Repaglinide is a novel, short-acting, non-sulfonylurea oral insulin secretagogue used primarily in the treatment of type 2 diabetes mellitus.
Basic Information
Generic Name: Repaglinide
Molecular Formula: C27H36N2O4
Molecular Weight: 452.59
CAS Registry Number: 135062-02-1
Pharmacological Action
Repaglinide works by stimulating the release of insulin from the pancreas, rapidly lowering blood glucose levels. This effect depends on functional β-cells in the pancreas. Its mechanism involves binding to distinct receptors, closing ATP-sensitive potassium channels in the β-cell membrane, causing β-cell depolarization, opening calcium channels, increasing calcium influx, and ultimately inducing insulin secretion from β-cells. Compared to other oral insulin secretagogues, Repaglinide exerts a faster insulinotropic effect.
Indications
Repaglinide is indicated for the treatment of type 2 diabetes mellitus (non-insulin-dependent) in patients whose hyperglycemia cannot be adequately controlled by diet, weight reduction, and exercise alone. It can also be used in combination with metformin, with a synergistic effect on glycemic control.