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rxlist.com (Glucophage ®) Keywords Rosiglitazone Trade Name: Avandia ® ( Currently not available in the US )(Avandia discontinued: Jan 10, 2024) Drug Class: oral hypoglycemic, thiazolidinedione (Tzd) derivatives, sometimes called “glitazones” Mechanism of Action: increases the body's sensitivity to insulin Their primary action is the nuclear regulation of genes involved in glucose & lipid metabolism and adipocyte differentiation Glitazones are ligands of the peroxisome peroliferator-activated receptor gamma (PPAR-γ) part of the steroid and thyroid superfamily of nuclear receptors PPAR-γ receptors are found in muscle, liver and fat PPAR-γ regulates the expression of genes involved in lipid and glucose metabolism, insulin signal transduction, and adipocyte differentiation In persons with diabetes, a major site of TZD action is (see Figure) adipose tissue Because the actions of these drugs involves changes in gene expression, they have a slow onset of therapeutic action , requiring weeks or even months to achieve maximal effect Figure
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