Acetohexamide pharmacokinetics

No pharmacokinetic studies have been reported in the literature. However, seventy to eighty percent of a single oral dose of 1 gram of acetohexamide was recovered as a metabolite within 24 hours in the urine of four human volunteers. It is suggested that acetohexamide is converted to hydroxyhexamide in the liver. Acetohexamide and hydroxyhexamide are probably converted to hydroxyacetohexamide and hydroxyhydroxyhexamide in both the liver and kidneys9. 

A simple HPLC assay of the drug in plasma was developed by Takagishi et al (33). A sample was extracted with a mixture of benzene and ethyl acetate at pH 5 and the organic phase was evaporated. A 50X solution In CHsCN of the residue was chromatographed using a Lichrosorb RP-8 reversed-phase column and a mobile phase composed of 0.2X acetic acid - methyl cyanide (1 1). The method can be used for bioavailability and clinical pharmacokinetic studies of acetohexamide. 

Nagamine et al (55) estimated the rates of available fraction for 4-acetam1doacetophenone, 4-acety1benzene-sulfonamide, and acetohexamide and their respective reduced compounds, 4-subst1tuted o-hydroxyethylphenyl derivatives. In rats. The study Indicated that the compounds are in a reversible drug-metabolite relationship. The pharmacokinetic profiles of the agents were studied after an Intraportal administration... 

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