Renal Excretion of N⁴-Acetyl Sulphanilamide and N⁴-Acetyl Sulphadimidine in Goats

Abstract

The renal excretion of N⁴-acetyl sulphanilamide and N⁴-acetyl sulphadimidine was studied in 19 experiments with 6 goats during continuous intravenous administration of the 2 sulphonamide derivatives. Deacetylation of both compounds takes place to a small extent only. Further it is shown that both sulphonamide derivatives are bound to plasma proteins to a greater extent than sulphanilamide and sulphadimidine. The excretion of the N⁴-acetylated sulphonamides is compared with the renal excretion of creatinine. The non-protein-bound fraction of the 2 N⁴-acetylated sulphonamides is excreted by filtration and active tubular secretion. The renal clearances of the acetyl derivatives are higher than those of the parent compounds.

Sammendrag

Den renale udskillelse af N⁴-acetylsulfanilamid og N⁴-acetylsulfadimidin er undersøgt ved 19 forsøg på 6 geder. Begge derivaterne deacetyleres in vivo omend kun i mindre omfang. Undersøgelserne viste endvidere, at begge N⁴-acetylderivaterne bindes til plasmaproteinerne i større udstrækning end de tilsvarende ikke-acetylerede forbindelser. Udskillelsen af de N⁴-acetylerede sulfonamider sammenlignes med udskillelsen af kreatinin, og det vises, at den ikke-proteinbundne del udskilles ved filtration og aktiv tubular sekretion. Den renale udskillelse af N⁴-acetylderivaterae er større end udskillelsen af de tilsvarende ikke-acetylerede forbindelser.