Description
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Pharmacological action
Antihypertensive agent. It is a non-peptide angiotensin II receptor blocker. It has high selectivity and affinity for AT1 type receptors (with the participation of which the main effects of angiotensin II are realized). By blocking these receptors, losartan prevents and eliminates the vasoconstrictive effect of angiotensin II, its stimulating effect on the secretion of aldosterone by the adrenal glands and some other effects of angiotensin II. It is characterized by a long-lasting effect (24 hours or more), which is due to the formation of its active metabolite.
Pharmacokinetics
After oral administration, losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It is metabolized during the “first passage” through the liver with the formation of a carboxylic metabolite, which has a more pronounced pharmacological activity than losartan, and a number of inactive metabolites. Cmax in the blood plasma of losartan and the active metabolite is reached after 1 hour and 3-4 hours, respectively. Binding to plasma proteins of losartan and the active metabolite is high – more than 98%. T1/2 of losartan and the active metabolite in the final phase is about 1.5-2.5 hours and 3-9 hours, respectively. Losartan is excreted in the urine and feces (with bile) unchanged and in the form of metabolites. About 35% is excreted in urine and about 60% is excreted in feces. Indications of active substances of the drug Kozaar Arterial hypertension. Reduction of the risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a decrease in the combined frequency of cardiovascular mortality, the frequency of stroke and myocardial infarction. Kidney protection in patients with type 2 diabetes mellitus with proteinuria is a slowdown in the progression of renal failure, manifested by a decrease in the frequency of hypercreatininemia, the frequency of end-stage CRF requiring hemodialysis or kidney transplantation, mortality rates, as well as a decrease in proteinuria. Chronic heart failure (as part of combination therapy, with intolerance or ineffectiveness of therapy with ACE inhibitors).
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