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Tolbutamide sodium is a potent and orally active antidiabetic agent. Tolbutamide sodium induces apoptosis in a Ca2+ dependent manner in pancreatic β-cells. Tolbutamide sodium has the potential for the research of non-insulin-dependent diabetes mellitus[1][2].

Tolbutamide sodium,1-butyl-3-(p-tolylsulfonyl)urea monosodium salt (OrinaseDiagnostic), is a white, crystalline powder, freely soluble inwater, soluble in alcohol and chloroform, and very slightlysoluble in ether.

This water-soluble salt of tolbutamide is used intravenouslyfor the diagnosis of mild diabetes mellitus and offunctioning pancreatic islet cell adenomas. The sterile drypowder is dissolved in sterile water for injection to make aclear solution, which then should be administered within1 hour. The main route of breakdown is to butylamine andsodium p-toluene sulfonamide.

[1] Trube G, et al. Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells. Pflugers Arch. 1986 Nov;407(5):493-9. DOI:10.1007/BF00657506
[2] Efanova IB, et al. Glucose and tolbutamide induce apoptosis in pancreatic beta-cells. A process dependent on intracellular Ca2+ concentration. J Biol Chem. 1998 Dec 11;273(50):33501-7. DOI:10.1074/jbc.273.50.33501