Tolbutamide is an oral antihyperglycemic agent from the sulfonylurea drug class. This drug is used to treat hyperglycemia in patients with type 2 diabetes mellitus (non-insulin-dependent diabetes mellitus (NIDDM)). It is structurally similar to acetohexamide, chlorpropamide, and tolazamide. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from beta cells of pancreatic islet tissue. Sulfonylureas inhibit the ATP-potassium channels by linking with the subunit called the ATP-binding cassette sub-family C member 8 on the beta cell membrane and potassium efflux. This binding results in the depolarization of the cell. In consequence, it causes an influx of calcium ions thus releasing the insulin-containing granules by exocytosis. This drug is also an inhibitor of the ATP-sensitive inward rectifier potassium channel 1 presents in the kidney. Its pharmacological action is still unknown. Tolbutamide is administered as an oral tablet.

Tolbutamide Pathway References