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LosartanSystematic (IUPAC) namephenyl}methyl)-1H-imidazol-5-yl]methanolIdentifiersCAS number114798-26-4ATC codeC09CA01PubChem3961DrugBankAPRD00052Chemical dataFormulaC22H23ClN6O Mol. mass422.91SMILESeMolecules & PubChemPharmacokinetic dataBioavailability25–35%MetabolismHepatic (CYP2C9, CYP3A4)Half life1.5–2 hoursExcretionRenal 13–25%, biliary 50–60%Therapeutic considerationsPregnancy cat.D(AU) D(US)Legal status℞ Prescription onlyRoutesOralLosartan (rINN) (pronounced /loʊˈsɑrtən/) is an angiotensin II receptor antagonist drug used mainly to treat high blood pressure (hypertension). Losartan was the first angiotensin II receptor antagonist to be marketed. It is currently marketed by Merck & Co. under the trade name Cozaar.XL sells Losartan under the brand name LIPEWIN & LIPEWIN-100 in Philippines & Vietnam. Chira Pharmaceuticals sells Losartan under the brand name Lozaris.// Clinical useAs with all angiotensin II receptor antagonists, losartan is indicated for the treatment of hypertension. Losartan may also delay progression of diabetic nephropathy and is also indicated 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 angiotensin II receptor antagonists are not usually considered first-line, because of the proven efficacy and lower costs of thiazide diuretics and beta blockers, losartan may be used first-line in patients with increased cardiovascular risk. The LIFE study demonstrated that 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. Combination with diureticLosartan is available in a combination formulation with a low dose thiazide diuretic to achieve an additive antihypertensive effect. The losartan/hydrochlorothiazide combination preparation is marketed by Merck under the trade name Hyzaar and by Xeno Pharmaceuticals under the name, Anzaplus. A Philiippine-based drug company, Chira Pharmaceuticals, markets the combination formulation under the trade name "2Zaris" in the country. PharmacokineticsLosartan is well absorbed following oral administration and undergoes significant first-pass metabolism to produce 5-carboxylic acid metabolite, designated as EXP3174. This metabolite is long-acting (6 to 8 hr), noncompetitive antagonist at the AT1 receptor and contribute to the pharmacological effects of Losartan. This metabolite is 10-40 times more potent in blocking AT1 receptors than the original Losartan. Its bioavailability is about 32%. ResearchLosartan has been found to downregulate the expression of transforming growth factor beta (TGF-β) types I and II receptors in the kidney of diabetic rats, which may partially account for its nephroprotective effects. Effects on TGF-β expression may also account for its potential efficacy in Marfan syndrome and Duchenne muscular dystrophy (DMD) – losartan has been shown to prevent aortic aneurysm and certain pulmonary complications in a mouse model of the disease. Mechanism of action & pharmacological actionsLosartan is a selective, competitive Angiotensin II receptor type 1 (AT1) receptor antagonist, reducing the end organ responses to angiotensin II. Losartan administration results in a decrease in total peripheral resistance (afterload) and cardiac venous return (preload) All of the physiological effects of angiotensin II, including stimulation of release of aldosterone, are antagonized in the presence of losartan. Reduction in blood pressure occurs independently of the status of the renin-angiotensin system. As a result of losartan dosing, plasma renin activity increases due to removal of the angiotensin II feedback. Other usesLosartan is an uricosuric.Because losartan can cause hyperkalemia, potassium supplements or salt substitutes containing potassium should not be used without consulting the prescribing physician.
By treating the blood pressure by using the therapy of drug, the base of prolongation of the life recommended a long ago that the members ask their doctors to prescribe Generic Cozaar or Hyzaar. These drugs are known as antagonists of receiver of angiotension II because of their single mechanism to block the sites of receiver of the. Since then we saw the arrival of several new classes of drugs for the treatment of this condition, beta-blockers, of the calcium antagonists, the inhibitors of C# and most recently.....Blood Pressure/CholesterolAbana, Inderal, Lopressor, Toprol XL, Cozaar, Norvasc, LipitorThe significant improvements of the treatment of hypertension started in the Sixties where the diurétique one and the alpha-adjusters were
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