Getzar Plus

Getzar Plus Mechanism of Action

losartan + hydrochlorothiazide




Getz Pharma
Full Prescribing Info
Pharmacology: Pharmacodynamics: Losartan Potassium: It is an angiotensin II receptor antagonist with antihypertensive activity due mainly to selective blockade of AT, receptors and the consequent reduced pressure effect of angiotensin II.
Pharmacokinetics: Losartan Potassium: Losartan potassium is readily absorbed from the gastrointestinal tract (GIT) following oral administration, with an oral bioavailability about 33%. It undergoes first-pass metabolism to form an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than losartan and some inactive metabolites. Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and E-317 occur at 1 hr and 3-4 hrs, respectively, after an oral dose. Both losartan and E-3174 are >98% bound to plasma proteins. Losartan is excreted in the urine and in the feces via bile, as unchanged drug and metabolites. Following oral dosing, about 35% of the dose is excreted in the urine and about 60% in the feces. The terminal elimination half-lives (t½) of losartan and E-3174 are about 1.5-2.5 hrs and 3-9 hrs, respectively.
Hydrochlorothiazide: It is a diuretic antihypertensive. It is fairly rapidly absorbed from the GIT. It is reported to have a bioavailability of about 65-70%. It has been estimated to have a plasma t½ of between about 5 and 15 hrs, and appears to be preferentially bound to red blood cells. It is excreted mainly unchanged in the urine. Hydrochlorothiazide crosses the placenta barrier and is distributed into breast milk.
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