In vitro and in vivo activities of clinafloxacin, CI-990 (PD 131112), and PD 138312 versus enterococci.

Abstract

Certain new fluoroquinolones have high activity against enterococci. Against Enterococcus faecalis (n = 18), MICs at which 90% of the isolates were inhibited were as follows (in micrograms per milliliter): clinafloxacin, 0.125; CI-990, 0.5; and PD 138312, 0.25 (compared with 1 microgram/ml for ciprofloxacin and 2 micrograms/ml for ofloxacin). Strains producing beta-lactamase or that were vancomycin resistant or resistant to high-level gentamicin were not quinolone cross-resistant. The drugs were bactericidal and were unaffected by 50% human serum. Oral efficacies (in milligrams per kilogram of body weight for 50% protective doses) in lethal mouse infections with quinolone-susceptible strains were 4.3 to 24 for clinafloxacin, 7.2 to 39 for CI-990, 7.2 to 76 for PD 138312, and 41 to > 100 for ciprofloxacin; when the drugs were given subcutaneously, the order was similar and values ranged from 1.1 to 12.5. Clinafloxacin, CI-990, and PD 138312 may have therapeutic potential in systemic enterococcal infections in humans.

• Authors: M A Cohen, S L Yoder, M D Huband, G E Roland, C L Courtney
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 39 Issue 9 Pg. 2123-7 (Sep 1995) ISSN: 0066-4804 [Print] United States
• PMID: 8540728 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Anti-Infective Agents
• Fluoroquinolones
• Naphthyridines
• PD 131112
• Quinolones
• PD 138312
• clinafloxacin

Topics

• Animals
• Anti-Infective Agents (pharmacology, therapeutic use)
• Drug Resistance, Microbial
• Enterococcus (drug effects)
• Enterococcus faecalis (drug effects)
• Female
• Fluoroquinolones
• Gram-Positive Bacterial Infections (drug therapy, microbiology)
• Mice
• Microbial Sensitivity Tests
• Naphthyridines (pharmacology, therapeutic use)
• Quinolones (pharmacology, therapeutic use)