Authors: Filippatos, T. D.; Mikhailidis, D. P.

Source: Current Pharmaceutical Design, Volume 15, Number 5, February 2009 , pp. 490-516(27)

Publisher: Bentham Science Publishers

Abstract:

This review considers the hypolipidaemic drugs that act on the gastrointestinal (GI) tract. We searched PubMed up to April 2008 and included randomized controlled trials, original papers, review articles and case reports. Bile acid sequestrants (BAS) have a well-established low density lipoprotein cholesterol (LDL-C) lowering effect, but may increase triglyceride (TG) levels. BAS have no systematic adverse effects, but are associated with increased GI adverse effects and interactions with the absorption of other drugs. Ezetimibe improves LDL-C, high density lipoprotein cholesterol and TG levels, as monotherapy or especially when given with a statin. Ezetimibe has not been associated with serious adverse effects. Ezetimibe has not been evaluated in large clinical trials with cardiovascular disease (CVD) endpoints. Phytosterols are not licensed drugs; they have a well-established LDL-C lowering effect, but there are no large long-term randomized clinical trials investigating their effects on CVD events. Orlistat is an antiobesity drug with a small additional LDL-C lowering effect independent of weight loss. Orlistat-assisted weight loss improves the overall lipid profile, carbohydrate metabolism and transaminase activities. However, its use should be limited to weight reduction. This drug is associated with increased GI adverse effects.

Keywords: Colestyramine; colestipol; colesevelam; colestimide; ezetimibe; phytosterols; orlistat; low density lipoprotein cholesterol

Document Type: Research article

DOI: http://dx.doi.org/10.2174/138161209787315738

Affiliations: 1: Department of Clinical Biochemistry (Vascular Disease Prevention Clinics), Royal Free Hospital campus, University College London (UCL), Pond Street, London NW3 2QG, UK.

Publication date: 2009-02-01

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• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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