tolbutamide

Tolbutamide is a first-generation sulfonylurea oral hypoglycemic agent used to manage type 2 diabetes mellitus when diet and exercise alone are insufficient. It acts by stimulating pancreatic β cells to release insulin, thereby lowering blood glucose levels. Tolbutamide increases both basal and meal-stimulated insulin secretion, enhances peripheral glucose utilization, decreases hepatic gluconeogenesis, and may increase the number and sensitivity of insulin receptors. Its effectiveness depends on residual pancreatic function; it is ineffective in type 1 diabetes or in patients with absolute insulin deficiency. Tolbutamide has a relatively short duration of action due to rapid hepatic metabolism and is excreted mainly via urine. It was discovered in 1956 and is less commonly used today due to the higher risk of adverse effects compared to newer sulfonylureas[1][3][4][5].

Brand names

OrinaseTol-Tab

Other names

甲苯磺丁脲Benzenesulfonamide, N-[(butylamino)carbonyl]-4-methyl-Diaben