rosiglitazone

Rosiglitazone is an oral thiazolidinedione antidiabetic medication that acts as a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist. By activating PPAR-γ, it improves insulin sensitivity in adipose tissue, skeletal muscle, and the liver, helping to lower blood glucose levels in adults with type 2 diabetes. It is used as monotherapy or in combination with other antidiabetic agents when glycemic control is insufficient with diet and exercise alone.

Rosiglitazone's role in therapy has been substantially affected by safety concerns. Evidence from cardiovascular outcome analyses led to regulatory actions in many countries, restricting use due to reported risks of myocardial infarction and death from cardiovascular causes. Consequently, access to rosiglitazone has been limited, with some regions removing it from the market entirely and others allowing only restricted use for patients who have not achieved adequate control with other therapies and for whom potential benefits outweigh risks. It is generally no longer considered a first-line agent.

Common adverse effects include edema and fluid retention, weight gain, and an increased risk of heart failure. Long-term use is associated with a higher risk of fractures, particularly in women. Liver toxicity is monitored with care, although severe hepatic injury is relatively rare. Contraindications include symptomatic heart failure and significant hepatic impairment; caution is advised during dosing and in patients with cardiovascular or hepatic comorbidity. Pharmacokinetically, rosiglitazone is absorbed orally, extensively metabolized in the liver primarily by CYP2C8 to active metabolites, and is excreted mainly via the bile.

Historically developed by GlaxoSmithKline and marketed as Avandia, rosiglitazone's clinical use has diminished substantially amid safety concerns and regulatory restrictions.