-
Gliclazide
- indication:For the treatment of diabetes mellitus
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: LD<sub>50</sub>=3000 mg/kg (orally in mice)
- absorprion: Rapidly and well absorbed but may have wide inter- and intra-individual variability.
- halflife: 11 hours (Campbell DB et al.,Diabetes Res Clin Pract.;14:S21-36)
- roouteelimination:
- volumedistribution:
- clearance: