily inactivated by beta lactamase.[A216921] Hetacillin locks up the offending amino group and prevents the decomposition of Hetacillin. Once hydrolyzed to ampicillin (and acetone), ampicillin binds to the penicillin binding proteins found in susceptible bacteria. This inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins.

null

Hydrolyzed to active ampicillin via esterases

null

Organic compounds

Organoheterocyclic compounds

Lactams

Beta lactams

[ "approved", "vet_approved", "withdrawn" ]

[ "J01CA", "J01C", "J01", "J", "J01CR", "J01C", "J01", "J" ]

[ "Enteric bacteria and other eubacteria" ]

[]

[]

[ "Natacillin", "Versapen" ]

[]

DB00740

Riluzole

A glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. Riluzole is marketed as Rilutek by Sanofi.

solid

For the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)

Riluzole, a member of the benzothiazole class, is indicated for the treatment of patients with amyotrophic lateral sclerosis (ALS). Riluzole extends survival and/or time to tracheostomy. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.

The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release (activation of glutamate reuptake), 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.

Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.

Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.

null

The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.

96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range.

null

Organic compounds

Organoheterocyclic compounds

Benzothiazoles

null

[ "approved", "investigational" ]

[ "N07XX", "N07X", "N07", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "18.77", "description": "Rilutek 50 mg tablet", "unit": "tablet" } ]

[ { "approved": "1996-06-18", "country": "United States", "expires": "2013-06-18", "number": "5527814" }, { "approved": "2005-09-20", "country": "Canada", "expires": "2013-12-10", "number": "2151604" }, { "approved": "2000-01-25", "country": "Canada", "expires": "2012-10-22", "number": "2117466" }, { "approved": "2014-07-01", "country": "United States", "expires": "2029-03-12", "number": "8765150" }, { "approved": "2013-12-10", "country": "United States", "expires": "2024-04-03", "number": "8603514" }, { "approved": "2014-07-01", "country": "United States", "expires": "2024-02-20", "number": "8765167" } ]

[ "Apo-riluzole", "Exservan", "Exservan", "Exservan", "Mylan-riluzole", "Rilutek", "Rilutek", "Rilutek", "Rilutek", "Rilutek", "Rilutek", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole", "Riluzole Zentiva", "Riluzole Zentiva", "Riluzole Zentiva", "Riluzole Zentiva", "Riluzole Zentiva", "Teglutik", "Teglutik", "Teglutik", "Tiglutik" ]

[ "Fanizan", "Laidec", "Lizolorol", "Lizorolol", "Rilustad", "Sclefic", "Xie Yi Li", "Zolerilis" ]

[]

[ "Q14524", "Q9UI33", "Q9UPY5" ]

[ "P04798", "P05177" ]

[]

[ "Q9UNQ0" ]

DB00742

Mannitol

Mannitol is an osmotic diuretic that is metabolically inert in humans and occurs naturally, as a sugar or sugar alcohol, in fruits and vegetables. Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and pressure may be reduced. Mannitol may also be used for the promotion of diuresis before irreversible renal failure becomes established; the promotion of urinary excretion of toxic substances; as an Antiglaucoma agent; and as a renal function diagnostic aid. On October 30, 2020, mannitol was approved by the FDA as add-on maintenance therapy for the control of pulmonary symptoms associated with cystic fibrosis in adult patients and is currently marketed for this indication under the name BRONCHITOL® by Chiesi USA Inc.[L20024]

solid

Used for the promotion of diuresis before irreversible renal failure becomes established, the reduction of intracranial pressure, the treatment of cerebral edema, and the promotion of urinary excretion of toxic substances. Mannitol is also indicated as add-on maintenance therapy for improving pulmonary function in cystic fibrosis patients aged 18 and over who have passed the BRONCHITOL tolerance test (BTT). It is recommended that patients take an orally inhaled short-acting bronchodilator 5-15 minutes prior to every inhaled mannitol dose.[L20024]

Chemically, mannitol is an alcohol and a sugar, or a polyol; it is similar to xylitol or sorbitol. However, mannitol has a tendency to lose a hydrogen ion in aqueous solutions, which causes the solution to become acidic. For this reason, it is not uncommon to add a substance to adjust its pH, such as sodium bicarbonate. Mannitol is commonly used to increase urine production (diuretic). It is also used to treat or prevent medical conditions that are caused by an increase in body fluids/water (e.g., cerebral edema, glaucoma, kidney failure). Mannitol is frequently given along with other diuretics (e.g., furosemide, chlorothiazide) and/or IV fluid replacement. Inhaled mannitol has the possibility to cause bronchospasm and hemoptysis; the occurrence of either should lead to discontinuation of inhaled mannitol.[L20024]

Mannitol is an osmotic diuretic that is metabolically inert in humans and occurs naturally, as a sugar or sugar alcohol, in fruits and vegetables. Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and pressure may be reduced. As a diurectic mannitol induces diuresis because it is not reabsorbed in the renal tubule, thereby increasing the osmolality of the glomerular filtrate, facilitating excretion of water, and inhibiting the renal tubular reabsorption of sodium, chloride, and other solutes. Mannitol promotes the urinary excretion of toxic materials and protects against nephrotoxicity by preventing the concentration of toxic substances in the tubular fluid. As an Antiglaucoma agent mannitol levates blood plasma osmolarity, resulting in enhanced flow of water from the eye into plasma and a consequent reduction in intraocular pressure. As a renal function diagnostic aid mannitol is freely filtered by the glomeruli with less than 10% tubular reabsorption. Therefore, its urinary excretion rate may serve as a measurement of glomerular filtration rate (GFR). The exact mechanism of action of inhaled mannitol in the symptomatic maintenance treatment of cystic fibrosis remains unclear.[A223199, L20024] It is hypothesized that mannitol produces an osmotic gradient across the airway epithelium that draws fluid into the extracellular space and alters the properties of the airway surface mucus layer, allowing easier mucociliary clearance.[A223199]

Approximately 7% of ingested mannitol is absorbed during gastrointestinal perfusion in uremic patients. Inhalation of 635 mg of mannitol powder yields a plasma Cmax of 13.71 μg/mL in 1.5 hours (Tmax) and a mean systemic AUC of 73.15 μg\*h/mL.[L20024]

Mannitol is metabolized only slightly, if at all, to glycogen in the liver.

Mannitol overdose may result in bronchoconstriction and should be counteracted using a short-acting bronchodilator and other symptomatic and supportive care, as necessary.[L20024]

Mannitol has an elimination half-life of 4.7 hours following oral administration; the mean terminal elimination half-life is similar regardless of administration route (oral, inhalation, and intravenous.[L20024]

null

Mannitol is primarily excreted unchanged in the urine. Following oral inhalation of 635 mg of mannitol in healthy volunteers, 55% of the total dose was recovered unchanged in the urine; following oral or intravenous administration of 500 mg, the corresponding values were 54 and 87%, respectively.[L20024]

Mannitol administered intravenously has a volume of distribution of 34.3 L.[L20024]

Intravenous administration of mannitol yields a total clearance of 5.1 L/hr and renal clearance of 4.4 L/hr.[L20024]

Organic compounds

Organic oxygen compounds

Organooxygen compounds

Carbohydrates and carbohydrate conjugates

[ "approved", "investigational" ]

[ "B05CX", "B05C", "B05", "B", "A06AD", "A06A", "A06", "A", "R05CB", "R05C", "R05", "R", "B05BC", "B05B", "B05", "B", "V04CX", "V04C", "V04", "V" ]

[ "Humans and other mammals" ]

[ { "cost": "0.01", "description": "Resectisol 5% solution", "unit": "ml" }, { "cost": "0.02", "description": "Mannitol 10% iv solution", "unit": "ml" }, { "cost": "0.02", "description": "Mannitol 5% iv solution", "unit": "ml" }, { "cost": "0.03", "description": "Mannitol 25% vial", "unit": "ml" }, { "cost": "0.03", "description": "Osmitrol 5% iv solution", "unit": "ml" }, { "cost": "0.04", "description": "Mannitol 15% iv solution", "unit": "ml" }, { "cost": "0.04", "description": "Mannitol 20% iv solution", "unit": "ml" }, { "cost": "0.05", "description": "Mannitol powder", "unit": "g" }, { "cost": "0.07", "description": "Osmitrol 10% iv solution", "unit": "ml" }, { "cost": "0.07", "description": "Osmitrol 15% iv solution", "unit": "ml" }, { "cost": "0.15", "description": "Osmitrol 20% iv solution", "unit": "ml" } ]

[]

[ "Additive Solution Sodium Adenine Glucose Mannitol (sagm)", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "Aridol", "Aridol", "Aridol", "Aridol", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Bronchitol", "Bronchitol", "Bronchitol", "Bronchitol", "Cpd/adsol", "Cpd/adsol", "Cpd/adsol", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "Curestem Cell Healer C10 Program", "Curestem Cell Healer C10 Program", "Curestem Cell Healer C20", "Curestem Cell Healer C5 Program", "Cystosol W 3% Hexitols", "GD11 Rx SCM C5", "IMUFLEX WB-RP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Removing Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "IMUFLEX WB-RP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Saving Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) and OPTISOL (AS-5) Red Cell Preservative for collection of 500mL of Blood", "IMUFLEX WB-SP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Saving Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) and OPTISOL (AS-5) Red Cell Preservative", "Leucoflex CGP", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol", "Mannitol Inj 10% Abbovac", "Mannitol Inj 25%", "Mannitol Inj 25%", "Mannitol Inj 5% Abbovac", "Mannitol Injection USP", "Mannitol Injection USP", "Mannitol Injection, USP", "MTL1 Leucoflex", "Osmitrol", "Osmitrol", "Osmitrol", "Osmitrol", "Osmitrol Injection 10%", "Osmitrol Injection 20%", "Qr Pain", "Qr Pain", "Resectisol (5% Mannitol Irrigation)", "Sag-M", "Sag-mannitol Solution", "Sorbitol Mannitol Irrigation", "Sorbitol-Mannitol", "Sorbitol-Mannitol", "TERUFLEX Blood Bag System Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL Red Cell Preservative", "TERUFLEX Blood Bag System with Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "TERUFLEX Blood Bag System with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "TERUFLEX Blood Bag System with Diversion Blood Sampling Arm Anticoagulant CPD with OPTISOL Red Cell Preservative Solution for Collection of 500mL of Blood", "TERUFLEX Blood with Diversion Blood Sampling Arm Anticoagulant CPD with OPTISOL Red Cell Preservative for Collection of 450mL of Blood" ]

[ "Anol", "Aridol", "Deltamannit", "Demanitol", "Diurecide", "Isotol", "Manicol", "Manit", "Manitol Mein", "Maniton", "Mannigen", "Mannisol", "Mannisol A", "Mannit", "Mannit-Lösung", "Mannite Actipharm", "Osmofundin", "Osmohale", "Osmosol", "Osmosteril", "Resectisol" ]

[ "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Cpd/adsol", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "Cpd/adsol", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Sorbitol-Mannitol", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "CPD/ADSOL Red Cell Preservation Solution System (PL 2209)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "Cpd/adsol", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "ADSOL Red Cell Preservation Solution System in Plastic Container (PL 146 Plastic)", "MTL1 Leucoflex", "Leucoflex CGP", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "Aridol Bronchial Challenge Test Kit", "IMUFLEX WB-SP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Saving Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) and OPTISOL (AS-5) Red Cell Preservative", "TERUFLEX Blood Bag System with Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "IMUFLEX WB-RP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Removing Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "TERUFLEX Blood Bag System with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL (AS-5) Red Cell Preservative", "TERUFLEX Blood Bag System Anticoagulant Citrate Phosphate Dextrose (CPD) AND OPTISOL Red Cell Preservative", "Additive Solution Sodium Adenine Glucose Mannitol (sagm)", "Curestem Cell Healer C5 Program", "Curestem Cell Healer C10 Program", "Curestem Cell Healer C10 Program", "Sorbitol-Mannitol", "Cystosol W 3% Hexitols", "Sag-mannitol Solution", "Sorbitol Mannitol Irrigation", "Sag-M", "Aridol", "Aridol", "Aridol", "Aridol", "Qr Pain", "Qr Pain", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "Adsol Red Cell Preservation", "TERUFLEX Blood Bag System with Diversion Blood Sampling Arm Anticoagulant CPD with OPTISOL Red Cell Preservative Solution for Collection of 500mL of Blood", "TERUFLEX Blood with Diversion Blood Sampling Arm Anticoagulant CPD with OPTISOL Red Cell Preservative for Collection of 450mL of Blood", "IMUFLEX WB-RP Blood Bag System with Integral Whole Blood Leukocyte Reduction Filter (Saving Platelets) with Diversion Blood Sampling Arm Anticoagulant Citrate Phosphate Dextrose (CPD) and OPTISOL (AS-5) Red Cell Preservative for collection of 500mL of Blood" ]

[]

DB00743

Gadobenic acid

Gadobenic acid, usually available in the salt form gadobenate dimeglumine, is a linear MRI gadolinium-based contrast agent (GBCA) used primarily for MR imaging of the liver.[A263086] It differs from other GBCAs due to the benzene ring that confers weak protein binding, thus leading to an increased R1 and R2 relaxivity.[A263166] As gadobenate dimeglumine is specifically taken up by hepatocytes and excreted through the biliary system, it is a useful contrast agent for liver MRI.[A1139] Gadobenate dimeglumine was approved by the FDA in November 2004 under the brand name MultiHance.[A263166]

liquid

Gadobenate dimeglumine is indicated for use in magnetic resonance imaging (MRI) of the central nervous system in adult and pediatric patients in order to visualize lesions with abnormal blood-brain barrier or abnormal vascularity of the brain, spine, and associated tissues.[L40888] It is also indicated for use in magnetic resonance angiography (MRA) to evaluate adults with known or suspected renal or aorto-ilio-femoral occlusive vascular disease.[L40888]

Unlike other paramagnetic contrast agents, gadobenate dimeglumine demonstrates weak and transient interactions with serum proteins that cause slowing in the molecular tumbling dynamics, resulting in strong increases in relaxivity in solutions containing serum proteins. The improved relaxation effect can contribute to increased contrast-to-noise ratio and lesion-to-brain ratio, which may improve visualization.[L49936] Disruption of the blood-brain barrier or abnormal vascularity allows enhancement by gadobenate dimeglumine of lesions such as neoplasms, abscesses, and infarcts. Uptake of gadobenate dimeglumine into hepatocytes has been demonstrated.[L49936]

Gadobenate dimeglumine is a paramagnetic agent and, as such, develops a magnetic moment when placed in a magnetic field. The large magnetic moment produced by the paramagnetic agent results in a large local magnetic field, which can enhance the relaxation rates of water protons in its vicinity leading to an increase of signal intensity (brightness) of tissue.[L49936] In magnetic resonance imaging (MRI), visualization of normal and pathological tissue depends in part on variations in the radiofrequency signal intensity that occur with 1) differences in proton density; 2) differences of the spin-lattice or longitudinal relaxation times (T1); and 3) differences in the spin-spin or transverse relaxation time (T2). When placed in a magnetic field, gadobenate dimeglumine decreases the T1 and T2 relaxation time in target tissues. At recommended doses, the effect is observed with the greatest sensitivity in the T1-weighted sequences.[L49936]

Three single-dose intravenous studies were conducted in 32 healthy male subjects to assess the pharmacokinetics of gadobenate dimeglumine. The doses administered in these studies ranged from 0.005 to 0.4 mmol/kg. Upon injection, the meglumine salt is completely dissociated from the gadobenate dimeglumine complex. Thus, the pharmacokinetics is based on the assay of gadobenate ion, the MRI contrast effective ion in gadobenate dimeglumine. Data for plasma concentration and area under the curve demonstrated linear dependence on the administered dose. The pharmacokinetics of gadobenate ion following intravenous administration can be best described using a two-compartment model.[L49936] A population pharmacokinetic analysis incorporated data from 25 healthy subjects (14 males and 11 females) and 15 subjects undergoing MR imaging of the central nervous system (7 males and 8 females) between ages of 2 and 16 years. The subjects received a single intravenous dose of 0.1 mmol/kg of gadobenate dimeglumine. The geometric mean Cmax was 62.3 µg/mL (n=16) in children 2 to 5 years of age, and 64.2 µg/mL (n=24) in children older than 5 years. The geometric mean AUC0-∞ was 77.9 μg⋅h/mL in children 2-5 years of age (n=16) and 82.6 μg⋅h/mL in children older than 5 years (n=24). The geometric mean half-life was 1.2 hours in children 2 to 5 years of age and 0.93 hours in children older than 5 years. There was no significant gender-related difference in the pharmacokinetic parameters in the pediatric patients. Pharmacokinetic simulations indicate similar AUC and Cmax values for gadobenate dimeglumine in pediatric subjects less than 2 years when compared to those reported for adults; no age-based dose adjustment is necessary for this pediatric population.[L49936]

There was no detectable biotransformation of gadobenate ion. Dissociation of gadobenate ion in vivo has been shown to be minimal, with less than 1% of the free chelating agent being recovered alone in feces.[L49936]

GBCAs cross the placenta and result in fetal exposure and gadolinium retention. The human data on the association between GBCAs and adverse fetal outcomes are limited and inconclusive. In animal reproduction studies, gadobenate dimeglumine has been shown to be teratogenic in rabbits following repeated intravenous administration during organogenesis at doses up to 6 times the recommended human dose. There were no adverse developmental effects observed in rats with intravenous administration of gadobenate dimeglumine during organogenesis at doses up to three times the recommended human dose. Because of the potential risks of gadolinium to the fetus, use gadobenate dimeglumine only if imaging is essential and cannot be delayed.[L49936] Clinical consequences of overdosage with gadobenate dimeglumine have not been reported. Treatment of an overdosage should be directed toward support of vital functions and prompt institution of symptomatic therapy. In a Phase 1 clinical study, doses up to 0.4 mmol/kg were administered to patients. Gadobenate dimeglumine has been shown to be dialyzable.[L49936] Long-term animal studies have not been performed to evaluate the carcinogenic potential of gadobenate dimeglumine.[L49936] The results for gadobenate dimeglumine were negative in the following genetic toxicity studies: 1) in vitro bacteria reverse mutation assays, 2) an in vitro gene mutation assay in mammalian cells, 3) an in vitro chromosomal aberration assay, 4) an in vitro unscheduled DNA synthesis assay, and 5) an in vivo micronucleus assay in rats.[L49936] Gadobenate dimeglumine had no effect on fertility and reproductive performance at IV doses of up to 2 mmol/kg/day (3 times the human dose on body surface basis) for 13 weeks in male rats and for 32 days in female rats. However, vacuolation in testes and abnormal spermatogenic cells were observed when gadobenate dimeglumine was intravenously administered to male rats at 3 mmol/kg/day (5 times the human dose on body surface basis) for 28 days. The effects were not reversible following 28-day recovery period. The effects were not reported in dog and monkey studies (at doses up to about 11 and 10 times the human dose on body surface basis for dogs (28 days dosing) and monkeys (14 days dosing), respectively).[L49936]

Gadobenate ion has a rapid distribution half-life (reported as mean ± SD) of 0.084 ± 0.012 to 0.605 ± 0.072 hours. The mean elimination half-life ranged from 1.17 ± 0.26 to 2.02 ± 0.60 hours.[L49936]

Although in vitro studies showed no appreciable binding of gadobenate ion to human serum proteins, in vivo studies have demonstrated a weak affinity binding of gadobenate to albumin.[A12073,A12075,L49936]

Gadobenate ion is eliminated predominately via the kidneys, with 78% to 96% of an administered dose recovered in the urine. A small percentage of the administered dose (0.6% to 4%) is eliminated via the biliary route and recovered in feces.[L49936]

The volume of distribution of the central compartment ranged from 0.074 ± 0.017 to 0.158 ± 0.038 L/kg, and estimates of volume of distribution by area ranged from 0.170 ± 0.016 to 0.282 ± 0.079 L/kg.[L49936]

The total plasma clearance and renal clearance estimates of gadobenate ion were similar, ranging from 0.093 ± 0.010 to 0.133 ± 0.270 L/hr/kg and 0.082 ± 0.007 to 0.104 ± 0.039 L/hr/kg, respectively. The clearance is similar to that of substances that are subject to glomerular filtration.[L49936]

null

[ "approved", "investigational" ]

[ "V08CA", "V08C", "V08", "V" ]

[ "Humans and other mammals" ]

[ { "cost": "6.87", "description": "Multihance 529 mg/ml vial", "unit": "ml" } ]

[ { "approved": "1990-04-10", "country": "United States", "expires": "2012-04-10", "number": "4916246" } ]

[ "MultiHance", "MultiHance", "MultiHance" ]

[ "Multihance Multipack" ]

[]

[ "P02768" ]

[]

[ "P02768" ]

[ "Q92887" ]

DB00744

Zileuton

Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. The immediate release tablet of Zileuton has been withdrawn from the US market.

solid

For the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.

Zileuton is an asthma drug that differs chemically and pharmacologically from other antiasthmatic agents. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway. Current data indicates that asthma is a chronic inflammatory disorder of the airways involving the production and activity of several endogenous inflammatory mediators, including leukotrienes. Sulfido-peptide leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, are derived from the initial unstable product of arachidonic acid metabolism, leukotriene A4 (LTA4), and can be measured in a number of biological fluids including bronchoalveolar lavage fluid (BALF) from asthmatic patients. In humans, pretreatment with zileuton attenuated bronchoconstriction caused by cold air challenge in patients with asthma.

Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. Due to the role of leukotrienes in the pathogenesis of asthma, modulation of leukotriene formation by interruption of 5-lipoxygenase activity may reduce airway symptoms, decrease bronchial smooth muscle tone, and improve asthma control.

Rapidly and almost completely absorbed. The absolute bioavailability is unknown.

Hepatic. Zileuton and its N-dehydroxylated metabolite are oxidatively metabolized by the cytochrome P450 isoenzymes 1A2, 2C9 and 3A4.

Minimum oral lethal dose of zileuton in various preparations was 500-4000 mg/kg in mice and 300-1000 mg/kg in rats (providing greater than 3 and 9 times the systemic exposure [AUC] achieved at the maximum recommended human daily oral dose, respectively).

2.5 hours

93% bound to plasma proteins, primarily to albumin.

Elimination of zileuton is predominantly via metabolism with a mean terminal half-life of 2.5 hours. The urinary excretion of the inactive N-dehydroxylated metabolite and unchanged zileuton each accounted for less than 0.5% of the dose.

* 1.2 L/kg

* Apparent oral cl=7 mL/min/kg

Organic compounds

Organoheterocyclic compounds

Benzothiophenes

1-benzothiophenes

[ "approved", "investigational", "withdrawn" ]

[]

[ "Humans and other mammals" ]

[ { "cost": "5.99", "description": "Zyflo 600 mg filmtab", "unit": "tablet" }, { "cost": "5.99", "description": "Zyflo cr 600 mg tablet", "unit": "tablet" }, { "cost": "6.23", "description": "Zyflo CR 600 mg 12 Hour tablet", "unit": "tablet" }, { "cost": "6.49", "description": "Zyflo 600 mg tablet", "unit": "tablet" } ]

[ { "approved": "1995-06-06", "country": "United States", "expires": "2012-06-06", "number": "5422123" }, { "approved": "1989-10-10", "country": "United States", "expires": "2010-12-09", "number": "4873259" } ]

[ "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zileuton", "Zyflo", "Zyflo", "Zyflo CR", "Zyflo CR" ]

[]

[ "P09917" ]

[ "P23219", "O60656", "P11712", "P05177", "P08684" ]

[ "P02768" ]

[]

DB00745

Modafinil

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA.

solid

To improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy.

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction.

The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects. It is possible that modafinil acts by a synergistic combination of mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors.

Rapid following oral administration.

Hepatic

null

23-215 hours

60%

The major route of elimination is metabolism (~90%), primarily by the liver, with subsequent renal elimination of the metabolites.

* 0.9 L/kg

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Diphenylmethanes

[ "approved", "investigational" ]

[ "N06BA", "N06B", "N06", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "13.58", "description": "Provigil 100 mg tablet", "unit": "tablet" }, { "cost": "15.33", "description": "Provigil 200 mg tablet", "unit": "tablet" } ]

[ { "approved": "2002-01-15", "country": "United States", "expires": "2014-10-06", "number": "RE37516" }, { "approved": "2005-08-02", "country": "Canada", "expires": "2014-06-14", "number": "2165824" }, { "approved": "2002-12-10", "country": "Canada", "expires": "2015-10-04", "number": "2201967" }, { "approved": "2007-11-20", "country": "United States", "expires": "2024-05-29", "number": "7297346" } ]

[ "Alertec", "Apo-modafinil", "Auro-modafinil", "Bio-modafinil", "Ipg-modafinil", "Jamp Modafinil", "Mar-modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil", "Modafinil Tablets", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Provigil", "Teva-modafinil" ]

[ "Alertex", "Aspendos", "Forcilin", "Mentix", "Modasomil", "Modavigil", "Modiodal", "Provake", "Resotyl", "Sparlon", "Stavigile", "Vigicer", "Vigil", "Zalux" ]

[]

[ "Q01959", "P35368" ]

[ "P33261", "P08684", "P20815", "P05177", "P20813", "P11712", "P10635" ]

[]

DB00746

Deferoxamine

Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.

solid

Used to treat acute iron or aluminum toxicity (an excess of aluminum in the body) in certain patients. Also used in certain patients with anemia who must receive many blood transfusions.

Deferoxamine, otherwise known as desferrioxamine or desferal, is a chelating agent used to remove excess iron or aluminum from the body. It acts by binding free iron or aluminum in the bloodstream and enhancing its elimination in the urine. By removing excess iron or aluminum, the agent reduces the damage done to various organs and tissues, such as the liver.

Deferoxamine works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming ferrioxamine, a stable complex which is eliminated via the kidneys. 100 mg of deferoxamine is capable of binding approximately 8.5 mg of trivalent (ferric) iron. Deferoxamine works in treating aluminum toxicity by binding to tissue-bound aluminum to form aluminoxamine, a stable, water-soluble complex. The formation of aluminoxamine increases blood concentrations of aluminum, resulting in an increased concentration gradient between the blood and dialysate, boosting the removal of aluminum during dialysis. 100 mg of deferoxamine is capable of binding approximately 4.1 mg of aluminum.

Deferoxamine is rapidly absorbed after intramuscular or subcutaneous administration, but only poorly absorbed from the gastrointestinal tract in the presence of intact mucosa.

Deferoxamine is mainly metabolised in the plasma and hepatic metabolism is minimal. A number of metabolites have been isolated but not characterised. Some metabolites of deferoxamine, most notably the product of oxidative deamination, also chelate iron, and thus the antidotal effect of the drug appears unaffected by hepatic metabolism.

Intravenous LD50 in mouse, rat, and rabbit is 340 mg/kg, 520 mg/kg, and 600 mg/kg, respectively. Subcutaneous LD50 in mouse and rat is 1600 mg/kg and >1000 mg/kg, respectively. Oral LD50 in mouse and rat is >3000 mg/kg and >1000 mg/kg, respectively. Nephrotoxicity, ototoxicity and retinal toxicity have been reported following long-term administration for chronic iron overload.

Biphasic elimination pattern in healthy volunteers with a first rapid phase half life of 1 hour and a second slow phase half-life of 6 hours.

Less than 10% bound to serum proteins in vitro.

Deferoxamine mesylate is metabolized principally by plasma enzymes, but the pathways have not yet been defined. Some is also excreted in the feces via the bile.

null

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Carboxylic acid derivatives

[ "approved", "investigational" ]

[ "V03AC", "V03A", "V03", "V" ]

[ "Humans and other mammals" ]

[ { "cost": "8.44", "description": "Desferrioxamine Mesilate 500 mg/vial", "unit": "vial" }, { "cost": "8.44", "description": "Pms-Deferoxamine 500 mg/vial", "unit": "vial" }, { "cost": "15.07", "description": "Desferal 500 mg/vial", "unit": "vial" }, { "cost": "23.92", "description": "Desferal 500 mg Solution Vial", "unit": "vial" }, { "cost": "33.89", "description": "Desferrioxamine Mesilate 2 g/vial", "unit": "vial" }, { "cost": "33.89", "description": "Pms-Deferoxamine 2 g/vial", "unit": "vial" }, { "cost": "46.25", "description": "Deferoxamine 2 gram vial", "unit": "vial" }, { "cost": "60.52", "description": "Desferal 2 g/vial", "unit": "vial" }, { "cost": "113.94", "description": "Desferal 2 gram vial", "unit": "vial" } ]

[]

[ "Deferoxamine", "Deferoxamine", "Deferoxamine Mesylate", "Deferoxamine Mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine Mesylate", "Deferoxamine Mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine mesylate", "Deferoxamine Mesylate for Injection", "Deferoxamine Mesylate for Injection", "Deferoxamine Mesylate for Injection", "Desferal", "Desferal", "Desferal 2g", "Desferal 500mg", "PMS-deferoxamine", "PMS-deferoxamine" ]

[ "Desferin" ]

[]

[ "P05067" ]

[ "P47989" ]

[]

DB00747

Scopolamine

Scopolamine is a tropane alkaloid isolated from members of the _Solanaceae_ family of plants, similar to [atropine] and [hyoscyamine], all of which structurally mimic the natural neurotransmitter [acetylcholine].[A228423, A228763] Scopolamine was first synthesized in 1959, but to date, synthesis remains less efficient than extracting scopolamine from plants.[A228763] As an acetylcholine analogue, scopolamine can antagonize muscarinic acetylcholine receptors (mAChRs) in the central nervous system and throughout the body, inducing several therapeutic and adverse effects related to alteration of parasympathetic nervous system and cholinergic signalling.[A228758, L31578] Due to its dose-dependent adverse effects, scopolamine was the first drug to be offered commercially as a transdermal delivery system, Scopoderm TTS®, in 1981.[A228423, A228758] As a result of its anticholinergic effects, scopolamine is being investigated for diverse therapeutic applications; currently, it is approved for the prevention of nausea and vomiting associated with motion sickness and surgical procedures.[A228773, L31578] Scopolamine was first approved by the FDA on December 31, 1979, and is currently available as both oral tablets and a transdermal delivery system.[L31578]

solid

Scopolamine is indicated in adult patients for the prevention of nausea and vomiting associated with motion sickness and for the prevention of postoperative nausea and vomiting (PONV) associated with anesthesia or opiate analgesia.[L31578]

Scopolamine is an anticholinergic belladonna alkaloid that, through competitive inhibition of muscarinic receptors, affects parasympathetic nervous system function and acts on smooth muscles that respond to acetylcholine but lack cholinergic innervation. Formulated as a patch, scopolamine is released continuously over three days and remains detectable in urine over a period of 108 hours. Scopolamine is contraindicated in angle-closure glaucoma and should be used with caution in patients with open-angle glaucoma due to scopolamine's ability to increase intraocular pressure. Also, scopolamine exhibits several neuropsychiatric effects: exacerbated psychosis, seizures, seizure-like, and other psychiatric reactions, and cognitive impairment; scopolamine may impair the ability of patients to operate machinery or motor vehicles, play underwater sports, or perform any other potentially hazardous activity. Women with severe preeclampsia should avoid scopolamine. Patients with gastrointestinal or urinary disorders should be monitored frequently for impairments, and scopolamine should be discontinued if these develop. Scopolamine can cause blurred vision if applied directly to the eye, and the transdermal patch should be removed before an MRI procedure to avoid skin burns. Due to its gastrointestinal effects, scopolamine can interfere with gastric secretion testing and should be discontinued at least 10 days before performing the test. Finally, scopolamine may induce dependence and resulting withdrawal symptoms, such as nausea, dizziness, vomiting, gastrointestinal disturbances, sweating, headaches, bradycardia, hypotension, and various neuropsychiatric manifestations following treatment discontinuation; severe symptoms may require medical attention.[L31578]

[Acetylcholine] (ACh) is a neurotransmitter that can signal through ligand-gated cation channels (nicotinic receptors) and G-protein-coupled muscarinic receptors (mAChRs). ACh signalling via mAChRs located in the central nervous system (CNS) and periphery can regulate smooth muscle contraction, glandular secretions, heart rate, and various neurological phenomena such as learning and memory.[A228738, A228743] mAChRs can be divided into five subtypes, M1-M5, expressed at various levels throughout the brain.[A228743] Also, M2 receptors are found in the heart and M3 receptors in smooth muscles, mediating effects apart from the direct modulation of the parasympathetic nervous system.[A228423] While M1, M3, and M5 mAChRs primarily couple to Gq proteins to activate phospholipase C, M2 and M4 mainly couple to Gi/o proteins to inhibit adenylyl cyclase and modulate cellular ion flow.[A228743] This system, in part, helps to control physiological responses such as nausea and vomiting.[L31578] Scopolamine acts as a non-selective competitive inhibitor of M1-M5 mAChRs, albeit with weaker M5 inhibition; as such, scopolamine is an anticholinergic with various dose-dependent therapeutic and adverse effects.[A228423, A228758, A228763] The exact mechanism(s) of action of scopolamine remains poorly understood. Recent evidence suggests that M1 (and possibly M2) mAChR antagonism at interneurons acts through inhibition of downstream neurotransmitter release and subsequent pyramidal neuron activation to mediate neurological responses associated with stress and depression.[A228773] Similar antagonism of M4 and M5 receptors is associated with potential therapeutic benefits in neurological conditions such as schizophrenia and substance abuse disorders.[A228743] The significance of these observations to scopolamine's current therapeutic indications of preventing nausea and vomiting is unclear but is linked to its anticholinergic effect and ability to alter signalling through the CNS associated with vomiting.[A228758, L31578]

