Butiulca Mihaela, Farczadi Lenard, Imre Silvia, Vari Camil Eugen, Vlase Laurian, Azamfirei Leonard, Lazar Alexandra Elena
Department of Anaesthesiology and Intensive Care Medicine, Faculty of General Medicine, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, Romania.
Department of Anaesthesiology and Intensive Care Medicine, Emergency County Hospital, 540136 Targu Mures, Romania.
Int J Mol Sci. 2025 Jul 12;26(14):6696. doi: 10.3390/ijms26146696.
Regional anesthesia techniques such as the ultrasound-guided PECS II (pectoral nerve block) block are increasingly employed to optimize perioperative analgesia while minimizing systemic anesthetic exposure. Ropivacaine is commonly used for its favorable pharmacological profile; however, clinical data on its pharmacokinetics and systemic metabolite behavior following interpectoral administration remain limited. This study aimed to characterize the plasma concentration-time profile of ropivacaine and its main active metabolite, 3-OH-ropivacaine, in patients undergoing interpectoral nerve block, using a validated LC-MS/MS (liquid chromatography coupled with mass spectrometry) method. Venous blood samples were collected from 18 patients at predefined time points (0, 1, 3, 6, and 24 h) following a PECS II block performed with a ropivacaine-lidocaine mixture. Plasma concentrations were quantified via a validated LC-MS/MS protocol in accordance with FDA (Food and Drug Administration) and EMA (European Medicines Agency) guidelines. Pharmacokinetic parameters were derived using non-compartmental analysis. Ropivacaine reached a mean peak plasma concentration (Cmax-maximum concentration) of 167.5 ± 28.3 ng/mL at 1.3 ± 0.2 h (Tmax-maximum time). The metabolite 3-OH-ropivacaine peaked at 124.1 ± 21.4 ng/mL at 2.3 ± 0.3 h. The terminal elimination half-life was 19.4 ± 2.8 h for ropivacaine and 29.2 ± 3.1 h for its metabolite. Plasma levels demonstrated prolonged systemic exposure with predictable pharmacokinetics. The PECS II block using ropivacaine results in sustained systemic levels of both the parent drug and its primary metabolite, supporting its role in prolonged perioperative analgesia. These data provide a pharmacokinetic foundation for personalized regional anesthesia protocols. This strategy facilitates the adaptation of anesthetic protocols to the individual characteristics of each patient, aligning with the principles of personalized medicine, particularly in patients with altered metabolic capacity.
区域麻醉技术，如超声引导下的胸肌间神经阻滞（PECS II），越来越多地被用于优化围手术期镇痛，同时尽量减少全身麻醉药物的暴露。罗哌卡因因其良好的药理学特性而被广泛使用；然而，关于其在胸肌间给药后的药代动力学和全身代谢物行为的临床数据仍然有限。本研究旨在使用经过验证的液相色谱-质谱联用（LC-MS/MS）方法，对接受胸肌间神经阻滞的患者中罗哌卡因及其主要活性代谢物3-羟基罗哌卡因的血浆浓度-时间曲线进行表征。在使用罗哌卡因-利多卡因混合物进行PECS II阻滞之后，于预定时间点（0、1、3、6和24小时）从18名患者采集静脉血样。根据美国食品药品监督管理局（FDA）和欧洲药品管理局（EMA）的指南，通过经过验证的LC-MS/MS方案对血浆浓度进行定量。使用非房室分析得出药代动力学参数。罗哌卡因在1.3±0.2小时（达峰时间-Tmax）时达到平均血浆峰浓度（Cmax-最高浓度）167.5±28.3 ng/mL。代谢物3-羟基罗哌卡因在2.3±0.3小时时达到峰值124.1±21.4 ng/mL。罗哌卡因的终末消除半衰期为19.4±2.8小时，其代谢物为29.2±3.1小时。血浆水平显示全身暴露时间延长，药代动力学具有可预测性。使用罗哌卡因进行PECS II阻滞可使母体药物及其主要代谢物在全身维持持续水平，支持其在延长围手术期镇痛中的作用。这些数据为个性化区域麻醉方案提供了药代动力学基础。该策略有助于使麻醉方案适应每位患者的个体特征，符合个性化医疗原则，尤其是在代谢能力改变的患者中。
