Pharmacokinetics of suiphametrole and its metabolite N₄-acetylsulphametrole in man

Abstract

Sulphametrole is metabolized into N4-acetylsulphametrole and both compounds are eliminated from the body with a similar T1/2 of about 10 h. Sulphametrole is acetylated in an unimodal way and there exists no acetylator phenotype. The renal clearance of sulphametrole is dependent on the urine flow and urine pH, while the renal clearance of the metabolite N4-acetylsulphametrole is not dependent on these variables of tubular reabsorption. No tubular secretion is involved in the renal excretion of sulphametrole while the metabolite N4-acetylsulphametrole is excreted predominantly by active tubular secretion. Probenecid co-medication decreases the rate of absorption of sulphametrole and the tubular secretion ofthe metabolite N4-acetylsulphametrole.