Vree T B, Hekster Y A, Damsma J E, Tijhuis M, Friesen W T
Eur J Clin Pharmacol. 1981;20(4):283-92. doi: 10.1007/BF00618779.
The pharmacokinetics of short acting sulphonamides and a series of N4-acetylsulphonamide derivatives has been investigated. Sulphonamides with a sulphur atom two atomic bond distances from the N1 atom are excreted by active tubular secretion, e.g. sulphamethizole, sulphaethidole and sulphathiasole. When the sulphur atom is replaced by an oxygen or nitrogen atom, active renal excretion no longer occurs. N4-acetylsulphonamides are excreted by active tubular secretion. The renal clearance values of the N4-acetylsulphonamides are not influenced by the substituent at the N1 position. Two groups of N4-acetylsulphonamides can be distinguished. One has a T1/2 of 4-6 h and a renal clearance value of 20-60 ml/min and the second has a T1/2 of 10-20 h and a renal clearance of less than 10 ml/min. N4-acetylsulphonamides are deacetylated to the extent of about 5%.
已对短效磺胺类药物及一系列N4 - 乙酰磺胺衍生物的药代动力学进行了研究。与N1原子相距两个原子键距离处带有硫原子的磺胺类药物通过肾小管主动分泌排出，例如磺胺甲噻二唑、磺胺乙噻唑和磺胺噻唑。当硫原子被氧原子或氮原子取代时，肾脏主动排泄不再发生。N4 - 乙酰磺胺类药物通过肾小管主动分泌排出。N4 - 乙酰磺胺类药物的肾脏清除率不受N1位取代基的影响。可区分出两组N4 - 乙酰磺胺类药物。一组的半衰期为4 - 6小时，肾脏清除率为20 - 60毫升/分钟，另一组的半衰期为10 - 20小时，肾脏清除率小于10毫升/分钟。N4 - 乙酰磺胺类药物的脱乙酰化程度约为5%。
