High doses of levofloxacin vs moxifloxacin against staphylococcal experimental foreign-body infection: the effect of higher MIC-related pharmacokinetic parameters on efficacy

J Infect. 2009 Mar;58(3):220-6. doi: 10.1016/j.jinf.2009.01.005. Epub 2009 Feb 12.

Abstract

Objectives: Since levofloxacin at high doses was the best therapy in staphylococcal tissue-cage model of foreign-body infection, we hypothesized that moxifloxacin with higher ratio of area under the concentration-time curve to the MIC (AUC/MIC) would provide better results.

Methods: MICs, MBCs, MPCs (mutant prevention concentration) and 24h kill-curves were determined in the log and stationary phases. Using the aforementioned model, we tested the efficacy of levofloxacin 100mg/kg/d, moxifloxacin 40mg/kg/d and moxifloxacin 80mg/kg/d; they were equivalent to human levels for 1000mg/d, 400mg/d and 800mg/d, respectively. We screened for the appearance of resistant strains.

Results: MICs and MBCs in logarithmic and stationary phases and MPCs of levofloxacin were 0.5, 1 and 4, 0.8microg/ml, respectively, and those of moxifloxacin 0.12, 0.25 and 2, 0.25microg/ml. AUC/MIC were 234 (levofloxacin), 431 (moxifloxacin 40) and 568 (moxifloxacin 80). Bacterial counts decreases in tissue-cage fluids (means of logCFU/ml) were -1.81 (n=25), -1.31 (23), and -1.46 (20), respectively; for controls it was 0.24 (22). All groups were better than controls (p<0.05); no differences between them existed.

Conclusions: Moxifloxacin with higher AUC/MIC ratio did not improve the efficacy of high doses of levofloxacin.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use*
  • Aza Compounds / administration & dosage
  • Aza Compounds / pharmacokinetics
  • Aza Compounds / pharmacology
  • Aza Compounds / therapeutic use*
  • Fluoroquinolones
  • Foreign Bodies / complications*
  • Levofloxacin*
  • Male
  • Microbial Sensitivity Tests
  • Microbial Viability
  • Models, Animal
  • Moxifloxacin
  • Ofloxacin / administration & dosage
  • Ofloxacin / pharmacokinetics
  • Ofloxacin / pharmacology
  • Ofloxacin / therapeutic use*
  • Quinolines / administration & dosage
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology
  • Quinolines / therapeutic use*
  • Rats
  • Rats, Wistar
  • Staphylococcal Infections / drug therapy*
  • Time Factors

Substances

  • Anti-Bacterial Agents
  • Aza Compounds
  • Fluoroquinolones
  • Quinolines
  • Levofloxacin
  • Ofloxacin
  • Moxifloxacin