Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Ezetimibe: a selective inhibitor of cholesterol absorption
Autore:
Catapano, AL;
Indirizzi:
Univ Studi Milano, Dipartimento Sci Farmacol, I-20133 Milan, Italy Univ Studi Milano Milan Italy I-20133 Sci Farmacol, I-20133 Milan, Italy
Titolo Testata:
EUROPEAN HEART JOURNAL SUPPLEMENTS
fascicolo: E, volume: 3, anno: 2001,
pagine: E6 - E10
SICI:
1520-765X(200106)3:E<E6:EASIOC>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
REMNANT LIPOPROTEINS; LIPASE INHIBITOR; ORLISTAT; SCH58235;
Keywords:
cholesterol absorption inhibitor; ezetimibe; pre-clinical studies; atherosclerosis; hypercholesterolaemia; statins;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Catapano, AL Univ Studi Milano, Dipartimento Sci Farmacol, Via G Balzaretti 9, I-20133 Milan, Italy Univ Studi Milano Via G Balzaretti 9 Milan ItalyI-20133 aly
Citazione:
A.L. Catapano, "Ezetimibe: a selective inhibitor of cholesterol absorption", EUR H J SUP, 3(E), 2001, pp. E6-E10

Abstract

Ezetimibe is a novel selective cholesterol absorption inhibitor that effectively blocks intestinal absorption of dietary and biliary cholesterol. Ezetimibe undergoes glucuronidation to a single metabolite and is localized inthe intestinal wall, where it prevents cholesterol absorption, Enterohepatic recirculation of ezetimibe and the glucuronide ensures repeated deliveryto the site of action and limits peripheral exposure. Ezetimibe does not affect the absorption of fat-soluble vitamins or triglycerides. Results frompre-clinical studies in various animal models have shown the lipid-lowering and anti-atherosclerotic properties of ezetimibe as a single agent. and asynergistic effect when combined with a statin. In cholesterol-fed rhesus monkeys, ezetimibe reduced both plasma cholesterol (ED50 = 0.0005 mg . kg(-1) . day(-1)) and low-density lipoprotein cholesterol levels in a dose-dependent manner. In apo E knockout mice, ezetimibe reduced serum cholesterol more than 50% and decreased carotid (97%) and aortic (47-87%) atherosclerosis. Ezetimibe inhibited the rise of plasma cholesterol in cholesterol-fed dogs (ED50 = 0.007 mg . kg(-1) . day(-1)). Co-administration of ezetimibe andlovastatin in chow-fed dogs synergistically reduced plasma cholesterol to levels lower than those achieved with either agent alone (P <0.05). These results suggest that ezetimibe combined with a statin may similarly reduce plasma cholesterol levels in patients with hypercholesterolaemia. (C) 2001 The European Society of Cardiology.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 19:16:39