Propofol does not alter the protein binding and unbound concentration of lidocaine at clinically targeted plasma concentrations in vitro – A short communication

IF 3.7 3区医学 Q1 ANESTHESIOLOGY

Anaesthesia Critical Care & Pain Medicine Pub Date : 2024-10-01 DOI:10.1016/j.accpm.2024.101419

Angela R Tognolini , Jason A Roberts , Saurabh Pandey , Steven C Wallis , Victoria A Eley

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引用次数: 0

Abstract

Background

Intravenous lidocaine is increasingly used as an analgesic adjunct during general anaesthesia. Lidocaine is highly protein-bound and changes to binding can alter drug efficacy or toxicity. We aimed to measure the effect of various propofol and lidocaine plasma concentration combinations on the protein binding and concentration of lidocaine in vitro.

Methods

Known targeted concentrations of propofol and lidocaine were added to drug-free human plasma in vitro. Samples were prepared and analysed in various clinically relevant concentration combinations; propofol at 0, 2, 4 and 6 µg/mL, and lidocaine at 1, 3 and 5 µg/mL. The total and unbound concentrations of lidocaine were measured by ultra-high performance liquid chromatography-mass spectrometry and percentage protein binding was determined. Data were presented as mean and standard deviation (SD) and differences between groups analysed.

Results

The overall mean protein binding of lidocaine was 68.8% (SD 5.5, range 57.5–80.9%). Beta regression analysis revealed no statistically significant difference in lidocaine percentage binding across a range of propofol and lidocaine concentration combinations.

Conclusion

Propofol did not alter the unbound and free pharmacologically active proportion of lidocaine at different clinically targeted concentrations of propofol and lidocaine in plasma in vitro. The percentage of plasma protein binding of lidocaine in this study was consistent with previously published results.

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丙泊酚在体外不会改变利多卡因在临床目标血浆浓度下的蛋白结合和未结合浓度--简短交流。

背景：静脉注射利多卡因越来越多地被用作全身麻醉期间的镇痛辅助药物。利多卡因与蛋白质的结合率很高，结合率的变化会改变药物的疗效或毒性。我们的目的是在体外测量各种丙泊酚和利多卡因血浆浓度组合对利多卡因蛋白结合和浓度的影响：方法：在体外将已知目标浓度的丙泊酚和利多卡因添加到不含药物的人体血浆中。制备并分析各种临床相关浓度组合的样本；异丙酚浓度为 0、2、4 和 6 µg/mL，利多卡因浓度为 1、3 和 5 µg/mL。采用超高效液相色谱-质谱法测量利多卡因的总浓度和未结合浓度，并测定蛋白质结合百分比。数据以平均值和标准差（SD）以及分析组之间的差异表示：结果：利多卡因的总平均蛋白结合率为 68.8%（标准差为 5.5，范围为 57.5-80.9%）。贝塔回归分析表明，在一系列丙泊酚和利多卡因浓度组合中，利多卡因的结合率没有显著的统计学差异：结论：丙泊酚不会改变血浆中不同临床目标浓度丙泊酚和利多卡因在体外的未结合和游离药理活性比例。本研究中利多卡因的血浆蛋白结合率与之前发表的结果一致。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Anaesthesia Critical Care & Pain Medicine ANESTHESIOLOGY-

CiteScore

6.70

自引率

5.50%

发文量

150

审稿时长

18 days

期刊介绍： Anaesthesia, Critical Care & Pain Medicine (formerly Annales Françaises d''Anesthésie et de Réanimation) publishes in English the highest quality original material, both scientific and clinical, on all aspects of anaesthesia, critical care & pain medicine.