Ezetrol® (Ezetimibe) is the first substance of a new class of selective cholesterol absorption inhibitors; it was registered in Switzerland in 2002. Ezetimibe is glucuronidised and recirculated in the enterohepatic circulation. It acts exclusively in the intestinal lumen, but has no effect on the absorption of bile acids and liposoluble vitamins. When given as monotherapy, the standard dose of 10 mg/day lowers the serum LDL cholesterol by about 15–20%. Combined therapy with statins is particularly useful, because in this way the adaptive increase in cholesterol synthesis is prevented; with this combination, the LDL cholesterol level can be lowered by up to 58%. The effect of ezetimibe is also pronounced in combination with low doses of statins. In contrast to the bile acid binders, ezetimibe slightly lowers the triglycerides and slightly raises the HDL cholesterol level. Other combinations have not been investigated in detail; up till now, side effects and drug interactions have scarcely been observed. Ezetimibe is suitable for use in the treatment of primary hypercholesterolaemia, in which monotherapy with statins has an inadequate effect on the target LDL cholesterol values. This is the case especially with severe familial (genetic) hypercholesterolaemia and/or hypercholesterolaemia in which treatment with statins has led to side effects or intolerance. Long-term studies with ezetimibe, investigating the cardiovascular morbidity or other long-term effects, have not been carried out to date.

Journal Section:
Review
Keywords:
Hypercholesterolaemia, Statins, Cholesterol absorption, Sitosterolaemia
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© 2003 S. Karger AG, Basel
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2004
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