Clinical profile of glimepiride.

In order to achieve appropriate blood glucose control, the treatment of non-insulin dependent (NIDDM) Type II diabetes usually starts with diet and exercise. If this still results in insufficient metabolic control, oral hypoglycaemic drugs or insulin are added to the non-pharmacological measures. Sulphonylureas have been used successfully as oral hypoglycaemic agents since the 1950s but there are aspects where medication could be better adjusted to the patients' needs. Preclinical investigations on animals and in vitro studies with glimepiride (HOE490), a new sulphonylurea, suggested some benefit over sulphonylureas currently available, including lower dosage, rapid onset and long duration of action, lower insulin and C-peptide levels, possibly due to less stimulation of insulin secretion and more pronounced extrapancreatic effects. The clinical relevance of these findings were studied in clinical trials. 19 phase II and 4 phase III clinical studies, in a total of about 3750 Type II diabetic patients, established efficacy and safety of glimepiride in comparison to placebo and glibenclamide and showed its therapeutic value. 1 mg per day induced a marked blood glucose reduction (FPG 2.4 mmol/l; HbA1c 1.2%) which could be enhanced by increasing the dose to the maximum effective 4 and 8 mg daily. In patients, glimepiride had a more rapid onset of action than glibenclamide, with a long duration of action. Glimepiride achieved metabolic control with the lowest dose (1-8 mg daily) of all the sulphonylureas. In addition, it maintained a more physiological regulation of insulin secretion than glibenclamide during physical exercise, suggesting that there may be less risk of hypoglycaemia with glimepiride.(ABSTRACT TRUNCATED AT 250 WORDS)