Repaglinide
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Drugs 2001; 61 (11): 1625-1660 0012-6667/01/0011-1625/$27.50/0 © Adis International Limited. All rights reserved.
Repaglinide A Review of its Therapeutic Use in Type 2 Diabetes Mellitus Christine R. Culy and Blair Jarvis Adid International Limited, Auckland, New Zealand Various sections of the manuscript reviewed by: R.B. Goldberg, Diabetes Research Institute, University of Miami School of Medicine, Miami, Florida, USA; G.D. Johnston, Department of Therapeutics and Pharmacology, The Queen’s University of Belfast, Belfast, Northern Ireland; R. Landgraf, Diabetes Center, Department of Internal Medicine, University of Munich, Germany; W.J. Malaisse, Laboratory of Experimental Medicine, Brussels Free University, Brussels, Belgium; T.C. Marbury, Orlando Clinical Research Center, Orlando, Florida, USA; A.D. Mooradian, Department of Internal Medicine, St Louis University Medical School, St Louis, Missouri, USA; R. Moses, Department of Biomedical Science, University of Wollongong, Wollongong, New South Wales, Australia. Data Selection Sources: Medical literature published in any language since 1966 on repaglinide, identified using AdisBase (a proprietary database of Adis International), Medline and EMBASE. Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug. Search strategy: AdisBase search terms were ‘repaglinide’ or ‘NN 623’. Medline search terms were ‘repaglinide’ or ‘NN 623’. EMBASE search terms were ‘repaglinide’ or ‘NN 623’. Searches were last updated 16 August, 2001. Selection: Studies in patients with type 2 diabetes mellitus who received repaglinide. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included. Index terms: Type 2 diabetes mellitus, noninsulin-dependent, repaglinide, pharmacodynamics, pharmacokinetics, therapeutic use, hypoglycaemia.
Contents Summary . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2. Pharmacodynamic Properties . . . . . . . . . . . . . . . . . . . . . . . . . . . 2.1 Cellular Mechanism of Action . . . . . . . . . . . . . . . . . . . . . . . . 2.2 Glucose-Lowering and Insulinotropic Effects . . . . . . . . . . . . . . . . 2.2.1. In Vitro and Animal Studies . . . . . . . . . . . . . . . . . . . . . . 2.2.2 In Healthy Volunteers . . . . . . . . . . . . . . . . . . . . . . . . . . 2.2.3 In Patients with Type 2 Diabetes Mellitus: Dose-Response Studies . 2.2.4 In Patients with Type 2 Diabetes Mellitus: Dose-Regimen Studies . 3. Pharmacokinetic Properties . . . . . . . . . . . . . . . . . . . . . . . . . . . . 3.1 Absorption and Distribution . . . . . . . . . . . . . . . . . . . . . . . . . . 3.2 Metabolism and Excretion . . .
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