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Sulfonylureas and meglitinides in the treatment of diabetes mellitus

David K McCulloch, MD
Section Editor
David M Nathan, MD
Deputy Editor
Jean E Mulder, MD


Two classes of oral hypoglycemic drugs directly stimulate release of insulin from pancreatic beta cells: the sulfonylureas and meglitinides. The pharmacology, efficacy, indications, and side effects of these drugs will be discussed here. A general discussion of initial and subsequent treatment of type 2 diabetes is reviewed separately.

(See "Initial management of blood glucose in adults with type 2 diabetes mellitus".)

(See "Management of persistent hyperglycemia in type 2 diabetes mellitus".)


Mechanism of action — Sulfonylureas are among the most widely used drugs for the treatment of patients with type 2 diabetes [1]. They work by stimulating insulin secretion so are useful only in patients with some beta cell function.

The sulfonylurea receptor is a component of the adenosine triphosphate (ATP)-sensitive potassium channel (K-ATP channel) in the pancreatic beta cells [2]. The K-ATP channel regulates the release of insulin from pancreatic beta cells. Sulfonylurea binding leads to inhibition of these channels, which alters the resting potential of the cell, leading to calcium influx and stimulation of insulin secretion. The net effect is increased responsiveness of beta cells to both glucose and non-glucose secretagogues (such as amino acids), resulting in more insulin being released at all blood glucose concentrations. Sulfonylureas may also have extrapancreatic effects, one of which is to increase tissue sensitivity to insulin, but the clinical importance of these effects is minimal [1].


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Literature review current through: Sep 2016. | This topic last updated: Sep 23, 2016.
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