The pharmacokinetics of scopolamine differ substantially between different dosage routes. Oral administration of 0.5 mg scopolamine in healthy volunteers produced a Cmax of 0.54 ± 0.1 ng/mL, a tmax of 23.5 ± 8.2 min, and an AUC of 50.8 ± 1.76 ng\*min/mL; the absolute bioavailability is low at 13 ± 1%, presumably because of first-pass metabolism.[A228758] By comparison, IV infusion of 0.5 mg scopolamine over 15 minutes resulted in a Cmax of 5.00 ± 0.43 ng/mL, a tmax of 5.0 min, and an AUC of 369.4 ± 2.2 ng\*min/mL.[A228758] Other dose forms have also been tested. Subcutaneous administration of 0.4 mg scopolamine resulted in a Cmax of 3.27 ng/mL, a tmax of 14.6 min, and an AUC of 158.2 ng\*min/mL. Intramuscular administration of 0.5 scopolamine resulted in a Cmax of 0.96 ± 0.17 ng/mL, a tmax of 18.5 ± 4.7 min, and an AUC of 81.3 ± 11.2 ng\*min/mL. Absorption following intranasal administration was found to be rapid, whereby 0.4 mg of scopolamine resulted in a Cmax of 1.68 ± 0.23 ng/mL, a tmax of 2.2 ± 3 min, and an AUC of 167 ± 20 ng\*min/mL; intranasal scopolamine also had a higher bioavailability than that of oral scopolamine at 83 ± 10%.[A228758] Due to dose-dependent adverse effects, the transdermal patch was developed to obtain therapeutic plasma concentrations over a longer period of time. Following patch application, scopolamine becomes detectable within four hours and reaches a peak concentration (tmax) within 24 hours. The average plasma concentration is 87 pg/mL, and the total levels of free and conjugated scopolamine reach 354 pg/mL.[L31578]

Little is known about the metabolism of scopolamine in humans, although many metabolites have been detected in animal studies.[A228758] In general, scopolamine is primarily metabolized in the liver, and the primary metabolites are various glucuronide and sulphide conjugates.[A228758, A228763] Although the enzymes responsible for scopolamine metabolism are unknown, _in vitro_ studies have demonstrated oxidative demethylation linked to CYP3A subfamily activity, and scopolamine pharmacokinetics were significantly altered by coadministration with grapefruit juice, suggesting that CYP3A4 is responsible for at least some of the oxidative demethylation.[A228758, A228923]

Scopolamine overdose may manifest as lethargy, somnolence, coma, confusion, agitation, hallucinations, convulsion, visual disturbance, dry flushed skin, dry mouth, decreased bowel sounds, urinary retention, tachycardia, hypertension, and supraventricular arrhythmias. In some cases, overdose symptoms may appear similar to those associated with withdrawal following discontinuation. However, withdrawal symptoms such as bradycardia, headache, nausea, abdominal cramps, and sweating can help to distinguish between these possibilities. Overdose management primarily involves the removal of all transdermal patch systems combined with symptomatic and supportive care. Ensuring an adequate airway, supplemental oxygen, establishing intravenous access, and continuous monitoring are recommended. In cases where patients have swallowed one or more patch systems, it may be necessary to remove them or administer activated charcoal.[L31578] Animal studies revealed an oral LD50 of 1880 mg/kg in mice and 1270 mg/kg in rats, and a subcutaneous LD50 of 1650 mg/kg in mice and 296 mg/kg in rats.[L31753]

The half-life of scopolamine differs depending on the route. Intravenous, oral, and intramuscular administration have similar half-lives of 68.7 ± 1.0, 63.7 ± 1.3, and 69.1 ±8/0 min, respectively. The half-life is greater with subcutaneous administration at 213 min.[A228758] Following removal of the transdermal patch system, scopolamine plasma concentrations decrease in a log-linear fashion with a half-life of 9.5 hours.[L31578]

Scopolamine may reversibly bind plasma proteins in humans.[L31578] In rats, scopolamine exhibits relatively low plasma protein binding of 30 ± 10%.[A228758]

Following oral administration, approximately 2.6% of unchanged scopolamine is recovered in urine.[A228758] Compared to this, using the transdermal patch system, less than 10% of the total dose, both as unchanged scopolamine and metabolites, is recovered in urine over 108 hours. Less than 5% of the total dose is recovered unchanged.[L31578]

The volume of distribution of scopolamine is not well characterized.[L31578] IV infusion of 0.5 mg scopolamine over 15 minutes resulted in a volume of distribution of 141.3 ± 1.6 L.[A228758]

IV infusion of 0.5 mg scopolamine resulted in a clearance of 81.2 ± 1.55 L/h, while subcutaneous administration resulted in a lower clearance of 0.14-0.17 L/h.[A228758]

Organic compounds

Organic acids and derivatives

Hydroxy acids and derivatives

Beta hydroxy acids and derivatives

[ "approved", "investigational" ]

[ "N05CM", "N05C", "N05", "N", "S01FA", "S01F", "S01", "S", "A04AD", "A04A", "A04", "A", "A04AD", "A04A", "A04", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "1.61", "description": "Methscopolamine brom 2.5 mg tablet", "unit": "tablet" }, { "cost": "1.67", "description": "Methscopolamine Bromide 2.5 mg tablet", "unit": "tablet" }, { "cost": "2.09", "description": "Methscopolamine brom 5 mg tablet", "unit": "tablet" }, { "cost": "2.17", "description": "Methscopolamine Bromide 5 mg tablet", "unit": "tablet" }, { "cost": "2.66", "description": "Pamine 2.5 mg tablet", "unit": "tablet" }, { "cost": "3.9", "description": "Pamine forte 5 mg tablet", "unit": "tablet" }, { "cost": "4.5", "description": "Buscopan 20 mg/ml", "unit": "ml" }, { "cost": "5.4", "description": "Scopolamine 0.4 mg/ml vial", "unit": "ml" }, { "cost": "5.59", "description": "Isopto hyoscine 0.25% drops", "unit": "ml" }, { "cost": "6.86", "description": "Scopolamine hbr crystals", "unit": "g" }, { "cost": "12.01", "description": "Transderm-scop 1.5 mg/72hr", "unit": "each" }, { "cost": "12.04", "description": "Transderm-Scop 1.5 mg (1 Box Contains 10 Patches)", "unit": "patch" }, { "cost": "14.87", "description": "Transderm-Scop 1.5 mg (1 Box Contains 4 Patches)", "unit": "patch" }, { "cost": "30.99", "description": "Isopto Hyoscine 0.25% Solution 5ml Bottle", "unit": "bottle" }, { "cost": "85.69", "description": "Oscion Cleanser 3% Lotion 340.2 gm Bottle", "unit": "bottle" }, { "cost": "88.56", "description": "Oscion Cleanser 6% Lotion 340.2 gm Bottle", "unit": "bottle" }, { "cost": "0.34", "description": "Buscopan 10 mg Tablet", "unit": "tablet" }, { "cost": "0.67", "description": "Scopace 0.4 mg tablet", "unit": "tablet" } ]

[]

[ "Atenolol Scopolamine", "Atenolol Scopolamine", "B-Donna", "Belladonna Alkaloids with Phenobarbital", "Belladonna Alkaloids with Phenobarbital", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Diban Cap", "Diban Cap", "Donnagel Liq", "Donnagel Liq", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "Donnatal Elixir", "Donnatal Elixir", "Donnatal Extentabs", "Donnatal Extentabs", "Donnatal Extentabs", "Donnatal Extentabs Srt", "Donnatal Tab", "Isopto Hyoscine", "Kimite", "Me-PB-Hyos", "Me-PB-Hyos", "PB Hyos", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids - Grape", "Phenobarbital with Belladonna Alkaloids - Grape", "Phenobarbital with Belladonna Alkaloids - Mint", "Phenobarbital with Belladonna Alkaloids - Mint", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate and Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate and Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenohytro", "Phenohytro", "Phenohytro", "Phenohytro", "Phenohytro", "Propranolol Scopolamine", "Propranolol Scopolamine", "Quadrapax", "Quadrapax", "Re-PB Hyos", "Re-PB Hyos", "Re-PB Hyos", "Re-PB Hyos Elixir", "Scopace", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine", "Scopolamine Bromide Trihydrate", "Scopolamine Hydrobromide", "Scopolamine Hydrobromide Injection", "Scopolamine Hydrobromide Injection", "Scopolamine Hydrobromide Injection USP", "Scopolamine Hydrobromide Injection USP", "Scopolamine Trandermal System", "Scopolamine Trandermal System", "Scopolamine Trandermal System", "Scopolamine Trandermal System", "Scopolamine Transdermal System", "Se-donna Pb Hyos", "Servira", "Servira", "Transderm Scop", "Transderm Scop", "Transderm Scop", "Transderm Scop", "Transderm Scop", "Vitetal" ]

[ "Scopoderm", "Transderm-Scop" ]

[ "Atenolol Scopolamine", "Atenolol Scopolamine", "Propranolol Scopolamine", "Propranolol Scopolamine", "Donnatal Extentabs", "Phenobarbital With Belladonna Alkaloids", "Phenohytro", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Donnatal", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital With Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids - Mint", "Phenobarbital with Belladonna Alkaloids - Grape", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate and Scopolamine Hydrobromide", "Donnatal", "Donnatal", "Donnatal", "Donnatal Elixir", "Donnatal Extentabs", "Diban Cap", "Donnagel Liq", "Donnatal Tab", "Donnatal Extentabs Srt", "Donnatal Elixir", "Donnagel Liq", "Diban Cap", "Re-PB Hyos", "Servira", "Servira", "Vitetal", "Quadrapax", "Re-PB Hyos Elixir", "PB Hyos", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Donnatal Extentabs", "Donnatal", "Belladonna Alkaloids with Phenobartbital", "Donnatal", "Belladonna Alkaloids with Phenobartbital", "Belladonna Alkaloids with Phenobartbital", "Re-PB Hyos", "Donnatal", "Donnatal", "Donnatal", "Donnatal", "B-Donna", "Se-donna Pb Hyos", "Belladonna Alkaloids with Phenobarbital", "Re-PB Hyos", "Belladonna Alkaloids with Phenobartbital", "Quadrapax", "Donnatal", "Phenobarbital With Belladonna Alkaloids", "Donnatal", "Donnatal", "Phenohytro", "Phenohytro", "Phenohytro", "Phenobarbital with Belladonna Alkaloids - Grape", "Phenobarbital with Belladonna Alkaloids", "Phenobarbital with Belladonna Alkaloids - Mint", "Phenohytro", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate and Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Phenobarbital, Hyoscyamine Sulfate, Atropine Sulfate, Scopolamine Hydrobromide", "Donnatal", "Donnatal", "Me-PB-Hyos", "Donnatal", "Donnatal", "Belladonna Alkaloids with Phenobarbital", "Donnatal", "Me-PB-Hyos" ]

[ "P11229", "P08172", "P20309", "P08173", "P08912", "P43681", "P17787", "P14410" ]

[ "P08684" ]

[]

DB00748

Carbinoxamine

Carbinoxamine is a first generation antihistamine that competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. The product label for carbinoxamine as an over the counter cough and cold medicine is being modified to state "do not use" in children under 4 years of age in order to prevent and reduce misuse, as many unapproved carbinoxamine-containing preparations contained inappropriate labeling, which promoted unapproved uses (including management of congestion, cough, the common cold, and the use in children under 2 years of age), which can potentially cause serious health risks.

liquid

For symptomatic relief of seasonal and perennial allergic rhinitis and vasomotor rhinitis, as well as allergic conjunctivitis caused by foods and inhaled allergens. Also for the relief of allergic reactions to blood or plasma, and the symptomatic management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.

Carbinoxamine is a first generation antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, carbinoxamine competes with free histamine for binding at HA-receptor sites. Carbinoxamine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of carbinoxamine.

Carbinoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Carbinoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown.

null

10 to 20 hours

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Benzylethers

[ "approved" ]

[ "R06AA", "R06A", "R06", "R" ]

[ "Humans and other mammals" ]

[ { "cost": "0.65", "description": "Carbinoxamine maleate 4 mg tablet", "unit": "tablet" }, { "cost": "0.87", "description": "Palgic 4 mg tablet", "unit": "tablet" } ]

[ { "approved": "2011-11-22", "country": "United States", "expires": "2029-03-29", "number": "8062667" }, { "approved": "2016-12-20", "country": "United States", "expires": "2027-06-15", "number": "9522191" } ]

(±)-carbinoxamine | {2-[(4-Chloro-phenyl)-pyridin-2-yl-methoxy]-ethyl}-dimethyl-amine | 2-(p-chloro-α-(2-(dimethylamino)ethoxy)benzyl)pyridine | Carbinoxamin | Carbinoxamina | Carbinoxamine | Carbinoxamine base | Carbinoxaminum | Paracarbinoxamine | H1-R | H1R | HH1R | AGP 1 | AGP1 | OMD 1 | Orosomucoid-1 | AGP 2 | AGP2 | OMD 2 | Orosomucoid-2

[ "Arbinoxa", "Arbinoxa", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate", "Carbinoxamine Maleate Extended-Release Oral Suspension", "Carbinoxamine/Pseudoephedrine/DM", "Coldec DS", "Karbinal ER", "Karbinal ER", "Palgic", "Palgic", "Rondamine DM", "RyVent" ]

[ "Allergefon", "Clistin", "Histin", "Karbinal", "Rotoxamine", "Satinmin" ]

[ "Coldec DS", "Rondamine DM", "Carbinoxamine/Pseudoephedrine/DM" ]

[ "P35367" ]

[]

[ "P02763", "P19652" ]

[]

DB00750

Prilocaine

A local anesthetic that is similar pharmacologically to lidocaine. Currently, it is used most often for infiltration anesthesia in dentistry. (From AMA Drug Evaluations Annual, 1992, p165)

solid

Used as a local anaesthetic and is often used in dentistry.

Prilocaine binds to the intracellular surface of sodium channels which blocks the subsequent influx of sodium into the cell. Action potential propagation and never function is, therefore, prevented. This block is reversible and when the drug diffuses away from the cell, sodium channel function is restored and nerve propagation returns.

Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.

null

Prilocaine is 55% protein bound in plasma at a concentraion of 0.5-1.0 mg/mL.[L39529]

Prilocaine is metabolized in both the liver and the kidney and excreted via the kidney.

null

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved" ]

[ "N01BB", "N01B", "N01", "N", "N01BB", "N01B", "N01", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "3.98", "description": "Prilocaine hcl powder", "unit": "g" } ]

[ { "approved": "2000-02-29", "country": "United States", "expires": "2017-04-01", "number": "6031007" } ]

[ "4% Citanest Forte Dental With Epinephrine 1:200,000", "4% Citanest Plain Dental", "ACAT SUK Kit (Accelerated COVID-19 Antibody Test Single Use Kit)", "ACT Kit (Accelerated COVID-19 Test Kit)", "AgonEaze", "AgonEaze", "Anodyne LPT", "Aprizio Pak", "Aprizio Pak II", "Cadira Compliant Blood Stat", "Citanest Forte", "Citanest Forte DENTAL", "Citanest Plain", "Citanest Plain", "Cyclopak", "Dentsply 4% Prilocaine and Epinephrine Injection 1:200,000", "Dentsply 4% Prilocaine Hydrochloride Dental Injection", "DermacinRx Cinlone-I CPI", "DermacinRx Cinlone-II CPI", "DermacinRx Empricaine", "DermacinRx Empricaine II", "DermacinRx Prikaan", "DermacinRx Prizopak", "Dibucaine HCl 0.5% / Lidocaine 15% / Phenylephrine HCl 1% / Prilocaine 5%", "Dolotranz", "Emla", "Emla", "Emla", "Emla", "Emla", "Emla", "Emla Cream", "Emla Patch", "EmReal", "Fortacin", "Fortacin", "Inflammation Reduction Pack", "IV Infusion CPI", "Leva Set with Occlusive Dressing", "Leva Set with Occlusive Dressing", "Lido Bdk", "Lido-Prilo Caine Pack", "Lidocaine 2.5% and Prilocaine 2.5% Cream", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine Cream", "Lidocaine and Prilocaine Cream", "Lidocaine-Prilocaine-Cream Base", "Lidopril", "Lidopril", "Lidopril XR", "Lidotor", "Lipritin", "Lipritin II", "LiProZonePak", "Livixil Pak", "Livixil Pak", "LP Lite PAK", "Medolor Pak Lidocaine and Prilocaine Cream Kit", "Microvix L", "Microvix L", "Microvix LP", "Nuvakaan", "Nuvakaan II", "Oraqix", "Oraqix", "PainGo KFT", "Prikaan", "Prikaan Lite", "Prilo Patch", "Prilo Patch-II", "Prilocaine", "Prilocaine HCl 4% Epineph 1:200000inj", "Prilocaine Hydrochloride", "Prilocaine Hydrochloride", "Prilocaine Hydrochloride", "Prilocaine Hydrochloride with Epinephrine", "Priloheal Plus 30", "Prilolid", "Prilopentin", "Prilopentin -II", "Prilovix", "PRILOVIX Lite", "PRILOVIX Lite Plus", "PRILOVIX Plus", "PRILOVIX Plus", "PRILOVIX Plus", "PRILOVIX UltraLite", "PRILOVIX Ultralite Plus", "Prilovixil", "Prilovixil", "Prilovixil", "PRILOVIXIL Plus", "PRILOVIXIL Plus", "PRILOVIXIL Plus", "Priloxx LP External Kit", "Prizopak II", "Prizotral", "Prizotral II", "Realheal-I", "Relador Pak Plus", "Relador Pak with Occlusive Dressing", "Senstend", "Senstend", "SkyaDerm-LP", "Truemed Group LLC", "VallaDerm-90", "Venipuncture CPI", "Zyvodol" ]

[ "Citanest", "Prilotekal", "Takipril", "Xylonest" ]

[ "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Prilocaine Hydrochloride with Epinephrine", "Emla", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Relador Pak with Occlusive Dressing", "Zyvodol", "Relador Pak Plus", "Inflammation Reduction Pack", "Lidocaine-Prilocaine-Cream Base", "Emla", "Lidocaine and Prilocaine", "Prilolid", "DermacinRx Prikaan", "Lidopril", "Lidopril", "Lidocaine and Prilocaine", "Lidopril XR", "Leva Set with Occlusive Dressing", "Lido-Prilo Caine Pack", "Anodyne LPT", "Emla", "Citanest Forte", "Lidocaine 2.5% and Prilocaine 2.5% Cream", "Leva Set with Occlusive Dressing", "Lidocaine and Prilocaine", "Emla", "Emla", "IV Infusion CPI", "LP Lite PAK", "Lidocaine and Prilocaine", "AgonEaze", "AgonEaze", "Emla", "Lidocaine and Prilocaine", "Oraqix", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Cadira Compliant Blood Stat", "Lido Bdk", "PRILOVIX Plus", "PRILOVIX Plus", "PRILOVIX Plus", "Lidocaine and Prilocaine", "PRILOVIX Lite", "Aprizio Pak", "Nuvakaan", "DermacinRx Empricaine", "Prizotral", "DermacinRx Prizopak", "Prilo Patch", "Dibucaine HCl 0.5% / Lidocaine 15% / Phenylephrine HCl 1% / Prilocaine 5%", "Livixil Pak", "Livixil Pak", "Lidocaine and Prilocaine", "PRILOVIX Lite Plus", "PRILOVIX Ultralite Plus", "PRILOVIX UltraLite", "Lidocaine and Prilocaine", "Prilopentin", "Lidocaine and Prilocaine", "Citanest Forte DENTAL", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine Cream", "Prilovixil", "Prilovixil", "Prilovixil", "Microvix LP", "Microvix L", "Microvix L", "Prilovix", "Lidocaine and Prilocaine", "PRILOVIXIL Plus", "PRILOVIXIL Plus", "PRILOVIXIL Plus", "Lipritin", "ACAT SUK Kit (Accelerated COVID-19 Antibody Test Single Use Kit)", "Lidocaine and Prilocaine", "DermacinRx Empricaine II", "Nuvakaan II", "Prizotral II", "Lipritin II", "Prizopak II", "Priloxx LP External Kit", "DermacinRx Cinlone-I CPI", "Lidocaine and Prilocaine", "Medolor Pak Lidocaine and Prilocaine Cream Kit", "Dolotranz", "Lidocaine and Prilocaine", "Prikaan Lite", "LiProZonePak", "Prikaan", "Lidocaine and Prilocaine", "Venipuncture CPI", "DermacinRx Cinlone-II CPI", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Aprizio Pak II", "Prilopentin -II", "Prilo Patch-II", "ACT Kit (Accelerated COVID-19 Test Kit)", "SkyaDerm-LP", "Cyclopak", "Lidocaine and Prilocaine", "Realheal-I", "Priloheal Plus 30", "VallaDerm-90", "Lidocaine and Prilocaine", "Oraqix", "4% Citanest Forte Dental With Epinephrine 1:200,000", "Emla Cream", "Emla Patch", "Prilocaine HCl 4% Epineph 1:200000inj", "Dentsply 4% Prilocaine and Epinephrine Injection 1:200,000", "PainGo KFT", "Lidotor", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "EmReal", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine", "Lidocaine and Prilocaine Cream", "Fortacin", "Fortacin", "Senstend", "Senstend" ]

[ "Q14524" ]

[]

DB00751

Epinastine

Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.

solid

For the prevention of itching associated with allergic conjunctivitis.

Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.

Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.

The absolute bioavailability of epinastine is about 40%.

Mainly excreted unchanged, less than 10% metabolized.

null

12 hours

64%

Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.

null

* 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]

Organic compounds

Organoheterocyclic compounds

Benzazepines

Dibenzazepines

[ "approved", "investigational" ]

[ "S01GX", "S01G", "S01", "S", "R06AX", "R06A", "R06", "R" ]

[ "Humans and other mammals" ]

[ { "cost": "22.94", "description": "Elestat 0.05% eye drops", "unit": "ml" }, { "cost": "116.58", "description": "Elestat 0.05% Solution 5ml Bottle", "unit": "bottle" } ]

[ { "approved": "2008-09-30", "country": "United States", "expires": "2020-11-29", "number": "7429602" } ]

[ "Elestat", "Epinastine", "Epinastine HCl", "Epinastine HCl", "Epinastine Hydrochloride", "Epinastine Hydrochloride", "Epinastine Hydrochloride", "Epinastine Hydrochloride", "Epinastine Hydrochloride", "Epinastine Hydrochloride" ]

[ "Alegain", "Alenapion", "Alesion", "Alesiotec", "Alket", "Allernothin", "Allerstin", "Alpeed", "Aplatin", "Aresten", "Asmot", "Atergit", "Azusaleon", "Elpinan", "Epinazion", "Epioftal", "Flurinol", "Helvottz", "Kai lai Zhi", "Pinasion", "Purivist", "Relenastine", "Relestat", "Talerc", "Timkent", "Yupitel" ]

[]

[ "P35367", "P25021", "P35348", "P08913", "P28223", "P34969" ]

[ "P20813", "P10635", "P08684" ]

[]

[ "P08183" ]

DB00752

Tranylcypromine

A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders (From AMA Drug Evaluations Annual, 1994, p311). Tranylcypromine is a racemate comprising equal amounts of (1R,2S)- and (1S,2R)-2-phenylcyclopropan-1-amine with the chiral centers both located on the cylopropane ring. An irreversible monoamine oxidase inhibitor that is used as an antidepressant (INN tranylcypromine).

solid

For the treatment of major depressive episode without melancholia.

Tranylcypromine belongs to a class of antidepressants called monoamine oxidase inhibitors (MAOIs). Tranylcypromine is a non-hydrazine monoamine oxidase inhibitor with a rapid onset of activity. MAO is an enzyme that catalyzes the oxidative deamination of a number of amines, including serotonin, norepinephrine, epinephrine, and dopamine. Two isoforms of MAO, A and B, are found in the body. MAO-A is mainly found within cells located in the periphery and catalyzes the breakdown of serotonin, norepinephrine, epinephrine, dopamine and tyramine. MAO-B acts on phenylethylamine, norepinephrine, epinephrine, dopamine and tyramine, is localized extracellularly and is found predominantly in the brain. While the mechanism of MAOIs is still unclear, it is thought that they act by increasing free serotonin and norepinephrine concentrations and/or by altering the concentrations of other amines in the CNS. It has been postulated that depression is caused by low levels of serotonin and/or norepinephrine and that increasing serotonergic and norepinephrinergic neurotransmission results in relief of depressive symptoms. MAO A inhibition is thought to be more relevant to antidepressant activity than MAO B inhibition. Selective MAO B inhibitors, such as selegiline, have no antidepressant effects.

Tranylcypromine irreversibly and nonselectively inhibits monoamine oxidase (MAO). Within neurons, MAO appears to regulate the levels of monoamines released upon synaptic firing. Since depression is associated with low levels of monoamines, the inhibition of MAO serves to ease depressive symptoms, as this results in an increase in the concentrations of these amines within the CNS.

Interindividual variability in absorption. May be biphasic in some individuals. Peak plasma concentrations occur in one hour following oral administration with a secondary peak occurring within 2-3 hours. Biphasic absorption may represent different rates of absorption of the stereoisomers of the drug, though additional studies are required to confirm this.

Hepatic.

In overdosage, some patients exhibit insomnia, restlessness and anxiety, progressing in severe cases to agitation, mental confusion and incoherence. Hypotension, dizziness, weakness and drowsiness may occur, progressing in severe cases to extreme dizziness and shock. A few patients have displayed hypertension with severe headache and other symptoms. Rare instances have been reported in which hypertension was accompanied by twitching or myoclonic fibrillation of skeletal muscles with hyperpyrexia, sometimes progressing to generalized rigidity and coma.

1.5-3.2 hours in patients with normal renal and hepatic function

null

1.1-5.7 L/kg

null

Organic compounds

Organic nitrogen compounds

Organonitrogen compounds

Amines

[ "approved", "investigational" ]

[ "N06AF", "N06A", "N06", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.25", "description": "Tranylcypromine sulf 10 mg tablet", "unit": "tablet" }, { "cost": "1.3", "description": "Tranylcypromine Sulfate 10 mg tablet", "unit": "tablet" }, { "cost": "1.64", "description": "Parnate 10 mg tablet", "unit": "tablet" }, { "cost": "0.41", "description": "Parnate 10 mg Tablet", "unit": "tablet" } ]

[]

[ "M-tranylcypromine", "Parnate", "Parnate", "Parnate", "Parnate", "Parnate", "Parnate", "Tranylcypromine", "Tranylcypromine", "Tranylcypromine", "Tranylcypromine", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate", "Tranylcypromine Sulfate" ]

[ "Jatrosom" ]

[]

[ "P27338", "P21397" ]

[ "P10635", "P11712", "P33261", "P05177", "P11509", "P08684" ]

[]

DB00753

Isoflurane

A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.

liquid

For induction and maintenance of general anesthesia.

Isoflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.

Isoflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Isoflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. Also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Isoflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.

null

Minimal

LC50=15300 ppm/3 hrs (inhalation by rat)

null

Organic compounds

Organohalogen compounds

Organofluorides

null

[ "approved", "vet_approved" ]

[ "N01AB", "N01A", "N01", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "0.24", "description": "Forane liquid", "unit": "ml" } ]

[]

[ "Forane", "Forane", "Forane Liq Inh", "Isoflurane", "Isoflurane", "Isoflurane", "Isoflurane", "Isoflurane USP", "Isoflurane USP", "Isoflurane USP", "Isoflurane USP", "Terrell", "Terrell" ]

[ "Aerrane", "Forene", "Isocane", "Isorane" ]

[]

[ "P14867", "P98194", "P23415", "P42261", "Q09470", "P14867", "P47869", "P34903", "P48169", "P31644", "Q16445", "P18505", "P47870", "P28472", "O14764", "P78334", "Q8N1C3", "P18507", "Q99928", "O00591", "Q9UN88", "P30049", "P43681", "P17787", "P0DP23", "P0DP24", "P0DP25" ]

[ "P20813", "P03886", "P05181" ]

[ "P02768" ]

[]

DB00754

Ethotoin

Ethotoin is a hydantoin derivative and anticonvulsant. Ethotoin exerts an antiepileptic effect without causing general central nervous system depression. The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges. Ethotoin is no longer commonly used.

solid

For the control of tonic-clonic (grand mal) and complex partial (psychomotor) seizures.

Ethotoin is a hydantoin derivative and anticonvulsant. Ethotoin exerts an antiepileptic effect without causing general central nervous system depression. The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges.

The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges. Ethotoin inhibits nerve impulses in the motor cortex by lowering sodium ion influx, limiting tetanic stimulation.

Fairly rapidly absorbed, however, the extent of oral absorption is not known.

Hepatic. The drug exhibits saturable metabolism with respect to the formation of N-deethyl and p-hydroxyl-ethotoin, the major metabolites.

Symptoms of overdose include drowsiness, loss of or impaired muscle coordination, nausea, visual disturbance, and, at very high doses, coma.

3 to 9 hours

null

Organic compounds

Organoheterocyclic compounds

Azolidines

Imidazolidines

[ "approved" ]

[ "N03AB", "N03A", "N03", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "1.33", "description": "Peganone 250 mg tablet", "unit": "tablet" } ]

[]

[ "Peganone", "Peganone", "Peganone" ]

[ "Accenon", "Pegoanone" ]

[]

[ "Q14524", "O75469" ]

[]

[ "P05543" ]

[]

DB00756

Hexachlorophene

A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797)

liquid

For use as a surgical scrub and a bacteriostatic skin cleanser. It may also be used to control an outbreak of gram-positive infection where other infection control procedures have been unsuccessful.

Hexachlorophene, a detergent cleanser, is an antibacterial sudsing emulsion for topical administration. It is a bacteriostatic cleansing agent. It cleanses the skin thoroughly and has bacteriostatic action against staphylococci and other gram-positive bacteria. Cumulative antibacterial action develops with repeated use. Cleansing with alcohol or soaps containing alcohol removes the antibacterial residue.

The primary mechanism of action of hexachlorophene, based on studies with Bacillus megatherium, is to inhibit the membrane-bound part of the electron transport chain, respiratory D-lactate dehydrogenase. It induces leakage, causes protoplast lysis, and inhibits respiration.

Detectable blood levels of hexachlorophene following absorption through intact skin have been found in subjects who regularly scrubbed with hexachlorophene.

null

Oral, rat LD50: 66 mg/kg. Signs of overdose include anorexia, vomiting, abdominal cramps, diarrhea, dehydration, convulsions, hypotension, and shock, and in several reported instances, fatalities.

null

92%

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Diphenylmethanes

[ "approved", "withdrawn" ]

[ "D08AE", "D08A", "D08", "D" ]

[ "Enteric bacteria and other eubacteria" ]

[ { "cost": "11.47", "description": "Hexachlorophene powder", "unit": "g" }, { "cost": "35.46", "description": "Phisohex 148ml Bottle", "unit": "bottle" }, { "cost": "0.05", "description": "Tersaseptic cleanser", "unit": "g" }, { "cost": "0.13", "description": "Phisohex 473ml Bottle", "unit": "ml" }, { "cost": "0.18", "description": "Phisohex 3% cleanser", "unit": "ml" } ]

[]

[ "Phisohex", "Phisohex", "Phisohex", "Phisohex", "Sapoderm" ]

[ "Acigena", "Aknefug", "Almederm", "Armohex", "Dermisan", "Dial", "Distodin", "E-Z scrub", "Exofene", "Gamophen", "Gamophene", "Germa-medica", "Hexa-Germ", "Hexabalm", "Hexafen", "Hexascrub", "Hexide", "Nabac", "Phiso-scrub", "Phisodan", "Pre-Op", "Pre-Op II", "Septi-soft", "Septisol", "Septofen", "Solu-Heks", "Soy-Dome", "Staphene O", "Ster-Zac", "Steral", "Steraskin", "Surgi-Cen", "Surgi-Cin", "Surofene", "Tersaseptic", "Turgex" ]

[]

[ "O14521", "P00367", "P03372" ]

[]

DB00757

Dolasetron

Dolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug is not shown to have activity at other known serotonin receptors, and has low affinity for dopamine receptors.

solid

For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including initial and repeat courses of chemotherapy. Also used for the prevention of postoperative nausea and vomiting. This drug can be used intravenously for the treatment of postoperative nausea and vomiting.

Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. It is structurally and pharmacologically related to other 5-HT3 receptor agonists. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Dolasetron is a selective serotonin 5-HT3 receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug's pharmacological activity. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.

