Kowalsky S F, Echols M, Schwartz M T, Bailie G R, McCormick E
Department of Pharmacy Practice, Albany College of Pharmacy, NY 12208.
Clin Nephrol. 1993 Jan;39(1):53-8.
The pharmacokinetics of a single, oral dose of 750 mg of ciprofloxacin were studied in 35 subjects with various degrees of renal function (Group 1, Clcr > or = 80 ml/min; Group II, Clcr 50-79 ml/min; Group III, Clcr 10-49 ml/min) and on hemodialysis (HD) or continuous ambulatory peritoneal dialysis (CAPD). Blood, urine and CAPD dialysate samples were collected over a period of 48 hours after dosing. Data were fitted using non-linear, least squares regression. The mean Cmax was 3.4 +/- 1.0 mg/l and tmax was 2.3 +/- 0.9 hours. The mean AUC in Group I was 14.7 mg.h/l, Group II was 33.7 (p < 0.001), Group III 63.8 (p < 0.001), HD 57.9 (p < 0.0001) and CAPD 44.3 (p < 0.001). Half-life in Group I was 4.6 h, and was shorter than Group III (11.1 h, p < 0.001), HD (13.4 h, p < 0.001) and CAPD (8.9 h, p < 0.001). Total body clearance and renal clearance demonstrated significant differences also. The dialysis clearance in CAPD patients was 0.53 +/- 0.39 l/h. Peritoneal effluent concentrations varied from 0.6 mg/l during the first exchange, to a peak of 2.2 mg/l during the second, to 0.13 mg/l in the 48 hour (9th) exchange. Dosage adjustments of ciprofloxacin in the presence of renal insufficiency are indicated for subjects with a Clcr < 20 ml/min/1.73m2.
在35名不同程度肾功能的受试者(第一组,肌酐清除率[Clcr]≥80 ml/分钟;第二组,Clcr 50 - 79 ml/分钟;第三组,Clcr 10 - 49 ml/分钟)以及接受血液透析(HD)或持续性非卧床腹膜透析(CAPD)的患者中,研究了单次口服750毫克环丙沙星的药代动力学。给药后48小时内收集血液、尿液和CAPD透析液样本。数据采用非线性最小二乘法回归拟合。平均血药峰浓度(Cmax)为3.4±1.0毫克/升,达峰时间(tmax)为2.3±0.9小时。第一组的平均药时曲线下面积(AUC)为14.7毫克·小时/升,第二组为33.7(p<0.001),第三组为63.8(p<0.001),HD组为57.9(p<0.0001),CAPD组为44.3(p<0.001)。第一组的半衰期为4.6小时,短于第三组(11.1小时,p<0.001)、HD组(13.4小时,p<0.001)和CAPD组(8.9小时,p<0.001)。总体清除率和肾脏清除率也显示出显著差异。CAPD患者的透析清除率为0.53±0.39升/小时。腹膜流出液浓度在第一次交换时为0.6毫克/升,第二次交换时达到峰值2.2毫克/升,在48小时(第9次)交换时为0.13毫克/升。对于Clcr<20 ml/分钟/1.73m²的受试者,肾功能不全时需调整环丙沙星剂量。