WILOPRES 100mg

Generic Name:
Losartan Potassium

Pharmacologic Category:
Angiotensin II Receptor Blocker

Pharmacodynamics and Pharmacokinetics:
Losartan Potassium is an angiotensin II receptor antagonist with antihypertensive activity due mainly to selective blockade of AT1 receptors and the consequent reduced pressor effect of angiotensin II.

Pharmacokinetics:

Losartan Potassium is readily absorbed from the gastrointestinal tract following oral administration, with an oral bioavailability of about 33%. It undergoes first pass metabolism to form an active carboxylic acid metabolite E-1374 (EXP-3174), which has greater pharmacological activity that losartan, and some inactive metabolites. Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and E-3174 are more than 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 of losartan and E-1374 are about 1.5 to 2.5 hours and 3 to 9 hours respectively.

Indications:

For the management of hypertension, particularly in patients who develop cough with ACE inhibitors; for the treatment of diabetic nephropathy.

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