Vree T B, O'Reilly W J, Hekster Y A, Damsma J E, van der Kleijn E
Clin Pharmacokinet. 1980 May-Jun;5(3):274-94. doi: 10.2165/00003088-198005030-00006.
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.
已对磺胺甲噻二唑、磺胺甲恶唑、磺胺嘧啶、磺胺吡啶和磺胺二甲嘧啶在人体中的药代动力学进行了研究。代谢产物N4-乙酰磺胺的肾清除率值比相应母体化合物的肾清除率值高6至20倍。磺胺类药物的肾清除率取决于尿流量。已构建了磺胺类药物血浆和尿液中N4-乙酰磺胺的浓度-时间曲线。血浆中N4-乙酰磺胺百分比-时间曲线是确定乙酰化表型的极佳工具，而从尿液样本构建的曲线则用处较小。有证据表明，磺胺二甲嘧啶由2种不同的同工酶进行代谢，而磺胺嘧啶、磺胺吡啶和磺胺甲恶唑由1种乙酰化同工酶进行代谢。磺胺甲噻二唑的乙酰化程度非常低。
