Drug Profile of Valsartan: A Review

Abstract

Valsartan is a new potent, highly selective and orally active antihypertensive drug belonging to the family of Angiotensin II type I receptor antagonists. Angiotensin II receptor type I antagonists have been widely used in the treatment of hypertension, heart failure, myocardial infraction and diabetic nephropathy. It is a lipophilic drug and it was first developed by Novartis and has a wide market in the developed and developing countries. It is available as single and in combination with other antihypertensive drugs. Valsartan is rapidly absorbed after oral administration. Volume of distribution at steady state has been estimated 17L and mean absolute bioavailability is 23%. Food decreases the exposure of Valsartan by about 40% and peak plasma concentration by about 50%. 94%-97% of drug bound to serum protein mainly albumin. It is eliminated by non-renal route. Plasma clearance of Valsartan is 2L/hours and renal clearance is 0.62L/hour. In this paper, the physicochemical properties, analytical determination methods, pharmacokinetics and pharmacodynamics of Valsartan are reviewed.