Ezetimibe: a novel option for lowering cholesterol.

Abstract

Elevated low-density lipoprotein (LDL)-cholesterol is associated with a significantly increased risk of coronary heart disease but lowering LDL-cholesterol to levels established in current National Cholesterol Education Program (NCEP) guidelines provides significant risk reduction. Nevertheless, many patients receiving lipid-lowering therapy, particularly those at highest coronary heart disease risk, do not reach LDL-cholesterol goals with their current medications. Ezetimibe (Zetia, Merck Schering-Plough) is the first of a new class of lipid-lowering drugs known as cholesterol absorption inhibitors. Ezetimibe has a favorable pharmacokinetic profile, which allows it to be administered once daily and to be given in conjunction with statins. In a series of randomized, controlled, multicenter studies, ezetimibe produced significant improvements in levels of LDL-cholesterol and other lipid parameters when used as monotherapy, with a safety profile comparable with that of placebo. Furthermore, coadministration of ezetimibe with a statin (simvastatin, atorvastatin, lovastatin, or pravastatin) was more effective than statin monotherapy in lowering LDL-cholesterol and improving other lipid parameters. Moreover, coadministration of ezetimibe with a statin allowed a greater percentage of patients to achieve treatment goals established in NCEP guidelines. The safety and side-effect profile of ezetimibe plus statin coadministration therapy was generally comparable with that of statin monotherapy. These studies establish ezetimibe as an effective lipid-lowering agent, which will likely be useful in the management of a broad range of patients with hypercholesterolemia. Ezetimibe can be used in conjunction with a statin at the beginning of therapy, or it can be added if patients do not achieve their LDL-cholesterol goal with statins alone.

• Authors: Michael H Davidson
• Journal: Expert review of cardiovascular therapy (Expert Rev Cardiovasc Ther) Vol. 1 Issue 1 Pg. 11-21 (May 2003) ISSN: 1477-9072 [Print] England
• PMID: 15030293 (Publication Type: Journal Article, Review)

Chemical References

• Anticholesteremic Agents
• Azetidines
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Ezetimibe

Topics

• Anticholesteremic Agents (administration & dosage, therapeutic use)
• Azetidines (administration & dosage, therapeutic use)
• Drug Therapy, Combination
• Ezetimibe
• Humans
• Hydroxymethylglutaryl-CoA Reductase Inhibitors (administration & dosage)
• Hypercholesterolemia (prevention & control)
• Randomized Controlled Trials as Topic