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Comparison of the bactericidal activities and post-antibiotic effects of the Des-F(6)-quinolone BMS-284756, levofloxacin, and ciprofloxacin against methicillin-susceptible and methicillin-resistant Staphylococcus aureus
- Source :
- European journal of clinical microbiologyinfectious diseases : official publication of the European Society of Clinical Microbiology. 21(1)
- Publication Year :
- 2002
-
Abstract
- The bactericidal activities and post-antibiotic effects of BMS-284756 (T-3811ME), levofloxacin, and ciprofloxacin were evaluated against a methicillin-susceptible and a methicillin-resistant Staphylococcus aureus strain. Minimum inhibitory concentrations (MICs), minimum bactericidal concentrations, post-antibiotic effects, and post-antibiotic sub-MIC effects were determined and time-kill studies were performed for BMS-284756, levofloxacin, and ciprofloxacin. At 4-times and 10-times the MIC, time-kill kinetics over 3 h and over 24 h were similar for all three quinolones when effects were considered as multiples of the MIC. All three quinolones achieved a 3 log10 reduction in cfu/ml within 2 h. At 10-times the MIC, the post-antibiotic effects of BMS-284756, levofloxacin, and ciprofloxacin were 1.6–2.6 h for the methicillin-susceptible Staphylococcus aureus strain and 1.5–1.9 h for the methicillin-resistant Staphylococcus aureus strain. When actual concentrations were considered, BMS-284756 achieved results comparable to levofloxacin and ciprofloxacin at concentrations nearly 10-fold less. When relating the pharmacokinetic properties of the three quinolones to their in vitro activities, the resulting Cmax/MIC and AUC/MIC ratios were, respectively, 120–240.7 and 1,321.7–2,643 for BMS-284756, 22.8 and 190 for levofloxacin, and 5.9–11.9 and 54.8–109.6 for ciprofloxacin. The greater in vitro activity and favorable human pharmacokinetics of BMS-284756 may translate to improved clinical effectiveness of this agent compared to currently marketed quinolones.
- Subjects :
- Microbiology (medical)
Blood Bactericidal Activity
Ofloxacin
Staphylococcus aureus
Indoles
medicine.drug_class
Antibiotics
Cmax
Levofloxacin
Microbial Sensitivity Tests
Quinolones
medicine.disease_cause
Sensitivity and Specificity
Microbiology
Methicillin
Anti-Infective Agents
Ciprofloxacin
medicine
Humans
Antibacterial agent
Chemistry
Drug Resistance, Microbial
General Medicine
biochemical phenomena, metabolism, and nutrition
bacterial infections and mycoses
Quinolone
Methicillin-resistant Staphylococcus aureus
Infectious Diseases
Methicillin Resistance
medicine.drug
Fluoroquinolones
Subjects
Details
- ISSN :
- 09349723
- Volume :
- 21
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- European journal of clinical microbiologyinfectious diseases : official publication of the European Society of Clinical Microbiology
- Accession number :
- edsair.doi.dedup.....760774d915dcc91d0ee600140a72995a