Clevidipine: an ultra short-acting calcium channel antagonist for acute hypertension.

OBJECTIVE: To review the safety, efficacy, and pharmacologic characteristics of clevidipine, a new ultra short-acting intravenous antihypertensive agent for the treatment of moderate-to-severe hypertension.

DATA SOURCES: A literature search was conducted through MEDLINE (1966-March 2009), International Pharmaceutical Abstracts (1970-March 2009), and EMBASE (1988-March 2009) using the search terms clevidipine, H324/38, hypertension, and hypertensive crisis.

STUDY SELECTION AND DATA EXTRACTION: Available studies, abstracts, and review articles published in English that evaluated the pharmacology, pharmacokinetics, safety, and clinical efficacy of clevidipine were reviewed and critically evaluated.

DATA SYNTHESIS: Clevidipine is a new third-generation dihydropyridine calcium-channel blocker available for intravenous management of moderate-to-severe hypertension. Clevidipine is an ultra short-acting, selective arteriolar vasodilator that acts similar to other L-type dihydropyridine calcium-channel blockers by inhibiting influx of extracellular calcium into the vascular smooth muscle. Its safety and efficacy have been primarily evaluated in the perioperative setting in patients undergoing cardiac surgery requiring management of elevated blood pressure. In comparison to most other intravenous antihypertensives, clevidipine has a rapid onset of action, is ultra short-acting, easily titratable with a predictable dose response, and is void of drug-drug interactions and need for dose adjustment in patients with hepatic or renal insufficiency, thus making it a valuable antihypertensive in both the intraoperative and critical care settings. In clinical trials, clevidipine was well tolerated at infusion rates from 2-32 mg per hour, for up to 72 hours.

CONCLUSIONS: Clevidipine is the first intravenous antihypertensive approved by the Food and Drug Administration in nearly a decade. Based on available published clinical trials, clevidipine appears to be safe and effective in the acute management of moderate-to-severe elevations in blood pressure and a viable alternative to other agents such as nitroglycerin, sodium nitroprusside, and nicardipine.