Mechanism of action of sparfloxacin against and mechanism of resistance in gram-negative and gram-positive bacteria.
The inhibition of DNA synthesis by sparfloxacin; accumulation of sparfloxacin into members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and staphylococci; induction of recA in Escherichia coli; and the optimum bactericidal concentration (OBC) were measured, and killing kinetics at the OBC were estimated. The OBC and maximum recA-inducing concentration in E. coli were both 1 microgram of sparfloxacin per ml. Accumulation was rapid; two- to threefold more sparfloxacin than ciprofloxacin accumulated in staphylococci and more sparfloxacin accumulated in staphylococci than in gram-negative bacteria. Laboratory mutants with decreased susceptibilities to quinolones alone or multiply resistant were selected from the Enterobacteriaceae and Staphylococcus aureus by using sparfloxacin.
Piddock
L J
LJ
Antimicrobial Agents Research Group, Medical School, University of Birmingham, United Kingdom.
Zhu
M
M
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D015342:DNA Probes; D004269:DNA, Bacterial / Q000096:biosynthesis; D004352:Drug Resistance, Microbial / Q000502:physiology; D004755:Enterobacteriaceae / Q000187:drug effects; D024841:Fluoroquinolones; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D009154:Mutation; D010641:Phenotype; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D015363:Quinolones / Q000378:metabolism / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D015342:DNA Probes; D004269:DNA, Bacterial; D024841:Fluoroquinolones; D015363:Quinolones; D002939:Ciprofloxacin; C061363:sparfloxacin