Rosiglitazone chemical structure
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Avandia

Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. It is being marketed as Avandia® by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet®). Another combination drug approved by the FDA is Avandaryl® (with glimepiride). more...

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Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a pure ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone (Mohanty et al).

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Two New Drugs Can Improve Body's Insulin Use - Avandia and Actos - Brief Article
From FDA Consumer, 9/1/99

Two new drugs to treat Type II diabetes have received FDA approval.

Avandia (rosiglitazone) and Actos (pioglitazone) improve the body's ability to use the insulin it naturally produces. The body's resistance to insulin is suspected to be an important underlying cause of Type II diabetes.

Either drug can be used alone or in combination with certain other diabetes drugs. But, while Actos can be used in combination with insulin, Avandia is approved only for patients who are not on insulin.

Avandia and Actos are in the thiazolidinedione class of drugs. This class includes Rezulin (troglitazone), which was recently limited in use following reports of severe liver toxicity and deaths (see accompanying article).

No evidence of liver toxicity was seen in clinical trials of Avandia or Actos. However, because of the liver toxicity problems associated with Rezulin, FDA recommends that patients taking Avandia or Actos undergo liver toxicity tests at the start of therapy, every two months during the first year, and periodically thereafter. Symptoms of liver problems include unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, or jaundice (yellowish skin and eyes). Patients experiencing any of these should have a liver toxicity test.

Patients taking Avandia or Actos should follow a careful diet and maintain an appropriate weight.

Avandia is made by SmithKline Beecham, Philadelphia. Actos is made by Takeda Chemical Industries, Ltd., and will be co-promoted in the United States by Takeda Pharmaceuticals America, Inc., and Eli Lilly and Co.

COPYRIGHT 1999 U.S. Government Printing Office
COPYRIGHT 2004 Gale Group

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