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.
journal_name
Chemotherapyjournal_title
Chemotherapyauthors
Bulitta JB,Kinzig M,Naber CK,Wagenlehner FM,Sauber C,Landersdorfer CB,Sörgel F,Naber KGdoi
10.1159/000329520subject
Has Abstractpub_date
2011-01-01 00:00:00pages
402-16issue
5eissn
0009-3157issn
1421-9794pii
000329520journal_volume
57pub_type
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