Population pharmacokinetics and penetration into prostatic, seminal, and vaginal fluid for ciprofloxacin, levofloxacin, and their combination

Jurgen Bulitta, Martina Kinzig, Christoph Naber, Florian Wagenlehner, Christian Sauber, Cornelia Landersdorfer, Fritz Sorgel, Kurt Naber

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16 Citations (Scopus)


Background: Our objectives were to assess the pharmacokinetic interaction and body fluid penetration of ciprofloxacin and levofloxacin. Methods: This study was a single-dose open randomized three-way crossover in 15 healthy volunteers receiving 500 mg oral levofloxacin, 500 mg oral ciprofloxacin, or 250 mg levofloxacin and 250 mg ciprofloxacin co-administered. Serum, urine, and body fluid concentrations were determined by high-performance liquid chromatography and analyzed via population pharmacokinetic modeling. Results: Modeling indicated that ciprofloxacin inhibited the renal reabsorption of levofloxacin. Ciprofloxacin increased the net renal clearance of levofloxacin by 13 , as its estimated affinity for a putative tubular reabsorption transporter was 12-fold higher (Km: 568 A?M) compared to levofloxacin (Km: 6,830 A?M). Levofloxacin increased the bioavailability of ciprofloxacin by 12 and achieved significantly (p <0.05) higher concentrations at 3 h in ejaculate, prostatic, seminal, and vaginal fluid compared to ciprofloxacin. Conclusion: Modeling suggested that ciprofloxacin inhibited the tubular reabsorption of levofloxacin due to a 12-fold higher affinity for a putative tubular reabsorption transporter compared to levofloxacin. This pharmacokinetic interaction was not clinically relevant.
Original languageEnglish
Pages (from-to)402 - 416
Number of pages15
Issue number5
Publication statusPublished - 2011

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