Bailey R R, Peddie B, Blake E
Drugs. 1981;22 Suppl 1:46-51. doi: 10.2165/00003495-198100221-00011.
Two studies evaluating the efficacy of cefoperazone in patients with chronic renal failure are described. In study A, 10 patients with severe chronic renal failure were given 1 g of cefoperazone intravenously over 3 minutes. The mean serum cefoperazone concentration at 30 minutes was 119.3 +/- 15.7 microgram/ml, and at 6 hours was 35.9 +/- 5.7 micrograms/ml. The mean serum half-life using the method of least squares was 6.6 +/- 1.15 hours (range, 2.5 to 15.1). The mean half-life from 2 hours onwards was 12.2 +/- 3.51 hours (range, 2.3 to 42.9). The mean peak urinary concentration of cefoperazone was 192 microgram/ml with a very wide individual range of 20 to 920 microgram/ml which was reached 0.5 to 9 hours after injection. In study B, 8 patients with chronic renal failure were treated with 1 to 2 g of cefoperazone intravenously every 12 hours for 5 to 14 days for complicated urinary tract infections. Serum and urine concentrations of cefoperazone were measured 6 hours after each morning dose. The mean 6-hour serum and urine concentrations of cefoperazone for the 4 patients treated with 2 g daily were 63 +/- 11.7 and 87 +/- 11.1 microgram/ml, respectively. The corresponding values for the 4 patients treated with 4 g daily were 106 +/- 20 and 258 +/- 32 microgram/ml. No drug accumulation occurred in any patient. No deterioration in renal function was noted. In conclusion, cefoperazone promises to be an effective and safe broad-spectrum antibiotic for patients with all degrees of renal function impairment. A dosage schedule of 2 to 4 g daily will not lead to significant drug accumulation in the presence of severe renal failure.
本文描述了两项评估头孢哌酮对慢性肾衰竭患者疗效的研究。在研究A中，10例严重慢性肾衰竭患者在3分钟内静脉注射1g头孢哌酮。30分钟时头孢哌酮的平均血清浓度为119.3±15.7μg/ml，6小时时为35.9±5.7μg/ml。采用最小二乘法计算的平均血清半衰期为6.6±1.15小时（范围为2.5至15.1小时）。从2小时起的平均半衰期为12.2±3.51小时（范围为2.3至42.9小时）。头孢哌酮的平均尿峰浓度为192μg/ml，个体差异范围很大，为20至920μg/ml，在注射后0.5至9小时达到。在研究B中，8例慢性肾衰竭患者因复杂性尿路感染，每12小时静脉注射1至2g头孢哌酮，持续5至14天。每天早晨给药后6小时测量头孢哌酮的血清和尿液浓度。每天接受2g治疗的4例患者的头孢哌酮平均6小时血清和尿液浓度分别为63±11.7和87±11.1μg/ml。每天接受4g治疗的4例患者的相应值为106±20和258±32μg/ml。所有患者均未出现药物蓄积。未观察到肾功能恶化。总之，头孢哌酮有望成为一种对所有程度肾功能损害患者均有效且安全的广谱抗生素。在严重肾衰竭的情况下，每日2至4g的给药方案不会导致明显的药物蓄积。
