Zhou Yangang, Peng Jiawei, Xu Ping, Wang Feng, Xi Jun, Zhang Hedong, Hu Shanbiao, Yan Han, Tan Liang, Cai Hualin, Zhang Bikui, Lan Gongbin
Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, China.
Institute of Clinical Pharmacy, Central South University, Changsha, Hunan, China.
Antimicrob Agents Chemother. 2025 Jun 4;69(6):e0156824. doi: 10.1128/aac.01568-24. Epub 2025 Apr 23.
The objectives of this study were to investigate the population pharmacokinetic (PK) characteristics of teicoplanin in renal transplant patients and to provide recommendations for optimal teicoplanin dosing regimens. A total of 99 renal transplant patients with 386 plasma samples were enrolled (306 in development and 80 in validation). A population PK analysis and simulations were performed to identify the optimal teicoplanin doses needed to provide an 80% probability of target attainment at 72 h and 168 h using both a trough concentration target of >15 µg/mL and the ratio of 24 h area under the concentration-time curve to the minimum inhibitory concentration >610.4. Teicoplanin was well described by a two-compartment PK model. The final model parameter estimates for clearance, central compartment volume of distribution, intercompartmental clearance, and peripheral compartment volume were 0.711 L/h, 11.3 L, 4.22 L/h, and 35.2 L, respectively. Creatinine clearance (CrCL) was the only covariate that significantly affected teicoplanin clearance. Dosing simulation results showed that standard dosing regimens were unable to meet the treatment needs of all patients, and CrCL-based individual dosing regimens are recommended for both loading dose and maintaining dose. Higher-than-standard teicoplanin doses are necessary to achieve prompt and appropriate drug exposure in renal transplant patients.
本研究的目的是调查替考拉宁在肾移植患者中的群体药代动力学(PK)特征,并为优化替考拉宁给药方案提供建议。共纳入99例肾移植患者,采集了386份血浆样本(306份用于模型建立,80份用于模型验证)。进行了群体PK分析和模拟,以确定在谷浓度目标>15μg/mL以及24小时浓度-时间曲线下面积与最低抑菌浓度之比>610.4的情况下,在72小时和168小时达到目标概率为80%所需的最佳替考拉宁剂量。替考拉宁可用二室PK模型很好地描述。清除率、中央室分布容积、室间清除率和外周室容积的最终模型参数估计值分别为0.711L/h、11.3L、4.22L/h和35.2L。肌酐清除率(CrCL)是唯一显著影响替考拉宁清除率的协变量。给药模拟结果表明,标准给药方案无法满足所有患者的治疗需求,建议基于CrCL的个体化给药方案用于负荷剂量和维持剂量。在肾移植患者中,需要高于标准的替考拉宁剂量才能实现快速且适当的药物暴露。