Discover

'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 not 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'. Ezetimibe was originally discovered by a team of four Schering-Plough research chemists; Drs. Stuart B. Rosenblum, Duane A. Burnett, John W. Clader and Brian A. McKittrick.

Contents

Pharmacology

Clinical use

Indications

Adverse effects

Dosage forms

References

See also

External links

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 a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells^[1] as well as in hepatocytes^[2]. 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:

★ Hypercholesterolaemia

★ Homozygous sitosterolaemia (phytosterolaemia)^[3]
On 9 June 2006, U.S. regulators approved the use of ezetimibe in combination with fenofibrate to treat mixed hyperlipidaemia.

Adverse effects

Common adverse drug reactions (≥1% of patients) associated with ezetimibe therapy include: headache and/or diarrhea. Infrequent adverse effects (0.1–1% of patients) include: myalgia and/or raised liver function test (ALT/AST) results. Rarely (<0.1% of patients), hypersensitivity reactions (rash, angioedema) or myopathy may occur.³

Dosage forms

Ezetimibe is available as 10 mg tablets in most markets, with 5 mg and 20 mg tablets also being available on the U.S. market. A combination preparation ezetimibe/simvastatin, which combines ezetimibe with a statin, is also available.

References

1. 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
2. Temel, Ryan E., Tang, Weiqing, Ma, Yinyan, Rudel, Lawrence L., Willingham, Mark C., Ioannou, Yiannis A., Davies, Joanna P., Nilsson, Lisa-Mari, Yu, Liqing.
Hepatic Niemann-Pick C1-like 1 regulates biliary cholesterol concentration and is a target of ezetimibe
J. Clin. Invest. 2007 0: JCI30060
3. Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3

See also

★ Ezetimibe/simvastatin

★ Statin

External links

★ U.S. Prescribing Information