A review of rosiglitazone in type 2 diabetes mellitus

The thiazolidinedione rosiglitazone maleate works primarily to improve insu lin sensitivity in muscle and adipose tissue. It may have additional pharma cologic effects, however, as its main target is peroxisome proliferator-act ivated receptor-gamma. Data using the homeostasis model assessment and proi nsulin: insulin ratio in patients with type 2 diabetes mellitus suggest tha t rosiglitazone may have the potential to sustain or improve beta -cell fun ction. In these patients the drug reduces fasting plasma glucose, glycosyla ted hemoglobin, insulin, and C-peptide. In clinical trials, rosiglitazone m onotherapy significantly reduced glycosylated hemoglobin by 1.5% compared w ith placebo and led to significant improvements in glycemic control when gi ven in combination with metformin, sulfonylureas, or insulin. A dosage of 4 mg twice/day significantly reduced fasting plasma glucose levels and produ ced comparable reductions in glycosylated hemoglobin compared with glyburid e. Rosiglitazone has a low risk of gastrointestinal side effects and hypogl ycemia, reduced insulin demand, potential sparing effects on beta -cells, a nd favorable drug interaction profile. Adverse events of clinical significa nce are edema, anemia, and weight gain. Premarketing data indicate no signi ficant difference in liver enzyme elevations for rosiglitazone, placebo, or active controls. Another drug in the thiazolidinedione class, troglitazone , was associated with idiosyncratic hepatotoxicity and was removed from the market. Therefore, until long-term data are available for rosiglitazone, l iver enzyme monitoring is recommended.