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Losartan
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DRUG INFO Losartan
Drug Name:
Losartan
Indication: For the treatment of hypertension
Pharmacology: Losartan is the first of a class of antihypertensive agents called angiotensin II (AG II) receptor antagonists. It is, along with its longer acting active metabolite (E-3174), a specific and selective AT1 receptor antagonist. Losartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland).
Mechanism Of Action: Losartan and its longer acting active metabolite (E-3174) interfere with the binding of angiotensin II to the angiotensin II AT1-receptor by, themselves, binding reversibly to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Neither Losartan or its metabolite inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels.
Drug Category: Antihypertensive Agents; Antiarrhythmic Agents; Angiotensin II Receptor Antagonists; ATC:C09CA01
Brand Names/Synonyms: CHEMBANK1667; Cozaar; DUP 89; Hyzaar; Lacidipine; Lortaan; Losartan
Dosage Forms: Tablets
Absorption: Well absorbed, the systemic bioavailability of losartan is approximately 33%
Interactions:
DrugBank: Interactions for Losartan
Interactions for Losartan:
No significant drug-drug pharmacokinetic interactions have been found in interaction studies with
hydrochlorothiazide, digoxin, warfarin, cimetidine and phenobarbital. Rifampin, an inducer of drug metabolism,
decreased the concentrations of losartan and its active metabolite. In humans, two inhibitors of P450 3A4 have been
studied. Ketoconazole did not affect the conversion of losartan to the active metabolite after intravenous
administration of losartan, and erythromycin had no clinically significant effect after oral administration.
Fluconazole, an inhibitor of P450 2C9, decreased active metabolite concentration and increased losartan
concentration. The pharmacodynamic consequences of concomitant use of losartan and inhibitors of P450 2C9 have not
been examined. Subjects who do not metabolize losartan to active metabolite have been shown to have a specific, rare
defect in cytochrome P450 2C9. These data suggest that the conversion of losartan to its active metabolite is
mediated primarily by P450 2C9 and not P450 3A4.
As with other drugs that block angiotensin II or its effects, concomitant use of potassium-sparing
diuretics (e.g., spironolactone, triamterene, amiloride), potassium supplements, or salt substitutes containing
potassium may lead to increases in serum potassium.
As with other antihypertensive agents, the antihypertensive effect of losartan may be blunted by the
non-steroidal anti-inflammatory drug indomethacin.
Chemical IUPAC Name: [2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-3H-imidazol-4-yl]methanol
Chemical Formula: C22H23ClN6O
Half Life: 2 hours
Drug Type: Approved Drug
# Accession No: APRD00052
CAS Registry Number: 114798-26-4
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Losartan News (When available)
DuPont "neutral," target price reduced Jan 13, 2006 New Ratings DuPont’s Cozaar/Hyzaar pharma patents are scheduled to expire in 2010, the analyst says. The EPS estimate for 2006 has been reduced from $2.75 to $2.30.
DuPont Shares Look 'Deceptively Cheap' Jan 12, 2006 Forbes ...and Rita, research analyst Kevin McCarthy said he remains cautious on DuPont due to the company's patent expirations for hypertension drugs Cozaar and Hyzaar ...
Merck Unveils Plan to Reclaim Leadership Position Dec 15, 2005 Business Wire (press release), PRODUCT 2005 SALES ----- ZOCOR (Cholesterol modifying) $4.2 to $4.5 billion FOSAMAX (Osteoporosis) $3.1 to $3.4 billion COZAAR/HYZAAR (Hypertension ...
Medicare Part D available starting Jan. 1 Dec 26, 2005 Saipan Tribune, ...per month premium-are $26 per prescription for common drugs such as Lipitor and Norvasc and up to $56 per prescription for drugs such as Pravachol and Cozaar. ...
DuPont Shares Look 'Deceptively Cheap' Jan 12, 2006 Forbes Rita, research analyst Kevin McCarthy said he remains cautious on DuPont due to the company's patent expirations for hypertension drugs Cozaar and Hyzaar and a ...
DuPont "neutral," target price reduced Jan 13, 2006 New Ratings DuPont’s Cozaar/Hyzaar pharma patents are scheduled to expire in 2010, the analyst says. The EPS estimate for 2006 has been reduced from $2.75 to $2.30.
Merck Unveils Plan to Reclaim Leadership Position Dec 15, 2005 Business Wire (press release), 2005 SALES ----- ZOCOR (Cholesterol modifying) $4.2 to $4.5 billion FOSAMAX (Osteoporosis) $3.1 to $3.4 billion COZAAR/HYZAAR (Hypertension) $2.9 ...
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