Olmesartan medoxomil: An angiotensin II-receptor blocker

Background: Regulation of the activity of the renin-angiotensin-aldosterone system has become important in the management of cardiovascular disease. Olmesartan medoxomil (CS-866) is the newest selective angiotensin II-receptor blocker (ARB) to be approved for the treatment of hypertension.

Objective: This review describes the mechanism of action, pharmacokinetics, adverse-effect profile, drug-interaction potential, and dosing of olmesartan medoxomil. The results of relevant clinical efficacy and safety trials are also discussed.

Methods: This review is based on data from published clinical efficacy and safety trials and abstracts of conference presentations. To identify appropriate English-language publications for review, MEDLINE (1966–October 2002) and EMBASE (1990–2002) were searched using the terms olmesartan medoxomil, CS-866, angiotensin II-receptor blocker, and hypertension.

Results: Olmesartan medoxomil has been reported to be an effective agent for the treatment of hypertension. Its blood pressure-lowering effects were comparable to those of other antihypertensive agents and other ARBs. Effects were seen as early as 2 weeks and persisted when olmesartan medoxomil was administered long term (for 1 year). The maximum recommended daily dose is 40 mg, except in the presence of severe renal insufficiency (creatinine clearance <20 mL/min) or moderate hepatic insufficiency (Child-Pugh score 7–9), when the daily dose should not exceed 20 mg. Olmesartan medoxomil was well tolerated. The most commonly reported adverse effect occurring significantly more often with olmesartan medoxomil than with placebo was dizziness (seen in ∼3% of patients). The occurrence of clinically significant drug interactions was minimal.

Conclusions: Based on the available literature, olmesartan medoxomil is an effective ARB for the treatment of hypertension, with a favorable adverse-effect and drug-interaction profile.