Pharmacokinetics of N1-Acetyl- and N4-Acetylsulphamethoxazole in Man

1 January 1979

journal article
review article
Published by Springer Nature in Clinical Pharmacokinetics

Vol. 4 (4) , 310-319
https://doi.org/10.2165/00003088-197904040-00004

Abstract

The pharmacokinetics of N₁-acetylsulphamethoxazole and N₄-acetylsulphamethoxazole in man are described. N₁-Acetylsulphamethoxazole is deacetylated to sulphamethoxazole and acetylated to N₄-acetylsulphamethoxazole. N₄-Acetylsulphamethoxazole is excreted almost unchanged in the urine. The renal excretion rate is independent of the urine flow and urinary pH. N₄-Acetylsulphonamides are less lipid soluble and more acidic than their corresponding parent sulphonamides.

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