PMID: 12773075May 30, 2003Paper

Ezetimibe for management of hypercholesterolemia

The Annals of Pharmacotherapy
Vincent F Mauro, Chad E Tuckerman

Abstract

To review the primary literature describing the pharmacology of ezetimibe and clinical trials investigating its use in the management of hypercholesterolemia. A MEDLINE search (1966-December 2002) was performed using SCH 48461, SCH 58235, ezetimibe, and 2-azetidinone as key words. English-language articles were identified and the references of these articles were used to further identify pertinent articles and abstracts. Given the paucity of published articles available on ezetimibe, many of the references cited are abstracts. All acquired articles that discussed the pharmacology, pharmacokinetics, chemistry, and clinical efficacy of ezetimibe were reviewed. Articles were selected based on content regarding the medicinal chemistry, pharmacology, and clinical use of ezetimibe. Ezetimibe, approved for use in October 2002, belongs to a new class of antihyperlipidemic agents that uniquely inhibit the absorption of cholesterol by inhibiting the cholesterol transport system located within intestinal cell walls. In humans, ezetimibe reduced cholesterol absorption by >50%. In clinical trials, ezetimibe 10 mg/d reduced low-density lipoprotein cholesterol (LDL-C) by approximately 18% and further enhanced the LDL-C-lowering effect of stat...Continue Reading

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Citations

Aug 16, 2014·International Journal of Pharmaceutical Investigation·Kiran ThadkalaJithan Aukunuru
Sep 16, 2006·Heart·Pathmaja Paramsothy, Robert Knopp
Jul 24, 2010·American Journal of Physiology. Gastrointestinal and Liver Physiology·Li YangPatrick Tso
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