Angiotensin II antagonism in clinical practice: Experience with valsartan

Angiotensin (Ang) II antagonists provide specific and selective blockade of Ang II at the AT, receptor, regardless of the enzymatic pathway of product ion. Valsartan has an affinity for the AT(1) receptor 30,000 times that of the AT(2) receptor. Valsartan is not a prodrug and undergoes little metabol ism. It has a half-life of approximately 9 h, but duration of antihypertens ive action at the usual dose of 80 or 160 mg daily is 24 h. The trough to p eak ratio is 0.66. Valsartan has antihypertensive efficacy at least equival ent to that of established antihypertensive drugs and has additive effects in combination. The efficacy of valsartan appears to be independent of age, sex, and race. Valsartan is effective in hypertensive patients with renal insufficiency and is associated with maintenance of renal function. It is w ell tolerated, with a side-effect profile indistinguishable from that of pl acebo, and does not cause cough. Ang II antagonists are a promising class o f cardiovascular drugs with considerable potential in clinical practice.