Orally-administered dolasetron is well absorbed

Hepatic

null

8.1 hours

69-77%

Hydrodolasetron is eliminated by multiple routes, including renal excretion and, after metabolism, mainly glucuronidation, and hydroxylation.

* 5.8 L/kg [adults]

* Apparent cl=9.4 mL/min/kg [Healthy volunteers with IV treatment dose up to 5 mg/kg]

Organic compounds

Organoheterocyclic compounds

Indoles and derivatives

Indolecarboxylic acids and derivatives

[ "approved", "investigational" ]

[ "A04AA", "A04A", "A04", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "2.66", "description": "Anzemet 20 mg/ml", "unit": "ml" }, { "cost": "18.74", "description": "Anzemet 12.5 mg carpuject", "unit": "syringe" }, { "cost": "32.16", "description": "Anzemet 100 mg Tablet", "unit": "tablet" }, { "cost": "58.67", "description": "Anzemet 50 mg tablet", "unit": "tablet" }, { "cost": "77.77", "description": "Anzemet 100 mg tablet", "unit": "tablet" } ]

[ { "approved": "1990-03-06", "country": "United States", "expires": "2011-07-02", "number": "4906755" }, { "approved": "1994-05-03", "country": "Canada", "expires": "2011-05-03", "number": "1329203" } ]

[ "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet", "Anzemet Injection 20 mg/ml" ]

[ "Anemet", "Zamanon" ]

[]

[ "P46098" ]

[ "P11712", "P08684", "P10635" ]

[]

DB00758

Clopidogrel

Clopidogrel is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke.[A180508,L7213] Clopidogrel is indicated to reduce the risk of myocardial infarction for patients with non-ST elevated acute coronary syndrome (ACS), patients with ST-elevated myocardial infarction, and in recent MI, stroke, or established peripheral arterial disease,[L7213] It has been shown to be superior to [aspirin] in reducing cardiovascular outcomes in patients with cardiovascular disease and provides additional benefit to patients with acute coronary syndromes already taking aspirin.[A180547] Clopidogrel was granted FDA approval on 17 November 1997.[L7213]

solid

Clopidogrel is indicated to reduce the risk of myocardial infarction for patients with non-ST elevated acute coronary syndrome (ACS), patients with ST-elevated myocardial infarction, and in recent MI, stroke, or established peripheral arterial disease,[L7213]

Clopidogrel is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke.[A180508,L7213] It has a long duration of action as it is taken once daily and a large therapeutic window as it is given in doses of 75-300mg daily.[L7213]

Clopidogrel is activated via a 2 steps reaction to an active thiol-containing metabolite.[A180508] This active form is a platelet inhibitor that irreversibly binds to P2Y12 ADP receptors on platelets.[L7213] This binding prevents ADP binding to P2Y12 receptors, activation of the glycoprotein GPIIb/IIIa complex, and platelet aggregation.[L7213]

A 75mg oral dose of clopidogrel is 50% absorbed from the intestine.[L7213] Clopidogrel can be taken with or without food.[L7213] A meal decreases the AUC of the active metabolite by 57%.[L7213] The active metabolite of clopidogrel reaches a maximum concentration after 30-60 minutes.[L7213] Clopidogrel reached a Cmax of 2.04±2.0ng/mL in 1.40±1.07h.[A180538] The AUC for a 300mg oral dose of clopidogrel was 45.1±16.2ng\*h/mL for poor metabolizers, 65.6±19.1ng\*h/mL for intermediate metabolizers, and 104.3±57.3ng\*h/mL for extensive metabolizers.[A180541] The Cmax was 31.3±13ng/mL for poor metabolizers, 43.9±14ng/mL for intermediate metabolizers, and 60.8±34.3ng/mL for extensive metabolizers.[A180541]

85-90% of an oral dose undergoes first pass metabolism by carboxylesterase 1 in the liver to an inactive carboxylic acid metabolite.[A180535] about 2% of clopidogrel is oxidized to 2-oxoclopidogrel.[A180535] This conversion is 35.8% by CYP1A2, 19.4% by CYP2B6, and 44.9% by CYP2C19[A180535] though other studies suggest CYP3A4, CYP3A5, and CYP2C9 also contribute.[A180508] 2-oxoclopidogrel is further metabolized to the active metabolite.[A180508,A180535] This conversion is 32.9% by CYP2B6, 6.79% by CYP2C9, 20.6% by CYP2C19, and 39.8% by CYP3A4.[A180508,A180535]

A single dose of clopidogrel at 1500-2000mg/kg was lethal to mice and rats while 3000mg/kg was lethal to baboons.[L7213] Symptoms of overdose include vomiting, breathing difficulty, gastrointestinal hemorrhage, and prostration.[L7213] Clopidogrel is irreversibly bound to platelets for their lifetime, which is approximately 11 days.[L7213] Overdoses of clopidogrel can be treated with platelet transfusions to restore clotting ability.[L7213]

That half life of clopidogrel is approximately 6 hours following a 75mg oral dose while the half life of the active metabolite is approximately 30 minutes.[L7213]

Both the active and inactive metabolites of clopidogrel are 98% protein bound in plasma.[A180511] Studies in cows show clopidogrel 71-85.5% bound to serum albumin.[A180514]

An oral dose of radiolabelled clopidogrel is excreted 50% in the urine and 46% in the feces over 5 days.[L7213] The remainder of clopidogrel is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.[A180544]

The apparent volume of distribution of clopidogrel is 39,240±33,520L.[A180538]

The clearance of a 75mg oral dose was 18,960±15,890L/h and for a 300mg oral dose was 16,980±10,410L/h.[A180538]

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved" ]

[ "B01AC", "B01A", "B01", "B" ]

[ "Humans and other mammals" ]

[ { "cost": "9.23", "description": "Plavix 75 mg tablet", "unit": "tablet" }, { "cost": "24.86", "description": "Plavix 300 mg tablet", "unit": "tablet" } ]

[ { "approved": "1989-07-11", "country": "United States", "expires": "2011-11-17", "number": "4847265" }, { "approved": "2005-03-15", "country": "Canada", "expires": "2019-06-10", "number": "2334870" }, { "approved": "1995-08-22", "country": "Canada", "expires": "2012-08-22", "number": "1336777" }, { "approved": "2002-08-06", "country": "United States", "expires": "2019-12-10", "number": "6429210" }, { "approved": "2003-01-07", "country": "United States", "expires": "2019-12-10", "number": "6504030" } ]

[ "Abbott-clopidogrel", "Accel-clopidogrel", "Accel-clopidogrel", "Act Clopidogrel", "Ag-clopidogrel", "Apo-clopidogrel", "Apo-clopidogrel", "Auro-clopidogrel", "Bio-clopidogrel", "Bio-clopidogrel", "Clopido Grel 1a Pharma", "Clopidogre Ratiopharm", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel", "Clopidogrel 1a Pharma", "Clopidogrel 1a Pharma", "Clopidogrel 1a Pharma", "Clopidogrel 1a Pharma", "Clopidogrel 1a Pharma", "Clopidogrel 1a Pharma", "Clopidogrel 75mg", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Acino Pharma Gmbh", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Apotex", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel Bgr", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel bisulfate", "Clopidogrel Bisulfate", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Bms", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hcs", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Hexal", "Clopidogrel Kit", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Krka D.D.", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Mylan", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Qualimed", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Ratiopharm Gmbh", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Sandoz", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Tad", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Teva Pharma B.V.", "Clopidogrel Viatris", "Clopidogrel Viatris", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel Zentiva", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Dom-clopidogrel", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Grepid", "Ipg-clopidogrel", "Ipg-clopidogrel", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Iscover", "Jamp-clopidogrel", "M-clopidogrel", "M-clopidogrel", "Mar-clopidogrel", "Mar-clopidogrel", "Mint-clopidogrel", "Mint-clopidogrel", "Mylan-clopidogrel", "Mylan-clopidogrel", "Nra-clopidogrel", "Nra-clopidogrel", "Plavi", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "Plavix", "PMS-clopidogrel", "Priva-clopidogrel", "Q-clopidogrel", "Rbx-clopidogrel", "Riva-clopidogrel", "Sandoz Clopidogrel", "Taro-clopidogrel", "Teva-clopidogrel", "Teva-clopidogrel", "Torrent-clopidogrel", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt", "Zyllt" ]

[]

[ "Clopidogrel Kit", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Duoplavin", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Zentiva", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan", "Clopidogrel/acetylsalicylic Acid Mylan" ]

[ "Q9H244" ]

[ "P11712", "P05177", "P10632", "P23141", "P08684", "P20813", "P20815", "P33261" ]

[ "P02768" ]

[ "P08183", "O15245", "O15244" ]

DB00760

Meropenem

Meropenem is a broad-spectrum carbapenem antibiotic. It is active against Gram-positive and Gram-negative bacteria. Meropenem exerts its action by penetrating bacterial cells readily and interfering with the synthesis of vital cell wall components, which leads to cell death. In August 2017, a combination antibacterial therapy under the market name vabomere was approved for treatment of adult patients with complicated urinary tract infections (cUTI). Vabomere consists of meropenem and [DB12107] and is intravenously admininstered. The treatment aims to resolve infection-related symptoms and achieve negative urine culture, where the infections are proven or strongly suspected to be caused by susceptible bacteria.

solid

For use as single agent therapy for the treatment of the following infections when caused by susceptible isolates of the designated microorganisms: complicated skin and skin structure infections due to Staphylococcus aureus (b-lactamase and non-b-lactamase producing, methicillin-susceptible isolates only), Streptococcus pyogenes, Streptococcus agalactiae, viridans group streptococci, Enterococcus faecalis (excluding vancomycin-resistant isolates), Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Bacteroides fragilis and Peptostreptococcus species; complicated appendicitis and peritonitis caused by viridans group streptococci, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacteroides fragilis, B. thetaiotaomicron, and Peptostreptococcus species. Also for use in the treatment of bacterial meningitis caused by Streptococcus pneumoniae, Haemophilus influenzae (b-lactamase and non-b-lactamase-producing isolates), and Neisseria meningitidis.

Meropenem is a broad-spectrum carbapenem antibiotic. It is active against Gram-positive and Gram-negative bacteria. Meropenem exerts its action by penetrating bacterial cells readily and interfering with the synthesis of vital cell wall components, which leads to cell death.

The bactericidal activity of meropenem results from the inhibition of cell wall synthesis. Meropenem readily penetrates the cell wall of most Gram-positive and Gram-negative bacteria to reach penicillin-binding- protein (PBP) targets. Its strongest affinities are toward PBPs 2, 3 and 4 of Escherichia coli and Pseudomonas aeruginosa; and PBPs 1, 2 and 4 of Staphylococcus aureus.

null

Primarily excreted unchanged. There is one metabolite which is microbiologically inactive.

In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.

Approximately 1 hour in adults and children 2 years of age and older with normal renal function. Approximately 1.5 hours in children 3 months to 2 years of age.

Approximately 2%.

Approximately 70% of the intravenously administered dose is recovered as unchanged meropenem in the urine over 12 hours, after which little further urinary excretion is detectable.

null

Organic compounds

Organoheterocyclic compounds

Lactams

Beta lactams

[ "approved", "investigational" ]

[ "J01DH", "J01D", "J01", "J", "J01DH", "J01D", "J01", "J" ]

[ "Enteric bacteria and other eubacteria" ]

[ { "cost": "48.79", "description": "Merrem 500 mg Solution Vial", "unit": "vial" }, { "cost": "78.19", "description": "Merrem iv 1 gm vial", "unit": "vial" }, { "cost": "81.32", "description": "Merrem 1 gm Solution Vial", "unit": "vial" } ]

[ { "approved": "1990-07-24", "country": "United States", "expires": "2010-06-21", "number": "4943569" }, { "approved": "1993-09-21", "country": "Canada", "expires": "2010-09-21", "number": "1322371" }, { "approved": "2017-07-04", "country": "United States", "expires": "2031-08-08", "number": "9694025" }, { "approved": "2014-03-25", "country": "United States", "expires": "2031-08-17", "number": "8680136" }, { "approved": "2019-01-22", "country": "United States", "expires": "2031-08-08", "number": "10183034" }, { "approved": "2019-01-08", "country": "United States", "expires": "2031-08-08", "number": "10172874" }, { "approved": "2020-02-18", "country": "United States", "expires": "2031-08-08", "number": "10561675" }, { "approved": "2021-05-18", "country": "United States", "expires": "2031-08-08", "number": "11007206" }, { "approved": "2019-04-06", "country": "United States", "expires": "2039-04-06", "number": "11376237" } ]

(4R,5S,6S)-3-{[(3S,5S)-5-(dimethylcarbamoyl)pyrrolidin-3-yl]thio}-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid | Meropenem | Meropenem anhydrous | Meropenemum | 3.4.16.4 | D-alanyl-D-alanine endopeptidase | DD-carboxypeptidase | DD-endopeptidase | PBP-4 | Penicillin-binding protein 4 | 3.5.2.6 | Beta-lactamase PSE-2 | oxa10 | pse2 | 3.4.13.19 | Beta-lactamase | Dehydropeptidase-I | hRDP | MDP | Microsomal dipeptidase | RDP | Renal dipeptidase

[ "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem", "Meropenem and Sodium Chloride", "Meropenem and Sodium Chloride", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection", "Meropenem for Injection Sdz", "Meropenem for Injection Sdz", "Meropenem for Injection USP", "Meropenem for Injection USP", "Meropenem for Injection USP", "Meropenem for Injection USP", "Meropenem for Injection USP and Sodium Chloride Injection USP", "Meropenem for Injection USP and Sodium Chloride Injection USP", "Meropenem for Injection, USP", "Meropenem for Injection, USP", "Merrem", "Merrem", "Merrem", "Merrem", "Merrem IV", "Merrem IV", "Merrem IV", "Merrem IV", "Taro-meropenem", "Taro-meropenem", "Vabomere", "Vabomere", "Vaborem" ]

[ "Aronem", "Aropen", "Carbanem", "Erope", "Fulspec", "I-penam", "Merenz", "Merofit", "Meronem", "Meronis", "Meropen", "Merotec", "Merrem I.V.", "Monan", "Ropenem", "Zeropenem" ]

[ "Vabomere", "Vabomere", "Vaborem" ]

[]

[ "P16444" ]

[]

DB00761

Potassium chloride

A white crystal or crystalline powder used as an electrolyte replenisher, in the treatment of hypokalemia, in buffer solutions, and in fertilizers and explosives. The FDA withdrew its approval for the use of all solid oral dosage form drug products containing potassium chloride that supply 100 mg or more of potassium per dosage unit, except for controlled-release dosage forms and those products formulated for preparation of solution prior to ingestion.[L43942]

solid

For use as an electrolyte replenisher and in the treatment of hypokalemia.

The potassium ion is in the principle intracellular cation of most body tissues. Potassium ions participate in a number of essential physiological processes including the maintenance of intracellular tonicity, the transmission of nerve impulses, the contraction of cardiac, skeletal and smooth muscle, and the maintenance of normal renal function. The intracellular concentration of potassium is approximately 150 to 160 mEq per liter. The normal adult plasma concentration is 3.5 to 5 mEq per liter. An active ion transport system maintains this gradient across the plasma membrane. Potassium is a normal dietary constituent and under steady-state conditions the amount of potassium absorbed from the gastrointestinal tract is equal to the amount excreted in the urine. The usual dietary intake of potassium is 50 to 100 mEq per day. Potassium depletion will occur whenever the rate of potassium loss through renal excretion and/or loss from the gastrointestinal tract exceeds the rate of potassium intake. Such depletion usually develops as a consequence of therapy with diuretics, primarily or secondary hyperaldosteronism, diabetic ketoacidosis, or inadequate replacement of potassium in patients on prolonged parenteral nutrition. Depletion can develop rapidly with severe diarrhea, especially if associated with vomiting. Potassium depletion due to these causes is usually accompanied by concomitant loss of chloride and is manifested by hypokalemia and metabolic alkalosis. Potassium depletion may produce weakness, fatigue, disturbances of cardiac rhythm (primarily ectopic beats), prominent U-waves in the electrocardiogram, and, in advanced cases, flaccid paralysis and/or impaired ability to concentrate urine. If potassium depletion associated with metabolic alkalosis cannot be managed by correcting the fundamental cause of the deficiency, e.g., where the patient requires long-term diuretic therapy, supplemental potassium in the form of high potassium food or potassium chloride may be able to restore normal potassium levels. In rare circumstances (e.g., patients with renal tubular acidosis) potassium depletion may be associated with metabolic acidosis and hyperchloremia. In such patients, potassium replacement should be accomplished with potassium salts other than the chloride, such as potassium bicarbonate, potassium citrate, potassium acetate, or potassium gluconate.

Supplemental potassium in the form of high potassium food or potassium chloride may be able to restore normal potassium levels.

Potassium is a normal dietary constituent and under steady-state conditions the amount of potassium absorbed from the gastrointestinal tract is equal to the amount excreted in the urine.

null

The administration of oral potassium salts to persons with normal excretory mechanisms for potassium rarely causes serious hyperkalemia. However, if excretory mechanisms are impaired, of if potassium is administered too rapidly intravenously, potentially fatal hyperkalemia can result. It is important to recognize that hyperkalemia is usually asymptomatic and may be manifested only by an increased serum potassium concentration (6.5-8.0 mEq/L) and characteristic electrocardiographic changes (peaking of T-waves, loss of P-wave, depression of S-T segment, and prolongation of the QT interval). Late manifestations include muscle paralysis and cardiovascular collapse from cardiac arrest (9-12 mEq/L).

null

Potassium is a normal dietary constituent and, under steady-state conditions, the amount of potassium absorbed from the gastrointestinal tract is equal to the amount excreted in the urine. Potassium depletion will occur whenever the rate of potassium loss through renal excretion and/or loss from the gastrointestinal tract exceeds the rate of potassium intake.

null

Inorganic compounds

Mixed metal/non-metal compounds

Alkali metal salts

Alkali metal chlorides

[ "approved", "withdrawn" ]

[ "A12BA", "A12B", "A12", "A", "B05XA", "B05X", "B05", "B", "A12BA", "A12B", "A12", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "1.21", "description": "Micro-K 8meq capsule", "unit": "capsule" }, { "cost": "1.41", "description": "Micro-K 10meq capsule", "unit": "capsule" }, { "cost": "1.43", "description": "K-lyte tablet eff", "unit": "tablet" }, { "cost": "1.43", "description": "K-lyte-cl 25 meq tablet eff", "unit": "tablet" }, { "cost": "1.92", "description": "K-Lor 20meq Packets", "unit": "packet" }, { "cost": "18.17", "description": "Colyte-Flavored 240 gm Solution", "unit": "bottle" }, { "cost": "26.0", "description": "Colyte 240 gm Solution", "unit": "bottle" }, { "cost": "36.99", "description": "Klor-Con 30 25meq Packets Box", "unit": "box" }, { "cost": "45.98", "description": "Rum-K-SF 15% Liquid 473ml Bottle", "unit": "bottle" }, { "cost": "58.99", "description": "Kay Ciel 30 20meq Packets Box", "unit": "box" }, { "cost": "106.77", "description": "Klor-Con 100 20meq Packets Box", "unit": "box" }, { "cost": "0.01", "description": "Colyte with flavor packets", "unit": "ml" }, { "cost": "0.01", "description": "Pms - Potassium Chloride 1.33 meq/ml Liquid", "unit": "ml" }, { "cost": "0.02", "description": "Potassium chloride crystals", "unit": "g" }, { "cost": "0.02", "description": "K-10 Oral Liquid 1.33 meq/ml Liquid", "unit": "ml" }, { "cost": "0.03", "description": "Potassium Chloride 20 Meq/15ml(10%) Liquid", "unit": "ml" }, { "cost": "0.06", "description": "Potassium Chloride 40 Meq/15ml(20%) Liquid", "unit": "ml" }, { "cost": "0.09", "description": "Apo-K 8 meq Sustained-Release Tablet", "unit": "tablet" }, { "cost": "0.1", "description": "Micro-K Extencaps 8 meq Sustained-Release Capsule", "unit": "capsule" }, { "cost": "0.16", "description": "Klor-con 8 meq tablet", "unit": "tablet" }, { "cost": "0.16", "description": "Slow K 8 meq Sustained-Release Tablet", "unit": "tablet" }, { "cost": "0.18", "description": "Potassium Chloride CR 8meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.21", "description": "K-Dur 20 meq Sustained-Release Tablet", "unit": "tablet" }, { "cost": "0.23", "description": "Kaon-cl 10 meq tablet sa", "unit": "tablet" }, { "cost": "0.23", "description": "Potassium cl 2 meq/ml vial", "unit": "ml" }, { "cost": "0.26", "description": "Potassium cl er 8 meq tablet", "unit": "tablet" }, { "cost": "0.27", "description": "Potassium Chloride CR 10meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.28", "description": "Potassium Chloride Crys CR 10meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.29", "description": "Potassium cl 10 meq tablet sa", "unit": "tablet" }, { "cost": "0.3", "description": "Kaon-Cl-10 10meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.3", "description": "Klor-con m10 tablet", "unit": "tablet" }, { "cost": "0.3", "description": "Potassium cl er 10 meq tablet", "unit": "tablet" }, { "cost": "0.34", "description": "Micro-k 8 meq extencaps", "unit": "each" }, { "cost": "0.4", "description": "Klor-con-ef 25 meq tablet eff", "unit": "tablet" }, { "cost": "0.49", "description": "Potassium cl er 20 meq tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Klor-con 10 meq tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Klor-con m15 tablet", "unit": "tablet" }, { "cost": "0.5", "description": "Klotrix 10meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.52", "description": "Potassium cl 20 meq tablet er", "unit": "tablet" }, { "cost": "0.52", "description": "Potassium cl 20 meq tablet sa", "unit": "tablet" }, { "cost": "0.53", "description": "Potassium Chloride Crys CR 20meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.55", "description": "Klor-Con M20 20meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.56", "description": "Klor-Con 8meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.57", "description": "Klor-con m20 tablet", "unit": "tablet" }, { "cost": "0.57", "description": "Klor-Con/EF 25meq Effervescent Tabs", "unit": "tab" }, { "cost": "0.58", "description": "K-tab 10 meq tablet sa", "unit": "tablet" }, { "cost": "0.58", "description": "K-Lyte 25 meq Effervescent Tablet", "unit": "tablet" }, { "cost": "0.59", "description": "Kaochlor-eff 20 meq tablet", "unit": "tablet" }, { "cost": "0.66", "description": "K-tab er 10 meq tablet", "unit": "tablet" }, { "cost": "0.68", "description": "K-Tabs 10meq Controlled Release Tabs", "unit": "tab" }, { "cost": "0.87", "description": "Potassium Chloride CR 8meq capsule", "unit": "capsule" }, { "cost": "0.9", "description": "Potassium Chloride CR 10meq capsule", "unit": "capsule" }, { "cost": "0.91", "description": "Micro-k 10 meq extencaps", "unit": "each" }, { "cost": "0.94", "description": "Potassium cl 25 meq tablet eff", "unit": "tablet" } ]

[ { "approved": "2007-11-06", "country": "United States", "expires": "2022-10-22", "number": "7291324" }, { "approved": "2007-01-30", "country": "United States", "expires": "2024-09-01", "number": "7169381" }, { "approved": "2010-02-09", "country": "United States", "expires": "2024-09-01", "number": "7658914" }, { "approved": "2006-08-01", "country": "United States", "expires": "2021-11-29", "number": "7084130" }, { "approved": "2016-05-03", "country": "United States", "expires": "2033-09-10", "number": "9326969" }, { "approved": "2017-03-14", "country": "United States", "expires": "2032-08-11", "number": "9592252" }, { "approved": "2017-07-18", "country": "United States", "expires": "2033-09-10", "number": "9707297" }, { "approved": "2015-04-07", "country": "United States", "expires": "2033-09-10", "number": "8999313" }, { "approved": "2018-07-10", "country": "United States", "expires": "2033-09-10", "number": "10016504" }, { "approved": "2020-05-12", "country": "United States", "expires": "2032-03-25", "number": "10646512" }, { "approved": "2020-10-06", "country": "United States", "expires": "2032-03-09", "number": "10792306" }, { "approved": "2020-09-22", "country": "United States", "expires": "2032-03-09", "number": "10780112" }, { "approved": "2018-12-04", "country": "United States", "expires": "2037-08-04", "number": "10143656" }, { "approved": "2021-02-16", "country": "United States", "expires": "2033-09-10", "number": "10918723" }, { "approved": "2021-06-15", "country": "United States", "expires": "2037-08-04", "number": "11033498" }, { "approved": "2017-08-04", "country": "United States", "expires": "2037-08-04", "number": "11382864" }, { "approved": "2012-03-09", "country": "United States", "expires": "2032-03-09", "number": "11529368" }, { "approved": "2017-08-04", "country": "United States", "expires": "2037-08-04", "number": "11638697" }, { "approved": "2013-09-10", "country": "United States", "expires": "2033-09-10", "number": "12083179" } ]

