Experimental and clinical pharmacology: Thiazolidinediones - mechanisms of action

Abstract

The thiazolidinediones (or ‘glitazones’) are a new class of drugs for the treatment of type 2 diabetes. They bind avidly to peroxisome proliferator-activated receptor gamma in adipocytes to promote adipogenesis and fatty acid uptake (in peripheral but not visceral fat). By reducing circulating fatty acid concentrations and lipid availability in liver and muscle, the drugs improve the patient’s sensitivity to insulin. Thiazolidinediones favourably alter concentrations of the hormones secreted by adipocytes, particularly adiponectin. They increase total body fat and have mixed effects on circulating lipids.