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Author(s):
Bulitta, Jurgen B.; Kinzig, Martina; Naber, Christoph K.; Wagenlehner, Florian M.E.; Sauber, Christian; Landersdorfer, Cornelia B.; Sörgel, Fritz; Naber, Kurt G. 
Title:
Population Pharmacokinetics and Penetration into Prostatic, Seminal, and Vaginal Fluid for Ciprofloxacin, Levofloxacin, and Their Combination 
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. 
Keywords:
Body fluid penetration; Chronic bacterial prostatitis; Prostatic fluid; Vaginal fluid; Ejaculate; Pharmacokinetic drug-drug interaction; Population pharmacokinetic modeling; Sperm cells 
Journal title:
Chemotherapy 
Year:
2011 
Journal volume:
57 
Journal issue:
Pages contribution:
402--416 
Fulltext / DOI:
Publisher:
S. Karger AG 
Publisher address:
Basel, Switzerland 
Print-ISSN:
1421-9794 
E-ISSN:
1421-9794 
Notes:
Dieser Beitrag ist mit Zustimmung des Rechteinhabers aufgrund einer (DFG-geförderten) Allianz- bzw. Nationallizenz frei zugänglich. This publication is with permission of the rights owner freely accessible due to an Alliance licence and a national licence (funded by the DFG, German Research Foundation) respectively.