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QuickView for Losartan (compound)

Name: Losartan
PubChem Compound ID: 11476710
Description: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Molecular formula: C22H22ClKN6O
Molecular weight: 461.001 g/mol
Name: Losartan
Name (isomeric): DB00678
Drug Type: small molecule
Description: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Losartan Potassium; DUP 89
Brand: Lacidipine, Cozaar, Hyzaar, Lortaan
Brand name mixture: Anzaplus(Losartan + Hydrochlorothiazide), Hyzaar(Losartan + Hydrochlorothiazide)
Category: Angiotensin II Type 1 Receptor Blockers, Antiarrhythmic Agents, Angiotensin II Receptor Antagonists, Anti-Arrhythmia Agents, Antihypertensive Agents
CAS number: 114798-26-4
Indication: May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Losartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
Losartan is the first of a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Losartan and its longer acting active metabolite, E-3174, are specific and selective type-1 angiotensin II receptor (AT1) antagonists which block the blood pressure increasing effects angiotensin II via the renin-angiotensin-aldosterone syste...
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Mechanism of Action:
Losartan competitively inhibits the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. Losartan is metabolized to its active metabolite, E-3174, which is 10 to 40 times more potent than losartan and acts as a non-competitive AT1 antagonist. Inhibition of angiotensin II binding to AT1 inhibits i...
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Absorption: Well absorbed, the systemic bioavailability of losartan is approximately 33%
Protein binding: 99.7%, primarily to albumin
Biotransformation: Hepatic. Losartan is metabolized to a 5-carboxylic acid derivative (E-3174) via an aldehyde intermediate (E-3179) primarily by cytochrome P450 (CYP) 2C9 and CYP3A4. E-3174 is an active metabolite with 10- to 40-fold higher potency than its parent compound, losartan. Approxiamtely 14% of losartan is converted to E-3174; however, the AUC of E-3174 was found to be 4- to 8-fold higher than losartan and E-3174 is considered the main contributor to the pharmacologic effects of this medication.
Route of elimination: After single doses of losartan administered orally, about 4% of the dose is excreted unchanged in the urine and about 6% is excreted in urine as active metabolite. Biliary excretion contributes to the elimination of losartan and its metabolites.
Half Life: The terminal t1/2 of losartan is 2 hours and that of E-3174 is 6-9 hours.
Clearance: 600 mL/min [Healthy volunteers after IV administration] Renal cl=56 +/- 23 mL/min [Hypertensive adults given 50 mg once daily for 7 days] Renal cl=53 +/- 33 mL/min [Hypertensive children (6-16 years old) given 0.7 mg/kg once daily for 7 days]
Toxicity: Hypotension and tachycardia; Bradycardia could occur from parasympathetic (vagal) stimulation, LD50= 1000 mg/kg (orally in rat)
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals. Take at same time each day. Food delays absorption, but does not affect the extent of absorption.
Drug interaction:
TrandolaprilThe angiotensin II receptor blocker, Losartan, may increase the adverse effects of Trandolapril.
IndomethacinIndomethacin decreases the effect of losartan
PotassiumIncreased risk of hyperkalemia
AmilorideIncreased risk of hyperkalemia
QuinupristinThis combination presents an increased risk of toxicity
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