A pharmacodynamic approach to antimicrobial activity in serum and epithelial lining fluid against in vivo-selected Streptococcus pneumoniae mutants and association with clinical failure in pneumonia

J Antimicrob Chemother. 2006 Aug;58(2):349-58. doi: 10.1093/jac/dkl250. Epub 2006 Jun 16.

Abstract

Objectives: Emergence of resistance may be prevented by killing both the parental infecting strain and subsequent less susceptible step-mutants. The present study analyses eradication and resistance selection in Streptococcus pneumoniae with moxifloxacin, levofloxacin and azithromycin, using a parental serotype 3 clinical strain (strain A) and its correspondent step-mutant derivatives resistant to these antibiotics (B, C, D), which were selected in vivo in a patient with pneumonia.

Methods: Moxifloxacin, levofloxacin and azithromycin MICs were 1, 2 and 0.5 mg/L for the parental strain; 4, 16 and 4 mg/L for isolate B; and 4, 16 and >128 mg/L for isolates C and D, respectively. A pharmacokinetic computerized device was used to simulate serum and epithelial lining fluid (ELF) concentrations. Initial inoculum was approximately 10(8) cfu/mL. Population analysis profiles were performed using plates with increasing antimicrobial concentrations.

Results: In ELF simulations, moxifloxacin showed a bactericidal pattern against all isolates with a minority (approximately 100 cfu/mL) of the surviving population (isolates B, C and D) growing on plates with moxifloxacin concentrations just above those in ELF. Levofloxacin and azithromycin showed a bactericidal pattern only against isolate A, with the whole population of isolates B, C and D growing on plates with levofloxacin concentrations higher (16-64 mg/L) than those in ELF and in plates with azithromycin concentrations as high as 2048 mg/L (for isolates C and D).

Conclusions: Antimicrobial activity in pulmonary tissue against possible emerging resistant mutants during pneumonia treatment may prevent failures more than the solely activity against the S. pneumoniae parental infecting strain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacology*
  • Aza Compounds / blood
  • Aza Compounds / pharmacology*
  • Azithromycin / blood
  • Azithromycin / pharmacology*
  • Community-Acquired Infections / microbiology
  • Drug Resistance, Bacterial* / genetics
  • Fluoroquinolones
  • Humans
  • Levofloxacin*
  • Microbial Sensitivity Tests
  • Models, Biological
  • Moxifloxacin
  • Mutation*
  • Ofloxacin / blood
  • Ofloxacin / pharmacology*
  • Pneumonia, Pneumococcal / microbiology
  • Quinolines / blood
  • Quinolines / pharmacology*
  • Serum Bactericidal Test
  • Streptococcus pneumoniae / drug effects*
  • Streptococcus pneumoniae / genetics
  • Streptococcus pneumoniae / isolation & purification

Substances

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