Rimonabant: A novel selective cannabinoid-1 receptor antagonist

Rimonabant: A novel selective cannabinoid-1 receptor antagonist for treatment of obesity

American Journal of Health-System Pharmacy, Vol. 64, Issue 5, 481-489


PRITI N. PATEL, PHARM.D., BCPS, is Assistant Clinical Professor, College of Pharmacy and Allied Health Professions, and Director, Drug Information Center, St. John’s University, Queens, NY. ROLEE PATHAK, PHARM.D., BCPS, is Clinical Assistant Professor, Ernest Mario College of Pharmacy, Rutgers University, Piscataway, NJ, and Clinical Coordinator, Englewood Hospital and Medical Center, Englewood, NJ.

Purpose. The pharmacology, pharmacokinetics, clinical efficacy, safety, drug interactions, and dosage and administration of rimonabant in the treatment of obesity and related metabolic factors are reviewed.

Summary. Discovery of the cannabinoid receptors has led to the development of rimonabant, a cannabinoid-1 (CB1) antagonist. Selective blockade of this receptor has been shown to lead to decreased appetite and food intake in animal models. Clinical studies have shown that rimonabant 20 mg once daily produces significant decreases in weight and waist circumference in obese human subjects and improves the lipid profile and glucose control. The frequency of metabolic syndrome also decreased significantly with rimonabant 20 mg daily. Limited data are available regarding the pharmacokinetics and pharmacodynamics of rimonabant. Preclinical data have demonstrated a long duration of action. As of yet, no drug–drug, drug–food, or drug– disease interactions have been identified with rimonabant. Adverse reactions occurred rarely, with nausea, dizziness, diarrhea, arthralgia, and back pain being the most common. Psychiatric disorders, including depression and anxiety, were the most common reasons for subjects to withdraw from rimonabant studies. Rimonabant has been shown to be safe for up to two years of treatment. Further research will clarify currently unknown areas, including pharmacokinetics, drug interactions, and the drug’s role in standard therapy.

Conclusion. Rimonabant, a selective CB1 antagonist, is a novel treatment option for obese and overweight individuals. Significant weight loss, decrease in waist circumference, and improvements in lipid profile and glucose control have been shown in clinical trials of rimonabant.