Abstract
We evaluated fleroxacin, a newer fluoroquinolone, against isolates from sputum from patients with cystic fibrosis. These isolates included rough and mucoid Pseudomonas aeruginosa, Pseudomonas cepacia, Staphylococcus aureus, Haemophilus influenzae, and Escherichia coli. Selected isolates were tested by the broth microdilution method to examine the influence of various pHs, inoculum sizes, and biological fluids (serum or sputum from patients with cystic fibrosis). Fleroxacin MICs for 50 and 90% of isolates of P. aeruginosa were 2.0 and 4 micrograms/ml, those for P. cepacia were 2 and 16 micrograms/ml, those for S. aureus were 0.5 and 1 microgram/ml, those for H. influenzae were 0.06 and 0.06 micrograms/ml, and those for E. coli were 0.01 and 0.03 micrograms/ml, respectively. Fleroxacin activity against mucoid P. aeruginosa was similar to the activities of enoxacin and ofloxacin but eightfold lower than that of ciprofloxacin. It was twofold more active than norfloxacin and enoxacin but was twofold less active than ciprofloxacin, ofloxacin, and nafcillin against S. aureus. Fleroxacin inhibitory activity against P. cepacia was two- to fourfold lower than that of ciprofloxacin but eightfold greater than those of the other quinolones tested. Alterations in pH, diluent, and inoculum size did not significantly affect fleroxacin activity. These results, combined with available pharmacokinetic and tissue distribution data, support the need for clinical evaluation of fleroxacin in pulmonary infections in patients with cystic fibrosis.
Full text
PDF




Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Aoyama H., Inoue M., Mitsuhashi S. In-vitro and in-vivo antibacterial activity of fleroxacin, a new fluorinated quinolone. J Antimicrob Chemother. 1988 Oct;22 (Suppl 500):99–114. doi: 10.1093/jac/22.supplement_d.99. [DOI] [PubMed] [Google Scholar]
- Bosso J. A., Black P. G., Matsen J. M. Ciprofloxacin versus tobramycin plus azlocillin in pulmonary exacerbations in adult patients with cystic fibrosis. Am J Med. 1987 Apr 27;82(4A):180–184. [PubMed] [Google Scholar]
- Bremner D. A., Dickie A. S., Singh K. P. In-vitro activity of fleroxacin compared with three other quinolones. J Antimicrob Chemother. 1988 Oct;22 (Suppl 500):19–23. doi: 10.1093/jac/22.supplement_d.19. [DOI] [PubMed] [Google Scholar]
- Bundtzen R. W., Gerber A. U., Cohn D. L., Craig W. A. Postantibiotic suppression of bacterial growth. Rev Infect Dis. 1981 Jan-Feb;3(1):28–37. doi: 10.1093/clinids/3.1.28. [DOI] [PubMed] [Google Scholar]
- Chin N. X., Brittain D. C., Neu H. C. In vitro activity of Ro 23-6240, a new fluorinated 4-quinolone. Antimicrob Agents Chemother. 1986 Apr;29(4):675–680. doi: 10.1128/aac.29.4.675. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Cozzarelli N. R. DNA gyrase and the supercoiling of DNA. Science. 1980 Feb 29;207(4434):953–960. doi: 10.1126/science.6243420. [DOI] [PubMed] [Google Scholar]
- Fuursted K. Post-antibiotic effect of ciprofloxacin on Pseudomonas aeruginosa. Eur J Clin Microbiol. 1987 Jun;6(3):271–274. doi: 10.1007/BF02017611. [DOI] [PubMed] [Google Scholar]
- Govan J. R. Mucoid strains of Pseudomonas aeruginosa: the influence of culture medium on the stability of mucus production. J Med Microbiol. 1975 Nov;8(4):513–522. doi: 10.1099/00222615-8-4-513. [DOI] [PubMed] [Google Scholar]
- Hodson M. E., Roberts C. M., Butland R. J., Smith M. J., Batten J. C. Oral ciprofloxacin compared with conventional intravenous treatment for Pseudomonas aeruginosa infection in adults with cystic fibrosis. Lancet. 1987 Jan 31;1(8527):235–237. doi: 10.1016/s0140-6736(87)90062-6. [DOI] [PubMed] [Google Scholar]
