Effect of Obesity on Pharmacokinetics of Lidocaine and its Active Metabolites in Chinese Patients Undergoing Laparoscopic Bariatric Surgery: A Prospective Clinical Study.
Mengyu Zhang, Ying Jin, Xueying Yuan, Chaoqun He, Mei Han, Faping Tu, Zhenlei Wang
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Abstract
Background and objective: Obesity can alter the physiological profile of individuals, potentially impacting the pharmacokinetics of anesthetic agents. This study compared the pharmacokinetic profiles of lidocaine and its metabolites between obese patients and normal-weight patients following a single intravenous bolus during surgical operation, to inform dosing strategies for the obese Chinese population.
Methods: Twenty-nine obese patients scheduled for laparoscopic sleeve gastrectomy and 29 normal-weight patients for laparoscopic cholecystectomy were enrolled. Lidocaine (2%, 1.5 mg/kg) was administered intravenously to obese patients and normal-weight patients on the basis of adjusted body weight (ABW) and total body weight, respectively. Plasma samples were collected to analyze the pharmacokinetic profiles of lidocaine and its metabolites. Adverse events (AEs) were recorded throughout the study.
Results: Obese patients had a significantly longer half-life for lidocaine (2.27 ± 0.69 h vs 0.94 ± 0.16 h, p < 0.0001), a higher volume of distribution (105 ± 27.3 L vs 54.9 ± 14.0 L, p < 0.0001), and a lower clearance (33.6 ± 9.08 L/h vs 40.5 ± 8.67 L/h, p = 0.008) compared to normal-weight patients. Although exposure to lidocaine was similar between groups within 2 hours, obese patients had lower metabolite concentrations due to decreased metabolic capacity. The plasma concentrations in all patients remained below the toxic concentration of 5 μg/mL, and no serious lidocaine-related AEs were reported.
Conclusions: Obesity significantly affects the pharmacokinetics of lidocaine and its active metabolites, and administering lidocaine intravenously via ABW is safe and reasonable for obese patients.
Clinical trial registration: ChiCTR2200064980, 25 October 2022.
背景和目的：肥胖可以改变个体的生理特征，潜在地影响麻醉剂的药代动力学。本研究比较了肥胖患者和正常体重患者手术期间单次静脉注射利多卡因及其代谢物的药代动力学特征，为中国肥胖人群的给药策略提供信息。方法：选取29例计划行腹腔镜袖胃切除术的肥胖患者和29例体重正常的腹腔镜胆囊切除术患者。肥胖患者和正常体重患者分别根据调整体重（ABW）和总体重静脉给予利多卡因（2%,1.5 mg/kg）。收集血浆样本，分析利多卡因及其代谢物的药代动力学特征。在整个研究过程中记录不良事件（ae）。结果：肥胖患者与正常体重患者相比，利多卡因半衰期明显延长（2.27±0.69 h vs 0.94±0.16 h, p < 0.0001），分布体积更高（105±27.3 L vs 54.9±14.0 L, p < 0.0001），清除率更低（33.6±9.08 L/h vs 40.5±8.67 L/h, p = 0.008）。虽然两组之间在2小时内暴露于利多卡因相似，但肥胖患者由于代谢能力下降，代谢物浓度较低。所有患者血药浓度均低于5 μg/mL的中毒浓度，未见严重的利多卡因相关不良反应。结论：肥胖显著影响利多卡因及其活性代谢物的药代动力学，肥胖患者经腹部静脉给药利多卡因是安全合理的。临床试验注册：ChiCTR2200064980, 2022年10月25日。
期刊介绍：
Clinical Pharmacokinetics promotes the continuing development of clinical pharmacokinetics and pharmacodynamics for the improvement of drug therapy, and for furthering postgraduate education in clinical pharmacology and therapeutics.
Pharmacokinetics, the study of drug disposition in the body, is an integral part of drug development and rational use. Knowledge and application of pharmacokinetic principles leads to accelerated drug development, cost effective drug use and a reduced frequency of adverse effects and drug interactions.
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