thiazolidinedioner

Thiazolidinediones, often abbreviated as TZDs or glitazones, are a class of antidiabetic drugs used in the management of type 2 diabetes mellitus. They function by improving insulin sensitivity in peripheral tissues such as muscle and fat, and in the liver. This action helps to lower blood glucose levels. TZDs are agonists of the peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor that regulates the expression of genes involved in glucose and lipid metabolism. By binding to PPARγ, TZDs promote the transcription of genes that enhance insulin signaling.

The development of TZDs marked a significant advancement in the treatment of type 2 diabetes, offering a mechanism of action distinct from other antidiabetic agents like sulfonylureas or metformin. Common side effects associated with TZDs include weight gain, fluid retention, and an increased risk of bone fractures. There have also been concerns regarding potential cardiovascular risks, though research on this aspect has yielded mixed results.

Currently, two TZDs are approved for use in the United States: pioglitazone and rosiglitazone. However, rosiglitazone's use has been significantly restricted due to concerns about cardiovascular safety. TZDs are typically administered orally and are often used in combination with other antidiabetic medications when monotherapy is insufficient to achieve glycemic targets. They are not recommended for patients with type 1 diabetes or diabetic ketoacidosis. The long-term benefits and risks of TZD therapy continue to be a subject of ongoing clinical investigation.