Rimonabant--a selective CB1 antagonist.
OBJECTIVE
To review the pharmacology, pharmacokinetics, clinical efficacy, and safety of rimonabant, a new selective cannabinoid receptor antagonist.


METHODS
Primary literature and review articles were obtained via a MEDLINE search (1966-November 2004) using the key terms obesity, smoking cessation, cannabinoid, rimonabant, SR 141716, and SR 141716a. Additional studies and abstracts were identified from the bibliographies of reviewed literature.


METHODS
Studies and review articles related to rimonabant and the endocannabinoid system were reviewed. Data pertinent to this article were included.


RESULTS
Rimonabant is a selective cannabinoid receptor antagonist. Recent data have demonstrated beneficial effects of rimonabant in obesity, smoking cessation, and metabolic syndrome. Animal studies using rimonabant have shown a positive role for reducing hunger, caloric intake, and body weight and in increasing satiety. In humans, rimonabant appears to be effective for treatment of obesity and smoking cessation. Ongoing studies will examine the effect of rimonabant on obesity, metabolic syndrome, smoking cessation, and alcohol abuse. To date, the incidence of adverse effects with rimonabant has been slightly greater than placebo, with the most common being nausea.


CONCLUSIONS
Rimonabant appears to be a promising drug in an entirely new class called selective cannabinoid CB1 receptor antagonists. The drug may be approved for treatment of obesity and smoking cessation in 2005. Additional studies are ongoing that may provide information on other clinical uses for this medication.
Boyd
Steven Thomas
ST
Department of Pharmacy Practice, School of Pharmacy and Health Professionals, Creighton University, Omaha, NE 67178-0401, USA. sboys@creighton.edu
Fremming
Brad Allen
BA
D000818:Animals; D015507:Drugs, Investigational / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010880:Piperidines / Q000494:pharmacology* / Q000627:therapeutic use; D011720:Pyrazoles / Q000494:pharmacology* / Q000627:therapeutic use; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000077285:Rimonabant
D015507:Drugs, Investigational; D010880:Piperidines; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D000077285:Rimonabant