Rosiglitazone

Rosiglitazone

Rosiglitazone ball-and-stick model

Avandia 2mg oral tablet

Rosiglitazone synthesis

Information about Rosiglitazone

Rosiglitazone is an insulin sensitizing agent and thiazolidinedione that is indicated for the treatment of type 2 diabetes.

Liver safety of Rosiglitazone

Rosiglitazone has been linked to rare instances of acute liver injury.

Mechanism of action of Rosiglitazone

Rosiglitazone (roe" si gli' ta zone) an insulin sensitizing agent that improves glucose control in patients with type 2 diabetes. Like other thiazolidinediones, it is thought to act by engagement of PPAR-? receptors which induce multiple genes involved in glucose and fatty acid metabolism. In clinical trials, rosiglitazone was found to lower blood glucose and HbA1c levels and had additive effects with the sulfonylureas and metformin.

FDA approval information for Rosiglitazone

Rosiglitazone was approved for use in the United States in 1999. While the initial thiazolidinedione – troglitazone – had been associated with high rates of serum aminotransferase elevations and multiple reports of severe liver injury and death from acute liver failure, rosiglitazone was associated with a lower rate of ALT elevations and with only rare instances of clinically apparent liver injury. Rosiglitazone is approved as an adjunct to diet and exercise in the glycemic control of patients with type 2 diabetes.

Dosage and administration for Rosiglitazone

Rosiglitazone is available as 2 and 4 mg tablets generically and under the brand name Avandia and the usual recommended dosage is 4 to 8 mg daily in two divided doses. Rosiglitazone is used as monotherapy as well as in combination with metformin, sulfonylureas or insulin.

Drug safety alert

In 2010, the FDA published a drug safety alert concerning the cardiovascular risks of rosiglitazone and the drug has been withdrawn in many countries of the world, because of these potential long term adverse effects. In the United States, it remains available but is recommended only for patients who are unable to achieve glycemic control with other diabetes medications.

• Dailymed label info on Rosiglitazone
• FDA Rosiglitazone