COMMON BRAND NAME(S): Orinase
GENERIC NAME(S): TOLBUTAMIDE
Description: Tolbutamide lowers blood glucose concentration principally by stimulating the secretion of endogenous insulin from pancreatic β-cells. It may enhance peripheral sensitivity to insulin and reduce basal hepatic glucose production during long-term admin.
Onset: 1 hr.
Duration: 6-24 hr.
Absorption: Readily absorbed from the GI tract. Time to peak plasma concentration: W/in 3-5 hr.
Distribution: Distributed into breast milk. Volume of distribution: 0.15 L/kg. Plasma protein binding: Approx 95%.
Metabolism: Metabolised in the liver via hydroxylation mediated by CYP2C9 isoenzyme.
Excretion: Via urine (75-85%) mainly as metabolites and faeces. Half-life: 4-7 hr.