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Effects of Temafloxacin and Ciprofloxacin on the Pharmacokinetics of Caffeine

  • Section 2: Drug Interactions
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Summary

A number of quinolone antibacterial agents, particularly enoxacin, pefloxacin, pipemidic acid and ciprofloxacin, are known to decrease the clearance of methylxanthines. The effects of temafloxacin and ciprofloxacin on the pharmacokinetics of caffeine were therefore compared in a 3-way crossover study in 12 healthy young volunteers. Each volunteer received 183mg once-daily doses of caffeine in conjunction with twice-daily placebo, temafloxacin 600mg and ciprofloxacin 750mg in 3 separate phases according to a randomised sequence.

A doubling of the area under the plasma concentration-time curve (77.8 vs 31.8 mg/L · h) and terminal-phase half-life (9.7 vs 4.5h) of caffeine were observed in the presence of ciprofloxacin. The magnitude of the reduction in the intrinsic clearance of caffeine produced by ciprofloxacin was greater than that described in the literature for ciprofloxacin and theophylline. This may partly be explained by intertriai differences in dosage and study design.

Coadministration of temafloxacin did not have any effect on the pharmacokinetics of caffeine, confirming results of other studies suggesting that this agent does not affect methylxanthine clearance. Accordingly, it appears that restriction of caffeine intake during temafloxacin therapy is not necessary.

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Authors and Affiliations

  1. IBMP - Institute for Biomedical and Pharmaceutical Research, Schleifweg 3, W-8501, Nürnberg-Heroldsberg, Germany

    G. Mahr,  F. Sörgel, M. Kinzig & P. Muth

  2. Drug Metabolism Department, Abbott Laboratories, Abbott Park, Illinois, USA

    G. R. Granneman

  3. Clinical Statistics Department, Abbott Laboratories, Abbott Park, Illinois, USA

    K. Patterson

  4. Department of Clinical Pharmacology, University of Frankfurt/Main, Frankfurt/Main, Germany

    U. Fuhr

  5. Department of Pharmaceutical Chemistry, University of Bonn, Bonn, Germany

    P. Nickel

  6. Department of Pediatrics, University of Essen, Essen, Germany

    U. Stephan

Authors
  1. G. Mahr
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  2. F. Sörgel
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  3. G. R. Granneman
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  4. M. Kinzig
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  5. P. Muth
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  6. K. Patterson
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  7. U. Fuhr
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  8. P. Nickel
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  9. U. Stephan
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Additional information

Data contained in this article form part of the PhD thesis of Gerhard Mahr, which is to be submitted to the University of Bonn.

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Mahr, G., Sörgel, F., Granneman, G.R. et al. Effects of Temafloxacin and Ciprofloxacin on the Pharmacokinetics of Caffeine. Clin. Pharmacokinet. 22 (Suppl 1), 90–97 (1992). https://doi.org/10.2165/00003088-199200221-00015

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  • DOI: https://doi.org/10.2165/00003088-199200221-00015

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