Clevidipine: a new intravenous option for the management of acute hypertension

Abstract

Purpose: The pharmacology, pharmacokinetics, efficacy, safety, dosage and administration, and place in therapy of clevidipine are reviewed.

Summary: Clevidipine is a new lipophilic, short-acting, third-generation dihydropyridine calcium channel blocker (CCB) approved for use in the management of acute hypertension when oral agents are not feasible. It exerts its hemodynamic effects through selective arterial vasodilation without effects on the venous circulation. Clevidipine has a half-life of approximately two minutes after i.v. administration, resulting in very rapid onset and offset of antihypertensive action. Unlike many current i.v. antihypertensive agents that are metabolized by the kidneys or liver, clevidipine is metabolized in the blood and tissues and does not accumulate in the body. Clevidipine does not appear to inhibit or induce cytochrome P-450 isoenzymes. Several Phase III clinical trials have reported the clinical efficacy and safety of clevidipine in patients with severe hypertension and in cardiac surgical patients with perioperative hypertension. The most frequent adverse events reported in clinical trials of clevidipine were headache, nausea, and vomiting. Risk of rebound hypertension, especially in patients not transitioned from clevidipine to oral antihypertensive therapy after prolonged infusions, should be monitored for at least eight hours after the drug is discontinued.

Conclusion: Clevidipine, a novel third-generation dihydropyridine CCB, has demonstrated efficacy and safety in patients with acute hypertension and preoperative, perioperative, and postoperative hypertension. While its short duration of action and short half-life are appropriate for use in acute settings, more information on its safety is needed to assess its appropriate use in therapy.