Pharmacodynamics and bactericidal activity of gatifloxacin in experimental pneumonia caused by penicillin-resistant Streptococcus pneumoniae

Chemotherapy. 2004 Jun;50(3):107-12. doi: 10.1159/000077883.

Abstract

Background: Antimicrobial resistance rates for Streptococcus pneumoniae continue to increase worldwide, and resistance to nearly every major class of antimicrobials used to treat pneumococcal infections has been reported. Gatifloxacin (GFLX) is one of the quinolones that have strong activity against S. pneumoniae.

Methods: We compared the bacteriological, pharmacological and histopathological effects of orally administered GFLX with those of levofloxacin (LVFX) and ciprofloxacin (CPFX) in a murine model of pneumonia caused by penicillin-resistant S. pneumoniae (PRSP).

Results: Treatment with GFLX resulted in a significant decrease in the number of viable bacteria (control, CPFX, LVFX, and GFLX: 6.48 +/- 0.36, 6.44 +/- 0.27, 5.51 +/- 0.15, and 4.89 +/- 0.28 log10 CFU/lung, respectively, mean +/- SD). A significant decrease in mortality was observed in the GFLX-treated group in comparison with the other groups. Histopathological examination revealed that inflammatory changes in GFLX-treated mice were less marked than in the other mice.

Conclusion: Our results suggest that orally administered GFLX is effective in PRSP pneumonia. The pharmacokinetic profiles also reflected the effectiveness of GFLX.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / therapeutic use*
  • Anti-Infective Agents / blood
  • Anti-Infective Agents / pharmacokinetics
  • Anti-Infective Agents / therapeutic use*
  • Ciprofloxacin / blood
  • Ciprofloxacin / pharmacokinetics
  • Ciprofloxacin / therapeutic use*
  • Drug Evaluation, Preclinical
  • Fluoroquinolones / blood
  • Fluoroquinolones / pharmacokinetics
  • Fluoroquinolones / therapeutic use*
  • Gatifloxacin
  • Levofloxacin*
  • Lung / drug effects*
  • Lung / metabolism
  • Lung / pathology
  • Mice
  • Mice, Inbred CBA
  • Ofloxacin / blood
  • Ofloxacin / pharmacokinetics
  • Ofloxacin / therapeutic use*
  • Penicillin Resistance
  • Pneumonia, Pneumococcal / drug therapy*
  • Pneumonia, Pneumococcal / mortality
  • Survival Rate

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Fluoroquinolones
  • Ciprofloxacin
  • Levofloxacin
  • Ofloxacin
  • Gatifloxacin