Klin Farmakol Farm. 2005;19(1):22-26

EZETIMIBE - THE FIRST AGENT OF A NOVEL CLASS OF SELECTIVE CHOLESTEROL ABSORPTION INHIBITORS

Lucie Sobolová

Department of Pharmacology University Hospital and Palacký University, Olomouc, Czech Republic

Current approaches of lipid lowering therapy include low fat diet and the use of wellestablished treatments. There is also the development of the novel agents which interfere with different levels of cholesterol metabolism are being developed. Ezetimibe is the first agent of a novel class of selective cholesterol absorption inhibitors. Ezetimibe inhibits the absorption of biliary and dietary cholesterol from the small intestine without affecting the absorption of fat-soluble vitamins, triglycerides or bile acids. The site of its pharmacological action is the brush border of the small intestine where it decreases cholesterol uptake into the enterocytes. There are many preclinical and clinical studies demonstrating lipid-lowering properties of ezetimibe as monotherapy and its synergistic effect in combination with HMG-CoA reductase inhibitors (statins). When given in monotherapy or in combination with a statin, ezetimibe significantly reduces low-density lipoprotein (LDL) cholesterol and increases high-density lipoprotein (HDL) cholesterol. Ezetimibe is well tolerated with a safety profile similar to that of placebo. In clinical practice, ezetimibe is indicated as monotherapy for patients who require modest LDL reduction or cannot tolerate other lipid-lowering agents. In combination therapy with a statin ezetimibe is used in patiens who cannot tolerate high statin doses or in those who need additional LDL reductions despite maximum statin doses.

Keywords: Key words: cholesterol absorption inhibitor, ezetimibe, hypercholesterolaemia, statins.

Published: January 1, 2006  Show citation