Propofol does not alter the protein binding and unbound concentration of lidocaine at clinically targeted plasma concentrations in vitro – A short communication - 01/10/24
Highlights |
• | Plasma protein binding affects free drug concentrations. |
• | Lidocaine is a lipophilic local anaesthetic that is highly protein-bound. |
• | In the presence of propofol, lidocaine protein-binding was unchanged. |
• | In vitro unbound lidocaine concentrations were unchanged in the presence of propofol. |
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.
Le texte complet de cet article est disponible en PDF.Abbreviations : AAG, LAST, PK, UHPLC-MS, US FDA
Keywords : Lidocaine, Propofol, Protein binding, Plasma concentration, Pharmacokinetic
Plan
Vol 43 - N° 5
Article 101419- octobre 2024 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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