Irbesartan CAS#138402-11-6

Irbesartan CAS#138402-11-6 is an angiotensin Ⅱreceptor inhibitor, angiotensin Ⅱ receptors are divided into AT1, AT2, irbesartan can inhibit AngⅠtransform into AngⅡby selectively blocking the AT1 receptor of AngⅡ, specifically antagonize angiotensin converting enzyme 1 receptor (AT1), the antagonism of AT1 is 8500 times than that of AT2, it can inhibit vasoconstriction and aldosterone release by selectively blocking the binding AngⅡ with AT1 receptor and result in the antihypertensive effect. This product does not inhibit angiotensin converting enzyme (ACE), renin, and other hormone receptors, neither suppress the blood pressure regulation and the balance of sodium ion channels. Irbesartan can also reduce electrical remodeling of the myocardium, thereby reduce the mortality rate of patients with hypertension, it is the most effective drug for treatment of hypertension and cardiovascular disease.
Angiotensin antagonists (ARB) is applied to the clinical treatment of hypertension and diabetic nephropathy. At present, domestic drugs for treating high blood pressure are divided into angiotensin converting enzyme inhibitors (ACEI), calcium channel blockers, beta blockers and so on according to different working parts. By contrast, ARB has better antihypertensive effect, while Irbesartan is a new type of angiotensin antagonist which has clear antihypertensive effect, and has an important role in inhibiting left ventricular hypertrophy and protecting the kidneys.
According to foreign reports, it can quickly absorb by oral and the bioavailability is 60-80%, not affected by food. Plasma tmax is 1-1.5 hours, plasma protein combined rate is 90%, elimination half-life is 11-15 hours, reaching steady state in three days. By aldehyde oxidation acidification or glucose metabolism, vitro studies have shown that mainly oxidation by cytochrome enzymes of P450 and 2C9. This product and its metabolites excrete by biliary tract and kidney.
Irbesartan (Emberd) produced by Sanofi-aventis hangzhou minsheng pharmaceutical co., LTD won the approval of the SFDA used in the treatment of hypertension in type 2 diabetic nephropathy on March 8, 2007, and becomes China's first effective antihypertensive drug.

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