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Effect of ciprofloxacin on the pharmacokinetics of intravenous lidocaine

Published online by Cambridge University Press:  15 September 2005

M. H. Isohanni ,
J. Ahonen ,
P. J. Neuvonen  and
K. T. Olkkola
M. H. Isohanni
Affiliation:
Diacor Hospital, Department of Anaesthesia, Finland University of Helsinki, Department of Clinical Pharmacology, Helsinki, Finland
J. Ahonen
Affiliation:
University of Helsinki, Department of Anaesthesiology and Intensive Care Medicine, Helsinki, Finland
P. J. Neuvonen
Affiliation:
University of Helsinki, Department of Clinical Pharmacology, Helsinki, Finland
K. T. Olkkola
Affiliation:
University of Turku, Department of Anaesthesiology and Intensive Care, Turku, Finland
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Summary

Background and objective: Recent studies have suggested that cytochrome P-450 isoenzyme 1A2 has an important role in lidocaine biotransformation. We have studied the effect of a cytochrome P-450 1A2 inhibitor, ciprofloxacin, on the pharmacokinetics of lidocaine. Methods: In a randomized, double-blinded, cross-over study, nine healthy volunteers ingested for 2.5 days 500 mg oral ciprofloxacin or placebo twice daily. On day 3, they received a single dose of 1.5 mg kg−1 lidocaine intravenously over 60 min. Plasma concentrations of lidocaine, 3-hydroxylidocaine and monoethylglycinexylidide were determined for 11 h after the start of the lidocaine infusion. Results: Ciprofloxacin increased the mean peak concentration and area under plasma concentration–time curve of lidocaine by 12% (range −6 to +46%; P < 0.05) and 26% (8–59%; P < 0.01), respectively. The mean plasma clearance of lidocaine was decreased by ciprofloxacin by 22% (7–38%; P < 0.01). Ciprofloxacin decreased the area under the plasma concentration–time curve of monoethylglycinexylidide by 21% (P < 0.01) and that of 3-hydroxylidocaine by 14% (P < 0.01). Conclusion: The plasma decay of intravenously administered lidocaine is modestly delayed by concomitantly administered ciprofloxacin. Ciprofloxacin may increase the systemic toxicity of lidocaine.

Keywords

ANAESTHETICS, LOCAL, lidocainePHARMACOKINETICS, lidocaineCYTOCHROME P-450 ENZYME SYSTEM, cytochrome P-450 CYP1A2, antagonists and inhibitors
Type
Original Article
Information
European Journal of Anaesthesiology , Volume 22 , Issue 10 , October 2005 , pp. 795 - 799
Copyright
© 2005 European Society of Anaesthesiology

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