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- Title
Population Pharmacokinetics and Penetration into Prostatic, Seminal, and Vaginal Fluid for Ciprofloxacin, Levofloxacin, and Their Combination.
- Authors
Bulitta, Jurgen B.; Kinzig, Martina; Naber, Christoph K.; Wagenlehner, Florian M.E.; Sauber, Christian; Landersdorfer, Cornelia B.; Sörgel, Fritz; Naber, Kurt G.
- Abstract
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 μM) compared to levofloxacin (Km: 6,830 μM). 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. Copyright © 2011 S. Karger AG, Basel
- Subjects
PHARMACOKINETICS; PROSTATE; BODY fluids; CIPROFLOXACIN; HIGH performance liquid chromatography; FLUOROQUINOLONES; BIOAVAILABILITY
- Publication
Chemotherapy (0009-3157), 2012, Vol 57, Issue 5, p402
- ISSN
0009-3157
- Publication type
Article
- DOI
10.1159/000329520