Schmidt P, Korn A, Hitzenberger G, Zazgornik J, Kopsa H, Pils P
Wien Med Wochenschr. 1980 Feb 29;130(4):171-3.
In 6 patients with regular dialysis treatment the pharmacokinetics of intravenously administered trimethoprim and sulfametrol were investigated not only during dialysis procedure but also during the dialysis-free interval. Half-life of the free plasma sulfametrol component is normal even in cases with absent renal function and can be markedly reduced by hemodialysis treatment. The N4-acetylated main metabolite of the sulfonamide is - similar to trimethoprim - hardly dialyzable. Half-life of the latter drug component is prolonged in patients with far advanced renal failure. Due to the excellent dialysanceof the free plasma sulfonamide component the elimination of total sulfametrol is normal during hemodialysis despite cumulation of the N4-acetylated metabolite. Because of the tendency of this metabolite to cumulation, in dialysis patients the compound preparation of trimethoprim and sulfametrol should be used only for trasient treatment of acute infections.
在6例接受常规透析治疗的患者中,研究了静脉注射甲氧苄啶和磺胺美曲唑的药代动力学,不仅在透析过程中进行了研究,而且在无透析间期也进行了研究。即使在肾功能缺失的情况下,游离血浆磺胺美曲唑成分的半衰期也是正常的,并且可以通过血液透析治疗显著缩短。磺胺类药物的N4 - 乙酰化主要代谢产物——与甲氧苄啶类似——几乎不能被透析清除。在晚期肾衰竭患者中,后一种药物成分的半衰期会延长。由于游离血浆磺胺类药物成分具有良好的透析性,尽管N4 - 乙酰化代谢产物会蓄积,但在血液透析期间磺胺美曲唑总量的清除是正常的。由于这种代谢产物有蓄积的倾向,在透析患者中,甲氧苄啶和磺胺美曲唑的复方制剂仅应用于急性感染的短期治疗。