REVIEW Tolbutamide is a first-generation potassium channel blocker and a sulfonylurea oral hypoglycemic drug which lowers blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue. Tolbutamide inhibits the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose. Since the pancreas must synthesize insulin in order for this drug to work, it is not effective in the management of type I diabetes.
REFERENCES
[1]
Buzas, Andre Substituted sulfonylureas (1964), FR 1376552 19641030.
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