Losartan

Losartan
Clinical data


Trade names	Cozaar
AHFS/Drugs.com	Monograph
MedlinePlus	a695008
License data	US DailyMed: 51286
Pregnancy category	AU: D US: D (Evidence of risk)
Routes of administration	Oral
ATC code	C09CA01 (WHO)
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	25–35%
Protein binding	99.7% (primarily albumin)
Metabolism	Hepatic (CYP2C9, CYP3A4)
Biological half-life	1.5–2 hours
Excretion	Renal 13–25%, biliary 50–60%
Identifiers
IUPAC name (2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanol
CAS Number	114798-26-4^Y
PubChem (CID)	3961
IUPHAR/BPS	590
DrugBank	DB00678^Y
ChemSpider	3824^Y
UNII	JMS50MPO89^Y
KEGG	D08146^Y
ChEBI	CHEBI:6541^Y
ChEMBL	CHEMBL191^Y
ECHA InfoCard	100.110.555
Chemical and physical data
Formula	C₂₂H₂₃ClN₆O
Molar mass	422.91 g/mol
3D model (Jmol)	Interactive image
SMILES Clc1nc(n(c1CO)Cc4ccc(c2ccccc2c3nnnn3)cc4)CCCC
InChI InChI=1S/C22H23ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,30H,2-3,8,13-14H2,1H3,(H,25,26,27,28)^Y Key:PSIFNNKUMBGKDQ-UHFFFAOYSA-N^Y

Losartan (rINN) /loʊˈsɑːrtən/ is an angiotensin II receptor antagonist drug used mainly to treat high blood pressure (hypertension). It was the first angiotensin II antagonist to be marketed. Losartan potassium is marketed by Merck & Co. Inc. under the trade name Cozaar, and is available in generic form.

As with all angiotensin II type 1 receptor (AT₁) antagonists, losartan is indicated for the treatment of hypertension. It may also delay progression of diabetic nephropathy and is associated with a positive clinical outcome in that regard. It is a suitable pharmacological agent for the reduction of renal disease progression in patients with type 2 diabetes, hypertension, and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours).

Although clinical evidence shows calcium channel blockers and thiazide-type diuretics are preferred first-line treatments for most patients (due to both efficacy and cost), an angiotensin II receptor antagonist such as losartan is recommended as first-line treatment in patients under the age of 55 who cannot tolerate an ACE inhibitor. The LIFE study demonstrated losartan was significantly superior to atenolol in the primary prevention of adverse cardiovascular events (myocardial infarction or stroke), with a significant reduction in cardiovascular morbidity and mortality for a comparable reduction in blood pressure. A study hints that losartan has a beneficial effect on by reversing age related dysfunction in maintaining normal blood pressure and cellular energy usage. The maximal effects on blood pressure usually occur within 3–6 weeks of starting losartan.

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Wikipedia