Rosiglitazone

Rosiglitazone, a thiazolidinedione antidiabetic agent, improves insulin res istance, a key underlying metabolic abnormality in most patients with type 2 (non-insulin-dependent) diabetes mellitus. In animal models of insulin re sistance, rosiglitazone decreased plasma glucose, insulin and triglyceride levels and also attenuated or prevented diabetic nephropathy and pancreatic islet cell degeneration. In contrast with troglitazone, rosiglitazone does not induce cytochrome P45 03A4 metabolism. It does not interact significantly with nifedipine, oral c ontraceptives, metformin, digoxin, ranitidine or acarbose. In clinical trials in patients with type 2 diabetes mellitus, rosiglitazone 2 to 12 mg/day las a single daily dose or 2 divided daily doses improved g lycaemic control, as shown by decreases In fasting plasma glucose and glyco sylated haemoglobin Addition of rosiglitazone 2 to 8 mg/day to existing sulphonylurea, metformi n or insulin therapy achieved further reductions in fasting plasma glucose and HbA(1c). Oral combinations Improved insulin sensitivity and p-cell func tion according to a homeostasis model assessment. Consistent with its mechanism of action, rosiglitazone appears to be associ ated with a low risk of hypoglycaemia (<2% of patients receiving monotherap y). There is no evidence to date that rosiglitazone shares the hepatotoxici ty of troglitazone.