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Published Online, 8 March 2005, www.theannals.com, DOI 10.1345/aph.1E499.
The Annals of Pharmacotherapy: Vol. 39, No. 4, pp. 684-690. DOI 10.1345/aph.1E499
© 2005 Harvey Whitney Books Company.
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NEW DRUG DEVELOPMENTS

Rimonabant—A Selective CB1 Antagonist

Steven Thomas Boyd, PharmD BCPS CDE CDM

Assistant Professor, School of Pharmacy and Health Professionals, Creighton University, Omaha, NE

Brad Allen Fremming, PharmD

Captain, USAF, BSC, Chief, Inpatient Pharmacy Services, Offutt Air Force Base, NE

Reprints: Dr. Boyd, Department of Pharmacy Practice, School of Pharmacy and Health Professions, Creighton University, 2500 California Plaza, Omaha, NE 68178-0401, fax 402/280-1268, sboyd{at}creighton.edu

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

DATA SOURCES: 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.

STUDY SELECTION AND DATA EXTRACTION: Studies and review articles related to rimonabant and the endocannabinoid system were reviewed. Data pertinent to this article were included.

DATA SYNTHESIS: 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.

Key Words: endocannabinoid, obesity, rimonabant, smoking cessation

Published Online, March 8, 2005. www.theannals.com, DOI 10.1345/aph.1E499


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