[ "(20 Mmol/l) Potassium Chloride In 3.3% Dextrose and 0.3% Sodium Chloride Injection USP", "(20 Mmol/l) Potassium Chloride In 5% Dextrose and 0.9% Sodium Chloride Injection USP", "(20 Mmol/l) Potassium Chloride In 5% Dextrose Injection USP", "(20mmol/l) Potassium Chloride In 0.9% Sodium Chloride Injection USP", "(20mmol/l) Potassium Chloride In 5% Dextrose and 0.2% Sodium Chloride Injection USP", "(20mmol/l) Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection USP", "(40 Mmol/l) Potassium Chloride In 0.9% Sodium Chloride Injection USP", "(40 Mmol/l) Potassium Chloride In 5% Dextrose Injection USP", "(40 Mmols/l) Potassium Chloride In Lactated Ringer's Injection USP", "(40mmol/l) Potassium Chloride In 3.3% Dextrose and 0.3% Sodium Chloride Injection USP", "(40mmol/l)potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection USP", "0.15% Potassium Chloride In 3.3% Dextrose and 0.30% Sodium Chloride Injection", "0.15% Potassium Chloride In 5% Dextrose and 0.20% Sodium Chloride Injection USP", "0.15% Potassium Chloride In 5% Dextrose and 0.33% Sodium Chloride Injection USP", "0.15% Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection", "0.15% Potassium Chloride In 5% Dextrose and 0.9% Sodium Chloride Injection", "0.15% Potassium Chloride In 5% Dextrose Injection USP", "0.30% Potassium Chloride In 5% Dextrose", "0.30% Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection", "5% Dextrose In Lactated Ringer's Injection", "Acetate Concentrate R07376", "Acid Concentrate (r04938)", "Acid Concentrate (r04968)", "Acid Concentrate (r04969)", "Acid Concentrate (r04974)", "Acid Concentrate (r04975)", "Acid Concentrate (r04976)", "Acid Concentrate (r04981)", "Acid Concentrate (r04984)", "Acid Concentrate (ro4147)", "Acid Concentrate (ro4148)", "Acid Concentrate (ro9503)", "Acid Concentrate (rz262c)", "Acid Concentrate (rz271c)", "Acid Concentrate (rz272c)", "Acid Concentrate (rz274c)", "Acid Concentrate (rz275c)", "Acid Concentrate 2101", "Acid Concentrate 2102", "Acid Concentrate 2105", "Acid Concentrate 2106", "Acid Concentrate 2109", "Acid Concentrate 2112", "Acid Concentrate 2113", "Acid Concentrate 2117", "Acid Concentrate 2120", "Acid Concentrate 2122", "Acid Concentrate 2123", "Acid Concentrate 2125", "Acid Concentrate 2126", "Acid Concentrate 2129", "Acid Concentrate 2131", "Acid Concentrate 2132", "Acid Concentrate 2135", "Acid Concentrate 2139", "Acid Concentrate 2147", "Acid Concentrate 2148", "Acid Concentrate 2151", "Acid Concentrate 2152", "Acid Concentrate 2155", "Acid Concentrate 2156", "Acid Concentrate 2161", "Acid Concentrate 2162", "Acid Concentrate 2163", "Acid Concentrate 2166", "Acid Concentrate 2168", "Acid Concentrate 2171", "Acid Concentrate 2175", "Acid Concentrate 2182", "Acid Concentrate 2185", "Acid Concentrate 2189", "Acid Concentrate 2190", "Acid Concentrate 2196", "Acid Concentrate 2198", "Acid Concentrate 3186", "Acid Concentrate 3187", "Acid Concentrate A1221", "Acid Concentrate A1222", "Acid Concentrate A1223", "Acid Concentrate A1224", "Acid Concentrate A1225", "Acid Concentrate A1226", "Acid Concentrate A1227", "Acid Concentrate A1228", "Acid Concentrate A1228", "Acid Concentrate A1229", "Acid Concentrate A1229", "Acid Concentrate A1231", "Acid Concentrate A1231", "Acid Concentrate A1241", "Acid Concentrate A1241", "Acid Concentrate A1242", "Acid Concentrate A1242", "Acid Concentrate A1243", "Acid Concentrate A1243", "Acid Concentrate A1245", "Acid Concentrate A1245", "Acid Concentrate A1246", "Acid Concentrate A1246", "Acid Concentrate A1251", "Acid Concentrate A1251", "Acid Concentrate A1252", "Acid Concentrate A1252", "Acid Concentrate A1253", "Acid Concentrate A1255", "Acid Concentrate A1255", "Acid Concentrate A1261", "Acid Concentrate A1262", "Acid Concentrate A1263", "Acid Concentrate A1263", "Acid Concentrate A1265", "Acid Concentrate A1265", "Acid Concentrate A1266", "Acid Concentrate A1267", "Acid Concentrate A1267", "Acid Concentrate A1268", "Acid Concentrate A1269", "Acid Concentrate A1274", "Acid Concentrate A1275", "Acid Concentrate A1276", "Acid Concentrate A1277", "Acid Concentrate A1278", "Acid Concentrate A1279", "Acid Concentrate A1280", "Acid Concentrate A1294", "Acid Concentrate A1295", "Acid Concentrate A1296", "Acid Concentrate A1297", "Acid Concentrate A1298", "Acid Concentrate Bp Ro4151", "Acid Concentrate Bp Ro9505", "Acid Concentrate Bp Ro9506", "Acid Concentrate Bp Ro9507", "Acid Concentrate Bp Rz267c", "Acid Concentrate Bp Rz278c", "Acid Concentrate Bp Rz279c", "Acid Concentrate D 12219 Liq", "Acid Concentrate D-12287", "Acid Concentrate D-18003", "Acid Concentrate D-18006", "Acid Concentrate D12028", "Acid Concentrate D12054", "Acid Concentrate D12067", "Acid Concentrate D12092", "Acid Concentrate D12093", "Acid Concentrate D12094", "Acid Concentrate D12095", "Acid Concentrate D12112", "Acid Concentrate D12117", "Acid Concentrate D12119", "Acid Concentrate D12132", "Acid Concentrate D12135", "Acid Concentrate D12143", "Acid Concentrate D12150", "Acid Concentrate D12167", "Acid Concentrate D12184", "Acid Concentrate D12185", "Acid Concentrate D12188", "Acid Concentrate D12196", "Acid Concentrate D12197", "Acid Concentrate D12200", "Acid Concentrate D12201", "Acid Concentrate D12204", "Acid Concentrate D12205", "Acid Concentrate D12207", "Acid Concentrate D12209", "Acid Concentrate D12220", "Acid Concentrate D12221", "Acid Concentrate D12236", "Acid Concentrate D12247", "Acid Concentrate D12248", "Acid Concentrate D12250", "Acid Concentrate D12252", "Acid Concentrate D12255", "Acid Concentrate D12259", "Acid Concentrate D12261", "Acid Concentrate D12262", "Acid Concentrate D12264", "Acid Concentrate D12265", "Acid Concentrate D12267", "Acid Concentrate D12268", "Acid Concentrate D12269", "Acid Concentrate D12272", "Acid Concentrate D12275", "Acid Concentrate D12282", "Acid Concentrate D12284", "Acid Concentrate D12285", "Acid Concentrate D12286", "Acid Concentrate D12290", "Acid Concentrate D12291", "Acid Concentrate D12292", "Acid Concentrate D12293", "Acid Concentrate D12294", "Acid Concentrate D12299", "Acid Concentrate D12300", "Acid Concentrate D12301", "Acid Concentrate D12302", "Acid Concentrate D12303", "Acid Concentrate D12305", "Acid Concentrate D12308", "Acid Concentrate D12308", "Acid Concentrate D12309", "Acid Concentrate D12309", "Acid Concentrate D12310", "Acid Concentrate D12311", "Acid Concentrate D12311", "Acid Concentrate D12315", "Acid Concentrate D12316", "Acid Concentrate D12318", "Acid Concentrate D13001", "Acid Concentrate D18001", "Acid Concentrate D18009", "Acid Concentrate Ro4137", "Acid Concentrate Ro4138", "Acid Concentrate Ro4144", "Acid Concentrate Ro4145", "Acid Concentrate Ro4947", "Acid Concentrate Ro4979", "Acid Concentrate Ro4983", "Acid Concentrate Ro9500", "Acid Concentrate Ro9501", "Acid Concentrate Ro9502", "Acid Concentrate Rx252c", "Acid Concentrate Rx253c", "Acid Concentrate Rz110c", "Acid Concentrate Rz111c", "Acid Concentrate Rz119c", "Acid Concentrate Rz127c", "Acid Concentrate Rz144c", "Acid Concentrate Rz153c", "Acid Concentrate Rz164c", "Acid Concentrate Rz167c", "Acid Concentrate Rz171c", "Acid Concentrate Rz183c", "Acid Concentrate Rz185c", "Acid Concentrate Rz194c", "Acid Concentrate Rz195c", "Acid Concentrate Rz196c", "Acid Concentrate Rz202c", "Acid Concentrate Rz203c", "Acid Concentrate Rz207c", "Acid Concentrate Rz208c", "Acid Concentrate Rz209c", "Acid Concentrate Rz210c", "Acid Concentrate Rz211c", "Acid Concentrate Rz212c", "Acid Concentrate Rz213c", "Acid Concentrate Rz247c", "Acid Concentrate Rz248c", "Acid Concentrate Rz249c", "Acid Concentrate Rz254c", "Acid Concentrate Rz264c", "Acid Concentrate Rz265c", "Acid Concentrate-r04948 Liq", "Acid Concentrate(36.83x) R04900", "Acid Concentrate(36.83x) R04906", "Acid Hemodialysis Conc Sb 1003", "Adrenogist Tab", "Aminosyn", "Aminosyn", "Aminosyn II 10% With Electrolytes", "Aminosyn II 7% M In 10% Dextrose(dual Chamber)", "Aminosyn II 8.5% M In 20% Dextrose (dual Chamber)", "Aminosyn II and Dextrose", "Aminosyn II in Dextrose", "Aminosyn II with Electrolytes", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Amo Endosol Extra", "Amo Endosol Solution", "Anaplex Tab", "Artisial", "Balanced Salt", "Balanced Salt", "Balanced Salt", "Balanced Salt", "Balanced Salt Solution", "Balanced Salt Solution", "Bi-peglyte", "Bicarb Hemodial Conc 36.83", "Bicarbolyte Bicar Hemodialsis Conc", "Bicarbolyte Bicar Hemodialysis Conc", "Bicarbolyte Bicar Hemodialysis Conc", "Bicarbolyte Bicar Hemodialysis Conc", "Bss", "Bss", "Bss Plus", "Bss Plus", "Bss Sterile Irrigating Solution", "Calcium Magnesium With Potassium Tab", "Cardioplegic", "Cardioplegic Solution", "Children's Chew Multi & Min Tab", "Children's Chew Multi & Min Tab", "Chlorure de potassium Proamp", "Citrasate C10125", "Citrasate C1125", "Citrasate C1150", "Citrasate C2125", "Citrasate C2150", "Citrasate C3125", "Citrasate C3150", "Citrasate C4125", "Clenz-Lyte", "Colyte", "Colyte", "Colyte", "Colyte with flavor packs", "Concentrated Haemodialysis Solution Bp-rz266c", "Concentrated Haemodialysis Solution Bp-rz270c", "Cytosol Ophthalmics - Balanced Salt Solution", "D-12043 Sol Conc Electrolyt Pour Dialy", "D12006", "D12046 Conc Electrolyte Renal Dialysis", "D12230 Liq", "Dextrose 2.5% In Half Strength Lactated Ringer's Injection, USP", "Dextrose 5% and Electrolyte No75 Inj", "Dextrose 50% Inj W Electrolytes PF Abbovac", "Dextrose and Electrolyte No. 48", "Dextrose and Electrolyte No. 75", "Dextrose in Lactated Ringers", "Dextrose in Ringers", "Dialysis Solution 35 K2", "Dialysis Solution 35 K4", "Dialyte", "Diphen", "Effervescent Potassium Chloride", "Electropeg Solution", "Elliott's Solution A", "Elliotts B", "Elliotts B", "Epiklor", "Epiklor/25", "Eye Stream", "Finazol", "Foliflex", "Folitin-Z", "Formula R Tab", "Formule No 204 Profil Tab", "FreAmine III", "GaviLyte - C TM", "Gavilyte G Tm", "GaviLyte-H and Bisacodyl", "Gavilyte-N", "Glycerolyte 57 Solution", "Glysol-500", "GoLYTELY", "GoLYTELY", "GoLYTELY", "GoLYTELY", "Golytely Gi Lavage Solution", "H-706", "H-710", "H.E.L.P.bicel", "Haemosol H-200", "Haemosol H-201", "Haemosol H-206", "Haemosol H-208", "Haemosol H-223", "Haemosol H-224", "Haemosol H-225", "Haemosol H-226", "Haemosol H-227", "Haemosol H-229", "Haemosol H-230", "Haemosol H-232", "Haemosol H-250", "Haemosol H-251", "Haemosol H-252", "Haemosol H-253", "Haemosol H-254", "Haemosol H-260", "Haemosol H-320", "Haemosol H-330", "Haemosol H-331", "Haemosol H-332", "Haemosol H-401", "Haemosol H-402", "Haemosol H-404", "Haemosol H-407", "Haemosol H-408", "Haemosol H-410", "Haemosol H-602", "Haemosol H-608", "Haemosol H-615", "Haemosol H-616", "Haemosol H-617", "Haemosol H-623", "Haemosol H-624", "Haemosol H-625", "Haemosol H-630", "Haemosol H-631", "Haemosol H-661", "Haemosol H-690", "HalfLytely and Bisacodyl", "HalfLytely and Bisacodyl", "HalfLytely and Bisacodyl Bowel Prep with Flavor Packs", "Hemasate Ultra Hs1125", "Hemasate Ultra Hs1150", "Hemasate Ultra Hs2125", "Hemasate Ultra Hs2150", "Hemasate Ultra Hs3125", "Hemasate Ultra Hs3150", "Hemasate Ultra Hs4125", "Hemosate Ultra Hs1125", "Hemosate Ultra Hs1150", "Hemosate Ultra Hs2125", "Hemosate Ultra Hs2150", "Hemosate Ultra Hs3125", "Hemosate Ultra Hs3150", "Hemosate Ultra Hs4125", "Hemosol Lg2", "Hemosol Lg4", "Hi Potency Potassium Chloride", "High Potency Multivitamins & Minerals Caplets", "High Potency Multivitamins & Minerals Caplets", "HUMCO Potassium Chloride 10 Percent", "HydroGold 9", "Hyperlyte (multi-electrolyte Concentrate)", "Iocare Balanced Salt Solution", "Iodine-potassium Tablets", "Ionosol and Dextrose", "Ionosol B and Dextrose", "Ionosol MB and Dextrose", "Ionosol MB and Dextrose", "Isolyte H in Dextrose", "Isolyte H With Dextrose 5% Inj", "Isolyte M In 5% Dextrose", "Isolyte M in Dextrose", "Isolyte P in Dextrose", "Isolyte R In 5% Dextrose", "Isolyte S", "Isolyte S (multi-electrolyte Injection)", "Isolyte S in Dextrose", "Isolyte S pH 7.4", "Isolyte S Ph 7.4 (multi-electrolyte Injection)", "Isolyte S With 5% Dextrose Inj", "Isoplate", "Isoplate", "Jamp-electropeg", "Jamp-electropeg With Flavour Packet", "Jamplyte", "Jamplyte", "Jamplyte + Bisacodyl", "K C1-rougier", "K Lor Granules 20meq", "K Lyte Cl Pwr", "K-dur", "K-dur", "K-dur", "K-lyte Cl", "K-med", "K-med 900 Tab 900mg", "K-Sol", "K-Sol", "K-tab", "K-Tab", "K-Tab", "K-Tab", "K-Tab", "K-Tab", "K-Tab", "K-Tab", "K+ 45", "K+36.8", "K1 Liq R04911", "K1 Liq R04978", "K2 Liq R04902", "K2 With Glucose Liq R04977", "Kabiven", "Kalium Durules Srt 750mg", "Kaochlor-10", "Kaochlor-20", "Kato Pws 1.5gm", "Kcl Solution A 20%", "Klean-prep", "Klean-prep", "Klor Con M", "Klor Con M", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-con", "Klor-con", "Klor-con", "Klor-con", "Klor-con", "Klor-con", "Klor-con", "Klor-con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-con", "Klor-con", "Klor-Con", "Klor-Con", "Klor-Con", "Klor-con", "Klor-Con Extended-release", "Klor-Con Extended-release", "Klor-Con Extended-release", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-con M", "Klor-con M", "Klor-Con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-Con M", "Klor-Con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-Con M", "Klor-con M", "Klor-con M", "Klor-Con M10", "Klor-Con M10", "Klor-Con M20", "Klor-con M20", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-Con Sprinkle", "Klor-con/25", "Klotrix", "Lacellate Solution - 1000", "Lacellate Solution - 250", "Lacellate Solution - 500", "Lactated Ringer's and 5% Dextrose", "Lactated Ringer's and 5% Dextrose Injection, USP", "Lactated Ringer's Injection", "Lactated Ringer's Injection USP", "Lactated Ringer's Injection, USP", "Lactated Ringer's Irrigation", "Lactated Ringer's Irrigation", "Lactated Ringer's Irrigation Sol", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Lactated Ringers Irrigation", "Lypholyte", "Lypholyte Multi-electrolyte Conc Inj", "Lyteprep", "Lyteprep", "Lyteprep", "Medi SM 24K Gold Hydrogel Peptide Mask Pack", "Micro K Extencaps Src 600mg", "Micro-K 10 Extencaps", "Micro-K Extencaps", "Micro-K Extencaps", "Micro-K-10 Extencaps Src 750mg", "Moi-stir Oral Swabsticks", "Moi-stir Oral Swabsticks", "Moi-stir Spray", "Moviprep", "MoviPrep", "MoviPrep", "Multiple Electrolyte Additive Inj", "Multiple Electrolyte Additive Liq Formula 1", "Multiple Electrolytes pH 5.5", "Multiple Electrolytes pH 7.4", "Multiple Vitamins and Minerals", "Multiple Vitamins and Minerals", "Multivitamins and Minerals Tablets", "Naturalyte H-200", "Naturalyte H-201", "Naturalyte H-206", "Naturalyte H-208", "Naturalyte H-223", "Naturalyte H-224", "Naturalyte H-225", "Naturalyte H-226", "Naturalyte H-227", "Naturalyte H-229", "Naturalyte H-230", "Naturalyte H-232", "Naturalyte H-251", "Naturalyte H-252", "Naturalyte H-260", "Naturalyte H-320", "Naturalyte H-330", "Naturalyte H-331", "Naturalyte H-332", "Naturalyte H-401", "Naturalyte H-402", "Naturalyte H-407", "Naturalyte H-408", "Naturalyte H-410", "Naturalyte H-602", "Naturalyte H-608", "Naturalyte H-615", "Naturalyte H-616", "Naturalyte H-617", "Naturalyte H-623", "Naturalyte H-624", "Naturalyte H-625", "Naturalyte H-630", "Naturalyte H-631", "Naturalyte H-661", "Naturalyte H-690", "Naturalyte H-706", "Navstel", "Neo K", "Normosol-R", "Normosol-R", "Normosol-R", "Normosol-R", "Normosol-R", "Normosol-R & 5% Dextrose", "Normosol-R and Dextrose", "Normosol-R and Dextrose", "Novo-lente K Tab 600mg", "NuLYTELY", "NuLYTELY", "NuLYTELY With Flavor Packs", "Nutrilyte", "Nxstage Pureflow Dialysate Concentrate (sak 303)", "Nxstage Pureflow Dialysate Concentrate (sak 304)", "Nxstage Pureflow Dialysate Concentrate (sak 305)", "Nxstage Pureflow Dialysate Concentrate (sak-301)", "Nxstage Pureflow Dialysate Concentrate (sak-302)", "Nxstage Pureflow Solution Rfp-204-can", "Nxstage Pureflow Solution Rfp-207-can", "Nxstage Pureflow Solution Rfp-209-can", "Ocl Solution", "Odan Balanced Salt Solution", "Olimel 3.3% E", "Olimel 4.4% E", "Olimel 5.7% E", "Olimel 7.6% E", "One A Day Advance Adults", "One A Day Advance Adults 50+", "One Daily Vitamin and Mineral Dietary Supplement", "One Per Day Vitamin and Mineral Dietary Supplement", "One Tablet Daily Mens Formula", "One Tablet Daily Mens Formula", "One-A-day Advance Men's", "One-A-day Advance Men's", "Osteo Formula", "Peg-3350", "PEG-3350 and Electrolytes", "PEG-3350 and Electrolytes", "PEG-3350 and Electrolytes", "PEG-3350 and Electrolytes", "PEG-3350 and Electrolytes", "PEG-3350, Electrolytes, and Ascorbate", "PEG-3350, sodium chloride, sodium bicarbonate and potassium chloride", "PEG-3350, sodium chloride, sodium bicarbonate and potassium chloride", "Peg-3350, Sodium Sulfate, Sodium Chloride, Potassium Chloride, Sodium Ascorbate and Ascorbic Acid", "Peglyte Powder", "Peglyte Solution", "Perikabiven", "Periolimel 2.5% E", "Phoxillum B22k4/0", "Phoxillum Bk4/2.5", "Physiolyte", "Physiosol", "Physiosol", "Physiosol", "Plasma-Lyte 148", "Plasma-Lyte 148", "Plasma-Lyte 148 (pH 7.4)", "Plasma-Lyte 148 and dextrose", "Plasma-Lyte A", "Plasma-Lyte A", "Plasma-lyte A Injection", "Plasma-Lyte M and Dextrose", "Plasma-Lyte R", "Plasmalyte 148 In 5% Dextrose Inj", "Plasmalyte 148 In Water", "Plegisol", "Plegisol", "Plenvu", "Plenvu", "Plenvu", "PMS-peglyte", "Pokonza", "Polyethylene Glycol 3350 and Electrolytes", "Polyethylene Glycol 3350 and electrolytes with Lemon Flavor", "Polyethylene Glycol 3350 and electrolyteswith Orange Flavor", "POLYETHYLENE GLYCOL 3350, SODIUM CHLORIDE, SODIUM BICARBONATE and POTASSIUM CHLORIDE", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride - Unflavored", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride with Lemon Flavor", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride with Orange Flavor", "Polyethylene Glycol-3350 and Electrolytes", "Polyethylene Glycol-3350 and Electrolytes with Flavor Pack", "Polyethylene Glycol-3350, Sodium Chloride, Potassium Chloride and Sodium Bicarbonate", "Potas Chlor 20meq 5% Dex and Lactate Ringer", "Potas Chlor 30meq 5% Dex and 0.2% Sod Chlor", "Potass Chlor 10meq 5% Dex and 0.2% Sod Chlor", "Potass Chlor 30meq 5% Dex and 0.33% Sod Chlor", "Potass Chlor 30meq 5% Dex and 0.45% Sod Chlor", "Potass Chlor 40meq 5% Dex and 0.2% Sod Chlor", "Potass Chlor 40meq 5% Dex and 0.33% Sod Chlor", "Potass Chlor 40meq 5% Dex and 0.9% Sod Chlor", "Potass Chloride 10meq In 5% Dextrose Inj USP", "Potass Chloride 30meq In 5% Dextrose Inj USP", "Potass Chloride 5% Dextr 0.45% Sod Chlor Inj", "Potassium 20meq 5% Dextrose and 0.33% Sodium Chloride", "Potassium and Iodine Tab", "Potassium Chlor 40meq 5% Dex & Lac Ring", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium chloride", "Potassium chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride", "Potassium Chloride 20 Meq In 0.9% Sodium Chloride", "Potassium Chloride 20 Meq In 3.3% Dextrose and 0.3% Sodium Chloride", "Potassium Chloride 20 Meq In 5% Dextrose", "Potassium Chloride 20 Meq In 5% Dextrose and 0.225% Sodium Chloride", "Potassium Chloride 20 Meq In 5% Dextrose and 0.45% Sodium Chloride", "Potassium Chloride 20 Meq In 5% Dextrose and 0.9% Sodium Chloride", "Potassium Chloride 40 Meq In 0.9% Sodium Chloride", "Potassium Chloride 40 Meq In 3.3% Dextrose and 0.3% Sodium Chloride", "Potassium Chloride 40 Meq In 5% Dextrose", "Potassium Chloride 40 Meq In 5% Dextrose and 0.45% Sodium Chloride", "Potassium Chloride 40 Meq In 5% Dextrose and 0.9% Sodium Chloride", "Potassium Chloride and Dextrose", "Potassium Chloride Bp - Additive for Concentrated Haemodialysis Solutions", "Potassium Chloride Bp - Additive for Concentrated Haemodialysis Solutions", "Potassium Chloride Bp - Additive for Concentrated Haemodialysis Solutions", "Potassium Chloride Bp - Additive for Concentrated Haemodialysis Solutions", "Potassium Chloride Bp - Additive for Concentrated Haemodialysis Solutions", "Potassium Chloride ER", "Potassium Chloride ER", "Potassium Chloride ER", "Potassium chloride extended release", "Potassium chloride extended release", "Potassium Chloride Extended Release", "Potassium Chloride Extended Release", "Potassium chloride extended release", "Potassium Chloride Extended Release", "Potassium Chloride Extended Release", "Potassium chloride extended release", "Potassium Chloride Extended Release", "Potassium chloride extended release", "Potassium Chloride Extended Release", "Potassium Chloride Extended Release", "Potassium chloride extended release", "Potassium chloride extended release", "Potassium chloride extended release", "Potassium Chloride Extended Release", "Potassium Chloride Extended Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-Release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride Extended-release", "Potassium Chloride for Hemodialysis 7.55", "Potassium Chloride for Injection Concentrate", "Potassium Chloride for Injection Concentrate", "Potassium Chloride for Injection Concentrate USP", "Potassium Chloride for Injection Concentrate USP", "Potassium Chloride for Injection Concentrate, USP (2 Meq/ml)", "Potassium Chloride for Oral Solution", "Potassium Chloride for Oral Solution", "Potassium Chloride for Oral Solution", "Potassium Chloride for Oral Solution", "Potassium Chloride for Oral Solution", "Potassium Chloride In Dextrose", "Potassium Chloride In Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride In Lactated Ringer's Injection", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride In Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride In Sodium Chloride Injection USP", "Potassium Chloride Inj 149mg/ml USP", "Potassium Chloride Inj 149mg/ml USP", "Potassium Chloride Inj 2meq/ml", "Potassium Chloride Inj 30meq", "Potassium Chloride Inj 40meq", "Potassium Chloride Inj USP Liq 149mg/ml", "Potassium Chloride Injection", "Potassium Chloride Injection", "Potassium Chloride Injection", "Potassium Chloride Injection", "Potassium Chloride Injection 2meq/ml", "Potassium SR 600mg Tablets", "Potassium-36.8 0.5-4.5 (code:k-30) - Powder", "Potassium-novartis", "Potrassium Chloride", "PrismaSol", "PrismaSol", "Prismasol 2", "Prismasol 4", "Prismasol B22gk4/0", "Prismasol Bgk2/0", "Prismasol Bgk2/3.5", "Prismasol Bgk4/0/1.2", "Prismasol Bgk4/2.5", "Prismasol Bgk4/3.5", "Pro-600k Srt 600mg", "ProcalAmine", "Proception Sperm Nutrient Douche", "Prolax - Pws", "R04903 Liq", "R04909 Liq", "R04919 Liq", "R04922 Liq", "R04931 Liq", "R04936 Liq", "R04946 Liq", "R04972 Liq", "R04973 Liq", "Ribotin-E", "Ringer's Inj", "Ringer's Injection USP", "Ringers", "Ringers", "Ringers", "Ringers", "Ringers", "Ringers", "Ringers", "Ringers", "Ringers and Dextrose", "Ringers and Dextrose", "Ringers Irrigation", "Rogenic", "Roychlor - 10% - Liq Orl", "Rs-274", "Salivart Aer", "Salivart Oral Moisturizer", "Sb 1000", "Sb 1004", "Sb-110", "Sb-111", "Sb-119", "Sb-127", "Sb-131", "Sb-132", "Selectbag One (ax 125 G)", "Selectbag One (ax 150 G)", "Selectbag One (ax 200 G)", "Selectbag One (ax 225 G)", "Selectbag One (ax 250 G)", "Selectbag One (ax 2525 G)", "Selectbag One (ax 2550 G)", "Selectbag One (ax 275 G)", "Selectbag One (ax 325 G)", "Selectbag One (ax 350 G)", "Selectbag One (ax 450 G)", "Slo-pot", "Slow K", "Slow K", "Smofkabiven", "Smofkabiven Extra Nitrogen", "Smofkabiven Peripheral", "Spectrum Performa Multivitamins and Minerals Tablets", "Ssp+", "Ssp+", "Strong Potass Chloride Inj 0.15gm/ml", "Suclear", "Suflave", "Super C-M-K", "Super Charged Energy", "Super Charged Energy", "Super Daily No 2", "Super-cell", "Sutab", "Tar-end", "Thermotabs Buffered Salt Supplement", "Tis-U-Sol", "Tis-U-sol", "Tis-U-sol Solution", "TPN Electrolytes", "TPN Electrolytes", "Tqm Acid Concentrate A1280", "TriLyte with Flavor Packs", "TRILYTE with flavor packs", "Vamin N", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Zintrexyl-C" ]

[ "Kaon Cl", "Kaon-CL 10", "Micro-K", "Sando-K", "Slow-K" ]

