The Current Role of Clevidipine in the Management of Hypertension

Am J Cardiovasc Drugs. 2022 Mar;22(2):127-139. doi: 10.1007/s40256-021-00494-6. Epub 2021 Sep 2.

Abstract

Acute hypertension, which may damage blood vessels, causes irreversible organ damage to the vasculature, central nervous system, kidney, and heart. Clevidipine, the first third-generation calcium channel antagonist approved by the Food and Drug Administration (FDA) in the past 20 years, is an ultra-short-acting calcium channel blocker that inhibits L-type calcium channels with high clearance and low distribution, can be rapidly metabolized into the corresponding inactive acid, and is rapidly hydrolyzed into inactive metabolites by esterase in arterial blood. Clevidipine is the same as nicardipine in that the main physiological effect is vasodilation and the main target is the arterial system, which has a limited effect on capacitor vessels. Unlike nitroglycerin, clevidipine has a limited effect on preload. In contrast to other direct-acting vasodilators, clevidipine has an ultra-short half-life due to metabolism by nonspecific blood and tissue esterases. Clevidipine trials conducted in adult populations have proven that it can rapidly control blood pressure in cardiac surgery situations and that adverse reactions to clevidipine are similar to those with other antihypertensive agents. In recent years, clinical trials have shown that clevidipine has excellent blood pressure-lowering capability in patients with acute neurological injury (hemorrhage, stroke, and subarachnoid and acute intracerebral hemorrhage), those undergoing coronary artery bypass graft or spinal surgery, and in those with cerebral aneurysm/pheochromocytoma, acute heart failure, acute aortic syndromes, or renal insufficiency with severe hypertension, and it is equivalent to commonly used blood pressure-lowering medicines such as nicardipine or nitroglycerin. However, there is a lack of large-scale clinical trial data on the efficacy and safety of clevidipine in children during the perioperative period.

Publication types

  • Review

MeSH terms

  • Adult
  • Antihypertensive Agents / adverse effects
  • Blood Pressure
  • Calcium Channel Blockers / adverse effects
  • Child
  • Humans
  • Hypertension* / drug therapy
  • Pyridines* / adverse effects

Substances

  • Antihypertensive Agents
  • Calcium Channel Blockers
  • Pyridines
  • clevidipine