Eliopoulos G M
Department of Medicine, New England Deaconess Hospital, Boston, Massachusetts 02215.
Rev Infect Dis. 1988 Jan-Feb;10 Suppl 1:S102-5. doi: 10.1093/clinids/10.supplement_1.s102.
Despite similarities in their chemical structures, the new fluoroquinolones differ greatly in the extent to which renal clearance contributes to their elimination. On the opposite ends of this spectrum are ofloxacin, which is almost entirely eliminated by the kidney as unmodified drug, and pefloxacin, which undergoes extensive biotransformation. Dosage adjustments in patients with renal insufficiency therefore are recommended for ofloxacin, but, on the basis of currently available data, adjustments do not appear to be required for pefloxacin. Both renal clearance of unmodified drug and metabolic transformation contribute substantially to the elimination of norfloxacin and ciprofloxacin. Because of the great antimicrobial potency of the new fluoroquinolones, it should be possible to employ them in the treatment of urinary tract infections caused by highly susceptible bacteria even in patients with marked impairment of renal function.
尽管新氟喹诺酮类药物的化学结构相似,但它们在肾清除率对其消除作用的贡献程度上有很大差异。在这个范围的两端分别是氧氟沙星和培氟沙星,氧氟沙星几乎完全以未修饰的药物形式经肾脏消除,而培氟沙星则经历广泛的生物转化。因此,对于肾功能不全的患者,建议调整氧氟沙星的剂量,但根据目前可得的数据,培氟沙星似乎不需要调整剂量。未修饰药物的肾清除率和代谢转化对诺氟沙星和环丙沙星的消除都有很大贡献。由于新氟喹诺酮类药物具有强大的抗菌效力,即使在肾功能严重受损的患者中,也应该能够使用它们来治疗由高度敏感细菌引起的尿路感染。