RESEARCH – September 2006

The endocannabinoid system receptor CB1 blocker – a new possibility in the management of metabolic syndrome


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The endocannabinoid system (EC) is a physiological system in the body responsible for controlling energy balance and breakdown of glucose and lipids and for regulating body weight.
The effects of the EC system on cells are mediated by CB1 receptors. Sustained food intake is associated with the chronic overactivity of the EC system in abdominal fat in the liver and in muscle, which leads to the dyslipidemia, and the insulin resistance. Overactivity of the EC system in the brain is associated with increased body weight and waist circumference. Through these mechanisms, the overactivity of the EC system is a significant risk factor for type 2 diabetes and cardiovascular diseases. Blocking of CB1 receptors in the brain and peripheral tissues has been hypothezided to result in a decrease in food intake, loss of body weight and improvements in cardiometabolic risk factors – blood sugar, HDL – cholesterol and triglycerides.Rimonabant (ACOMPLIA) is the first in a new class of drugs selectively blocking CB1 receptors in the brain, fat cells, liver and muscle.
In the Rimonabant in Obesity (RIO) phase III clinical trials are involved more than 6 600 patients. The programme included the following studies: RIO–Diabetes, RIO-Europe, RIO-Lipids and RIO North America. In these studies Rimonabant has been shown to improve a wide array of cardiometabolic risk factors as well as to promote sustained weight loss. Approximately half of observed improvement HDL-colesterol, triglycerides and HbA-1c in the patients who received ACOMPLIA was beyond that expected from weight loss alone. Use of ACOMPLIA for patients seeking to achieve weight loss for cosmetic reasons is not appropriate.