[ "Plasma-Lyte 148 and dextrose", "Dextrose and Electrolyte No. 75", "Plasma-Lyte R", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Polyethylene Glycol-3350, Sodium Chloride, Potassium Chloride and Sodium Bicarbonate", "Polyethylene Glycol-3350 and Electrolytes with Flavor Pack", "Glysol-500", "Cytosol Ophthalmics - Balanced Salt Solution", "Moviprep", "PEG-3350 and Electrolytes", "GoLYTELY", "NuLYTELY", "Ringers and Dextrose", "Physiosol", "Elliotts B", "Peg-3350", "HalfLytely and Bisacodyl", "HalfLytely and Bisacodyl", "Ionosol and Dextrose", "Aminosyn II in Dextrose", "Aminosyn II and Dextrose", "FreAmine III", "Isoplate", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Aminosyn II with Electrolytes in Dextrose with Calcium", "Tis-U-Sol", "Dextrose in Ringers", "Isolyte M in Dextrose", "Isolyte H in Dextrose", "Clenz-Lyte", "POLYETHYLENE GLYCOL 3350, SODIUM CHLORIDE, SODIUM BICARBONATE and POTASSIUM CHLORIDE", "HalfLytely and Bisacodyl Bowel Prep with Flavor Packs", "Lactated Ringers", "Balanced Salt", "Suclear", "Balanced Salt", "Polyethylene Glycol 3350 and Electrolytes", "Dextrose in Lactated Ringers", "GaviLyte - C TM", "Lactated Ringers", "Gavilyte-N", "Ionosol B and Dextrose", "Potassium Chloride In Dextrose", "Potassium Chloride In Dextrose", "Plasma-Lyte M and Dextrose", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Nutrilyte", "Lactated Ringers", "Plasma-Lyte 148", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Colyte", "Polyethylene Glycol-3350 and Electrolytes", "Colyte with flavor packs", "Effervescent Potassium Chloride", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Sodium Chloride", "Potassium Chloride and Dextrose", "PrismaSol", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "PrismaSol", "Medi SM 24K Gold Hydrogel Peptide Mask Pack", "HydroGold 9", "Elliotts B", "PEG-3350 and Electrolytes", "PEG-3350 and Electrolytes", "Isoplate", "Ringers", "Normosol-R and Dextrose", "Balanced Salt", "Lactated Ringers", "Tis-U-sol", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Physiosol", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Lactated Ringers", "Bss", "Ringers", "Thermotabs Buffered Salt Supplement", "Lactated Ringers", "TriLyte with Flavor Packs", "Isolyte P in Dextrose", "Plasma-Lyte 148", "Plasma-Lyte A", "Isolyte S pH 7.4", "Potassium Chloride In Sodium Chloride", "Lactated Ringers", "Lactated Ringers and Dextrose", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Lactated Ringers and Dextrose", "Bss Plus", "Bss", "Gavilyte G Tm", "Lactated Ringers and Dextrose", "Lactated Ringers", "Normosol-R", "Normosol-R", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride - Unflavored", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride with Lemon Flavor", "Polyethylene Glycol 3350, Sodium Chloride, Sodium Bicarbonate and Potassium Chloride with Orange Flavor", "Lactated Ringers", "Ringers", "Potassium Chloride in Lactated Ringers and Dextrose", "Potassium Chloride in Lactated Ringers and Dextrose", "Physiolyte", "TPN Electrolytes", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Potassium Chloride in Dextrose", "Physiosol", "MoviPrep", "NuLYTELY With Flavor Packs", "PEG-3350, sodium chloride, sodium bicarbonate and potassium chloride", "Polyethylene Glycol 3350 and electrolytes with Lemon Flavor", "Polyethylene Glycol 3350 and electrolyteswith Orange Flavor", "Dextrose and Electrolyte No. 48", "Lactated Ringers", "Plenvu", "Plenvu", "Lacellate Solution - 1000", "Lacellate Solution - 500", "Lacellate Solution - 250", "PEG-3350 and Electrolytes", "GaviLyte-H and Bisacodyl", "Ringers", "Lactated Ringers and Dextrose", "Lactated Ringers", "Ringers", "Colyte", "Potassium Chloride in Dextrose", "Lactated Ringers", "Prismasol Bgk4/2.5", "Prismasol Bgk4/3.5", "Prismasol Bgk2/3.5", "Prismasol Bgk2/0", "Prismasol B22gk4/0", "Prismasol Bgk4/0/1.2", "Phoxillum Bk4/2.5", "Phoxillum B22k4/0", "One Daily Vitamin and Mineral Dietary Supplement", "One Per Day Vitamin and Mineral Dietary Supplement", "Lactated Ringers", "Ringers", "Ringers", "ProcalAmine", "Isolyte S", "Lactated Ringers Irrigation", "Lactated Ringers", "Lactated Ringers and Dextrose", "Potassium Chloride in Sodium Chloride", "Cardioplegic", "Plegisol", "Ionosol MB and Dextrose", "Aminosyn II with Electrolytes", "Aminosyn", "Aminosyn", "PEG-3350, sodium chloride, sodium bicarbonate and potassium chloride", "Ringers", "Ringers and Dextrose", "TRILYTE with flavor packs", "Potassium Chloride in Sodium Chloride", "GoLYTELY", "GoLYTELY", "GoLYTELY", "Ionosol MB and Dextrose", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Normosol-R", "Potassium Chloride in Lactated Ringers and Dextrose", "Lactated Ringers", "Lactated Ringers and Dextrose", "Lactated Ringers", "Normosol-R", "Isolyte S in Dextrose", "Peg-3350, Sodium Sulfate, Sodium Chloride, Potassium Chloride, Sodium Ascorbate and Ascorbic Acid", "NuLYTELY", "PEG-3350, Electrolytes, and Ascorbate", "Lactated Ringers", "Potassium Chloride in Dextrose", "Sutab", "Ribotin-E", "Folitin-Z", "Zintrexyl-C", "Potassium Chloride", "Potassium Chloride", "Ringers Irrigation", "Foliflex", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "Potassium Chloride in Sodium Chloride", "(20 Mmol/l) Potassium Chloride In 5% Dextrose Injection USP", "(40 Mmol/l) Potassium Chloride In 5% Dextrose Injection USP", "(20mmol/l) Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection USP", "(40mmol/l)potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection USP", "Acid Concentrate 2117", "Acid Concentrate D12207", "(20 Mmol/l) Potassium Chloride In 5% Dextrose and 0.9% Sodium Chloride Injection USP", "Potass Chlor 40meq 5% Dex and 0.9% Sod Chlor", "Tis-U-sol Solution", "Lactated Ringer's Injection USP", "Lactated Ringer's Injection, USP", "Lactated Ringer's and 5% Dextrose Injection, USP", "Acid Concentrate D12265", "Acid Concentrate D12264", "Acid Concentrate D12262", "Acid Concentrate D12255", "Acid Concentrate D12248", "Acid Concentrate 2161", "Acid Concentrate D12236", "Acid Concentrate D12290", "Acid Concentrate D12293", "Acid Concentrate D12302", "Acid Concentrate D12300", "Acid Concentrate D12275", "Acid Concentrate D12299", "Acid Concentrate D12286", "Acid Concentrate D12305", "Acid Concentrate D12294", "Acid Concentrate D12291", "0.15% Potassium Chloride In 5% Dextrose and 0.20% Sodium Chloride Injection USP", "Isolyte S Ph 7.4 (multi-electrolyte Injection)", "(20 Mmol/l) Potassium Chloride In 3.3% Dextrose and 0.3% Sodium Chloride Injection USP", "(40mmol/l) Potassium Chloride In 3.3% Dextrose and 0.3% Sodium Chloride Injection USP", "Acid Concentrate D12272", "Acid Concentrate D12316", "Potassium Chloride 20 Meq In 5% Dextrose and 0.45% Sodium Chloride", "Potassium Chloride 40 Meq In 3.3% Dextrose and 0.3% Sodium Chloride", "Potassium Chloride 20 Meq In 3.3% Dextrose and 0.3% Sodium Chloride", "Acid Concentrate 2182", "Bss Plus", "Potassium Chloride 40 Meq In 5% Dextrose and 0.45% Sodium Chloride", "Acid Concentrate 2151", "Acid Concentrate 2156", "Bss Sterile Irrigating Solution", "Golytely Gi Lavage Solution", "Colyte", "Acid Concentrate 2126", "Potassium Chloride In Lactated Ringer's Injection", "Acid Concentrate A1243", "Acid Concentrate A1251", "Acid Concentrate A1252", "Acid Concentrate A1255", "Acid Concentrate A1228", "Acid Concentrate A1241", "Acid Concentrate A1242", "Acid Concentrate A1231", "Elliott's Solution A", "Acid Concentrate A1229", "Acid Concentrate A1265", "Acid Concentrate A1267", "Potassium Chloride In Sodium Chloride Injection USP", "Potassium Chloride 20 Meq In 0.9% Sodium Chloride", "Potassium Chloride 40 Meq In 0.9% Sodium Chloride", "Potassium Chloride 20 Meq In 5% Dextrose and 0.9% Sodium Chloride", "Potassium Chloride 40 Meq In 5% Dextrose and 0.9% Sodium Chloride", "Naturalyte H-690", "Naturalyte H-661", "Bi-peglyte", "Naturalyte H-252", "Naturalyte H-617", "Naturalyte H-229", "Naturalyte H-625", "Naturalyte H-706", "Naturalyte H-616", "Naturalyte H-602", "Naturalyte H-631", "Naturalyte H-401", "Naturalyte H-332", "Naturalyte H-260", "Naturalyte H-407", "Naturalyte H-226", "Naturalyte H-402", "Naturalyte H-225", "Naturalyte H-615", "Naturalyte H-224", "Naturalyte H-330", "Naturalyte H-410", "Naturalyte H-408", "Naturalyte H-223", "Naturalyte H-208", "Naturalyte H-623", "Naturalyte H-201", "Naturalyte H-624", "Naturalyte H-630", "Naturalyte H-608", "Naturalyte H-200", "Naturalyte H-230", "Naturalyte H-206", "Naturalyte H-331", "Naturalyte H-320", "Naturalyte H-251", "Naturalyte H-232", "Naturalyte H-227", "Plasma-lyte A Injection", "MoviPrep", "Nxstage Pureflow Dialysate Concentrate (sak-301)", "Nxstage Pureflow Dialysate Concentrate (sak 304)", "Nxstage Pureflow Dialysate Concentrate (sak-302)", "Citrasate C1125", "Citrasate C2125", "Citrasate C3125", "Citrasate C4125", "Citrasate C1150", "Citrasate C2150", "Citrasate C3150", "Acid Concentrate 2102", "H.E.L.P.bicel", "Acid Concentrate 2135", "Peglyte Powder", "(40 Mmol/l) Potassium Chloride In 0.9% Sodium Chloride Injection USP", "Lactated Ringer's Irrigation Sol", "Acid Concentrate D12201", "Acid Concentrate D12188", "Acid Concentrate D18001", "Acid Concentrate D12196", "Acid Concentrate D12184", "Acid Concentrate D12209", "Dextrose 5% and Electrolyte No75 Inj", "Acid Concentrate D12150", "Acid Concentrate D 12219 Liq", "Salivart Aer", "Moi-stir Spray", "Moi-stir Oral Swabsticks", "Adrenogist Tab", "Amo Endosol Extra", "Acid Concentrate 3187", "Acid Concentrate 2105", "Acid Concentrate 3186", "Acid Concentrate 2112", "Lypholyte Multi-electrolyte Conc Inj", "Acid Concentrate (r04984)", "Acid Concentrate Ro4983", "Acid Concentrate Ro9501", "Acid Concentrate Ro9500", "Potassium-novartis", "Acid Concentrate (r04981)", "K2 With Glucose Liq R04977", "K1 Liq R04978", "K1 Liq R04911", "K2 Liq R04902", "Acid Concentrate (r04938)", "Acid Concentrate-r04948 Liq", "Acid Concentrate (r04968)", "Acid Concentrate Ro4979", "Acid Concentrate (ro9503)", "Acid Concentrate Ro9502", "Acid Concentrate D-18006", "Acid Concentrate D-18003", "Acid Concentrate D12269", "Acid Concentrate D12268", "Acid Concentrate D12267", "Acid Concentrate D12261", "Acid Concentrate D12259", "Acid Concentrate D12250", "Acid Concentrate D12247", "Acid Concentrate D12221", "Acid Concentrate D12220", "R04972 Liq", "R04973 Liq", "Acid Concentrate (r04974)", "R04922 Liq", "R04919 Liq", "R04909 Liq", "R04931 Liq", "R04936 Liq", "Acid Concentrate Ro4947", "Acid Concentrate (r04976)", "Acid Concentrate (r04975)", "Acid Concentrate (r04969)", "R04946 Liq", "Acid Concentrate(36.83x) R04900", "R04903 Liq", "Acid Concentrate(36.83x) R04906", "Acid Concentrate Rz164c", "Acid Concentrate Rz195c", "Acid Concentrate Rz207c", "Acid Concentrate Rz167c", "Acid Concentrate Rz110c", "Acid Concentrate Rz111c", "Acid Concentrate Rz202c", "Acid Concentrate Rz254c", "Acid Concentrate Rz171c", "Acid Concentrate Rz127c", "Acid Concentrate Rz119c", "Acid Concentrate Ro4144", "Acid Concentrate Ro4138", "Acid Concentrate Ro4137", "Acid Concentrate Rz183c", "Acid Concentrate Rz185c", "Acid Concentrate Rz208c", "Acid Concentrate Rz211c", "Acid Concentrate Rz212c", "Acid Concentrate Rz249c", "Acid Concentrate Rx252c", "Acid Concentrate Rz194c", "Acid Concentrate Rx253c", "Acid Concentrate Rz210c", "Acid Concentrate Rz247c", "Acid Concentrate Rz153c", "Acid Concentrate Rz144c", "Acid Concentrate Rz203c", "Acetate Concentrate R07376", "Acid Concentrate Rz248c", "Acid Concentrate Rz196c", "Acid Concentrate Rz209c", "Acid Concentrate 2113", "Acid Concentrate 2132", "Acid Concentrate 2166", "Acid Concentrate D12315", "Acid Concentrate D12318", "Acid Concentrate D12301", "Acid Concentrate D12282", "Acid Concentrate D12285", "Acid Concentrate D12284", "Acid Concentrate D12303", "Acid Concentrate D18009", "Anaplex Tab", "Lactated Ringer's Irrigation", "Proception Sperm Nutrient Douche", "Neo K", "Lypholyte", "Prolax - Pws", "Acid Concentrate D12252", "Acid Concentrate 2162", "Acid Concentrate 2189", "Acid Concentrate 2168", "Acid Concentrate 2175", "Multiple Electrolyte Additive Inj", "Dextrose 50% Inj W Electrolytes PF Abbovac", "Dialyte", "Acid Concentrate Rz264c", "Acid Concentrate Rz265c", "Acid Concentrate Ro4145", "Acid Concentrate Rz213c", "Hemosol Lg4", "Hemosol Lg2", "Electropeg Solution", "Haemosol H-200", "Concentrated Haemodialysis Solution Bp-rz266c", "Acid Concentrate Bp Rz267c", "Haemosol H-223", "Haemosol H-208", "Haemosol H-206", "Haemosol H-201", "Haemosol H-226", "Haemosol H-227", "Haemosol H-225", "Haemosol H-251", "Haemosol H-250", "Haemosol H-224", "Haemosol H-260", "Haemosol H-320", "Acid Concentrate 2122", "Concentrated Haemodialysis Solution Bp-rz270c", "Acid Concentrate (rz271c)", "Acid Concentrate (rz272c)", "Acid Concentrate (rz274c)", "Acid Concentrate (rz275c)", "Acid Concentrate (rz262c)", "Acid Concentrate Bp Rz278c", "Moi-stir Oral Swabsticks", "Acid Concentrate 2148", "Acid Concentrate 2147", "Acid Concentrate 2131", "Acid Concentrate 2129", "Acid Concentrate 2190", "Acid Concentrate 2185", "Acid Concentrate D-12287", "Acid Concentrate 2155", "Acid Concentrate 2196", "Haemosol H-331", "Haemosol H-330", "Lyteprep", "Acid Concentrate 2106", "Haemosol H-229", "Acid Concentrate Bp Ro4151", "Acid Concentrate Bp Rz279c", "Haemosol H-404", "Haemosol H-401", "Haemosol H-402", "Acid Concentrate Bp Ro9505", "Acid Concentrate Bp Ro9506", "Acid Concentrate Bp Ro9507", "Salivart Oral Moisturizer", "Acid Concentrate (ro4147)", "Acid Concentrate (ro4148)", "Sb-111", "Sb-119", "Sb-132", "Rs-274", "Sb 1000", "Sb 1004", "Acid Hemodialysis Conc Sb 1003", "Sb-110", "Sb-131", "Sb-127", "D12006", "Acid Concentrate D12092", "Acid Concentrate D12093", "Acid Concentrate D12094", "Haemosol H-230", "Acid Concentrate 2123", "Haemosol H-410", "D-12043 Sol Conc Electrolyt Pour Dialy", "Haemosol H-232", "Acid Concentrate D12095", "Acid Concentrate D12067", "One A Day Advance Adults 50+", "One A Day Advance Adults", "Haemosol H-252", "Haemosol H-253", "Haemosol H-254", "Spectrum Performa Multivitamins and Minerals Tablets", "Haemosol H-332", "Haemosol H-407", "Haemosol H-408", "Haemosol H-624", "Haemosol H-602", "Haemosol H-690", "Haemosol H-630", "Haemosol H-616", "Haemosol H-615", "Haemosol H-625", "Haemosol H-661", "Haemosol H-631", "Haemosol H-623", "Haemosol H-608", "Haemosol H-617", "Multivitamins and Minerals Tablets", "D12046 Conc Electrolyte Renal Dialysis", "Acid Concentrate D12054", "Acid Concentrate D13001", "Acid Concentrate D12028", "H-710", "H-706", "Artisial", "Acid Concentrate D12112", "Balanced Salt Solution", "Acid Concentrate 2101", "Acid Concentrate D12117", "Acid Concentrate D12119", "Klean-prep", "Acid Concentrate 2109", "Acid Concentrate D12132", "Acid Concentrate D12143", "K+36.8", "K-med", "Ocl Solution", "Iocare Balanced Salt Solution", "Peglyte Solution", "Acid Concentrate D12135", "Acid Concentrate D12185", "Acid Concentrate D12200", "D12230 Liq", "Acid Concentrate D12167", "Acid Concentrate D12205", "Acid Concentrate D12204", "Acid Concentrate D12197", "Acid Concentrate D12308", "Acid Concentrate D12309", "Acid Concentrate D12310", "Acid Concentrate D12311", "Acid Concentrate D12308", "Acid Concentrate D12309", "Acid Concentrate D12311", "Acid Concentrate A1246", "Acid Concentrate A1245", "Acid Concentrate A1263", "Citrasate C10125", "Jamplyte", "Navstel", "Jamplyte", "Jamp-electropeg", "Jamp-electropeg With Flavour Packet", "Hemosate Ultra Hs1125", "Hemosate Ultra Hs2125", "Hemosate Ultra Hs3125", "Hemosate Ultra Hs4125", "Hemosate Ultra Hs1150", "Hemosate Ultra Hs2150", "Hemosate Ultra Hs3150", "Selectbag One (ax 2550 G)", "Hemasate Ultra Hs2150", "Hemasate Ultra Hs4125", "Hemasate Ultra Hs1150", "Hemasate Ultra Hs1125", "Hemasate Ultra Hs2125", "Hemasate Ultra Hs3125", "Hemasate Ultra Hs3150", "Multiple Electrolyte Additive Liq Formula 1", "Nxstage Pureflow Dialysate Concentrate (sak 303)", "Nxstage Pureflow Dialysate Concentrate (sak 305)", "Selectbag One (ax 225 G)", "Selectbag One (ax 325 G)", "Selectbag One (ax 250 G)", "Periolimel 2.5% E", "Olimel 4.4% E", "Olimel 5.7% E", "Olimel 3.3% E", "(20mmol/l) Potassium Chloride In 5% Dextrose and 0.2% Sodium Chloride Injection USP", "Ringer's Inj", "(40 Mmols/l) Potassium Chloride In Lactated Ringer's Injection USP", "Nxstage Pureflow Solution Rfp-204-can", "Nxstage Pureflow Solution Rfp-207-can", "Nxstage Pureflow Solution Rfp-209-can", "Bicarb Hemodial Conc 36.83", "Bicarbolyte Bicar Hemodialysis Conc", "Bicarbolyte Bicar Hemodialysis Conc", "Bicarbolyte Bicar Hemodialsis Conc", "Bicarbolyte Bicar Hemodialysis Conc", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "Vivia Acid", "(20mmol/l) Potassium Chloride In 0.9% Sodium Chloride Injection USP", "Dialysis Solution 35 K4", "Dialysis Solution 35 K2", "Selectbag One (ax 275 G)", "Selectbag One (ax 2525 G)", "Selectbag One (ax 350 G)", "Selectbag One (ax 450 G)", "Eye Stream", "Klean-prep", "Odan Balanced Salt Solution", "Tqm Acid Concentrate A1280", "Isolyte S (multi-electrolyte Injection)", "Potass Chloride 10meq In 5% Dextrose Inj USP", "Potass Chloride 30meq In 5% Dextrose Inj USP", "Potass Chlor 10meq 5% Dex and 0.2% Sod Chlor", "Potas Chlor 30meq 5% Dex and 0.2% Sod Chlor", "Potass Chlor 40meq 5% Dex and 0.2% Sod Chlor", "Potassium 20meq 5% Dextrose and 0.33% Sodium Chloride", "Potass Chlor 30meq 5% Dex and 0.33% Sod Chlor", "Potass Chlor 40meq 5% Dex and 0.33% Sod Chlor", "Potass Chlor 30meq 5% Dex and 0.45% Sod Chlor", "Potas Chlor 20meq 5% Dex and Lactate Ringer", "Potassium Chlor 40meq 5% Dex & Lac Ring", "Potass Chloride 5% Dextr 0.45% Sod Chlor Inj", "0.15% Potassium Chloride In 3.3% Dextrose and 0.30% Sodium Chloride Injection", "Isolyte H With Dextrose 5% Inj", "0.15% Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection", "Acid Concentrate 2152", "Acid Concentrate 2163", "Acid Concentrate D12292", "0.15% Potassium Chloride In 5% Dextrose Injection USP", "0.30% Potassium Chloride In 5% Dextrose and 0.45% Sodium Chloride Injection", "0.15% Potassium Chloride In 5% Dextrose and 0.33% Sodium Chloride Injection USP", "0.15% Potassium Chloride In 5% Dextrose and 0.9% Sodium Chloride Injection", "Dextrose 2.5% In Half Strength Lactated Ringer's Injection, USP", "Isolyte R In 5% Dextrose", "Isolyte M In 5% Dextrose", "Isolyte S With 5% Dextrose Inj", "Ringer's Injection USP", "Hyperlyte (multi-electrolyte Concentrate)", "0.30% Potassium Chloride In 5% Dextrose", "Acid Concentrate 2171", "Acid Concentrate 2198", "Acid Concentrate 2120", "Acid Concentrate 2125", "Acid Concentrate 2139", "TPN Electrolytes", "Potassium Chloride 20 Meq In 5% Dextrose and 0.225% Sodium Chloride", "Plegisol", "Glycerolyte 57 Solution", "Balanced Salt Solution", "Lactated Ringer's Injection", "Potassium Chloride 20 Meq In 5% Dextrose", "Potassium Chloride 40 Meq In 5% Dextrose", "Lactated Ringer's Irrigation", "Normosol-R & 5% Dextrose", "Selectbag One (ax 125 G)", "Selectbag One (ax 150 G)", "Selectbag One (ax 200 G)", "Plasmalyte 148 In 5% Dextrose Inj", "PMS-peglyte", "Lactated Ringer's and 5% Dextrose", "Amo Endosol Solution", "Plasmalyte 148 In Water", "5% Dextrose In Lactated Ringer's Injection", "Ssp+", "Ssp+", "Super Daily No 2", "Children's Chew Multi & Min Tab", "Children's Chew Multi & Min Tab", "Calcium Magnesium With Potassium Tab", "Formula R Tab", "Rogenic", "Potassium and Iodine Tab", "Tar-end", "Multiple Vitamins and Minerals", "Multiple Vitamins and Minerals", "Osteo Formula", "One-A-day Advance Men's", "One-A-day Advance Men's", "Iodine-potassium Tablets", "One Tablet Daily Mens Formula", "One Tablet Daily Mens Formula", "Super C-M-K", "Lyteprep", "Lyteprep", "Formule No 204 Profil Tab", "Super-cell", "High Potency Multivitamins & Minerals Caplets", "High Potency Multivitamins & Minerals Caplets", "Smofkabiven", "Vamin N", "Aminosyn II 8.5% M In 20% Dextrose (dual Chamber)", "Aminosyn II 7% M In 10% Dextrose(dual Chamber)", "Aminosyn II 10% With Electrolytes", "Smofkabiven Peripheral", "Prismasol 2", "Normosol-R", "Super Charged Energy", "Super Charged Energy", "Smofkabiven Extra Nitrogen", "Balanced Salt", "Cardioplegic Solution", "Diphen", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Lactated Ringers and Dextrose", "Multiple Electrolytes pH 5.5", "Multiple Electrolytes pH 7.4", "Acid Concentrate A1251", "Acid Concentrate A1246", "Acid Concentrate A1263", "Acid Concentrate A1252", "Acid Concentrate A1229", "Acid Concentrate A1255", "Acid Concentrate A1243", "Acid Concentrate A1228", "Acid Concentrate A1241", "Acid Concentrate A1245", "Acid Concentrate A1242", "Acid Concentrate A1231", "Acid Concentrate A1265", "Acid Concentrate A1267", "Potassium Chloride in Dextrose and Sodium Chloride", "Potassium Chloride in Dextrose and Sodium Chloride", "Lactated Ringers and Dextrose", "Lactated Ringers and Dextrose", "Perikabiven", "Lactated Ringers", "Lactated Ringers", "PEG-3350 and Electrolytes", "Suflave", "Acid Concentrate A1253", "Acid Concentrate A1227", "Acid Concentrate A1226", "Acid Concentrate A1225", "Acid Concentrate A1224", "Acid Concentrate A1223", "Acid Concentrate A1222", "Acid Concentrate A1221", "Acid Concentrate A1261", "Acid Concentrate A1262", "Acid Concentrate A1268", "Acid Concentrate A1294", "Acid Concentrate A1277", "Acid Concentrate A1278", "Acid Concentrate A1279", "Acid Concentrate A1269", "Acid Concentrate A1274", "Acid Concentrate A1276", "Acid Concentrate A1280", "Acid Concentrate A1295", "Acid Concentrate A1297", "Acid Concentrate A1275", "Acid Concentrate A1296", "Acid Concentrate A1298", "Kabiven", "Acid Concentrate A1266", "Olimel 7.6% E", "Lactated Ringers", "Prismasol 4", "Plenvu", "Finazol", "Lactated Ringers", "Lactated Ringers", "Jamplyte + Bisacodyl", "Plasma-Lyte A", "Lactated Ringers", "Plasma-Lyte 148 (pH 7.4)", "Normosol-R and Dextrose", "Lactated Ringers", "Lactated Ringers" ]

[ "P55011", "Q13621", "Q9H2X9", "Q9UHW9", "Q9Y666", "Q9UP95" ]

[]

[ "P55011", "Q13621", "Q9H2X9", "Q9UHW9", "Q9Y666", "Q9UP95" ]

DB00762

Irinotecan

Irinotecan is a topoisomerase inhibitor used for chemotherapy. It is a water-soluble analogue of [camptothecin], which is extracted from the Chinese tree _Camptotheca acuminate_.[A263376] The bis-piperidine side chain in the structure of irinotecan bestows enhanced water solubility.[A263381] As an anticancer drug, irinotecan was first commercially available in Japan in 1994 to treat various cancers such as lung, cervical and ovarian cancer.[A263376] Approved by the FDA in 1996,[A263366] irinotecan is used to treat colorectal cancer and pancreatic adenocarcinoma.[L50181, L50186, L50201] Irinotecan liposome was approved by the FDA in February 2024.[L50186] The active metabolite SN-38 is also a potent inhibitor of DNA topoisomerase I. Both irinotecan and SN-38 mediate antitumor activity by forming a complex with topoisomerase I and blocking its enzymatic activity, thereby interfering with DNA synthesis. This leads to the arrest of the cell cycle in the S-G2 phase and cancer cell death.[A263376]

solid

Irinotecan is indicated for the treatment of: - Metastatic carcinoma of the colon or rectum as first-line treatment in combination with [fluorouracil] and [leucovorin].[L50181, L50201] - Metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial fluorouracil-based therapy, as monotherapy [L50201] or in combination with [fluorouracil] and [leucovorin].[L50181] Irinotecan liposome injection is used in adults for the treatment of: - Metastatic pancreatic adenocarcinoma in combination with [oxaliplatin], [fluorouracil], and [leucovorin] as first-line treatment.[L50186] - Metastatic pancreatic adenocarcinoma in combination with [fluorouracil] and [leucovorin] after disease progression following gemcitabine-based therapy.[L50186]

Irinotecan is an antineoplastic agent. The administration of irinotecan has resulted in antitumor activity in mice bearing cancers of rodent origin and in human carcinoma xenografts of various histological types.[L50181]

DNA topoisomerase I is a nuclear enzyme that ensures proper DNA topology during replication and transcription.[A263381] It relieves torsional strain in the DNA double helix during replication and transcription by creating reversible single-strand breaks.[A263371, L50181] Upon administration, irinotecan is converted into its active metabolite, SN-38, by carboxylesterase in the liver and gastrointestinal tract.[A263366] Irinotecan and SN-38 both inhibit DNA topoisomerase I, acting on the S and G2 phases of the cell cycle.[A263371, L50181] Irinotecan and SN-38 bind to the topoisomerase I-DNA complex and prevent the religation of single-strand breaks.[L50181] The ternary complex formed by topoisomerase I, DNA, and either irinotecan or SN-38 interferes with the moving replication fork, inducing replication arrest and lethal double-stranded breaks in DNA. Because double-stranded breaks cannot be efficiently repaired by mammalian cells, apoptosis of cancer cells occurs.[L50181]

Over the recommended dose range of 50 to 350 mg/m2, the AUC of irinotecan increases linearly with dose; the AUC of SN-38 increases less than proportionally with dose. Maximum concentrations of the active metabolite SN-38 are generally seen within 1 hour following the end of a 90-minute infusion of irinotecan.[L50181] The plasma levels of SN-38 are much lower than that of irinotecan.[A1169, L50181] Following intravenous infusion in patients with solid tumours, the mean (± standard deviation) Cmax was 1,660 ± 797 ng/mL at a dose of 125 mg/m2 and 3,392 ± 874 ng/mL at a dose of 340 mg/m2. The AUC0–24 was 10,200 ± 3,270 ng x h/mL at a dose of 125 mg/m2 and 20,604 ± 6,027 ng x h/mL at a dose of 340 mg/m2.[L50181]

Upon administration, irinotecan is converted primarily in the liver into its active metabolite, SN-38, by carboxylesterase.[A263366] SN-38 is formed by cleavage of the carbamate bond between the camptothecin moiety and the dipiperidino side chain.[L50181] While in vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies, SN-38 is approximately 1000 times as potent as irinotecan as an inhibitor of topoisomerase I.[A1169, L50181] SN-38 can further be glucuronidated by UGT1A1 to form SN-38G.[A1168, A263366, L50181] Irinotecan can also undergo CYP3A4-mediated oxidation to form NPC and APC. While some sources state that NPC and APC are weak inhibitors of topoisomerase I,[A1168, A1169] they are unlikely to contribute to the pharmacological activity of irinotecan.

The oral LD50 is 1045 mg/kg in mice and 867 mg/kg in rats.[L50196] In clinical trials involving patients with various cancers, single doses of up to 750 mg/m2 of irinotecan were associated with similar adverse events reported with the recommended dosage and regimen. There have been reports of overdosage at doses up to approximately twice the recommended therapeutic dose, which may be fatal. The most significant adverse reactions reported were severe neutropenia and severe diarrhea. Because there is no known antidote for overdosage of irinotecan, maximum supportive care should be instituted to prevent dehydration due to diarrhea and to treat any infectious complications.[L50181]

After intravenous infusion of irinotecan in humans, the mean terminal elimination half-life of irinotecan is about 6 to 12 hours. The mean terminal elimination half-life of the active metabolite SN-38 is about 10 to 20 hours.[L50181]

Irinotecan is about 30% to 68% bound to plasma proteins. SN-38 is approximately 95% bound to plasma proteins. Irinotecan and SN-38 are mainly bound to albumin.[L50181]

The disposition of irinotecan has not been fully elucidated in humans. The urinary excretion of irinotecan, SN-38, and SN-38 glucuronide are 11% to 20%, <1%, and 3%, respectively. The cumulative biliary and urinary excretion of irinotecan and its metabolites (SN-38 and SN-38 glucuronide) over a period of 48 hours in two patients ranged from approximately 25% (100 mg/m2) to 50% (300 mg/m2).[L50181]

Following intravenous infusion in patients with solid tumours, the mean (± standard deviation) volume of distribution of terminal elimination phase was 110 ± 48.5 L/m2 at a dose of 125 mg/m2 and 234 ± 69.6 L/m2 at a dose of 340 mg/m2.[L50181]

The mean (± standard deviation) total systemic clearance of irinotecan in patients with solid tumours was 13.3 ± 6.01 L/h/m2 at a dose of 125 mg/m2 and 13.9 ± 4.0 L/h/m2 at a dose of 340 mg/m2.[L50181]

Organic compounds

Alkaloids and derivatives

Camptothecins

null

[ "approved", "investigational" ]

[ "L01CE", "L01C", "L01", "L" ]

[ "Humans and other mammals" ]

[ { "cost": "22.2", "description": "Irinotecan hcl 40 mg/2 ml vial", "unit": "ml" }, { "cost": "36.0", "description": "Camptosar 20 mg/ml vial", "unit": "ml" }, { "cost": "138.07", "description": "Irinotecan hcl 40 mg/2 ml inj", "unit": "ml" } ]

[ { "approved": "2005-05-03", "country": "Canada", "expires": "2015-10-11", "number": "2202531" }, { "approved": "2005-01-18", "country": "Canada", "expires": "2018-07-27", "number": "2294031" }, { "approved": "2002-06-11", "country": "United States", "expires": "2020-10-28", "number": "6403569" }, { "approved": "2004-09-21", "country": "United States", "expires": "2020-11-01", "number": "6794370" }, { "approved": "2014-04-22", "country": "United States", "expires": "2025-05-02", "number": "8703181" }, { "approved": "2012-12-11", "country": "United States", "expires": "2025-05-02", "number": "8329213" }, { "approved": "2015-03-31", "country": "United States", "expires": "2025-05-02", "number": "8992970" }, { "approved": "2012-04-03", "country": "United States", "expires": "2028-08-29", "number": "8147867" }, { "approved": "2016-06-14", "country": "United States", "expires": "2033-06-12", "number": "9364473" }, { "approved": "2016-11-15", "country": "United States", "expires": "2033-06-12", "number": "9492442" }, { "approved": "2016-05-17", "country": "United States", "expires": "2033-06-12", "number": "9339497" }, { "approved": "2016-09-27", "country": "United States", "expires": "2033-06-12", "number": "9452162" }, { "approved": "2017-08-01", "country": "United States", "expires": "2033-06-12", "number": "9717724" }, { "approved": "2017-08-15", "country": "United States", "expires": "2025-05-02", "number": "9730891" }, { "approved": "2017-08-08", "country": "United States", "expires": "2025-05-02", "number": "9724303" }, { "approved": "2017-10-10", "country": "United States", "expires": "2025-05-02", "number": "9782349" }, { "approved": "2019-10-29", "country": "United States", "expires": "2036-10-15", "number": "10456360" }, { "approved": "2020-07-28", "country": "United States", "expires": "2025-05-02", "number": "10722508" }, { "approved": "2021-04-20", "country": "United States", "expires": "2033-06-12", "number": "10980795" }, { "approved": "2021-05-04", "country": "United States", "expires": "2036-10-15", "number": "10993914" }, { "approved": "2013-06-12", "country": "United States", "expires": "2033-06-12", "number": "11369597" }, { "approved": "2016-08-19", "country": "United States", "expires": "2036-08-19", "number": "11344552" }, { "approved": "2016-10-15", "country": "United States", "expires": "2036-10-15", "number": "12059497" } ]

[ "Camptosar", "Camptosar", "Camptosar", "Camptosar", "Camptosar", "Irinotecan", "Irinotecan for Injection", "Irinotecan hydrochloide", "Irinotecan hydrochloide", "Irinotecan hydrochloide", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan hydrochloride", "Irinotecan hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan hydrochloride", "Irinotecan hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride", "Irinotecan Hydrochloride 100 mg/ 5 mL", "Irinotecan Hydrochloride 100 mg/5 mL", "Irinotecan Hydrochloride 40 mg/2 mL", "Irinotecan Hydrochloride 40 mg/2 mL", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection", "Irinotecan Hydrochloride Injection USP", "Irinotecan Hydrochloride Injection USP", "Irinotecan Hydrochloride Injection, USP", "Irinotecan Hydrochloride Trihydrate for Injection", "Irinotecan Hydrochloride Trihydrate Injection", "Onivyde", "Onivyde", "Onivyde", "Onivyde Pegylated Liposomal" ]

[ "Biotecan", "Campto" ]

[]

[ "Q969P6", "P11387" ]

[ "P08684", "P20815", "P24462", "P22309", "O60656", "O00748", "P23141" ]

[ "P02768" ]

[ "O75751", "Q9Y6L6", "P33527", "Q9UNQ0", "P08183", "Q92887" ]

DB05482

SN-38

7-ethyl-10-hydroxycamptothecin (SN 38) is a liposomal formulation of the active metabolite of Irinotecan [DB00762], a chemotherapeutic pro-drug approved for the treatment of advanced colorectal cancer. SN 38 has been used in trials studying the treatment of Cancer, Advanced Solid Tumors, Small Cell Lung Cancer, Metastatic Colorectal Cancer, and Triple Negative Breast Cancer, among others.

solid

Investigated for use/treatment in colorectal cancer.

SN-38 (7-ethyl-10-hydroxycamptothecin) is the active metabolite of Irinotecan (CPT-11). Irinotecan is a topoisomerase I inhibitor commercially available as Camptosar®. SN-38 has been found to be 200–2000 times more cytotoxic than CPT-11, but has not been used as an anticancer drug due to its poor solubility in pharmaceutically acceptable solvents and low affinity to lipid membranes. SN-38 also undergoes a reversible conversion to an inactive open lactone ring structure at physiological pH. LE-SN-38 is a novel lipsome based formulation containing liposomes of uniform size distribution (<200 nm). Drug entrapment efficiency of the formulation is>95%.

The entrapment of SN-38 in lipsomes results in a more stable and more soluble form of the drug. This allows for increased affinity of SN-38 to lipid membranes and improved delivery of the drug to tumor sites. SN-38 is a highly effective cytotoxic topoisomerase I inhibitor.

null

Organic compounds

Alkaloids and derivatives

Camptothecins

null

[ "investigational" ]

[]

[]

[ "NeoLipid Camptosar" ]

[]

[ "P11387" ]

[ "P08684" ]

[]

DB00763

Methimazole

Methimazole is a thionamide antithyroid agent that inhibits the synthesis of thyroid hormones.[A184559,A184733,A184694] It was first introduced as an antithyroid agent in 1949[A184502] and is now commonly used in the management of hyperthyroidism, particularly in those for whom more aggressive options such as surgery or radioactive iodine therapy are inappropriate.[L8336,L8339] On a weight basis, methimazole is 10 times more potent than the other major antithyroid thionamide used in North America, [propylthiouracil],[L8339] and is the active metabolite of the pro-drug [carbimazole], which is an antithyroid medication used in the United Kingdom and parts of the former British Commonwealth.[A184733] Traditionally, methimazole has been preferentially used over propylthiouracil due to the risk of fulminant hepatotoxicity carried by the latter,[A184757] with propylthiouracil being preferred in pregnancy due to a perceived lower risk of teratogenic effects. Despite documented teratogenic effects in its published labels,[L8336,L8339] the true teratogenicity of methimazole appears to be unclear[A184643,A184757,A184763] and its place in therapy may change in the future.

solid

In the United States, methimazole is indicated for the treatment of hyperthyroidism in patients with Graves' disease or toxic multinodular goiter for whom thyroidectomy or radioactive iodine therapy are not appropriate treatment options. Methimazole is also indicated for the amelioration of hyperthyroid symptoms in preparation for thyroidectomy or radioactive iodine therapy.[L8336] In Canada, methimazole carries the above indications and is also indicated for the medical treatment of hyperthyroidism regardless of other available treatment options.[L8339]

Methimazole inhibits the synthesis of thyroid hormones resulting in an alleviation of hyperthyroidism.[L8336][L8339] Onset of action occurs within 12 to 18 hours, and its duration of action is 36 to 72 hours, likely due to concentration of methimazole and some metabolites within the thyroid gland after administration.[A184643] The most serious potential side effect of methimazole therapy is agranulocytosis, and patients should be instructed to monitor for, and report, any signs or symptoms of agranulocytosis such as fever or sore throat. Other cytopenias may also occur during methimazole therapy. There also exists the potential for severe hepatic toxicity with the use of methimazole, and monitoring for signs and symptoms of hepatic dysfunction, such as jaundice, anorexia, pruritus, and elevation in liver transaminases, is prudent in patients using this therapy.[L8336,L8339]

Methimazole's primary mechanism of action appears to be interference in an early step in thyroid hormone synthesis involving thyroid peroxidase (TPO), however the exact method through which methimazole inhibits this step is unclear.[A184559] TPO, along with hydrogen peroxide, normally catalyzes the conversion of iodide to iodine and then further catalyzes the incorporation of this iodine onto the 3 and/or 5 positions of the phenol rings of tyrosine residues in thyroglobulin. These thyroglobulin molecules then degrade within thyroid follicular cells to form either thyroxine (T4) or tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland.[A184697] Methimazole may directly inhibit TPO, but has been shown in vivo to instead act as a competitive substrate for TPO, thus becoming iodinated itself and interfering with the iodination of thyroglobulin.[A184559] Another proposed theory is that methimazole’s sulfur moiety may interact directly with the iron atom at the centre of TPO’s heme molecule, thus inhibiting its ability to iodinate tyrosine residues.[A184694] Other proposed mechanisms with weaker evidence include methimazole binding directly to thyroglobulin or direct inhibition of thyroglobulin itself.[A184559]

Absorption of methimazole after oral administration is rapid and extensive,[A184514,A184541,A184499] with an absolute bioavailability of approximately 0.93[A184499] and a Tmax ranging from 0.25 to 4.0 hours.[A184514,A184499] Cmax is slightly, but not significantly, higher in hyperthyroid patients, and both Cmax and AUC are significantly affected by the oral dose administered.[A184514]

Methimazole is rapidly and extensively metabolized by the liver, mainly via the CYP450 and FMO enzyme systems.[A184571,A184574] Several metabolites have been identified, though the specific enzyme isoforms responsible for their formation are not entirely clear. One of the first methimazole metabolites identified, 3-methyl-2-thiohydantoin, may contribute to antithyroid activity - its antithyroid activity has been demonstrated in rats and may explain the prolonged duration of iodination inhibition following administration despite methimazole's relatively short half-life.[A184541] A number of metabolites have been investigated as being the culprits behind methimazole-induced hepatotoxicity. Both glyoxal and N-methylthiourea have established cytotoxicity and are known metabolic products of methimazole's dihydrodiol intermediate. Sulfenic and sulfinic acid derivatives of methimazole are thought to be the ultimate toxicants responsible for hepatotoxicity, though their origin is unclear - they may arise from direct oxidation of methimazole via FMO, or from oxidation of N-methylthiourea further downstream in the metabolic process.[A184571,A184574]

The oral LD50 of methimazole in rats is 2250 mg/kg.[L8333] Signs and symptoms of methimazole overdose may include gastrointestinal distress, headache, fever, joint pain, pruritus, and edema. More serious adverse effects, such as aplastic anemia or agranulocytosis, may manifest within hours to days.[L8336,L8339] Hepatitis, nephrotic syndrome, exfoliative dermatitis, and CNS effects such as neuropathy or CNS depression/stimulation are also potential, albeit less frequent, results of overdose.[L8336,L8339] Management of overdose involves supportive treatment as dictated by the patient's status.[L8336,L8339] This may involve monitoring of the patient's vital signs, blood gases, serum electrolytes, or bone marrow function as indicated.[L8339]

Following a single intravenous bolus injection of 10mg of methimazole, the t1/2 of the distribution phase was 0.17 hours and the t1/2 of the elimination phase was 5.3 hours.[A184499] Methimazole's primary active metabolite, 3-methyl-2-thiohydantoin, has a half-life approximately 3 times longer than its parent drug.[A184541] Renal impairment does not appear to alter the half-life of methimazole, but patients with hepatic impairment showed an increase in half-life roughly proportional to the severity of their impairment - moderate insufficiency resulted in a elimination t1/2 of 7.1 hours, while severe insufficiency resulted in an elimination t1/2 of 22.1 hours.[A184499] There does not appear to be any significant differences in half-life based on thyroid status (i.e. no difference between euthyroid and hyperthyroid patients).[A184499,A184502,A184514]

Methimazole exhibits little-to-no protein binding, existing primarily as free drug in the serum.[A184526,A184541,A184643]

Urinary excretion of unchanged methimazole has been reported to be between 7% and 12%. Elimination via feces appears to be limited, with a cumulative fecal excretion of 3% after administration of methimazole.[A184514] Enterohepatic circulation also appears to play a role in the elimination of methimazole and its metabolites, as significant amounts of these substances are found in the bile post-administration.[A184643]

The apparent volume of distribution of methimazole has been reported as roughly 20 L.[A184541] Following oral administration, methimazole is highly concentrated in the thyroid gland - intrathyroidal methimazole levels are approximately 2 to 5 times higher than peak plasma levels, and remain high for 20 hours after ingestion.[A184559]

Following a single intravenous bolus injection of 10mg of methimazole, clearance was found to be 5.70 L/h.[A184499] Renal impairment does not appear to alter clearance of methimazole, but patients with hepatic impairment showed a reduction in clearance roughly proportional to the severity of their impairment - moderate insufficiency resulted in a clearance of 3.49 L/h, while severe insufficiency resulted in a clearance of 0.83 L/h.[A184499] There does not appear to be any significant differences in clearance based on thyroid status (i.e. no difference between euthyroid and hyperthyroid patients).[A184499,A184502,A184514]

Organic compounds

Organoheterocyclic compounds

Azolines

Imidazolines

[ "approved" ]

[ "H03BB", "H03B", "H03", "H", "H03BB", "H03B", "H03", "H" ]

[ "Humans and other mammals" ]

[ { "cost": "1.45", "description": "Tapazole 10 mg tablet", "unit": "tablet" }, { "cost": "1.9", "description": "Methimazole 20 mg tablet", "unit": "tablet" }, { "cost": "9.49", "description": "Methimazole powder", "unit": "g" }, { "cost": "0.29", "description": "Northyx 5 mg tablet", "unit": "tablet" }, { "cost": "0.45", "description": "Methimazole 5 mg tablet", "unit": "tablet" }, { "cost": "0.47", "description": "Northyx 10 mg tablet", "unit": "tablet" }, { "cost": "0.66", "description": "Tapazole 5 mg tablet", "unit": "tablet" }, { "cost": "0.78", "description": "Methimazole 10 mg tablet", "unit": "tablet" }, { "cost": "0.82", "description": "Northyx 15 mg tablet", "unit": "tablet" }, { "cost": "0.94", "description": "Northyx 20 mg tablet", "unit": "tablet" } ]

[]

[ "Apo-methimazole", "Dom-methimazole", "Jamp Methimazole", "Jamp Methimazole", "Mar-methimazole", "Mar-methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole", "Methimazole Tablets USP", "Methimazole Tablets USP", "Methimazole Tablets USP", "PHL-methimazole", "PMS-methimazole", "Tapazole", "Tapazole", "Tapazole", "Tapazole", "Tapazole", "Tapazole", "Tapazole" ]

[ "Danantizol", "Favistan", "Metizol", "Strumazol", "Strumazole", "Thacapzol", "Thycapzol", "Thyrozol", "Tirozol" ]

[]

[ "P07202" ]

[ "P05177", "P11509", "P20813", "P33261", "P11712", "P10635", "P05181", "P08684", "P31513" ]

[]

DB00764

Mometasone

Mometasone is a corticosteroid not currently used in medical products. [Mometasone furoate] however, is still in use.

solid

The inhaler is indicated for the maintenance treatment of asthma as prophylactic therapy. The nasal spray is indicated for the treatment of the nasal symptoms of seasonal allergic and perennial allergic rhinitis.

Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. When glucocorticoids are discontinued, asthma stability may persist for several days or longer. Mometasone has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone. The clinical significance of these findings is unknown.

Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Inflammation is decreased by diminishing the release of leukocytic acid hydrolases, prevention of macrophage accumulation at inflamed sites, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Mometasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone.

Nasal spray is virtually undetectable in plasma

Hepatic. Extensive metabolism to multiple metabolites. There are no major metabolites detectable in plasma. Upon in vitro incubation, one of the minor metabolites formed is 6ß-hydroxy-mometasone furoate. In human liver microsomes, the formation of the metabolite is regulated by cytochrome P-450 3A4.

The potential for acute toxic effects following overdose with the mometasone inhaler is low. However, habitual overuse of the product can cause symptoms of steroid overload, including menstrual irregularities, acne, obesity, and muscle weakness. Single oral doses up to 8000 µg have been studied on human volunteers with no adverse events reported.

5.8 hours

98% to 99% (in a concentration range of 5 to 500 ng/mL).

null

Organic compounds

Lipids and lipid-like molecules

Steroids and steroid derivatives

Pregnane steroids

[ "experimental" ]

[ "R03AL", "R03A", "R03", "R", "R01AD", "R01A", "R01", "R", "R03AK", "R03A", "R03", "R" ]

[ "Humans and other mammals" ]

[]

[ { "approved": "1995-03-07", "country": "United States", "expires": "2012-06-25", "number": "5394868" }, { "approved": "2004-11-09", "country": "Canada", "expires": "2018-03-16", "number": "2282360" }, { "approved": "1997-04-08", "country": "Canada", "expires": "2011-09-06", "number": "2091360" }, { "approved": "2000-10-03", "country": "United States", "expires": "2018-04-03", "number": "6127353" }, { "approved": "2001-06-05", "country": "United States", "expires": "2017-08-20", "number": "6240918" }, { "approved": "2012-05-08", "country": "United States", "expires": "2018-09-17", "number": "8173172" }, { "approved": "2003-01-07", "country": "United States", "expires": "2018-09-17", "number": "6503537" }, { "approved": "1998-11-03", "country": "United States", "expires": "2016-05-03", "number": "5829434" }, { "approved": "2000-05-30", "country": "United States", "expires": "2017-08-27", "number": "6068832" }, { "approved": "2006-06-27", "country": "United States", "expires": "2020-11-21", "number": "7067502" }, { "approved": "2009-07-28", "country": "United States", "expires": "2020-11-21", "number": "7566705" }, { "approved": "2012-02-07", "country": "United States", "expires": "2024-03-12", "number": "8109918" }, { "approved": "2011-05-31", "country": "United States", "expires": "2024-03-12", "number": "7951131" }, { "approved": "2011-09-27", "country": "United States", "expires": "2027-06-12", "number": "8025635" }, { "approved": "2017-03-07", "country": "United States", "expires": "2026-04-04", "number": "9585681" }, { "approved": "2011-05-31", "country": "United States", "expires": "2024-03-12", "number": "7951130" }, { "approved": "2009-06-09", "country": "United States", "expires": "2026-11-29", "number": "7544192" }, { "approved": "2011-05-31", "country": "United States", "expires": "2024-03-12", "number": "7951133" }, { "approved": "2010-05-11", "country": "United States", "expires": "2024-03-12", "number": "7713255" }, { "approved": "2010-02-16", "country": "United States", "expires": "2024-03-12", "number": "7662141" }, { "approved": "2014-07-01", "country": "United States", "expires": "2032-02-08", "number": "8763222" } ]

[]

[ "P04150", "P06401" ]

[ "P10632", "P08684", "P20815" ]

[]

DB00765

Metyrosine

An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma. (Martindale, The Extra Pharmacopoeia, 30th ed)

solid

For use in the treatment of patients with pheochromocytoma, for preoperative preparation of patients for surgery, management of patients when surgery is contraindicated, and chronic treatment of patients with malignant pheochromocytoma.

In patients with pheochromocytoma, who produce excessive amounts of norepinephrine and epinephrine, administration of one to four grams of metyrosine per day has reduced catecholamine biosynthesis from about 35 to 80 percent as measured by the total excretion of catecholamines and their metabolites (metanephrine and vanillylmandelic acid). The maximum biochemical effect usually occurs within two to three days, and the urinary concentration of catecholamines and their metabolites usually returns to pretreatment levels within three to four days after metyrosine is discontinued. Most patients with pheochromocytoma treated with metyrosine experience decreased frequency and severity of hypertensive attacks with their associated headache, nausea, sweating, and tachycardia. In patients who respond, blood pressure decreases progressively during the first two days of therapy with metyrosine; after withdrawal, blood pressure usually increases gradually to pretreatment values within two to three days.

Metyrosine inhibits tyrosine hydroxylase, which catalyzes the first transformation in catecholamine biosynthesis, i.e., the conversion of tyrosine to dihydroxyphenylalanine (DOPA). Because the first step is also the rate-limiting step, blockade of tyrosine hydroxylase activity results in decreased endogenous levels of catecholamines and their synthesis. This consequently, depletes the levels of the catecholamines dopamine, adrenaline and noradrenaline in the body,usually measured as decreased urinary excretion of catecholamines and their metabolites. One main end result of the catecholamine depletion is a decrease in blood presure.

Well absorbed from the gastrointestinal tract.

Little biotransformation, with catechol metabolites accounting for less than 1% of the administered dose.

Signs of metyrosine overdosage include those central nervous system effects observed in some patients even at low dosages. At doses exceeding 2000 mg/day, some degree of sedation or feeling of fatigue may persist. Doses of 2000-4000 mg/day can result in anxiety or agitated depression, neuromuscular effects (including fine tremor of the hands, gross tremor of the trunk, tightening of the jaw with trismus), diarrhea, and decreased salivation with dry mouth. The acute toxicity of metyrosine was 442 mg/kg and 752 mg/kg in the female mouse and rat respectively.

3.4 to 3.7 hours

null

Because the first step is also the rate-limiting step, blockade of tyrosine hydroxylase activity results in decreased endogenous levels of catecholamines, usually measured as decreased urinary excretion of catecholamines and their metabolites.

null

Organic compounds

Phenylpropanoids and polyketides

Phenylpropanoic acids

null

[ "approved" ]

[ "C02KB", "C02K", "C02", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "19.35", "description": "Demser 250 mg capsule", "unit": "capsule" } ]

[]

[ "Demser", "Demser", "Metyrosine", "Metyrosine", "Metyrosine" ]

[]

[ "P07101" ]

[]

DB00766

Clavulanic acid

Clavulanic acid is a beta-lactamase inhibitor that is frequently combined with [Amoxicillin] or [Ticarcillin] to fight antibiotic resistance by preventing their degradation by beta-lactamase enzymes, broadening their spectrum of susceptible bacterial infections.[T665] Clavulanic acid is derived from the organism Streptomyces clavuligerus.[A182228]When it is combined with amoxicillin, clavulanic acid is frequently known as Augmentin, Co-Amoxiclav, or Clavulin.[L7880,L7904,L7910]

solid

Clavulanic acid combined with other antibiotics is indicated to prevent the development of drug-resistant strains of bacteria and promotes their therapeutic antibacterial effects.[L7880,L7904] The following conditions, when they produced beta-lactamases, have been treated with a combination of amoxicillin and clavulanic acid or ticarcillin and clavulanic acid[L7880,L7904]: Acute otitis media caused by H. influenzae and M. catarrhalis Sinusitis due to H. influenzae and M. catarrhalis Lower respiratory tract infections due to Haemophilus influenzae, S.aureus, Klebsiella species, and Moraxella catarrhalis Skin and skin structure infections caused by Staphylococcus aureus, Escherichia coli, and Klebsiella species Urinary Tract Infections due to E. coli, Klebsiella species of bacteria, and Enterobacter species of bacteria, S.marcescens, or S.aureus Gynecologic infections due to a variety of bacteria, including P.melaninogenicus, Enterobacter species, E.Coli species, Klebsiella species, S. aureus, S.epidermidis Septicemia due to a variety of bacteria, including Klebsiella species, E.Coli species, S.aureus, or Pseudomonas species Bone and joint infections due to S.aureus Intraabdominal infections due to E.Coli, K.pnemoniae, or B.fragilis group **A note on susceptibility** It should be noted that it is only to be administered in infections that are confirmed or highly likely to be caused by susceptible bacteria. Culture and susceptibility tests should be performed if possible and used in selecting whether this antibiotic is prescribed. When beta-lactamase enzyme production is not detected during microbiological testing, clavulanic acid should not be used. When these tests are not available patterns of local infection and susceptibility may be used to determine the appropriateness of using clavulanic acid.[L7880] Ticarcillin with clavulanate has shown particular efficacy in mixed infections in addition to empiric therapy before determining the susceptibility of causative organisms. The ticarcillin-clavulanic acid combination may prove to be an effective single-agent antibiotic therapy to treat infections where a regimen of several drugs may normally be used.[L7904]

Clavulanic acid inactivates some beta-lactamase enzymes that are produced by bacteria, therefore preventing enzymatic destruction of amoxicillin. This helps to treat a variety of bacterial infections which would otherwise be resistant to antibiotics without the addition of clavulanic acid.[L7880,L7886,L7904]

Clavulanic acid contains a beta-lactam ring in its structure that binds in an irreversible fashion to beta-lactamases, preventing them from inactivating certain beta-lactam antibiotics, with efficacy in treating susceptible gram-positive and gram-negative infections.[A182228,A182234]

Clavulanic acid, when taken orally, is well absorbed in the gastrointestinal tract. After administration of radiolabeled clavulanic acid to four human subjects, a minimum of 73% absorption and the average absolute bioavailability was calculated at 64%.[A182267] The mean Cmax in a group of 8 healthy research volunteers was 2.098 ± 0.441 micrograms/ml in a pharmacokinetic study. The same study reported a mean Tmax of 1.042 ± 0.80 hours.[A182264] Tmax is reported to be 40-120 minutes according to another pharmacokinetic study.[A182261]

Clavulanic acid is heavily metabolized to form the metabolites 2,5-dihydro-4-(2- hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butan-2-one.[A182267,L7886] The first metabolite was found to account for 15.6% of the dose while the second metabolite was reported to account for 8.8% of the dose in one pharmacokinetic study.[A182267]

**LD50 information** Clavulanic acid has demonstrated low oral acute toxicity in adult rodents, having an LD50 of more than 2000 mg/kg. The toxicity of clavulanic acid on pre-weaning rats was also studied. Gastrointestinal disturbance and mortality occurred, even at lower clavulanic acid doses of 125 mg/kg.[L7898] **Overdose information** Overdose information has been obtained for the combination of amoxicillin and clavulanic acid, as these drugs are frequently administered together in a single product.[L7880,L7886] Changes in fluid and electrolyte balances and gastrointestinal symptoms may occur in the case of an overdose. Offer symptomatic treatment or gastrointestinal disturbances, while considering the importance of fluid and electrolyte balance. This drug may be removed by a session of hemodialysis. When coadministered with amoxicillin, crystalluria causing renal failure has been observed.[L7886] Seizures may also occur in a case of overdose, or in a patient with renal failure.[L7904]

The half-life of clavulanic acid is reported to be similar to amoxicillin, and last 45-90 minutes.[A182261] A study of radiolabeled clavulanic acid administered to 4 healthy volunteers determined a half-life of 0.8 h.[A182267]

The plasma protein binding of amoxicillin is about 25%.[L7886]

About 40 to 65% of the clavulanic acid is excreted as unchanged drug in urine during the first 6 hours following ingestion. The metabolites of clavulanic acid are found to be excreted in the urine and feces and as carbon dioxide in expired air. Clavulanate is cleared by both renal and non-renal processes.[L7886] About 17% of radiolabeled dose of clavulanic acid was found to be exhaled in expired air and 8% of a dose was found to be excreted in the feces.[A182267]

A study in 4 healthy volunteers administered a radiolabeled dose of clavulanic acid determined a volume of distribution of 12L.[A182267]Clavulanic acid is distributed to various tissues and interstitial fluid. Clinically significant concentrations have been measured in the gallbladder, abdomen, skin, fat, and muscle tissues. Bile, pus, synovial and peritoneal fluids are also found to have therapeutic concentrations of clavulanic acid.[L7886] Studies of animals have demonstrated that clavulanic crosses the placenta.[L7886]

The clearance of clavulanic acid in a pharmacokinetic study of 4 healthy volunteers administered a radiolabeled dose of clavulanic acid was 0.21 l/min.[A182267] Another resource indicates the average clearance of clavulanic acid is 12.20 liters/h/70 kg.[A182270] Dose adjustments may be required in patients with renal failure.[L7880]

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved", "vet_approved" ]

[]

[ "Enteric bacteria and other eubacteria" ]

[]

[ { "approved": "2005-04-12", "country": "United States", "expires": "2020-04-04", "number": "6878386" }, { "approved": "2007-05-15", "country": "United States", "expires": "2020-04-04", "number": "7217430" }, { "approved": "2007-07-31", "country": "United States", "expires": "2020-04-04", "number": "7250176" }, { "approved": "2004-08-31", "country": "United States", "expires": "2020-04-04", "number": "6783773" }, { "approved": "2004-06-08", "country": "United States", "expires": "2020-04-04", "number": "6746692" } ]

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[]

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"Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin/Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Augmentin XR", "Amoxicillin and Clavulanate Potassium", "Amoxicillin", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin Sodium and Potassium Clavulanate for Injection", "Amoxicillin Sodium and Potassium Clavulanate for Injection", "Amoxicillin Sodium and Potassium Clavulanate for Injection", "Clavulin 500 F Tab", "Clavulin 875", "Apo-amoxi Clav", "Apo-amoxi Clav", "Ratio-aclavulanate", "Ratio-aclavulanate 250 F", "Apo-amoxi Clav", "Ratio-aclavulanate", "Amoxi-clav", "Timentin", "Clavulin 250 Tab", "Ratio-aclavulanate", "Timentin", "Novo-clavamoxin 125", "Novo-clavamoxin 250", "Novo-clavamoxin 875", "Clavulin 125 F Oral Sus", "Clavulin 250 F Oral Sus", "Clavulin 400", "Clavulin 200", "PMS-amclav-875", "PMS-amclav-400", "PMS-amclav-200", "Apo-amoxi Clav 125mg/31.25mg Per 5ml", "Apo-amoxi Clav 250mg/62.5mg Per 5ml", "Apo-amoxi Clav", "Ratio-aclavulanate 125 F", "Auro-amoxiclav", "Auro-amoxiclav", "Auro-amoxiclav", "Amoxi-clav", "Sandoz Amoxi-clav Tablet", "Sandoz Amoxi-clav Tablet", "Jamp Amoxi Clav", "Jamp Amoxi Clav", "Jamp Amoxi Clav", "Ag-amoxi Clav", "Ag-amoxi Clav", "Ag-amoxi Clav", "Mint-amoxi/clav", "Mint-amoxi/clav", "Mint-amoxi/clav", "Apo-amoxicillin-clavulanate", "Apo-amoxicillin-clavulanate", "Apo-amoxicillin-clavulanate", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Augmentin Es-600", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin/Clav Pot Oral Susp", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Truemed Group LLC", "M-amoxi Clav", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Augmentin", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin/clav", "Amoxicillin/clav", "Pro-amoxi Clav", "Pro-amoxi Clav", "Pro-amoxi Clav", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Jamp Amoxi Clav Suspension", "Jamp Amoxi Clav Suspension", "Jamp Amoxi Clav Suspension", "Augmentin", "Ag-amoxi Clav Suspension", "Ag-amoxi Clav Suspension", "Ag-amoxi Clav Suspension", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "M-amoxi Clav", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and clavulanate potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium", "Amoxicillin and Clavulanate Potassium" ]

[]

[ "P13866" ]

DB00767

Benzquinamide

Benzquinamide is a discontinued antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties. The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors.

solid

Used to prevent and treat nausea and vomiting associated with anesthesia and surgery, administered intramuscularly or intravenously.

Benzquinamide is an antiemetic compound with antihistaminic, mild anticholinergic, and sedative properties.

The mechanism of action is not known, but presumably benzquinamide works via antagonism of muscarinic acetycholine receptors and histamine H1 receptors.

Incomplete, with 33–39% bioavailability via the capsule and suppository routes, relative to the intramuscular route.

null

1-1.6 hours (for all formulations)

null

Organic compounds

Organoheterocyclic compounds

Tetrahydroisoquinolines

null

[ "withdrawn" ]

[]

[ "Humans and other mammals" ]

[]

benzquinamida | Benzquinamide | BZQ | H1-R | H1R | HH1R

[]

[ "Benzchinamide", "Emete-con", "Emeticon", "Promecon", "Quantril" ]

[]

[ "P35367", "P08173", "P11229", "P08912", "P08172", "P20309" ]

[]

DB00768

Olopatadine

Olopatadine is a selective histamine H1 antagonist and mast cell stabilizer that works by attenuating inflammatory and allergic reactions. It is a structural analog of [doxepin], which has a minimal anti-allergic activity.[L6790] Olopatadine works by blocking the effects of histamine, which is a primary inflammatory mediator that causes inflammatory and allergic reactions. An ophthalmic solution of olopatadine was approved by the FDA and European Union for the treatment of seasonal and perennial allergic conjunctivitis in 1996 and 2002, respectively.[A1172] In comparison to other anti-allergenic ophthalmic medications, olopatadine displays a good comfort and tolerability profile since it does not cause perturbation of cell membranes.[A179809] Olopatadine is used for the symptomatic treatment of ocular itching associated with allergic conjunctivitis in ophthalmic formulations and seasonal allergic rhinitis in intranasal formulations. It is currently marketed under several brand names, including Pazeo, Patanase, and Opatanol.

solid

Olopatadine is indicated for the symptomatic treatment of ocular itching associated with allergic conjunctivitis as ophthalmic solution.[L6781] As a nasal spray, as a monotherapy or in combination with [mometasone furoate], olopatadine is indicated for the symptomatic relief of seasonal allergic rhinitis in patients 12 years of age and older.[L6784,L39845]

Inflammatory reactions in response to various stimuli are mediated by endogenous mediators and other pro-inflammatory factors. Histamine receptor activation and mast cell degranulation are primary mechanisms that cause inflammatory reactions such as ocular itching, hyperemia, chemosis, eyelid swelling, and tearing of seasonal allergic conjunctivitis.[A179704] Olopatadine is an anti-allergenic molecule and mast cell stabilizer that inhibits the _in vivo_ type 1 immediate hypersensitivity reaction.[L6790] By blocking the effects of histamine, olopatadine works to reduce the symptoms of allergies and inflammation at various sites of administration, including the eyes and nose. It has shown to exert antihistaminic effects in isolated tissues, animal models, and humans.[L6784] Olopatadine also demonstrated dose-dependent inhibition of immunologically-stimulated release of histamine from rat basophilic leukemia cells and human conjunctival mast cells _in vitro_.[A179704] Olopatadine has a relatively rapid onset of action and prolonged duration, where it was shown to mediate anti-histaminic effects at 5 minutes to 24 hours post-administration.[A179704] While olopatadine is a non-sedating antihistamine agent, there have been reports of somnolence in some patients taking nasal olopatadine during clinical trials.[L6784] Temporary blurred vision or other visual disturbances were observed following ophthalmic administration. Olopatadine has negligible effects on alpha-adrenergic, dopamine, muscarinic type 1 and 2, and serotonin receptors.[L6790] In clinical trials, there was no evidence of any effect of olopatadine on QT prolongation was observed following intranasal administration.[L6784]

Histamine is a biogenic vasoactive amine that binds to its receptors, which are G-protein coupled receptors. Signaling through the histamine H1 receptor is thought to primarily promote the activation of inflammatory reactions, such as allergy, asthma, and autoimmune diseases.[A179731] H1 receptor signaling activates the intracellular transcription factors, such as IP3, PLC, PKC, DAG, and intracellular calcium ions, which all work to activate further downstream cascades. Activated downstream cascades lead to the production of cytokines, the release of mast cell inflammatory mediators, synthesis of prostacyclins, activation of platelet factor, as well as the synthesis of nitric oxide, arachidonic acid, and thromboxane, which all contribute to inflammatory reactions.[A179731] Olopatadine is an anti-allergic molecule that works via several mechanisms. As a mast cell stabilizer, it stabilizes rodent basophils and human conjunctival mast cells and inhibits the immunologically-stimulated release of histamine.[A179704] Olopatadine acts as an antagonist at the histamine H1 receptors with high selectivity, which is explained by a unique receptor binding pocket that consists of the aspartate residue in the third transmembrane helix and other sites in the H1 receptor.[A1170] Upon binding, olopatadine blocks the H1 receptor signaling pathway, inhibiting the release of inflammatory mediators, such as tryptase, prostaglandin D2, TNF-alpha, as well as pro-inflammatory cytokines.[L6790] It also decreases chemotaxis and inhibits eosinophil activation.[L6781] _In vitro_, olopatadine was shown to inhibit epithelial cell intercellular adhesion molecule-1 (ICAM-1), which promotes the recruitment of migrating pro-inflammatory mediators.[A179704]

Ocular administration of olopatadine in healthy subjects resulted in the Cmax of 1.6 ± 0.9 ng/mL, which was reached after about 2.0 hours. The AUC was 9.7 ± 4.4 ngxh/mL.[L6781] The average absolute bioavaiability of intranasal olopatadine is about 57%. Following intranasal administration in healthy subjects, the Cmax of 6.0 ± 8.99 ng/mL at steady-state was reached between 30 minutes to 1 hour after twice daily intranasal administration. The average AUC was 66.0 ± 26.8 ng·h/mL. In patients with seasonal allergic rhinitis, the Cmax of 23.3 ± 6.2 ng/mL at steady-state was reached between 15 minutes and 2 hours post-dosing and the average AUC was 78.0 ± 13.9 ng·h/mL.[L6784]

Olopatadine undergoes hepatic metabolism in a non-extensive manner.[L6784,L6787] Based on oral pharmacokinetic studies, there are at least 6 circulating metabolites in human plasma.[L6784] Following topical ocular application of olopatadine, olopatadine N-oxide is formed by metabolism catalyzed by flavin-containing monooxygenase (FMO) 1 and 3 [L6784] and was detected in the plasma after 4 hours post-dosing in less than 10% of the total plasma in half of the patients.[L6781] Mono-desmethyl olopatadine, or N-desmethyl olopatadine, is formed by CYP3A4 [L6784] and may be detected in minimal levels.[L6781]

Based on the findings of an acute toxicity study in animals, the oral LD50 of olopatadine was >1150 mg/kg in mice and >3870 mg/kg in rats.[L6790] The Lowest published toxic dose via the oral route was 20 mg/kg in rat and 0.1 mg/kg in mouse.[MSDS] There are no known reports on overdosage following oral, ophthalmic, or intranasal administration of olopatadine. Likely symptoms of antihistamine overdose may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness in children. In case of suspected overdose, supportive and symptomatic treatment is recommended.[L6784]

Following ocular administration, the elimination half-life of olopatadine was 3.4 ± 1.2 hours. In oral pharmacokinetics study, the elimination half-life was reported to be 8 to 12 hours.[L6787]

About 55% of total olopatadine is bound to human serum proteins, with serum albumin being the primary protein of binding.[L6784]

Olopatadine is mainly eliminated through urinary excretion. Following oral administration, about 70% and 17% of the total dose was recovered in the urine and feces, respectively.[L6784]

In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent volume of distribution was 133.83 L.[A179740]

In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent oral clearance (CL/F) was 23.45 L/h.[A179740]

Organic compounds

Organoheterocyclic compounds

Benzoxepines

Dibenzoxepines

[ "approved" ]

[ "S01GX", "S01G", "S01", "S", "R01AC", "R01A", "R01", "R" ]

[ "Humans and other mammals" ]

[ { "cost": "3.83", "description": "Patanase 0.6% nasal spray", "unit": "g" }, { "cost": "21.38", "description": "Patanol 0.1% eye drops", "unit": "ml" }, { "cost": "52.98", "description": "Pataday 0.2% eye drops", "unit": "ml" }, { "cost": "111.2", "description": "Patanol 0.1% Solution 5ml Bottle", "unit": "bottle" } ]

[ { "approved": "1992-05-26", "country": "United States", "expires": "2010-12-18", "number": "5116863" }, { "approved": "2002-02-26", "country": "Canada", "expires": "2016-05-03", "number": "2195094" }, { "approved": "1995-11-21", "country": "Canada", "expires": "2012-11-21", "number": "1337603" }, { "approved": "2006-02-07", "country": "United States", "expires": "2024-05-12", "number": "6995186" }, { "approved": "2008-07-22", "country": "United States", "expires": "2022-12-19", "number": "7402609" }, { "approved": "2013-03-19", "country": "United States", "expires": "2023-03-17", "number": "8399508" }, { "approved": "2011-07-12", "country": "United States", "expires": "2023-08-02", "number": "7977376" }, { "approved": "2014-07-29", "country": "United States", "expires": "2032-05-19", "number": "8791154" }, { "approved": "1997-06-24", "country": "United States", "expires": "2015-12-06", "number": "5641805" }, { "approved": "2017-01-03", "country": "United States", "expires": "2032-05-19", "number": "9533053" }, { "approved": "2020-09-08", "country": "United States", "expires": "2034-09-04", "number": "10765686" }, { "approved": "2020-09-01", "country": "United States", "expires": "2034-09-04", "number": "10758550" }, { "approved": "2020-05-12", "country": "United States", "expires": "2034-09-04", "number": "10646500" }, { "approved": "2020-02-04", "country": "United States", "expires": "2034-09-04", "number": "10548907" }, { "approved": "2018-07-10", "country": "United States", "expires": "2034-09-04", "number": "10016443" }, { "approved": "2019-12-31", "country": "United States", "expires": "2034-09-04", "number": "10517880" }, { "approved": "2017-09-05", "country": "United States", "expires": "2034-09-04", "number": "9750754" }, { "approved": "2015-07-14", "country": "United States", "expires": "2034-09-04", "number": "9078923" }, { "approved": "2018-04-10", "country": "United States", "expires": "2034-09-04", "number": "9937189" }, { "approved": "2019-08-13", "country": "United States", "expires": "2034-09-04", "number": "10376526" }, { "approved": "2016-06-21", "country": "United States", "expires": "2034-09-04", "number": "9370483" }, { "approved": "2020-02-18", "country": "United States", "expires": "2034-09-04", "number": "10561672" }, { "approved": "2014-09-04", "country": "United States", "expires": "2034-09-04", "number": "11400101" }, { "approved": "2018-09-03", "country": "United States", "expires": "2038-09-03", "number": "11679210" }, { "approved": "2014-09-04", "country": "United States", "expires": "2034-09-04", "number": "12064442" } ]

[ "Act Olopatadine 0.1%", "Act Olopatadine 0.2%", "Apo-olopatadine", "Apo-olopatadine", "Clear Eyes Once Daily Eye Allergy Itch Relief", "CVS Eye Allergy Itch Relief Once Daily", "CVS Eye Allergy Itch Relief Twice Daily", "Eye Allergy Itch and Redness Relief", "Eye Allergy Itch and Redness Relief", "Eye Allergy Itch and Redness Relief", "Eye Allergy Itch and Redness Relief Twice Daily Relief", "Eye Allergy Itch Relief", "Eye Allergy Itch Relief", "Eye Allergy Itch Relief Once Daily Relief", "Eye Allergy Itch Relief Once Daily Relief", "Jamp-olopatadine", "Mint-olopatadine", "Mint-olopatadine 0.2%", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine", "Olopatadine 0.2%", "Olopatadine Hcl", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine hydrochloride", "Olopatadine hydrochloride", "Olopatadine hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride", "Olopatadine Hydrochloride Nasal", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution", "Olopatadine Hydrochloride Ophthalmic Solution Once Daily", "Olopatadine Hydrochloride Ophthalmic Solution Once Daily Relief", "Olopatadine Hydrochloride Ophthalmic Solution Twice Daily", "Olopatadine Ophthalmic Solution", "Once Daily Relief", "Opatanol", "Opatanol", "Pataday", "Pataday", "Pataday", "Pataday", "Pataday Once Daily Relief", "Pataday Once Daily Relief", "Pataday Twice A Day Relief", "Patanase", "Patanase", "Patanase", "Patanase", "Patanol", "Patanol", "Patanol", "Patanol", "Pazeo", "Pazeo", "Retaine Allergy", "Ryaltris", "Ryaltris", "Sandoz Olopatadine", "Sandoz Olopatadine 0.2%", "Teva-olopatadine" ]

[ "Alchek", "Alerchek", "Allelock", "Patanol S" ]

[ "Ryaltris", "Ryaltris" ]

[ "P35367", "P25021", "Q9Y5N1", "P23297", "P80511", "P04271", "Q99584", "P29034" ]

[ "P08684", "Q01740", "P31513" ]

[ "P02768" ]

[ "P08183" ]

DB00769

Hydrocortamate

Hydrocortamate is a synthetic glucocorticoid used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects.

solid

Used topically as an antiinflammatory in the treatment of steroid-responsive dermatoses

Hydrocortamate is a synthetic glucocorticoid used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.

