Zavřelová Alžběta, Merdita Sara, Žák Pavel, Radocha Jakub, Víšek Benjamin, Lánská Miriam, Maláková Jana, Michálek Pavel, Slanař Ondřej, Šíma Martin
4th Department of Internal Medicine - Hematology, University Hospital Hradec Kralove and Faculty of Medicine in Hradec Kralove, Charles University, Hradec Kralove, Czech Republic.
Institute of Pharmacology, First Faculty of Medicine, Charles University and General University Hospital in Prague, Prague, Czech Republic.
Clin Transl Sci. 2025 Sep;18(9):e70346. doi: 10.1111/cts.70346.
The objective of this study was to develop a population pharmacokinetic model for linezolid in hematooncological patients with sepsis, and to propose dosing optimization based on pharmacokinetic covariates that would lead to improved achievement of the PK/PD target. Therapeutic drug monitoring data from hematooncological patients treated with linezolid for suspected or proven sepsis were analyzed. A pharmacokinetic population model for linezolid was constructed using a nonlinear mixed-effects modeling approach. Monte Carlo simulations were then used to compare various dosing regimens in terms of PK/PD target attainment. A total of 197 linezolid serum concentrations obtained from 22 patients were included in the analysis. Patients' age was found to be the most predictive covariate for linezolid pharmacokinetics. In a patient with a median age of 59 years, the volume of distribution and clearance of linezolid were 46.2 L and 12.1 L/h, respectively. During the first 4 days of therapy, linezolid clearance decreased by 33%. The probability of PK/PD target attainment increased through the individualization of the dose according to the patient's age, administration of a loading dose, and administration of linezolid via continuous infusion. For this scenario, an easy-to-use nomogram was designed.
本研究的目的是为患有败血症的血液肿瘤患者建立利奈唑胺的群体药代动力学模型,并根据药代动力学协变量提出给药优化方案,以提高PK/PD目标的达成率。分析了利奈唑胺治疗疑似或确诊败血症的血液肿瘤患者的治疗药物监测数据。采用非线性混合效应建模方法构建了利奈唑胺的药代动力学群体模型。然后使用蒙特卡罗模拟来比较各种给药方案在PK/PD目标达成方面的情况。分析纳入了从22例患者获得的197个利奈唑胺血清浓度。发现患者年龄是利奈唑胺药代动力学最具预测性的协变量。在中位年龄为59岁的患者中,利奈唑胺的分布容积和清除率分别为46.2L和12.1L/h。在治疗的前4天,利奈唑胺清除率下降了33%。通过根据患者年龄个体化给药剂量、给予负荷剂量以及持续输注利奈唑胺,PK/PD目标达成的概率增加。针对这种情况,设计了一个易于使用的列线图。