Pfizer, Inc, 500 Arcola Rd, Collegeville, PA 19426-3982, USA.
J Clin Pharmacol. 2012 Sep;52(9):1379-87. doi: 10.1177/0091270011416938. Epub 2011 Sep 27.
The pharmacokinetic parameters of tigecycline were assessed in subjects with severe renal impairment (creatinine clearance <30 mL/min, n = 6), subjects receiving hemodialysis (4 received tigecycline before and 4 received tigecycline after hemodialysis), and subjects with age-adjusted, normal renal function (n = 6) after administration of single 100-mg doses. Serial serum and urine samples were collected and assayed using validated liquid chromatography with tandem mass spectrometer (LC/MS/MS) methods. Concentration-time data were then analyzed using noncompartmental pharmacokinetic methods. Tigecycline renal clearance in subjects with normal renal function represented approximately 20% of total systemic clearance. Tigecycline clearance was reduced by approximately 20%, and area under the tigecycline concentration-time curve increased by approximately 30% in subjects with severe renal impairment. Tigecycline was not efficiently removed by dialysis; thus, it can be administered without regard to timing of hemodialysis. Based on these pharmacokinetic data, tigecycline requires no dosage adjustment in patients with renal impairment.
替加环素的药代动力学参数在严重肾功能不全患者（肌酐清除率 <30 mL/min，n = 6）、接受血液透析的患者（4 例在血液透析前接受替加环素治疗，4 例在血液透析后接受替加环素治疗）和年龄调整后肾功能正常的患者（n = 6）中进行了评估，这些患者单次给予 100mg 剂量后。采集并使用经过验证的液相色谱-串联质谱（LC/MS/MS）方法检测血清和尿液中的药物浓度。然后使用非房室药代动力学方法分析浓度-时间数据。在肾功能正常的患者中，替加环素的肾清除率约为总系统清除率的 20%。在严重肾功能不全的患者中，替加环素的清除率降低了约 20%，替加环素浓度-时间曲线下面积增加了约 30%。替加环素不能被透析有效地清除；因此，无需考虑血液透析的时间。基于这些药代动力学数据，替加环素在肾功能不全的患者中无需调整剂量。
