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Pharmacology: Pharmacodynamics: Ezetimibe, a cholesterol absorption inhibitor, is an antilipemic agent that differs chemically and pharmacologically from other currently available antilipemic agents. Following absorption, the drug localizes at the brush border of the small intestine and inhibits absorption of cholesterol, resulting in decreased delivery of intestinal cholesterol to the liver. This causes a reduction in hepatic cholesterol stores, a compensatory increase in hepatic uptake of cholesterol from systemic circulation, and consequently, an increase in systemic clearance of cholesterol. Ezetimibe does not appear to inhibit hepatic cholesterol synthesis or increase bile acid excretion.
Pharmacokinetics: Ezetimibe is rapidly absorbed when given orally and undergoes extensive conjugation in the small intestine and liver to an active glucuronide metabolite. Both ezetimibe and the glucuronide are more than 90% bound to plasma proteins. Ezetimibe is excreted primarily in the faeces via bile and undergoes enterohepatic recycling. After an oral dose, about 78% is excreted in the faeces, mainly as ezetimibe, and about 11% is excreted in the urine, mainly as the glucuronide. The elimination half-life for both ezetimibe and the glucuronide is about 22 hours.
