About Pioglitazone Thiazolidinedione (TZD) derivative, Insulin Sensitizer, Oral anti diabetic. Mechanism of Action of Pioglitazone The drug exerts antidiabetic action by acting as a selective agonist for the nuclear "peroxisome proliferator-activated receptor Gama (PPAR Gama)- which enhances the transcription of several insulin responsive genes. It reverses insulin resistance by stimulating GLUT4 (glucose transporter 4) expression and translocation and improves entry of glucose in to muscle and adipose tissue. It also suppresses hepatic gluconeogenesis. Activation of genes regulating fatty acid metabolism and lipogenesis in adipose tissue also contributes to the insulin sensitizing action of drug. It reduces blood glucose and HbA1c- improves glycaemic control and lowers circulating levels of Insulin. It also raises HDL level and lowers serum triglyceride level without significant change in LDL level.