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Rimonabant.

Abstract
Rimonabant is the first of a new class of selective cannabinoid receptor-1 blockers. It reduces the overactivity of the endocannabinoid system, improving lipid and glucose metabolism and regulating food intake and energy balance. In four randomised, double-blind clinical trials in overweight or obese adults with or without type 2 diabetes and/or dyslipidaemia, oral rimonabant 20mg once daily reduced weight and waist circumference to a significantly greater extent than placebo. A significantly greater proportion of rimonabant than placebo recipients achieved the clinically significant weight-loss target of > or =5% or > or =10% of initial weight. Rimonabant was associated with significant improvements in glycaemic control relative to placebo, with approximately equal to 57% of the reduction in glycosylated haemoglobin being independent of the effects of weight loss in one trial. Improvements in other cardiometabolic risk factors (i.e. increases in high-density lipoprotein-cholesterol [HDL-C] and decreases in triglyceride [TG] levels) were significantly greater with rimonabant than with placebo. The improvement in lipid profile also demonstrated a weight-independent effect, with approximately equal to 47-58% of the improvement in HDL-C and TG being beyond that expected through weight loss alone. Rimonabant was generally well tolerated, with most adverse events considered mild to moderate in severity.
AuthorsSheridan Henness, Dean M Robinson, Katherine A Lyseng-Williamson
JournalDrugs (Drugs) Vol. 66 Issue 16 Pg. 2109-19; discussion 2120-1 ( 2006) ISSN: 0012-6667 [Print] New Zealand
PMID17112304 (Publication Type: Journal Article)
Chemical References
  • Anti-Obesity Agents
  • Blood Glucose
  • Piperidines
  • Pyrazoles
  • Receptor, Cannabinoid, CB1
  • Rimonabant
Topics
  • Adult
  • Animals
  • Anti-Obesity Agents (pharmacokinetics, pharmacology, therapeutic use)
  • Blood Glucose (metabolism)
  • Clinical Trials as Topic
  • Diet, Reducing
  • Drug Approval
  • Europe
  • Humans
  • Obesity (drug therapy)
  • Piperidines (adverse effects, pharmacokinetics, pharmacology, therapeutic use)
  • Pyrazoles (adverse effects, pharmacokinetics, pharmacology, therapeutic use)
  • Receptor, Cannabinoid, CB1 (antagonists & inhibitors)
  • Rimonabant

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