CANDESARTAN CILEXETIL - A NEW, LONG-ACTING, EFFECTIVE ANGIOTENSIN-II TYPE-1 RECEPTOR BLOCKER

Candesartan is a potent and selective angiotensin II type 1 receptor b locker which binds tightly to and dissociates slowly from the AT(1) re ceptor. It is administered orally as the prodrug candesartan cilexetil , which is rapidly and completely converted to the active compound, ca ndesartan, during gastrointestinal absorption. In hypertensive patient s, candesartan cilexetil dose-dependently lowers diastolic and systoli c blood pressure (BP) over the 24-h dose interval and it maintains its antihypertensive effects in the long term. Clinical trials indicate t hat a once-daily dose of 4-16 mg provides a clinically relevant reduct ion in BP. The usual maintenance doses of candesartan cilexetil are ex pected to be 8 mg and 16 mg once-daily and dosage adjustment does not appear to be necessary in elderly patients or those with mild to moder ate renal or hepatic impairment. Adverse events during treatment with candesartan cilexetil occur at a similar low incidence as with placebo and no dose-dependent events or adverse metabolic effects have been n oted. As once-daily monotherapy, candesartan cilexetil 8 mg is as effe ctive as enalapril 10-20 mg, amlodipine 5 mg or hydrochlorothiazide 25 mg, and candesartan cilexetil 16 mg is more effective than losartan 5 0 mg. The trough to peak ratio for the reduction in BP with candesarta n cilexetil has been shown to be in the order of 80-100%, confirming t he smooth 24-h BP-lowering profile of the drug. Combined treatment wit h candesartan cilexetil and hydrochlorothiazide or amlodipine provides an enhanced BP-lowering effect that is useful in patients with inadeq uate response to initial treatment after step-up titration. Candesarta n cilexetil is similarly well tolerated as placebo, both when given as monotherapy, and in combination for example with hydrochlorothiazide. Candesartan cilexetil with its flexible dosage regimen therefore appe ars to offer an effective and well-tolerated alternative to other esta blished agents in the treatment of a wide range of hypertensive patien ts.