Patel I H, Sugihara J G, Weinfeld R E, Wong E G, Siemsen A W, Berman S J
Antimicrob Agents Chemother. 1984 Apr;25(4):438-42. doi: 10.1128/AAC.25.4.438.
The effects of renal impairment on the pharmacokinetics of ceftriaxone in humans were examined after intravenous infusion of a 1-g dose over 15 min to 30 renally impaired patients. The study included 12 dialysis patients and 18 patients with severe, moderate, or mild renal impairment. Plasma and, where appropriate, urine and dialysate samples were collected at predetermined times and analyzed for ceftriaxone by high-pressure liquid chromatography. The elimination half-life (group mean ranged from 11.7 to 17.3 h) and plasma clearance (group mean ranged from 529 to 705 ml/h) did not correlate linearly with creatinine clearance. The renal clearance and fraction of dose excreted unchanged in urine were related linearly, however weakly, with creatinine clearance. Ceftriaxone was not removed from plasma to a significant extent during hemodialysis. The half-life was prolonged twofold, the plasma clearance was lowered less than 50%, and the volume of distribution was relatively unchanged in renally impaired patients compared with young or elderly healthy subjects with normal renal function at an equivalent dose. Since these changes are moderate, adjustment in the dosage regimen of ceftriaxone for patients with impaired renal function should not be necessary when ceftriaxone dosage is 2 g or less per day (2 g every 24 h or 1 g every 12 h). It was reported that the elimination half-life of ceftriaxone is substantially prolonged in a small percentage of patients with end-stage renal disease maintained on hemodialysis. Therefore, plasma concentrations of ceftriaxone should be monitored in dialysis patients to determine whether dosage adjustments are necessary.
对30例肾功能受损患者静脉输注1g剂量头孢曲松15分钟后，研究了肾功能损害对头孢曲松在人体内药代动力学的影响。该研究包括12例透析患者以及18例重度、中度或轻度肾功能损害患者。在预定时间采集血浆样本，必要时采集尿液和透析液样本，并用高压液相色谱法分析头孢曲松。消除半衰期（组均值范围为11.7至17.3小时）和血浆清除率（组均值范围为529至705ml/h）与肌酐清除率无线性相关性。然而，肾清除率和尿液中以原形排泄的剂量分数与肌酐清除率呈线性相关，但相关性较弱。血液透析期间，头孢曲松未从血浆中大量清除。与肾功能正常的年轻或老年健康受试者相比，在同等剂量下，肾功能受损患者的半衰期延长两倍，血浆清除率降低不到50%，分布容积相对不变。由于这些变化程度适中，当头孢曲松剂量为每天2g或更低（每24小时2g或每12小时1g）时，肾功能受损患者无需调整头孢曲松的给药方案。据报道，一小部分接受血液透析的终末期肾病患者中，头孢曲松的消除半衰期会大幅延长。因此，应对透析患者的头孢曲松血浆浓度进行监测，以确定是否需要调整剂量。
