Rosiglitazone is an antihyperglycemic agent. It helps the body respond better to insulin and it reduces the amount of sugar produced by the liver. It can help control blood sugar levels. Rosiglitazone is used, along with diet and exercise, in the treatment of non-insulin-dependent diabetes mellitus (type II diabetes). Rosiglitazone may also be used with a sulfonylurea (e.g., Diabeta, Glucotrol, Micronase, others), metformin (Glucophage), or insulin when diet and exercise plus any one of these medicines alone do not result in adequate blood sugar control. Rosiglitazone is mainly used for patients with the type 2 variety of diabetes. In addition to decreasing blood/sugar levels in patients, Rosiglitazone has also been shown to lower triglyceride and insulin levels. It also has been accredited to stop a certain disease in the kidney, cell nephropathy.
Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity while reducing circulating insulin levels. Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator–activated receptor-gamma (PPAR). In humans, PPAR receptors are found in key target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In addition, PPAR-responsive genes also participate in the regulation of fatty acid metabolism.
By targeting this resistance at the cellular level, Rosiglitazone attaches itself to specific protein receptors called the peroxisome proliferator activated receptor (PPAR)g receptor, which in turn attach themselves to specific base sequences in DNA which causes amongst other things, proteins to be produced that help lower the production of glucose, or raise the sensitivity to insulin, this depends on where the proteins are situated. The cell will then take more glucose in, and therefore lower the amount of sugar in the bloodstream.