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For the treatment of diabetes mellitus
Gliclazide binds to the beta cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the beta cells. This opens voltage-dependent calcium channels in the beta cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.
LD<sub>50</sub>=3000 mg/kg (orally in mice)
Rapidly and well absorbed but may have wide inter- and intra-individual variability.
11 hours (Campbell DB et al.,Diabetes Res Clin Pract.;14:S21-36)