Wednesday 28 December 2011

CARDIOMETABOLIC RISK FACTORS AND ITS IMPACT ON CB1 RECEPTOR BLOCKAGE

 Rimonabant, the first selective CB (1) receptor antagonist in clinical use, has been extensively investigated in the rimonabant in Obesity (RIO) programme, comprising rimonabant 20 mg daily consistently reduced body weight, waist circumference, triglycerides, blood pressure, insulin resistance and creactive protein levels, and increased HDL cholesterol concentrations in both non-diabetic and type-2 diabetic overweight/obese patients. Adiponectin levels were increased, an affect that correlated with HDL cholesterol augmentation, while small dense LDL cholesterol levels were decreased in patients receiving rimonabant 20 mg compared with those receiing placebo in RIO Lipids. Furthermore, in RIO Diabetes, a 0.7% reduction in glycated haemoglobin (HbA1c) levels was observed in metformin or sulphonylurea-treated patients with type-2 diabetes. Almost half of metabolic changes occurred beyond weight loss, in agreement with direct peripheral effects. Rimonabant was mostly well-tolerated, but with a slightly higher incidence of depressed mood disorders, anxiety, nausea and dizziness compared with placebo. Overweight/obese subjects with cardiometabolic risk factors and with no major depressive illness and/or ongoing anti depressive treatment, in order to both maximise efficacy and minimise safety issues.

No comments:

Post a Comment