The Metabolism of 5-p-Aminobenzenesulphonamido-3-Methylisothiazole (Sulphasomizole)

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Abstract
The fate of the sulphonamide drug, sulphasomizole, in man, dog, rabbit and rat has been studied. In man, rat and rabbit, the major urinary metabolite, is N4-acetylsulphasomizole together with the unchanged drug. In man about 60 per cent of an oral dose of 30 mg./kg. is excreted in the urine in 24 hr., just over a third being acetylated. In the rabbit about 80 per cent of an oral dose (150 mg./kg. is excreted in 24 hr. and about two-thirds is acetylated. In the rat about 70 per cent of the dose (150 mg./kg.) is excreted in 24 hr. and just under one third is acetylated. In the dog, the main excretory product is the unchanged drug, there being no acetylation. All four species excrete small amounts (1 per cent) of the N4-glucuronide of sulphasomizole. Other minor metabolites detected were the N4-sulphate of sulphasomizole which was found in rat and dog urine, and an unidentified oxidation product present as a glucuronide which was detected in rabbit and dog urine.