Rimonabant: an antagonist drug of the endocannabinoid system for the treatment of obesity.
Obesity, an ever-increasing problem in the industrialized world, has long been a target of research for a cure or, at least, control of its expansion. In the search for treatment, the recently discovered endocannabinoid system has emerged as a new target for controlling obesity and its associated conditions. The endocannabinoid system plays an important role in controlling weight and energy balance in humans. This system is activated to a greater extent in obese patients, and the specific blockage of its receptors is the aim of rimonabant, one of the most recent drugs created for the treatment of obesity. This drug acts as a blockade for endocannabinoid receptors found in the brain and peripheral organs that play an important role on carbohydrate and fat metabolism. Clinical studies have confirmed that, when used in combination with a low calorie diet, rimonabant promotes loss in body weight, loss in abdominal circumference, and improvements in dyslipidemia. Rimonabant is also being tested as a potential anti-smoking treatment since endocannabinoids are related to the pleasurable effect of nicotine. Thus, rimonabant constitutes a new therapeutic approach to obesity and cardiovascular risk factors. Studies show effectiveness in weight loss; however, side effects such as psychiatric alterations have been reported, including depression and anxiety. These side effects have led the FDA (Food and Drug Administration) to not approve this drug in the United States. For a more complete evaluation on the safety of this drug, additional studies are in progress.
Leite
Carlos E
CE
Toxicology Institute, Pontifical Catholic University of Rio Grande do Sul, Av. Ipiranga 6681, Prédio 12, Bloco D, Sala 140, CEP: 90619-900, Porto Alegre - RS, Brazil.
Mocelin
Clei A
CA
Petersen
Guilherme O
GO
Leal
Mirna B
MB
Thiesen
Flavia V
FV
D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology*; D063385:Cannabinoid Receptor Modulators / Q000037:antagonists & inhibitors*; D002986:Clinical Trials as Topic; D017277:Drug Approval; D063388:Endocannabinoids; D006801:Humans; D010880:Piperidines / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D011720:Pyrazoles / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D043884:Receptor, Cannabinoid, CB1 / Q000187:drug effects / Q000502:physiology; D043885:Receptor, Cannabinoid, CB2 / Q000187:drug effects / Q000502:physiology; D000077285:Rimonabant
D019440:Anti-Obesity Agents; D063385:Cannabinoid Receptor Modulators; D063388:Endocannabinoids; D010880:Piperidines; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D000077285:Rimonabant