Hydrocortamate binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.

null

Primarily hepatic via CYP3A4

Side effects include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria.

null

Organic compounds

Lipids and lipid-like molecules

Steroids and steroid derivatives

Pregnane steroids

[ "approved" ]

[]

[ "Humans and other mammals" ]

[]

[]

[ "Etacort", "Magnacort", "Ulcort", "Ulcort top" ]

[]

[ "P04150" ]

[ "P08684" ]

[]

DB00770

Alprostadil

Alprostadil is a chemically-identical synthetic form of prostaglandin E1 (PGE1), a potent vasodilator produced endogenously. In 1996, the FDA approved the use of alprostadil, administered either with an intracavernosal injection or an intraurethral suppository, for the treatment of erectile dysfunction, and it is used in men for whom oral treatment is either contraindicated or ineffective. After administration, alprostadil promotes smooth muscle relaxation of the corpus cavernosal.[A257068,A257088] Alprostadil is also used in neonatal patients with congenital heart defects that depend on a patent ductus for survival until corrective or palliative surgery can be performed. This drug causes vasodilation by directly affecting vascular and ductus arteriosus (DA) smooth muscle, preventing or reversing the functional closure of the DA that occurs shortly after birth. This results in increased pulmonary or systemic blood flow in infants.[A34474,L45038,L45063]

solid

Alprostadil is indicated for palliative, not definitive, therapy to temporarily maintain the patency of the ductus arteriosus until corrective or palliative surgery can be performed in neonates who have congenital heart defects and who depend upon the patent ductus for survival.[L45038] It is also indicated for the treatment of erectile dysfunction due to neurogenic, vasculogenic, psychogenic, or mixed etiology,[L45028,L45033] and as an adjunct to other diagnostic tests in the diagnosis of erectile dysfunction.[L45028]

Prostaglandin E1 is produced endogenously to relax vascular smooth muscle and cause vasodilation. As a synthetic form of prostaglandin E1, alprostadil has the same pharmacodynamic effects.[A257068] Alprostadil inhibits platelet aggregation, has anti-inflammatory effects, interferes with immune responses, and stimulates factor X, a blood coagulation enzyme.[A34470] In adult males, the use of alprostadil may lead to prolonged erection and priapism, penile fibrosis, hypotension, and injection site bleeding.[L45028] In patients treated up to 24 months with alprostadil, the incidence of prolonged erections (>4 hours long) was 4% of all, and the incidence of priapism (erections greater than 6 hours in duration) was <1%.[L45033] Patients with preexisting cardiovascular disease treated with alprostadil may also have higher cardiac risk.[L45028] Neonates with congenital heart defects treated with alprostadil may experience apnea. Apnea is experienced by 10-12% of neonates and is more common in those weighing less than 2 kg at birth. The administration of alprostadil to neonates may also result in gastric outlet obstruction secondary to antral hyperplasia.[L45038]

Alprostadil is a smooth muscle relaxant that promotes vasodilation and platelet aggregation inhibition. In neonatal patients with ductus arteriosus patency, alprostadil relaxes the ductus arteriosus (DA) smooth muscle, preventing or reversing the functional closure of the DA that occurs shortly after birth. This results in increased pulmonary or systemic blood flow in infants. Alprostadil appears to be most effective within 96 hours after birth since the DA rapidly loses its responsiveness to alprostadil.[L45063] When administered by intracavernosal injection or as an intraurethral suppository, alprostadil acts locally to relax the trabecular smooth muscle of the corpora cavernosa and the cavernosal arteries. Swelling, elongation, and rigidity of the penis result when arterial blood rapidly flows into the corpus cavernosum to expand the lacunar spaces. The entrapped blood reduces the venous blood outflow as sinusoids compress against the tunica albuginea leading to penile rigidity. This is referred to as the corporal veno-occlusive mechanism.[A257073,L45033,L45068]

In patients with erectile dysfunction given 20 μg of alprostadil intracavernously, the systemic plasma concentrations of prostaglandin E1 increased from a baseline of 0.8 pg/mL to a Cmax of 16.8 pg/mL (corrected for baseline). The tmax and AUC for this group of patients were 4.8 min and 173 pg⋅min/mL, respectively.[L45033] In patients given 20 μg of alprostadil intravenously, AUC was similar to the one detected in patients that received alprostadil intracavernously (174 pg⋅min/mL); however, they had a higher tmax (25.5 min) and a lower Cmax (7.09 pg/mL). Compared to the same dose given by a short-term intravenous infusion, the absolute bioavailability of alprostadil estimated from systemic exposure was about 98%.[L45033]

Alprostadil is rapidly metabolized in the human body. Following intracavernous administration, alprostadil is metabolized in the corpus cavernosum, and a smaller portion is absorbed from the penis into systemic circulation.[L45033] After intravenous or arterial administration, alprostadil is metabolized and distributed throughout the entire body except for the central nervous system.[L45063] As much as 60-90% of the circulating alprostadil may be metabolized in the lungs through first-pass pulmonary elimination, in a process known as beta- and omega-oxidation.[L45033] The enzymatic oxidation of the C15-hydroxy group of alprostadil leads to the formation of 15-keto-PGE1, while the reduction of the C13, 14-double bond produces 15-keto-PGE0, and 13,14-dihydro-PGE1 (PGE0). The 15-keto metabolites are inactive, but the PGE0 metabolite has a similar potency to alprostadil in isolated animal organs.[L45033] The major metabolite of alprostadil is 15-keto-PGE0.[A257068]

In neonatal patients given alprostadil intravenously, apnea, bradycardia, pyrexia, hypotension, and flushing may be signs of drug overdosage. In patients with apnea or bradycardia, discontinue the infusion, and provide appropriate medical treatment. Caution should be used in restarting the infusion. In patients with pyrexia or hypotension, reduce the infusion rate until these symptoms subside. Flushing is usually a result of incorrect intraarterial catheter placement, and the catheter should be repositioned.[L45038] For patients given alprostadil intracavernosally for the treatment of erectile dysfunction, there is limited data on overdosage. Systemic reactions are uncommon with the intracavernous use of alprostadil, and hypotension occurrs in less than 1% of patients treated with this drug. A prolonged erection or priapism is the main symptom of an alprostadil overdose in this group of patients. Erections lasting more than 6 hours should be treated due to the potential for tissue hypoxia and possible necrosis. In the event of an intracavernous overdose, the patient is strongly encouraged to go to the nearest emergency room if his personal physician is not available. Supportive therapy according to the presence of other symptoms is recommended.[L45028,L45033] The oral LD50 of alprostadil in mice and rats is 186 mg/kg and 228 mg/kg, respectively.[L45043,L45073]

In healthy adults and neonates given a single intravenous dose of alprostadil, half-life goes from 5 to 10 minutes.[L45063]

Alprostadil is bound in plasma primarily to albumin (81% bound) and, to a lesser extent, alpha-globulin IV-4 fraction (55% bound).[L45028]

Following the degradation of alprostadil by beta- and omega-oxidation, metabolites are excreted primarily by the kidney, and excretion is essentially complete within 24 hours after administration (92%).[L45063] Approximately 88% and 12% of alprostadil metabolites are excreted through urine and feces, respectively, over 72 hours. Alprostadil and its metabolites are not retained in tissues, and unchanged alprostadil has not been detected in urine.[L45033,L45063]

The volume of distribution of alprostadil has yet to be determined.[L45028]

In patients with erectile dysfunction given an intravenous infusion of alprostadil (20 μg), the total body clearance was 115 L/min.[L45033]

null

[ "approved", "investigational" ]

[ "C01EA", "C01E", "C01", "C", "G04BE", "G04B", "G04", "G" ]

[ "Humans and other mammals" ]

[ { "cost": "29.39", "description": "Muse 125 mcg urethral suppository", "unit": "suppository" }, { "cost": "30.56", "description": "Muse 125 mcg Pellets", "unit": "pellet" }, { "cost": "30.76", "description": "Muse 250 mcg urethral suppository", "unit": "suppository" }, { "cost": "31.99", "description": "Muse 250 mcg Pellets", "unit": "pellet" }, { "cost": "32.92", "description": "Muse 500 mcg urethral suppository", "unit": "suppository" }, { "cost": "34.23", "description": "Muse 500 mcg Pellets", "unit": "pellet" }, { "cost": "35.54", "description": "Muse 1000 mcg urethral suppository", "unit": "suppository" }, { "cost": "36.23", "description": "Caverject impulse 10 mcg kit", "unit": "each" }, { "cost": "36.97", "description": "Muse 1000 mcg Pellets", "unit": "pellet" }, { "cost": "37.51", "description": "Caverject Impulse 1 Box = 2 Blister Trays, 10 mcg", "unit": "box" }, { "cost": "46.66", "description": "Caverject impulse 20 mcg kit", "unit": "each" }, { "cost": "47.77", "description": "Caverject Impulse 1 Box = 2 Blister Trays, 20 mcg", "unit": "box" }, { "cost": "66.0", "description": "Alprostadil 500 mcg/ml vial", "unit": "ml" }, { "cost": "74.88", "description": "Edex 10 mcg cartridge kit", "unit": "kit" }, { "cost": "77.22", "description": "Edex Cartridge 2 Pack 10 mcg Kit Box", "unit": "box" }, { "cost": "96.47", "description": "Edex 20 mcg cartridge kit", "unit": "kit" }, { "cost": "97.47", "description": "Edex 2 Pack 20 mcg Kit Box", "unit": "box" }, { "cost": "108.0", "description": "Prostin vr 500 mcg/ml ampul", "unit": "ml" }, { "cost": "132.18", "description": "Edex 40 mcg cartridge kit", "unit": "kit" }, { "cost": "135.23", "description": "Edex Cartridge 2 Pack 40 mcg Kit Box", "unit": "box" }, { "cost": "233.65", "description": "Edex Cartridge 6 Pack 10 mcg Kit Box", "unit": "box" }, { "cost": "266.72", "description": "Prostin Vr 500 mcg/ml", "unit": "ml" }, { "cost": "272.05", "description": "Caverject 6 20 mcg Solution, 1 Box Contains 6 Vials Box", "unit": "box" }, { "cost": "301.0", "description": "Edex 6 Pack 20 mcg Kit Box", "unit": "box" }, { "cost": "341.78", "description": "Caverject 6 40 mcg Solution Box", "unit": "box" }, { "cost": "412.4", "description": "Edex Cartridge 6 Pack 40 mcg Kit Box", "unit": "box" }, { "cost": "5049.0", "description": "Alprostadil powder", "unit": "g" } ]

[ { "approved": "1998-06-30", "country": "United States", "expires": "2010-04-25", "number": "5773020" }, { "approved": "1995-04-25", "country": "Canada", "expires": "2012-04-25", "number": "1335346" }, { "approved": "1999-03-23", "country": "United States", "expires": "2016-03-23", "number": "5886039" } ]

[ "Alprostadil", "Alprostadil", "Alprostadil", "Alprostadil", "Alprostadil Injection USP", "Alprostadil Injection, USP", "Caverject", "Caverject", "Caverject", "Caverject", "Caverject Impulse", "Caverject Impulse", "Caverject Impulse", "Caverject Impulse", "Caverject Impulse", "Caverject Sterile Powder", "Caverject Sterile Powder - Kit 11.9mcg /vial", "Caverject Sterile Powder - Pws 11.9mcg/vial", "Caverject Sterile Powder - Pws 23.2mcg/vial", "Edex", "Edex", "Edex", "Edex", "Edex", "Edex", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Muse", "Prostin Vr Pediatric", "Prostin Vr Pediatric", "Prostin Vr Sterile Solution", "Vitaros", "Vitaros" ]

[ "Alista", "Alprostan", "Alprostapint", "Alprostar", "Alprostin", "Alprox-TD", "Altesil", "Alyprost", "Apistandin", "Aplicav", "Befar", "Bolesi", "Bondil", "Cardiobron", "Caverject DC", "Caverject Dual", "Eglandin", "Femprox", "Kai Tong", "Kaishi", "Karon", "Liple", "Minprog", "Palux", "Pridax", "Prink", "Prolisina VR", "Prostandin", "Prostavasin", "Prostin VR", "Prostivas", "Sugiran", "Tandetron", "Topiglan", "Vasaprostan", "Vasoprost", "Vasostenoon", "Viridal" ]

[ "Caverject Sterile Powder - Kit 11.9mcg /vial" ]

[ "P21731", "P34995", "P43116", "P43115", "P35408", "Q9Y5Y4" ]

[ "P15428" ]

[ "P02768" ]

[ "O15439", "O15440", "Q92959", "Q9UIG8", "O94956", "Q4U2R8" ]

DB00771

Clidinium

Clidinium is a synthetic anticholinergic agent which has been shown in experimental and clinical studies to have a pronounced antispasmodic and antisecretory effect on the gastrointestinal tract. It inhibits muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.

solid

For the treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome. In combination with chlordiazepoxide, clidinium is indicated to control emotional and somatic factors in gastrointestinal disorders, and is used as adjunctive therapy in the treatment of peptic ulcer, irritable bowel syndrome and acute enterocolitis.[L44893]

Clidinium is a synthetic anticholinergic agent which has been shown in experimental and clinical studies to have a pronounced antispasmodic and antisecretory effect on the gastrointestinal tract.

Inhibits muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites primarily by inhibiting the M1 muscarinic receptors.

null

Signs of toxicity include confusion, paralytic ileus, urinary hesitancy/retention, and blurred vision.

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

Diphenylmethanes

[ "approved" ]

[ "A03CA", "A03C", "A03", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "0.23", "description": "Quarzan 2.5 mg capsule", "unit": "capsule" }, { "cost": "0.3", "description": "Quarzan 5 mg capsule", "unit": "capsule" } ]

[]

[ "Chlorax", "Chlordiazepoxide Clidinium", "Chlordiazepoxide HCl and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "CHLORDIAZEPOXIDE HYDROCHLORIDE and CLIDINIUM BROMIDE", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride And Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "CHLORDIAZEPOXIDE HYDROCHLORIDE and CLIDINIUM BROMIDE", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride And Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide hydrochloride and clidinium bromide", "Chlordiazepoxide hydrochloride and clidinium bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Corium Cap", "Librax", "Librax", "Not applicable", "Nu-chlorax Capsules USP", "Pro Chlorax" ]

[ "Dolibrax", "Porsucon", "Quarzan", "Sedaspa" ]

[ "Chlordiazepoxide Clidinium", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "CHLORDIAZEPOXIDE HYDROCHLORIDE and CLIDINIUM BROMIDE", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride And Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "CHLORDIAZEPOXIDE HYDROCHLORIDE and CLIDINIUM BROMIDE", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Librax", "Chlordiazepoxide Hydrochloride And Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Not applicable", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride/Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlorax", "Librax", "Corium Cap", "Pro Chlorax", "Nu-chlorax Capsules USP", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide HCl and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide hydrochloride and clidinium bromide", "Chlordiazepoxide hydrochloride and clidinium bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide", "Chlordiazepoxide Hydrochloride and Clidinium Bromide" ]

[ "P11229" ]

[]

DB00772

Malathion

Malathion is a parasympathomimetic organophosphate compound that is used as an insecticide for the treatment of head lice. Malathion is an irreversible cholinesterase inhibitor and has low human toxicity.

liquid

For patients infected with Pediculus humanus capitis (head lice and their ova) of the scalp hair.

Malathion is an organophosphate insecticide commonly used to control mosquitos and other flying insects. Pharmaceutically, malathion is used to eliminate head lice. The principal toxicological effect of malathion is cholinesterase inhibition, due primarily to malaoxon and to phosphorus thionate impurities.

Malathion is a nonsystemic, wide-spectrum organophosphate insecticide. It inhibits acetylcholinesterase activity of most eukaryotes. Malathion is toxic to aquatic organisms, but has a relatively low toxicity for birds and mammals. The major metabolites of malathion are mono- and di-carboxylic acid derivatives, and malaoxon is a minor metabolite. However, it is malaoxon that is the strongest cholinesterase inhibitor. Cholinesterases catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxins, causing muscle spasms and ultimately death.

Malathion in an acetone vehicle has been reported to be absorbed through normal human skin only to the extent of 8% of the applied dose. Absorption may be increased when malathion is applied to damaged skin. Malathion is rapidly and effectively absorbed by practically all routes including the gastrointestinal tract, skin, mucous membranes, and lungs. However, it is readily excreted in the urine, and does not accumulate in organs or tissues.

The major metabolites of malathion are the diacid and monoacid metabolites, namely, malathion dicarboxylic acid (DCA) and malathion monocarboxylic acid (MCA). Malaoxon, the active cholinesterase-inhibiting metabolite of malathion, is a minor metabolite. Both malathion and malaoxon are detoxified by carboxyesterases leading to polar, water-soluble compounds that are excreted.

Malathion is slightly toxic via the oral route, with reported oral LD50 values of 1000 mg/kg to greater than 10,000 mg/kg in the rat. It is also slightly toxic via the dermal route, with reported dermal LD50 values of greater than 4000 mg/kg in rats. Moderate poisoning can result in chest tightness, difficulty breathing, bradycardia, tachycardia, tremor/ataxia, blurred vision, and confusion. Severe, life-threatening signs include coma, seizures, respiratory arrest, and paralysis. Malathion may also be irritating to the skin and eyes.

8-24 hours

null

Organic compounds

Lipids and lipid-like molecules

Fatty Acyls

Fatty acid esters

[ "approved", "investigational" ]

[ "P03AX", "P03A", "P03", "P" ]

[ "Head lice" ]

[ { "cost": "2.65", "description": "Malathion 0.5% lotion", "unit": "ml" }, { "cost": "2.95", "description": "Ovide 0.5% lotion", "unit": "ml" }, { "cost": "180.8", "description": "Ovide 0.5% Lotion 59ml Bottle", "unit": "bottle" } ]

[ { "approved": "2009-07-14", "country": "United States", "expires": "2027-02-01", "number": "7560445" }, { "approved": "2011-07-12", "country": "United States", "expires": "2026-08-14", "number": "7977324" } ]

[ "Malathion", "Malathion", "Malathion", "Malathion", "Malathion lotion, 0.5%", "Ovide", "Ovide" ]

[ "Derbac-M", "Noury", "Prioderm" ]

[]

[ "P06276", "P22303" ]

[ "P05177", "P20813" ]

[]

DB00773

Etoposide

A semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle.

solid

For use in combination with other chemotherapeutic agents in the treatment of refractory testicular tumors and as first line treatment in patients with small cell lung cancer. Also used to treat other malignancies such as lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme.

Etoposide is an antineoplastic agent and an epipodophyllotoxin (a semisynthetic derivative of the podophyllotoxins). It inhibits DNA topoisomerase II, thereby ultimately inhibiting DNA synthesis. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases. Two different dose-dependent responses are seen. At high concentrations (10 µg/mL or more), lysis of cells entering mitosis is observed. At low concentrations (0.3 to 10 µg/mL), cells are inhibited from entering prophase. It does not interfere with microtubular assembly. The predominant macromolecular effect of etoposide appears to be the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals.

Etoposide inhibits DNA topoisomerase II, thereby inhibiting DNA re-ligation. This causes critical errors in DNA synthesis at the premitotic stage of cell division and can lead to apoptosis of the cancer cell. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases of cell division. Inhibition of the topoisomerase II alpha isoform results in the anti-tumour activity of etoposide. The drug is also capable of inhibiting the beta isoform but inhibition of this target is not associated with the anti-tumour activity. It is instead associated with the carcinogenic effect.

Absorbed well, time to peak plasma concentration is 1-1.5 hrs. Mean bioavailability is 50% (range of 25% - 75%). Cmax and AUC values for orally administered etoposide capsules display intra- and inter-subject variability. There is no evidence of first-pass effect for etoposide.

Primarily hepatic (through O-demethylation via the CYP450 3A4 isoenzyme pathway) with 40% excreted unchanged in the urine. Etoposide also undergoes glutathione and glucuronide conjugation which are catalyzed by GSTT1/GSTP1 and UGT1A1, respectively. Prostaglandin synthases are also responsible for the conversion of etoposide to O-demethylated metabolites (quinone).

Side effects include alopecia, constipation, diarrhea, nausea and vomiting and secondary malignancies (leukemia).

4-11 hours

97% protein bound.

Etoposide is cleared by both renal and nonrenal processes, i.e., metabolism and biliary excretion. Glucuronide and/or sulfate conjugates of etoposide are also excreted in human urine. Biliary excretion of unchanged drug and/or metabolites is an important route of etoposide elimination as fecal recovery of radioactivity is 44% of the intravenous dose. 56% of the dose was in the urine, 45% of which was excreted as etoposide.

The disposition of etoposide is a biphasic process with a distribution half-life of 1.5 hours. It does not cross into cerebrospinal fluid well. Volume of distribution, steady state = 18 - 29 L.

* Total body clearance = 33 - 48 mL/min [IV administration, adults] * Mean renal clearance = 7 - 10 mL/min/m^2

Organic compounds

Lignans, neolignans and related compounds

Lignan lactones

Podophyllotoxins

[ "approved" ]

[ "L01CB", "L01C", "L01", "L" ]

[ "Humans and other mammals" ]

[ { "cost": "1.06", "description": "Toposar 500 mg/25 ml vial", "unit": "ml" }, { "cost": "1.12", "description": "Toposar 1000 mg/50 ml vial", "unit": "ml" }, { "cost": "2.25", "description": "Toposar 100 mg/5 ml vial", "unit": "ml" }, { "cost": "28.89", "description": "Etoposide 100 mg/5 ml vial", "unit": "ml" }, { "cost": "47.64", "description": "Etoposide 50 mg capsule", "unit": "capsule" }, { "cost": "159.55", "description": "Etopophos 100 mg vial", "unit": "vial" }, { "cost": "1273.41", "description": "VePesid 20 50 mg capsule Box", "unit": "box" } ]

[]

[ "Dom-etoposide", "Eposin", "Etopophos", "Etopophos", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide", "Etoposide - Liq IV 20mg/ml", "Etoposide Injection", "Etoposide Injection", "Etoposide Injection", "Etoposide Injection USP", "Etoposide Injection, USP", "Etoposide Injection, USP", "PMS-etoposide", "Toposar", "Toposar", "Toposar", "VePesid", "VePesid", "VePesid", "VePesid", "VePesid", "VePesid", "Vepesid Inj 20mg/ml" ]

[ "Etopofos", "Lastet", "Nexvep", "Vepesid K", "Vépéside" ]

[]

[ "P11388", "Q02880" ]

[ "P05177", "P05181", "P20815", "P22309", "P30711", "P09211", "P35354", "P23219", "P08684" ]

[]

[ "O15438", "O95255", "P08183", "P33527", "Q5T3U5", "Q92887", "Q9UNQ0" ]

DB00775

Tirofiban

Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.

solid

For treatment, in combination with heparin, of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy.

Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation. When administered intravenously, tirofiban inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. When given according to the recommended regimen, >90% inhibition is attained by the end of the 30-minute infusion. Tirofiban has been recently shown in patients with unstable angina to reduce ischemic events at 48 hours following infusion when compared to standard heparin therapy.

Tirofiban is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban.

null

Metabolism appears to be limited.

null

2 hours

65%

It is cleared from the plasma largely by renal excretion, with about 65% of an administered dose appearing in urine and about 25% in feces, both largely as unchanged tirofiban.

* 22 to 42 L

* 213 - 314 mL/min [Healthy subjects] * 152 - 267 mL/min [patients with coronary artery disease]

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved" ]

[ "B01AC", "B01A", "B01", "B" ]

[ "Humans and other mammals" ]

[ { "cost": "10.62", "description": "Aggrastat 250 mcg/ml vial", "unit": "ml" } ]

[ { "approved": "1997-08-19", "country": "United States", "expires": "2010-09-27", "number": "5658929" }, { "approved": "2000-02-08", "country": "Canada", "expires": "2016-10-23", "number": "2234364" }, { "approved": "1998-05-26", "country": "Canada", "expires": "2011-09-23", "number": "2052073" }, { "approved": "2004-08-03", "country": "United States", "expires": "2023-05-01", "number": "6770660" }, { "approved": "1999-10-12", "country": "United States", "expires": "2016-10-23", "number": "5965581" }, { "approved": "1999-11-02", "country": "United States", "expires": "2017-10-08", "number": "5978698" }, { "approved": "1998-03-31", "country": "United States", "expires": "2016-10-23", "number": "5733919" }, { "approved": "1999-10-26", "country": "United States", "expires": "2016-10-23", "number": "5972967" }, { "approved": "2000-10-24", "country": "United States", "expires": "2019-01-29", "number": "6136794" } ]

[ "Aggrastat", "Aggrastat", "Aggrastat", "Aggrastat", "Aggrastat", "Aggrastat", "Tirofiban", "Tirofiban", "Tirofiban Hydrochloride", "Tirofiban hydrochloride", "Tirofiban Hydrochloride", "Tirofiban Hydrochloride", "Tirofiban Hydrochloride", "Tirofiban Hydrochloride" ]

[ "Aggribloc", "Agrastat" ]

[]

[ "P08514", "P05106" ]

[]

DB00777

Propiomazine

Propiomazine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, propiomazine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.

solid

Propiomazine is largely used for its antihistamininc sleep inducing effects in treating insomnia.

Although propiomazine is a phenothiazine, it is not used as an antipsychotic. It posesses antihistamine effects and is mostly used as a sedative in treating insomnia.

Propiomazine acts as an antagonist of dopamine 1, 2, and 4 receptors, serotonin (5-HT) receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Its main use as a sedative is due to its antihistamine effect.

null

Unknown, but most likely hepatic as with other phenothiazines.

Although rare, serious adverse events may be seen with propiomazine. Such events include convulsions (seizures), difficult or unusually fast breathing, fast or irregular heartbeat or pulse, fever (high), high or low blood pressure, loss of bladder control, muscle stiffness (severe), unusual increase in sweating, unusually pale skin, and unusual tiredness or weakness.

null

81%

null

Organic compounds

Organoheterocyclic compounds

Benzothiazines

Phenothiazines

[ "approved" ]

[ "N05CM", "N05C", "N05", "N" ]

[ "Humans and other mammals" ]

[]

[]

[ "Dorevan", "Dorevane", "Indorm", "Largon", "Propavan", "Serentin" ]

[]

[ "P35367", "P11229", "P08172", "P20309", "P08173", "P08912", "P35348", "P14416", "P28223", "P28335" ]

[]

DB00779

Nalidixic acid

Nalidixic acid is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase.

solid

For the treatment of urinary tract infections caused by susceptible gram-negative microorganisms, including the majority of E. Coli, Enterobacter species, Klebsiella species, and Proteus species.

Nalidixic acid is a quinolone antibacterial agent for oral administration. Nalidixic acid has marked antibacterial activity against gram-negative bacteria including Enterobacter species, Escherichia coli, Morganella Morganii; Proteus Mirabilis, Proteus vulgaris, and Providencia rettgeri. Pseudomonas species are generally resistant to the drug. Nalidixic acid is bactericidal and is effective over the entire urinary pH range. Conventional chromosomal resistance to nalidixic acid taken in full dosage has been reported to emerge in approximately 2 to 14 percent of patients during treatment; however, bacterial resistance to nalidixic acid has not been shown to be transferable via R factor.

Evidence exists for Nalidixic acid that its active metabolite, hydroxynalidixic acid, binds strongly, but reversibly, to DNA, interfering with synthesis of RNA and, consequently, with protein synthesis.

Following oral administration, nalidixic acid is rapidly absorbed from the gastrointestinal tract. Bioavailability is approximately 96%. Absorption may be delayed if taken with antacids.

Hepatic. 30% of administered dose is metabolized to the active metabolite, hydroxynalidixic acid. Rapid conjugation of parent drug and active metabolite to inactive metabolites. Metabolism may vary widely among individuals. In the urine, hydroxynalidixic acid represents 80 to 85% of the antibacterial activity.

ORAL (LD50): Acute: 1160 mg/kg [Rat]. 572 mg/kg [Mouse]. Toxic psychosis, convulsions, increased intracranial pressure, or metabolic acidosis may occur in patients taking more than the recommended dosage. Vomiting, nausea, and lethargy may also occur following overdosage.

1.1 to 2.5 hours in healthy adult patients, and up to 21 hours in patients with impaired renal function.

Nalidixic acid is 93% bound to protein in the blood, and the active metabolite, hydroxynalidixic acid is 63% bound.

Following oral administration, NegGram is rapidly absorbed from the gastrointestinal tract, partially metabolized in the liver, and rapidly excreted through the kidneys. Approximately four percent of NegGram is excreted in the feces.

null

Organic compounds

Organoheterocyclic compounds

Diazanaphthalenes

Naphthyridines

[ "approved", "investigational" ]

[ "J01MB", "J01M", "J01", "J" ]

[ "Enteric bacteria and other eubacteria" ]

[ { "cost": "7.2", "description": "Nalidixic acid powder", "unit": "g" } ]

[]

[ "NegGram", "NegGram" ]

[ "Adix", "Curiemylon", "Degram", "Delugi", "Dixicon", "Glanega", "Gramazine", "Gramoneg", "Huei Yi", "Lisalenb", "Litalon", "Nadixin", "Nadon", "Nagomin", "Nal-acid", "Nalic", "Nalicid", "Nalid", "Nalidin", "Nalidix", "Naligram", "Nalitomylon", "Nalix", "Nalixid", "Nalixin", "Nebactil", "Negachine", "Nevigramon", "Unaserus", "Wintomylon", "Wintorin", "Youdix", "Zuno-Nathasid" ]

[]

[ "Q02880", "P11388" ]

[ "P48775", "P05177" ]

[]

[ "Q4U2R8" ]

DB00780

Phenelzine

Phenelzine, with the formula β-phenylethylhydrazine, is a monoamine oxidase inhibiting antidepressant that is effective in the treatment of panic disorder and social anxiety disorder.[A15753] It was developed by Parke Davis and originally FDA approved on June 9th, 1961. It is currently approved under prescription by the name of Nardil.

liquid

Phenelzine is indicated for the treatment of nonendogenous, neurotic or atypical depression for patients that do not tolerate other forms of therapy.[L1356] Atypical depression has a high prevalence rate, starts in early life, tends to last longer, is more likely to occur in people with bipolar disorder, has a high comorbidity with anxiety disorder and carries more risk of suicidal behavior. It is important to specify the atypical feature to predict the clinical course of depression and hence generate the best treatment and service. The featuring symptoms of the atypical feature include mood reactivity, two or more of this symptoms: 1) increased appetite, 2) increased sleep, 3) leaden paralysis and 4) interpersonal rejection sensitivity and should not have melancholic or catatonic features of depression.[A31917] Neurotic depression is a depression of an emotionally unstable person. It is a secondary condition to major personality disorder, neuroses and drug use disorders. Likewise, a primary depression with a family history of depression spectrum disease would fit in this category.[A31922] A nonendogenous depression is characterized by a disturbance in mood and general outlook. The physical symptoms tend to be less severe and it often occurs in response to stressful life events that keep occurring over a large period of time generating a continuous stress in the daily living.[A31924]

The elimination of monoamine oxidase by phenelzine results in the elevation of brain amines such as 2-phenylethylamine which is a metabolite of phenelzine. These amines have then marked effects on the uptake and release of catecholamines and serotonin in nerve endings.[A31925] Phenelzine is shown to elevate brain levels of the gamma-aminobutyric acid (GABA) and alanine (ALA) as well as to inhibit the activity of the transaminases that normally metabolize these amino acids. In preclinical studies, it has been shown to be neuroprotective in cerebral ischemia.[A15753]

The basic mechanism of action of phenelzine acts as an inhibitor and substrate of monoamine oxidase which subsequently causes an elevation in brain levels of catecholamines and serotonin. It also presents a similar structure to amphetamine which explains the effect on the uptake and release of dopamine, noradrenaline, and serotonin. Phenelzine has been reported to inhibit tyrosine aminotransferase, aromatic amino acid decarboxylase, and dopamine B-hydroxylase.[A31925]

Phenelzine is rapidly absorbed from the gastrointestinal tract. The decay of the drug action is not dependent on the pharmacokinetic parameters but on the rate of protein synthesis which restores the functional levels of monoamine oxidase.[L1365] The mean Cmax is 19.8 ng/ml and it occurs after 43 minutes of dose administration.[FDA label]

For the metabolic studies, it is assumed that phenelzine is acetylated. Some of the metabolites of phenelzine are phenylacetic acid, 2-phenylethylamine and 4-hydroxyphenylacetic acid as major metabolites and N-acetyl-phenelzine as a minor metabolite.[A31925]

Phenelzine, as must of the monoamine oxidase inhibitors, can cause transient, mild and asymptomatic aminotransferase elevations. It has also been reported to be associated with cases of liver injury after 1-3 months of treatment.[A31929]

After administration phenelzine presents a very short half-life of 11.6 hours in humans.[L1365]

Unchanged phenelzine presents a high protein binding which reduced its bioavailability.[T114]

The elimination of the administered dose is mainly composed of the phenelzine metabolites, phenylacetic acid and parahydroxyphenylacetic acid that constitute 79% of the dose found in the urine in the first 96 hours.[A31928]

The volume of distribution of phenelzine is hard to determine as drugs from this kind penetrate the CNS very well into the tissue where their activity is desired.[T113]

null

Organic compounds

Benzenoids

Benzene and substituted derivatives

null

[ "approved" ]

[ "N06AF", "N06A", "N06", "N" ]

[ "Humans and other mammals" ]

[ { "cost": "51.0", "description": "Phenelzine sulfate powder", "unit": "g" }, { "cost": "0.39", "description": "Nardil 15 mg Tablet", "unit": "tablet" }, { "cost": "0.95", "description": "Nardil 15 mg tablet", "unit": "tablet" } ]

[]

[ "Greenstone Brand Phenelzine Sulfate", "Nardil", "Nardil", "Nardil Phenelzine Sulfate", "Phenelzine Sulfate", "Phenelzine Sulfate", "Phenelzine Sulfate", "Phenelzine Sulfate" ]

[ "Margyl", "Nardelzine" ]

[]

[ "P21397", "P27338", "Q16853", "P80404", "P24298", "Q8TD30", "Q9UGI5" ]

[ "P33261", "P10632", "P08684", "P20815", "P24462", "P10635", "P08684", "Q9HB55", "P20815", "P24462", "P21397", "P27338", "P05181" ]

[]

DB00782

Propantheline

A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.

solid

For the treatment of enuresis. It has also been used for hyperhidrosis, and cramps or spasms of the stomach, intestines or bladder.

