<p>Combination of two antidiabetic agents with different mechanisms of action to improve glycemic control in patients with type 2 diabetes: Rosiglitazone maleate, a member of the thiazolidinedione class, and Metformin hydrochloride, a member of the biguanide class. Thiazolidinediones are insulin sensitizing agents that act primarily by enhancing peripheral glucose utilization, whereas biguanides act primarily by decreasing endogenous hepatic glucose production.<br />
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Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator&ndash;activated receptor-gamma (PPAR&gamma;). Activation of PPAR&gamma; nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In addition, PPAR&gamma;-responsive genes also participate in the regulation of fatty acid metabolism.<br />
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The pharmacologic mechanism of action of Metformin is different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and increases peripheral glucose uptake and utilization. Unlike sulfonylureas, With Metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin&nbsp;response may actually decrease.</p>