title: Determination of the acetylator phenotype and pharmacokinetics of some sulphonamides in man.
abstract: The pharmacokinetics of sulphamethizole, sulphamethoxazole, sulphadiazine, sulphapyridine and sulphadimidine have been studied in man. Renal clearance values of the metabolite N4-acetylsulphonamide are 6 to 20 times higher than those of the corresponding parent compound. The renal clearance of sulphonamides is dependent on the urine flow. N4-Acetylsulphonamide concentration-time profiles for plasma and urine have been constructed for the sulphonamides. The percentage N4-acetylsulphonamide-time profiles for plasma are excellent tools for establishing the acetylator phenotype, while those constructed from urine samples are less useful. Evidence is obtained that sulphadimidine is metabolically processes by 2 different isoenzymes, while sulphadiazine, sulphapyridine and sulphamethoxazole are processes by 1 acetylating isoenzyme. Sulphamethizole is acetylated to very little extent.
mesh_terms: D000107:Acetylation; D006801:Humans; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D010641:Phenotype; D013449:Sulfonamides / Q000097:blood / Q000378:metabolism* / Q000652:urine; D013997:Time Factors
chemical_list: D013449:Sulfonamides