The TZD class of antidiabetic agents, including rosiglitazone canadian and pioglitazone generic, enhances glycemic control by improving insulin sensitivity in the peripheral tissues by selectively activating the peroxisome proliferator-activated receptor (PPAR)-gamma and by inhibiting hepatic gluconeogenesis. The TZDs are used in the management of type-2 diabetes mellitus and depend on the presence of insulin for their mechanism of action.
It is available as 15-, 30-, and 45-mg tablets; rosi-glitazone is available as 2-, 4-, and 8-mg tablets. PPAR receptors are found in tissues that play a role in insulin action, such as in adipose tissue, skeletal muscle, and the liver. Activation of PPAR-gamma nuclear receptors modulates the transcription of a number of insulin-responsive genes involved in the control of glucose and lipid metabolism.
In animal models of diabetes, both of these TZDs reduce the hyperglycemia, hyperinsulinemia, and hypertriglyceridemia that are characteristic of insulin-resistant states such as type-2 diabetes. In animal models, rosiglitazone’s antidiabetic activity has been shown to be mediated by increased sensitivity to insulin’s action in the liver, muscle, and fat. The expression of the insulin-regulated glucose transporter GLUT-4 is increased in adipose tissue. Rosiglitazone drug does not induce hypoglycemia in animal models with type-2 diabetes or with impaired glucose tolerance.