Transformation and Excretion of Drugs in Biological Systems. V. Correlation between Renal Excretion and Biotransformation of Sulfadimethoxine

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Sulfadimethoxine and its three biotransformed products in man were applied to renal clearance experiments in dogs to elucidate their renal excretion mechanisms.<BR>Clearance ratio of sulfadimethoxine is extremely low compared with each biotransformed product. Of three biotransformed products, clearance ratio of sulfadimethoxine-N1-glucuronide greatly exceeded over the clearance ratio of the other two biotransformed products.<BR>Considerable proximal tubular secretion of sulfadimethoxine-N4-acetate was observed. On the contrary, the proximal tubular secretion of sulfadimethoxine-N1-glucuronide and sulfadimethoxine were insufficient.<BR>Sulfadimethoxine-N1-glucuronide considerably reduced the affinity to dog plasma protein compared with sulfadimethoxine and sulfadimethoxine-N4-acetate.

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