Albany College of Pharmacy and Health Sciences, Albany, New York, USA.
Antimicrob Agents Chemother. 2012 Feb;56(2):725-30. doi: 10.1128/AAC.05515-11. Epub 2011 Nov 14.
Scant data exist for the pharmacokinetics (PK) of ertapenem in patients on continuous ambulatory peritoneal dialysis (CAPD). The goals of this study were to characterize the PK profile of ertapenem during CAPD, determine the extent of ertapenem penetration into the peritoneal cavity, and quantify the probability of the target attainment (PTA) profile in the serum and peritoneal cavity. A single-dose PK study was conducted in seven patients on CAPD. Population PK modeling and Monte Carlo simulation determined the probability that ertapenem at 500 mg intravenously (i.v.) every 24 h (q24h) would achieve concentrations in excess of the MIC for 40% of the dosing interval (40% T>MIC, where T is time) in the serum and peritoneal cavity. Monte Carlo simulation was also used to calculate the peritoneal cavity/serum mean and median penetration ratios by estimating the area under the concentration-time curve in the peritoneal cavity and serum (AUC(Peritoneal) and AUC(Serum), respectively) from zero to infinity after a single simulated dose. The population mean (± standard deviation [SD]) values for the apparent volume in the central compartment, clearance, and apparent volume in the peritoneal cavity were 2.78 (0.62) liters, 0.24 (0.07) liters/hr, and 5.81 (2.05) liters, respectively. The mean (SD) AUC(Peritoneal)/AUC(Serum) ratio was 1.039 (0.861), and the median penetration ratio was 0.801 (interquartile range, 0.486 to 1.317). In both the serum and peritoneal cavity, ertapenem at 500 mg i.v. q24h was very likely (>90%) to achieve the pharmacodynamic target for MICs of ≤2 mg/liter. The simulations suggest that 500 mg of ertapenem i.v. q24h is very likely to achieve the exposure target associated with clinical efficacy in both the serum and peritoneal cavity against the range of MIC values deemed susceptible by the Clinical and Laboratory Standards Institute.
在接受持续不卧床腹膜透析 (CAPD) 的患者中,厄他培南的药代动力学 (PK) 数据很少。本研究的目的是描述 CAPD 期间厄他培南的 PK 特征,确定厄他培南渗透到腹腔的程度,并量化血清和腹腔中目标浓度(T>MIC)的概率(PTA)特征。对 7 名 CAPD 患者进行了单次剂量 PK 研究。群体 PK 建模和蒙特卡罗模拟确定了 500mg 厄他培南每 24 小时静脉注射(i.v.)一次(q24h)在血清和腹腔中超过 MIC 的浓度超过 40%的给药间隔(40% T>MIC,其中 T 是时间)的概率。蒙特卡罗模拟也用于通过估计单次模拟剂量后腹腔和血清中的浓度-时间曲线下面积(AUC(腹腔)和 AUC(血清))来计算腹腔/血清平均和中位数渗透比。在中央隔室的表观体积、清除率和腹腔的表观体积的群体平均值(±标准偏差 [SD])分别为 2.78(0.62)升、0.24(0.07)升/小时和 5.81(2.05)升。AUC(腹腔)/AUC(血清)比值的平均值(SD)为 1.039(0.861),中位数渗透比为 0.801(四分位距,0.486 至 1.317)。在血清和腹腔中,500mg i.v. q24h 的厄他培南非常可能(>90%)达到 MIC 为≤2mg/L 的药效学目标。模拟表明,500mg 厄他培南 i.v. q24h 非常可能在血清和腹腔中达到与临床疗效相关的暴露目标,针对临床和实验室标准协会认为敏感的 MIC 值范围。