Olmesartan for the Treatment of Arterial Hypertension

Abstract

Angiotensin-receptor blockers (ARBs) are an important class of agents used for the treatment of arterial hypertension. Olmesartan medoxomil, the seventh latest ARB approved by the US FDA, is an oral, once-daily, AT(1)-receptor selective ARB with high receptor affinity. Pharmacologically, it acts as a competitive and insurmountable Ang II antagonist with linear pharmacokinetics and without cytochrome P450 interaction. The drug is licensed for the treatment of arterial hypertension alone or in combination with other antihypertensive agents. Olmesartan has demonstrated its dose-dependent inhibitory effect on Ang I-induced blood pressure responses between 10 and 80 mg in Phase II studies. These results, confirmed in an international clinical trial programme covering over 3000 hypertensive patients in numerous studies, demonstrated rapid blood pressure-lowering effects within 1 week. A daily oral dose of 20 mg olmesartan is considered to be the optimal dose. In clinical trials and postmarketing studies, olmesartan has been shown to be safe and well tolerated with an adverse event profile similar to the placebo. Active comparative studies demonstrated either similar or superior efficacy of olmesartan compared with other ARBs, angiotensin-converting enzymes inhibitors, beta-blockers or calcium-channel blockers. Besides its antihypertensive efficacy, olmesartan was shown in clinical trials to reduce vascular microinflammation, decrease intrarenal vascular resistance, significantly reduce vascular remodeling of small resistance arteries and exert antiatherosclerotic effects by significantly reducing the volume of large atherosclerotic plaques.