Propantheline is an anticholinergic drug, a medication that reduces the effect of acetylcholine, a chemical released from nerves that stimulates muscles, by blocking the receptors for acetylcholine on smooth muscle (a type of muscle). It also has a direct relaxing effect on smooth muscle. Propantheline is used to treat or prevent spasm in the muscles of the gastrointestinal tract in the irritable bowel syndrome. In addition, Propantheline inhibits gastrointestinal propulsive motility and decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretions.

Action is achieved via a dual mechanism: (1) a specific anticholinergic effect (antimuscarinic) at the acetylcholine-receptor sites and (2) a direct effect upon smooth muscle (musculotropic).

null

Approximately 70% of the dose is excreted in the urine, mostly as metabolites.

null

Organic compounds

Organoheterocyclic compounds

Benzopyrans

1-benzopyrans

[ "approved" ]

[ "A03AB", "A03A", "A03", "A", "A03CA", "A03C", "A03", "A" ]

[ "Humans and other mammals" ]

[ { "cost": "7.77", "description": "Propantheline bromide powder", "unit": "g" }, { "cost": "0.6", "description": "Propantheline 15 mg tablet", "unit": "tablet" }, { "cost": "0.76", "description": "Propantheline Bromide 15 mg tablet", "unit": "tablet" } ]

[]

Propantheline

[ "Pro-Banthine", "Pro-Banthine", "Pro-banthine Tablets 15mg", "Pro-banthine Tablets 7.5 mg", "Propanthel Tab 15mg", "Propantheline Bromide" ]

[ "Ercoril", "Methaphyllin", "Pro Banthine", "Prokind", "Propanline", "Propantheline", "Spastheline" ]

[]

[ "P11229" ]

[]

DB00785

Cryptenamine

Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects. Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known.

solid

For the treatment of hypertension.

Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects.

Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known. Some evidence has suggested that cryptenamine acts in a similar fashion to atropine, which lowers the "rest and digest" activity of all muscles and glands regulated by the parasympathetic nervous system. This occurs because atropine is a competitive inhibitor of the muscarinic acetylcholine receptors (acetylcholine is the neurotransmitter used by the parasympathetic nervous system). Therefore muscarinic acetylcholine receptors will be listed as experimental targets for cryptenamine.

null

[ "approved" ]

[]

[ "Humans and other mammals" ]

[]

[]

[ "Unitensen" ]

[]

[ "P08172", "P08588", "P07550", "P13945" ]

[]

DB00786

Marimastat

Used in the treatment of cancer, Marmiastat is an angiogenesis and metastasis inhibitor. As an angiogenesis inhibitor it limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.

solid

For the treatment of various cancers

Used in the treatment of cancer, it is an angiogenesis and metastasis inhibitor. As an angiogenesis inhibitor it limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.

Marimastat is a broad spectrum matrix metalloprotease inhibitor. It mimics the peptide structure of natural MMP substrates and binds to matrix metalloproteases, thereby preventing the degradation of the basement membrane by these proteases. This antiprotease action prevents the migration of endothelial cells needed to form new blood vessels. Inhibition of MMPs also prevents the entry and exit of tumor cells into existing blood cells, thereby preventing metastasis.

null

Organic compounds

Organic oxygen compounds

Organooxygen compounds

Alcohols and polyols

[ "investigational" ]

[]

[ "Humans and other mammals" ]

[]

Marimastat | 3.4.24.7 | CLG | Fibroblast collagenase | Matrix metalloproteinase-1 | MMP-1 | 3.4.24.24 | 72 kDa gelatinase | CLG4A | Gelatinase A | Matrix metalloproteinase-2 | MMP-2 | TBE-1 | 3.4.24.17 | Matrix metalloproteinase-3 | MMP-3 | SL-1 | STMY1 | Transin-1 | 3.4.24.23 | Matrin | Matrix metalloproteinase-7 | MMP-7 | MPSL1 | Pump-1 protease | PUMP1 | Uterine metalloproteinase | 3.4.24.34 | CLG1 | Matrix metalloproteinase-8 | MMP-8 | PMNL collagenase | PMNL-CL | 3.4.24.35 | 92 kDa gelatinase | 92 kDa type IV collagenase | CLG4B | Gelatinase B | GELB | MMP-9 | 3.4.24.22 | Matrix metalloproteinase-10 | MMP-10 | SL-2 | STMY2 | Transin-2 | 3.4.24.- | Matrix metalloproteinase-11 | MMP-11 | SL-3 | ST3 | STMY3 | 3.4.24.65 | HME | Macrophage elastase | Matrix metalloproteinase-12 | ME | MME | MMP-12 | 3.4.24.- | Matrix metalloproteinase-13 | MMP-13 | 3.4.24.80 | Membrane-type matrix metalloproteinase 1 | Membrane-type-1 matrix metalloproteinase | MMP-14 | MMP-X1 | MT-MMP 1 | MT1-MMP | MT1MMP | MTMMP1 | 3.4.24.- | Membrane-type matrix metalloproteinase 2 | Membrane-type-2 matrix metalloproteinase | MMP-15 | MT-MMP 2 | MT2-MMP | MT2MMP | MTMMP2 | SMCP-2 | 3.4.24.- | C8orf57 | Membrane-type matrix metalloproteinase 3 | Membrane-type-3 matrix metalloproteinase | MMP-16 | MMP-X2 | MMPX2 | MT-MMP 3 | MT3-MMP | MT3MMP | MTMMP3 | 3.4.24.- | Membrane-type matrix metalloproteinase 4 | Membrane-type-4 matrix metalloproteinase | MMP-17 | MT-MMP 4 | MT4-MMP | MT4MMP | MTMMP4 | 3.4.24.- | Matrix metalloproteinase RASI | Matrix metalloproteinase-18 | MMP-18 | MMP-19 | MMP18 | RASI | 3.4.24.- | Enamel metalloproteinase | Enamelysin | MMP-20 | 3.4.24.- | MMP-21 | 3.4.24.- | Femalysin | Matrix metalloproteinase-21 | Matrix metalloproteinase-22 | MIFR-1 | MMP-21 | MMP-22 | MMP-23 | MMP21 | MMP22 | 3.4.24.- | Membrane-type matrix metalloproteinase 5 | Membrane-type-5 matrix metalloproteinase | MMP-24 | MT-MMP 5 | MT5-MMP | MT5MMP | MTMMP5 | 3.4.24.- | Leukolysin | Membrane-type matrix metalloproteinase 6 | Membrane-type-6 matrix metalloproteinase | MMP-25 | MMP20 | MMPL1 | MT-MMP 6 | MT6-MMP | MT6MMP | MTMMP6 | 3.4.24.- | Endometase | Matrilysin-2 | MMP-26 | 3.4.24.- | MMP-27 | 3.4.24.- | Epilysin | MMP-28 | MMP25

[]

[ "P03956", "P08253", "P08254", "P09237", "P22894", "P14780", "P09238", "P24347", "P39900", "P45452", "P50281", "P51511", "P51512", "Q9ULZ9", "Q99542", "O60882", "Q8N119", "O75900", "Q9Y5R2", "Q9NPA2", "Q9NRE1", "Q9H306", "Q9H239" ]

[]

DB00787

Acyclovir

Acyclovir is a deoxynucleoside analog antiviral used to treat herpes simplex, _Varicella zoster_, herpes zoster, herpes labialis, and acute herpetic keratitis.[L7303,L7315,L7318,L7321,L7324,L7327] Acyclovir is generally used first line in the treatment of these viruses and some products are indicated for patients as young as 6 years old.[L7321] Acyclovir was granted FDA approval on 29 March 1982.[L7318]

solid

An acyclovir topical cream is indicated to treat recurrent herpes labialis in immunocompetent patients 12 years and older.[L7303] Acyclovir oral tablets, capsules, and suspensions are indicated to treat herpes zoster, genital herpes, and chickenpox.[L7315] An acyclovir topical ointment is indicated to treat initial genital herpes and limited non-life-threatening mucocutaneous herpes simplex in immunocompromised patients.[L7318] An acyclovir cream with hydrocortisone is indicated to treat recurrent herpes labialis, and shortening lesion healing time in patients 6 years and older.[L7321] An acyclovir buccal tablet is indicated for the treatment of recurrent herpes labialis.[L7324] An acyclovir ophthalmic ointment is indicated to treat acute herpetic keratitis.[L7327]

Acyclovir is a deoxynucleoside analog that inhibits the action of viral DNA polymerase and DNA replication of different herpesvirus.[L7303,L7315,L7318,L7321,L7324,L7327] Acyclovir has a wide therapeutic window as overdose is rare in otherwise healthy patients.[L7315]

Acyclovir is becomes acyclovir monophosphate due to the action of viral thymidine kinase.[A180757] Acyclovir monophosphate is converted to the diphosphate form by guanylate kinase.[A903] Acyclovir diphosphate is converted to acyclovir triphosphate by nucleoside diphosphate kinase, pyruvate kinase, creatine kinase, phosphoglycerate kinase, succinyl-CoA synthetase, phosphoenolpyruvate carboxykinase and adenylosuccinate synthetase.[A903,A180781] Acyclovir triphosphate has higher affinity for viral DNA polymerase than cellular DNA polymerase and incorporates into the DNA where the missing 2' and 3' carbons causes DNA chain termination.[A180757] In other cases acyclovir triphosphate competes so strongly for viral DNA polymerase that other bases cannot associate with the enzyme, inactivating it.[A180757]

The oral bioavailability of acyclovir is 10-20% but decreases with increasing doses.[L7315] Acyclovir ointment is <0.02-9.4% absorbed.[L7318] Acyclovir buccal tablets and ophthalmic ointment are minimally absorbed.[L7324,L7327] The bioavailability of acyclovir is not affected by food.[L7315] Acyclovir has a mean Tmax of 1.1±0.4 hours, mean Cmax of 593.7-656.5ng/mL, and mean AUC of 2956.6-3102.5h/*ng/mL.[A180793]

Acyclovir is <15% oxidized to 9-carboxymethoxymethylguanine by alcohol dehydrogenase and aldehyde dehydrogenase and 1% 8-hydroxylated to 8-hydroxy-acyclovir by aldehyde oxidase.[A180730] Acyclovir is becomes acyclovir monophosphate due to the action of viral thymidine kinase.[A180757] Acyclovir monophosphate is converted to the diphosphate form by guanylate kinase.[A903] Acyclovir diphosphate is converted to acyclovir triphosphate by nucleoside diphosphate kinase, pyruvate kinase, creatine kinase, phosphoglycerate kinase, succinyl-CoA synthetase, phosphoenolpyruvate carboxykinase and adenylosuccinate synthetase.[A903,A180781]

Symptoms of overdose include agitation, coma, seizures, lethargy, and precipitation in renal tubules.[L7315] These symptoms are more common in patients given high doses without monitoring of fluid and electrolyte balance or reduced kidney function.[L7315,A180730,A180775] In the case of an overdose, treat with symptomatic and supportive care.[L7321]

The clearance of acyclovir varies from 2.5-3 hours depending on the creatinine clearance of the patient.[A180757] The plasma half life of acyclovir during hemodialysis is approximately 5 hours.[L7315] The mean half life in patients from 7 months to 7 years old is 2.6 hours.[L7315]

Acyclovir is 9-33% protein bound in plasma.[A180775,L7315]

The majority of acyclovir is excreted in the urine as unchanged drug.[A180730,L7324] 90-92% of the drug can be excreted unchanged through glomerular filtration and tubular secretion.[A180757] <2% of the drug is recovered in feces and <0.1% is expired as CO2.[A180787]

The volume of distribution of acyclovir is 0.6L/kg.[A180775]

The renal clearance of acyclovir is 248mL/min/1.73m2.[A180787] The total clearance in neonates if 105-122mL/min/1.73m2.[A180787]

Organic compounds

Organoheterocyclic compounds

Imidazopyrimidines

Purines and purine derivatives

[ "approved" ]

[ "J05AB", "J05A", "J05", "J", "D06BB", "D06B", "D06", "D", "S01AD", "S01A", "S01", "S", "D06BB", "D06B", "D06", "D" ]

[ "Human Herpes Virus" ]

[ { "cost": "1.01", "description": "Acyclovir 200 mg capsule", "unit": "capsule" }, { "cost": "1.44", "description": "Zovirax 200 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Apo-Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Mylan-Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Novo-Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Nu-Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "1.63", "description": "Ratio-Acyclovir 400 mg Tablet", "unit": "tablet" }, { "cost": "2.26", "description": "Acyclovir 400 mg tablet", "unit": "tablet" }, { "cost": "2.9", "description": "Zovirax 400 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Apo-Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Mylan-Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Novo-Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Nu-Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "2.99", "description": "Ratio-Acyclovir 800 mg Tablet", "unit": "tablet" }, { "cost": "3.08", "description": "Zovirax 200 mg capsule", "unit": "capsule" }, { "cost": "3.81", "description": "Acyclovir 800 mg tablet", "unit": "tablet" }, { "cost": "5.71", "description": "Zovirax 800 mg Tablet", "unit": "tablet" }, { "cost": "6.09", "description": "Zovirax 400 mg tablet", "unit": "tablet" }, { "cost": "11.83", "description": "Zovirax 800 mg tablet", "unit": "tablet" }, { "cost": "30.22", "description": "Zovirax 5% cream", "unit": "g" }, { "cost": "69.44", "description": "Zovirax 5% Cream 2 gm Tube", "unit": "tube" }, { "cost": "165.07", "description": "Zovirax 5% Cream 5 gm Tube", "unit": "tube" }, { "cost": "191.56", "description": "Zovirax 5% Ointment 15 gm Tube", "unit": "tube" }, { "cost": "264.95", "description": "Zovirax 200 mg/5ml Suspension 473ml Bottle", "unit": "bottle" }, { "cost": "0.28", "description": "Zovirax 40 mg/ml Suspension", "unit": "ml" }, { "cost": "0.3", "description": "Acyclovir 200 mg/5ml Suspension", "unit": "ml" }, { "cost": "0.81", "description": "Acyclovir 200 mg Tablet", "unit": "tablet" }, { "cost": "0.81", "description": "Apo-Acyclovir 200 mg Tablet", "unit": "tablet" }, { "cost": "0.81", "description": "Mylan-Acyclovir 200 mg Tablet", "unit": "tablet" }, { "cost": "0.81", "description": "Novo-Acyclovir 200 mg Tablet", "unit": "tablet" }, { "cost": "0.81", "description": "Ratio-Acyclovir 200 mg Tablet", "unit": "tablet" } ]

[ { "approved": "2001-07-03", "country": "Canada", "expires": "2012-01-29", "number": "2098108" }, { "approved": "2006-09-05", "country": "United States", "expires": "2016-08-02", "number": "RE39264" }, { "approved": "2003-02-04", "country": "United States", "expires": "2019-01-24", "number": "6514980" }, { "approved": "2007-05-29", "country": "United States", "expires": "2021-07-24", "number": "7223387" }, { "approved": "2014-06-10", "country": "United States", "expires": "2027-06-03", "number": "8747896" }, { "approved": "2014-07-29", "country": "United States", "expires": "2027-03-23", "number": "8791127" }, { "approved": "2013-11-26", "country": "United States", "expires": "2030-06-16", "number": "8592434" } ]

[ "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", 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"Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir", "Acyclovir Sodium", "Acyclovir Sodium", "Acyclovir Sodium", "Acyclovir Sodium for Injection", "Acyclovir Sodium for Injection", "Acyclovir Sodium for Injection", "Acyclovir Sodium for Injection", "Acyclovir Sodium Injection", "Acyclovir Sodium Injection", "Acyclovir Sodium Injection", "Acyclovir Sodium Injection", "Acyclovir Sodium Injection", "Acyclovir Sodium Injection", "Acyclovir suspension", "Acyclovir-200", "Acyclovir-400", "Acyclovir-800", "Acyclovix", "Alti-acyclovir - 400mg", "Alti-acyclovir - 800mg", "Alti-acyclovir - Tab 200mg", "Apo-acyclovir", "Apo-acyclovir", "Apo-acyclovir", "Apo-acyclovir Ointment", "LidoVir", "Mint-acyclovir", "Mint-acyclovir", "Mint-acyclovir", "Mylan-acyclovir", "Mylan-acyclovir", "Mylan-acyclovir", "Ntp-acyclovir", "Ntp-acyclovir", "Ntp-acyclovir", "Ratio-acyclovir", "Ratio-acyclovir", "Ratio-acyclovir", "Sitavig", "Sitavig", "Sitavig", "Taro-acyclovir", "Teva-acyclovir", "Teva-acyclovir", "Teva-acyclovir", "Xerese", "Xerese", "Xerese", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax", "Zovirax 400", "Zovirax 800", "Zovirax Cap 200mg", "Zovirax Tab 200mg" ]

[ "Zovir" ]

[ "Xerese", "LidoVir", "Xerese", "Acyclovix", "Xerese" ]

[]

[ "Q16774", "P15531", "P22392", "P30613", "P14618", "P12277", "P06732", "P17540", "P12532", "P00558", "P07205", "Q9P2R7", "P53597", "Q96I99", "Q16822", "P35558", "Q8N142", "P30520" ]

[ "P02768" ]

[ "O15245", "Q4U2R8", "Q8TCC7", "Q12908", "Q96FL8", "Q86VL8" ]

DB00789

Gadopentetic acid

A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see pentetic acid), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)

solid

For use with magnetic resonance imaging (MRI) in adults, and pediatric patients (2 years of age and older) to visualize lesions with abnormal vascularity in the brain (intracranial lesions), spine and associated tissues as well as lesions with abnormal vascularity in the head and neck. Also used to facilitate the visualization of lesions with abnormal vascularity in the body (excluding the heart).

null

Based on the behavior of protons when placed in a strong magnetic field, which is interpreted and transformed into images by magnetic resonance (MR) instruments. MR images are based primarily on proton density and proton relaxation dynamics. MR instruments are sensitive to two different relaxation processes, the T1 (spin-lattice or longitudinal relaxation time) and T2 (spin-spin or transverse relaxation time). Paramagnetic agents contain one or more unpaired electrons that enhance the T1 and T2 relaxation rates of protons in their molecular environment. The proton relaxation effect (PRE) of an unpaired electron is 700 times stronger than that of a proton itself. In MRI, visualization of normal and pathological brain tissue depends in part on variations in the radio frequency signal intensity that occur with changes in proton density, alteration of the T1, and variation in T2. When placed in a magnetic field, gadopentetate dimeglumine shortens the T1 and T2 relaxation times in tissues where it accumulates. In the central nervous system (CNS), gadopentetate dimeglumine enhances visualization of normal tissues that lack a blood-brain barrier, such as the pituitary gland and the meninges. Gadopentetate dimeglumine does not cross the intact blood-brain barrier; therefore, it does not accumulate in normal brain tissue or in CNS lesions that have not caused an abnormal blood-brain barrier (e.g., cysts, mature post-operative scars). Abnormal vascularity or disruption of the blood-brain barrier allows accumulation of gadopentetate dimeglumine in lesions such as neoplasms, abscesses, and subacute infarcts. Outside the CNS, gadopentetate dimeglumine rapidly reaches equilibrium in the interstitial compartment and enhances signal in all tissues as a function of delivery and size of the interstitial compartment. This compound has also been found to inhibit human erythrocyte 6-phosphogluconate dehydrogenase.

null

No detectable biotransformation or decomposition.

null

Distribution half life 12 minutes, elimination half 100 minutes

null

Gadopentetate is exclusively eliminated in the urine with 83 ± 14% (mean ± SD) of the dose excreted within 6 hours and 91 ± 13% (mean ± SD) by 24 hours, post-injection.

* 266 ± 43 mL/kg

* 1.94 +/- 0.28 mL/min/kg [Normal subjects]

null

[ "approved" ]

[ "V08CA", "V08C", "V08", "V" ]

[ "Humans and other mammals" ]

[ { "cost": "5.54", "description": "Magnevist vial", "unit": "ml" } ]

[ { "approved": "1996-10-01", "country": "United States", "expires": "2013-10-01", "number": "5560903" }, { "approved": "1994-11-08", "country": "United States", "expires": "2011-11-08", "number": "5362475" } ]

[ "Gadopentetate dimeglumine", "Gadopentetate Dimeglumine Injection", "Gadopentetate Dimeglumine Injection, USP", "Magnevist", "Magnevist" ]

[]

[ "P52209" ]

[]

DB00790

Perindopril

Perindopril is a nonsulfhydryl prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to perindoprilat, its active metabolite, following oral administration. Perindoprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Perindopril may be used to treat mild to moderate essential hypertension, mild to moderate congestive heart failure, and to reduce the cardiovascular risk of individuals with hypertension or post-myocardial infarction and stable coronary disease.

solid

For the treatment of mild to moderate essential hypertension, mild to moderate congestive heart failure, and to reduce the cardiovascular risk of individuals with hypertension or post-myocardial infarction and stable coronary disease.

Perindopril is a nonsulfhydryl prodrug that is metabolized via first pass effect (62%) and systemic hydrolysis (38%) to perindoprilat, its active metabolite, following oral administration. Perindoprilat lowers blood pressure by antagonizing the effect of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. In the blood stream, renin cleaves circulating angiotensinogen to ATI, which is subsequently cleaved to ATII by ACE. ATII increases blood pressure using a number of mechanisms. First, it stimulates the secretion of aldosterone from the adrenal cortex. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. Second, ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. Third, ATII increases blood pressure through direct arterial vasoconstriction. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction. In addition to these major effects, ATII induces the thirst response via stimulation of hypothalamic neurons. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAAS-induced increases in blood pressure. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin, a vasodilator. Inhibiting the deactivation of bradykinin increases bradykinin levels and may sustain the effects of perindoprilat by causing increased vasodilation and decreased blood pressure.

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Perindoprilat, the active metabolite of perindopril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Perindopril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors.

Rapidly absorbed with peak plasma concentrations occurring approximately 1 hour after oral administration. Bioavailability is 65-75%. Following absorption, perindopril is hydrolyzed to perindoprilat, which has an average bioavailability of 20%. The rate and extent of absorption is unaffected by food. However, food decreases the extent of biotransformation to peridoprilat and reduces its bioavailability by 35%.

Extensively metabolized, with only 4-12% of the dose recovered in urine following oral administration. Six metabolites have been identified: perindoprilat, perindopril glucuronide, perindoprilat glucuronide, a perindopril lactam, and two perindoprilat lactams. Only perindoprilat is pharmacologically active. Peridoprilat and perindoprilat glucuronide are the two main circulating metabolites.

The most likely symptom of overdose is severe hypotension. The most common adverse effects observed in controlled clinical trials include cough, digestive symptoms, fatigue, headache, and dizziness.

Perindopril, 1.2 hours; Peridoprilat, 30-120 hours. The long half life of peridoprilat is due to its slow dissociation from ACE binding sites.

Perindoprilat, 10-20% bound to plasma proteins

Perindopril is extensively metabolized following oral administration, with only 4 to 12% of the dose recovered unchanged in the urine.

null

* 219 - 362 mL/min [oral administration]

Organic compounds

Organic acids and derivatives

Carboxylic acids and derivatives

Amino acids, peptides, and analogues

[ "approved" ]

[ "C09BX", "C09B", "C09", "C", "C09BA", "C09B", "C09", "C", "C10BX", "C10B", "C10", "C", "C10BX", "C10B", "C10", "C", "C09AA", "C09A", "C09", "C", "C09BX", "C09B", "C09", "C", "C10BX", "C10B", "C10", "C", "C09BB", "C09B", "C09", "C", "C10BX", "C10B", "C10", "C", "C10BX", "C10B", "C10", "C", "C10BX", "C10B", "C10", "C", "C09BX", "C09B", "C09", "C", "C09BX", "C09B", "C09", "C" ]

[ "Humans and other mammals" ]

[ { "cost": "1.23", "description": "Coversyl 8 mg Tablet", "unit": "tablet" }, { "cost": "1.98", "description": "Perindopril erbumine 2 mg tablet", "unit": "tablet" }, { "cost": "2.22", "description": "Aceon 2 mg tablet", "unit": "tablet" }, { "cost": "2.3", "description": "Perindopril erbumine 4 mg tablet", "unit": "tablet" }, { "cost": "2.58", "description": "Aceon 4 mg tablet", "unit": "tablet" }, { "cost": "2.8", "description": "Perindopril erbumine 8 mg tablet", "unit": "tablet" }, { "cost": "3.14", "description": "Aceon 8 mg tablet", "unit": "tablet" }, { "cost": "0.7", "description": "Coversyl 2 mg Tablet", "unit": "tablet" }, { "cost": "0.88", "description": "Coversyl 4 mg Tablet", "unit": "tablet" } ]

[ { "approved": "1992-11-10", "country": "United States", "expires": "2009-11-10", "number": "5162362" }, { "approved": "2010-05-18", "country": "Canada", "expires": "2023-01-22", "number": "2473205" }, { "approved": "2001-03-06", "country": "Canada", "expires": "2018-03-06", "number": "1341196" }, { "approved": "2010-12-07", "country": "United States", "expires": "2029-10-05", "number": "7846961" }, { "approved": "2004-02-24", "country": "United States", "expires": "2023-04-15", "number": "6696481" } ]

(2S,3aS,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxopentan-2-yl]amino}propanoyl]octahydro-1H-indole-2-carboxylic acid | Perindopril | Perindoprilum | 3.4.15.1 | ACE | DCP | DCP1 | Dipeptidyl carboxypeptidase I | Kininase II | Frizzled protein, human endometrium | FRPHE | sFRP-4 | 3.1.1.8 | Acylcholine acylhydrolase | Butyrylcholine esterase | CHE1 | Choline esterase II | Pseudocholinesterase | Intestinal H(+)/peptide cotransporter | Oligopeptide transporter, small intestine isoform | PEPT1 | Peptide transporter 1 | Kidney H(+)/peptide cotransporter | Oligopeptide transporter, kidney isoform | PEPT2 | Peptide transporter 2

[ "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Aceon", "Ag-perindopril", "Ag-perindopril", "Ag-perindopril", "Ag-perindopril Erbumine", "Ag-perindopril Erbumine", "Ag-perindopril Erbumine", "Apo-perindopril", "Apo-perindopril", "Apo-perindopril", "Apo-perindopril Arginine", "Apo-perindopril Arginine", "Apo-perindopril Arginine", "Apo-perindopril Tablets", "Apo-perindopril Tablets", "Apo-perindopril Tablets", "Apo-perindopril-indapamide", "Apo-perindopril-indapamide", "Apo-perindopril-indapamide", "Apo-perindopril/amlodipine", "Apo-perindopril/amlodipine", "Apo-perindopril/amlodipine", "Arcosyl", "Arcosyl", "Arcosyl", "Arcosyl", "Arcosyl", "Arcosyl", "Arcosyl Plus", "Arcosyl Plus", "Arcosyl Plus Ld", "Auro-perindopril", "Auro-perindopril", "Auro-perindopril", "Bio-perindopril", "Bio-perindopril", "Bio-perindopril", "Coversyl", "Coversyl", "Coversyl", "Coversyl Plus", "Coversyl Plus", "Coversyl Plus Hd", "Coversyl Plus Ld", "Jamp Perindopril", "Jamp Perindopril", "Jamp Perindopril", "Jamp Perindopril Erbumine", "Jamp Perindopril Erbumine", "Jamp Perindopril Erbumine", "M-perindopril Erbumine", "M-perindopril Erbumine", "M-perindopril Erbumine", "Mar-perindopril", "Mar-perindopril", "Mar-perindopril", "Mint-perindopril", "Mint-perindopril", "Mint-perindopril", "Mylan-perindopril Arginine", "Mylan-perindopril Arginine", "Mylan-perindopril Arginine", "Mylan-perindopril Erbumine", "Mylan-perindopril Erbumine", "Mylan-perindopril Erbumine", "Mylan-perindopril/indapamide", "Mylan-perindopril/indapamide", "Mylan-perindopril/indapamide", "Nra-perindopril", "Nra-perindopril", "Nra-perindopril", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine", "Perindopril Erbumine/ Indapamide", "Perindopril Erbumine/ Indapamide Hd", "Perindopril Erbumine/indapamide", "Perindopril Erbumine/indapamide Hd", "Perindopril Erbumine/indapamide Ld", "Perindopril/indapamide", "Perindopril/indapamide", "Perindopril/indapamide", "PMS-perindopril", "PMS-perindopril", "PMS-perindopril", "PMS-perindopril-amlodipine", "PMS-perindopril-amlodipine", "PMS-perindopril-amlodipine", "PMS-perindopril-indapamide", "PMS-perindopril-indapamide", "PMS-perindopril-indapamide", "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Priva-perindopril Erbumine", "Priva-perindopril Erbumine", "Priva-perindopril Erbumine", "Riva-perindopril", "Riva-perindopril", "Riva-perindopril", "Sandoz Perindopril Erbumine", "Sandoz Perindopril Erbumine", "Sandoz Perindopril Erbumine", "Sandoz Perindopril Erbumine/ Indapamide", "Sandoz Perindopril Erbumine/ Indapamide Hd", "Sandoz Perindopril Erbumine/ Indapamide Ld", "Teva-perindopril", "Teva-perindopril", "Teva-perindopril", "Teva-perindopril/indapamide", "Teva-perindopril/indapamide", "Teva-perindopril/indapamide", "Viacoram", "Viacoram", "Viacoram" ]

[]

[ "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Prestalia", "Coversyl Plus Ld", "Coversyl Plus", "Coversyl Plus Hd", "Arcosyl Plus", "Arcosyl Plus Ld", "Arcosyl Plus", "Coversyl Plus", "Teva-perindopril/indapamide", "Teva-perindopril/indapamide", "Sandoz Perindopril Erbumine/ Indapamide Ld", "Sandoz Perindopril Erbumine/ Indapamide", "Sandoz Perindopril Erbumine/ Indapamide Hd", "Apo-perindopril-indapamide", "Mylan-perindopril/indapamide", "Mylan-perindopril/indapamide", "Mylan-perindopril/indapamide", "Apo-perindopril-indapamide", "Apo-perindopril-indapamide", "Teva-perindopril/indapamide", "Perindopril Erbumine/ Indapamide", "Perindopril Erbumine/ Indapamide Hd", "Perindopril/indapamide", "Perindopril/indapamide", "Perindopril/indapamide", "Viacoram", "Viacoram", "Viacoram", "Apo-perindopril/amlodipine", "Apo-perindopril/amlodipine", "Apo-perindopril/amlodipine", "Perindopril Erbumine/indapamide Ld", "Perindopril Erbumine/indapamide", "Perindopril Erbumine/indapamide Hd", "PMS-perindopril-indapamide", "PMS-perindopril-indapamide", "PMS-perindopril-indapamide", "PMS-perindopril-amlodipine", "PMS-perindopril-amlodipine", "PMS-perindopril-amlodipine" ]

[ "P12821", "Q6FHJ7" ]

[ "P06276" ]

[]

[ "P46059", "Q16348" ]

DB00791

Uracil mustard

Nitrogen mustard derivative of uracil. It is a alkylating antineoplastic agent that is used in lymphatic malignancies, and causes mainly gastrointestinal and bone marrow damage.

solid

Used for its antineoplastic properties.

Uracil Mustard selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Uracil Mustard-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed.

After activation, it binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function.

null

5%

null

Organic compounds

Organic nitrogen compounds

Organonitrogen compounds

Nitrogen mustard compounds

[ "approved" ]

[ "L01AD", "L01A", "L01", "L" ]

[ "Humans and other mammals" ]

[]

[]

[ "Uracil Mustard" ]

[]