What is the role of cannabinoid-receptor antagonists in the treatment of obesity?

Updated: Jun 09, 2021
  • Author: Osama Hamdy, MD, PhD; Chief Editor: Romesh Khardori, MD, PhD, FACP  more...
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The central cannabinoid system has an increasingly recognized role in appetite and feeding disorders. [169, 170, 171, 172] In particular, activation of the cannabinoid type 1 (CB1) receptor is associated with increased appetite and appears to be the basis for the effectiveness of dronabinol in enhancing diet in patients with acquired immunodeficiency syndrome (AIDS) and other wasting syndromes.

CB1-receptor antagonists showed great potential for weight management in several human trials. Rimonabant, the most-developed CB1-receptor antagonist, caused a mean weight loss of 3-6 kg over a 1-year follow-up at doses of 5-20 mg/day. Adverse effects, which were most prevalent at high doses, included dizziness, depression and suicidal ideation, headaches, nausea, vomiting, and diarrhea. The drug was rejected by the FDA because of side effects of depression and suicidal ideation; in Europe, it was approved but later recalled.

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