Repaglinide - a new compound for the treatment of patients with type 2 diabetes

Repaglinide is a new oral blood glucose lowering agent, a member of the car bamoylmethyl benzoic acid (CMBA) family. Its mechanism of action is partly similar to that of the sulphonylurea: the release of insulin from the pancr eatic beta cells is stimulated by closure of ATP-dependent potassium channe ls. However, repaglinide regulates these channels via a different binding s ite on the beta cell than glibenclamide, and the drug does not cause insuli n release in the absence of glucose, or during voltage-clamping. After oral administration the drug is rapidly absorbed and eliminated. It i s therefore used in a meal-related dosing regimen; repaglinide is taken wit h each main meal. This meal-related use may give a more physiological mimic k of daytime insulin requirement than once-daily or twice-daily use of sulp honylurea. Patients using repaglinide are less likely to develop hypoglycae mic symptoms when they miss or postpone a meal in comparison with patients on glibenclamide treatment. In long-term comparative phase 3 clinical studi es it was found that repaglinide is equally effective in maintaining glycae mic control as existing sulphonylurea, but it gives significantly better co ntrol of postprandial blood glucose levels. Repaglinide can be used as mono therapy both in obese and non-obese type 2 diabetic patients, and is also v ery effective in combination with drugs like metformin or thiazolidines. Be cause of its excretion through liver and bile it is also an attractive drug for diabetic patients with diminished kidney function, especially the elde rly diabetic. Although the overall incidence of hypoglycaemia was similar d uring use of repaglinide and of sulphonylurea, fewer serious hypoglycaemic episodes were observed in repaglinide-treated patients. (See Editorial p. 2 09) (C) 1999 Elsevier Science B.V. All rights reserved.