Inhibits sterol transporter at brush border and, consequently, intestinal absorption of cholesterol, which in turn decreases delivery of cholesterol to the liver and reduces hepatic cholesterol stores. Ezetimibe has a unique mechanism of action compared to other classes of lipid-lowering agents. Ezetimibe does not, however, affect triglyceride absorption. NPC1L1 (Niemann-Pick C1-Like 1) is a protein that transports sterols and cholesterol across the gut lining and absorbs them in the body [15, 16, 17]. Zetia binds to NPC1L1 and blocks the absorption of cholesterol and plant sterols in the intestine. In a 2-week clinical study in 18 hypercholesterolemic patients, ZETIA inhibited intestinal cholesterol absorption by 54%, compared with placebo. 12.1 Mechanism of Action. It inhibits the absorption of dietary and biliary cholesterol decreasing the intestinal absorption by 54%. 2 Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. Since less cholesterol is absorbed, less of it is delivered to the liver. Yolanda. After graduating in Pharmacy in Australia, she moved to Italy to study the Mediterranean way of life and continue learning about health and medicine. Mechanism of Action. Peak plasma time: 4-12 hr (parent drug); 1-2 hr (metabolite) Mechanism of Action. Absorption. Yolanda is a passionate medical writer who loves to help people understand how health and different treatments work. Bioavailability: Variable. ZETIA is an inhibitor of intestinal cholesterol (and related phytosterol) ... 12.1 Mechanism of Action 12.2 Pharmacodynamics 12.3 Pharmacokinetics 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility 13.2 Animal Toxicology and/or Pharmacology .


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