Acetohexamide

A first generation sulfonylurea

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100mg

￥537.00

430.00

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500mg

￥862.00

690.00

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Background

Acetohexamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (K_IR6.2) with K_i values of 22.9 and 14.2 ?M in HEK293 cells transfected with the human receptor and in rat brain, respectively.¹ It is metabolized to the hypoglycemic compound L-hydroxyhexamide in vivo.^2,3 Formulations containing acetohexamide have previously been used in the treatment of type 2 diabetes.

1.Gopalakrishnan, M., Molinari, E.J., Char-Change, S., et al.Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK-293 cellsBr. J. Pharmacol.129(7)1323-1332(2000) 2.McMahon, R.E., Marshall, F.J., and Culp, H.W.The nature of the metabolites of acetohexamide in the rat and in the humanJ. Pharmacol. Exp. Ther.149(2)272-279(1965) 3.Imamura, Y., Sanai, K., Seri, K., et al.Hypoglycemic effect of S(-)-hydroxyhexamide, a major metabolite of acetohexamide, and its enantiomer R(+)-hydroxyhexamideLife Sci.69(16)1947-1955(2001)