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Antimicrobial Agents and Chemotherapy, December 2003, p. 3789-3794, Vol. 47, No. 12
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.12.3789-3794.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

Concentrations in Plasma, Urinary Excretion, and Bactericidal Activity of Linezolid (600 Milligrams) versus Those of Ciprofloxacin (500 Milligrams) in Healthy Volunteers Receiving a Single Oral Dose

Florian M. E. Wagenlehner,1 Stephan Wydra,1 Hajime Onda,1 Martina Kinzig-Schippers,2 Fritz Sörgel,2 and Kurt G. Naber1*

Department of Urology, St. Elisabeth Hospital, Straubing,1 Institute for Biomedical and Pharmaceutical Research (IBMP), Nürnberg-Heroldsberg, Germany2

Received 4 April 2003/ Returned for modification 30 May 2003/ Accepted 2 September 2003

In a randomized crossover study, 12 volunteers (6 males, 6 females) received a single oral dose of 600 mg of linezolid or 500 mg of ciprofloxacin to assess the concentrations in plasma (up to 24 h), urinary excretion (by high-pressure liquid chromatography), and bactericidal titers in urine (UBT) at intervals up to 120 h. The mean maximum concentration of linezolid in plasma was 13.1 mg/liter, and that of ciprofloxacin was 2.46 mg/liter. The median cumulative levels of renal excretion of the administered dose of the parent drug were 44% for linezolid (range, 28 to 47%; mean ± standard deviation, 40% ± 7.8%) and 43% for ciprofloxacin (range, 20 to 56%; mean ± standard deviation, 40% ± 9.3%). The UBTs, i.e., the highest twofold dilution (with antibiotic-free urine used as the diluent) of urine that was still bactericidal, were determined for a reference strain and five gram-positive clinical uropathogens for which the MICs of linezolid and ciprofloxacin were as follows: Staphylococcus aureus ATCC 27278, 2 and 0.25 mg/liter, respectively; Staphylococcus aureus (methicillin susceptible), 1 and 16 mg/liter, respectively; Staphylococcus aureus (methicillin resistant), 2 and 64 mg/liter, respectively; Staphylococcus saprophyticus (methicillin susceptible), 1 and 0.25 mg/liter, respectively; Enterococcus faecalis, 2 and 1 mg/liter, respectively; and Enterococcus faecium, 2 and 1 mg/liter, respectively. The median UBTs of linezolid measured within the first 6 h were 1:96 for each of the two enterococcal strains and between 1:128 and 1:256 for the four staphylococcal strains. The median UBTs of ciprofloxacin were 1:64 for the two enterococcal strains; between 1:384 and 1:512 for the two ciprofloxacin-susceptible strains; and 1 (bactericidal activity of undiluted urine only) and 1:2 for the two resistant staphylococcal strains, respectively. The areas under the UBT-time curve (AUBT) for linezolid and ciprofloxacin showed no statistically significant (P < 0.05) differences except for a better AUBT for linezolid for the two ciprofloxacin-resistant staphylococcal strains. For linezolid there were no statistically significant differences in UBTs or AUBTs for ciprofloxacin-susceptible and -resistant strains. Thus, the bactericidal activities of linezolid and ciprofloxacin against susceptible strains in urine were comparable, whereas linezolid also exhibited the same good bactericidal activity against ciprofloxacin-resistant strains. Therefore, linezolid should be tested for use as empirical treatment for complicated urinary tract infections due to gram-positive uropathogens in an appropriate clinical trial.

* Corresponding author. Mailing address: Department of Urology, Hospital St. Elisabeth, St. Elisabeth-Str. 23, D-94315 Straubing, Germany. Phone: 49-9421-710-1700. Fax: 49-9421-710-1717. E-mail: NaberK{at}Klinikum-Straubing.de.

Antimicrobial Agents and Chemotherapy, December 2003, p. 3789-3794, Vol. 47, No. 12
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.12.3789-3794.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



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