Cor Vasa 2004, 45(9):452-456
How to reach the target levels of LDL-cholesterol? The place of ezetimibe in current cholesterol-lowering therapy
- III. interní klinika, Centrum preventivní kardiologie, Všeobecná fakultní nemocnice a 1. lékařská fakulta Univerzity Karlovy, Praha, Česká republika
At present, there is an adequate body of evidence indicating that the benefit of lipid lowering is dependent primarily on the maximal lipid-modifying effects of therapy. As regards LDL lowering, the following hypothesis applies: "The lower, the better". Despite this evidence, treatment protocols have failed to reach target levels recommended by US as well as European guidelines. The paper reviews some possible explanations as well as solutions to this situation. Combination therapy constitutes a rational approach to maximizing LDL lowering. Recently, the first cholesterol intestinal absorbtion inhibitor, ezetimibe (trade mark EZETROL) has been approved for clinical practice. Ezetimibe is usually used in combination with statins. The mode of action of this combination is "dual inhibition" which acts at two important sites of cholesterol production. Ezetimibe inhibits cholesterol absorbtion thereby enhancing cholesterol synthesis in hepatocytes. However, this increase is inhibited by the statin. This "dual effect" leads to a decrease in LDL-cholesterol by more than 50% when the starting (low) dose of a statin and the common 10 mg dose of ezetimibe are used, or as much as 60% if a higher dose of the statin is used.
Keywords: Ezetimibe; Statins; Combined lipid-lowering therapy; Target levels; LDL-cholesterol; Hypercholesterolemia
Published: September 1, 2004 Show citation