pharmaceutical material losartan potassium for antihypertensive

description:

1. losartan potassium,losartan is well absorbed following oral administration and undergoes significant first-pass metabolism to produce the 5-carboxylic acid metabolite, designated as exp3174. about 14% of an oral dosage is converted to this metabolite, which is long-acting (6 to 8 hr) and a noncompetitive antagonist at the at1 receptor, contributing to the pharmacological effects of losartan. exp3174 is 10-40 times more potent in blocking at1 receptors than losartan. losartan's bioavailability is about 32%.

2. losartan potassium,metabolism is primarily by cytochrome p450 isoenzymes cyp2c9 and cyp3a4. peak plasma concentrations of losartan and exp3174 occur about one hour and three to four hours, respectively, after an oral dose. both losartan and exp3174 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. about 4% of an oral dose is excreted unchanged in urine, and about 6% is excreted in urine as the active metabolite. the terminal elimination half lives of losartan and exp3174 are about 1.5 to 2.5 hours and 3 to 9 hours, respectively.

specification:

usage:

1.a nonpeptide angiotensin ii at1-receptor antagonist. antihypertensive.

2.antihypertensive, at1 angiotensin ii antagonist

3.coronary vasodilator used in the diagnosis of coronary heart disease (adenosine a2a agonist).