Ezetimibe (IPA: ) is an anti-hyperlipidemic medication which is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. It may be used alone when other cholesterol-lowering medications are unable to be tolerated, or together with statins (e.g. ezetimibe/simvastatin) when cholesterol levels are unable to be controlled on statins alone. It is marketed by Schering-Plough and Merck under the trade names Ezetrol, Zetia and Ezemibe.
Pharmacology
Ezetimibe localises at the
brush border of the
small intestine, where it inhibits the absorption of
cholesterol from the diet. Specifically, it appears to bind to the
Niemann-Pick C1-Like 1 (NPC1L1) protein on the
gastrointestinal tract epithelium, a critical mediator of cholesterol absorption.
[Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, et al. The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1). Proc Natl Acad Sci U S A 2005;102(23):8132-7. PMID 15928087] In addition to this direct effect, decreased cholesterol absorption leads to an increase in
LDL-cholesterol uptake into cells, thus decreasing levels in the
blood plasma.
Clinical use
Indications
Ezetimibe is indicated as an adjunct to dietary measures in the management of:
More on
[ Ezetimibe ]
Zetia (Ezetimibe) - Manufacturer's information for consumers and healthcare professionals including prescribing information in PDF format.
Zetia Consumer Information - Brief FAQ on Zetia from the FDA
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