- Hohl P., Felber A. M. Effect of method, medium, pH and inoculum on the in-vitro antibacterial activities of fleroxacin and norfloxacin. J Antimicrob Chemother. 1988 Oct;22 (Suppl 500):71–80. doi: 10.1093/jac/22.supplement_d.71. [DOI] [PubMed] [Google Scholar]
- Jorgensen J. H., Redding J. S., Maher L. A., Howell A. W. Improved medium for antimicrobial susceptibility testing of Haemophilus influenzae. J Clin Microbiol. 1987 Nov;25(11):2105–2113. doi: 10.1128/jcm.25.11.2105-2113.1987. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Klinger J. D., Aronoff S. C. In-vitro activity of ciprofloxacin and other antibacterial agents against Pseudomonas aeruginosa and Pseudomonas cepacia from cystic fibrosis patients. J Antimicrob Chemother. 1985 Jun;15(6):679–684. doi: 10.1093/jac/15.6.679. [DOI] [PubMed] [Google Scholar]
- Lester A., Andreasen J. J. In vitro susceptibility of Pseudomonas aeruginosa from bacteremic and fibrocystic patients to four quinolones and five other antipseudomonal antibiotics. Scand J Infect Dis. 1988;20(5):525–529. doi: 10.3109/00365548809032501. [DOI] [PubMed] [Google Scholar]
- Manek N., Andrews J. M., Wise R. In vitro activity of Ro 23-6240, a new difluoroquinolone derivative, compared with that of other antimicrobial agents. Antimicrob Agents Chemother. 1986 Aug;30(2):330–332. doi: 10.1128/aac.30.2.330. [DOI] [PMC free article] [PubMed] [Google Scholar]
- McDonald P. J., Craig W. A., Kunin C. M. Persistent effect of antibiotics on Staphylococcus aureus after exposure for limited periods of time. J Infect Dis. 1977 Feb;135(2):217–223. doi: 10.1093/infdis/135.2.217. [DOI] [PubMed] [Google Scholar]
- Mulligan M. E., Ruane P. J., Johnston L., Wong P., Wheelock J. P., MacDonald K., Reinhardt J. F., Johnson C. C., Statner B., Blomquist I. Ciprofloxacin for eradication of methicillin-resistant Staphylococcus aureus colonization. Am J Med. 1987 Apr 27;82(4A):215–219. [PubMed] [Google Scholar]
- Neu H. C., Kumada T., Chin N. X., Mandell W. The post-antimicrobial suppressive effect of quinolone agents. Drugs Exp Clin Res. 1987;13(2):63–67. [PubMed] [Google Scholar]
- Ogle J. W., Reller L. B., Vasil M. L. Development of resistance in Pseudomonas aeruginosa to imipenem, norfloxacin, and ciprofloxacin during therapy: proof provided by typing with a DNA probe. J Infect Dis. 1988 Apr;157(4):743–748. doi: 10.1093/infdis/157.4.743. [DOI] [PubMed] [Google Scholar]
- Paganoni R., Herzog C., Braunsteiner A., Hohl P. Fleroxacin: in-vitro activity worldwide against 20,807 clinical isolates and comparison to ciprofloxacin and norfloxacin. J Antimicrob Chemother. 1988 Oct;22 (Suppl 500):3–17. doi: 10.1093/jac/22.supplement_d.3. [DOI] [PubMed] [Google Scholar]
- Stutman H. R., Akaniro J. C., Vidaurre C. E., Marks M. I. In vitro activity of E-1040, a 3-substituted cephalosporin, against pathogens from cystic fibrosis sputum. Antimicrob Agents Chemother. 1990 Jul;34(7):1366–1370. doi: 10.1128/aac.34.7.1366. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Weidekamm E., Portmann R., Suter K., Partos C., Dell D., Lücker P. W. Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrob Agents Chemother. 1987 Dec;31(12):1909–1914. doi: 10.1128/aac.31.12.1909. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wise R., Kirkpatrick B., Ashby J., Griggs D. J. Pharmacokinetics and tissue penetration of Ro 23-6240, a new trifluoroquinolone. Antimicrob Agents Chemother. 1987 Feb;31(2):161–163. doi: 10.1128/aac.31.2.161. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wolfson J. S., Hooper D. C. Fluoroquinolone antimicrobial agents. Clin Microbiol Rev. 1989 Oct;2(4):378–424. doi: 10.1128/cmr.2.4.378. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Zweerink M. M., Edison A. Inhibition of Micrococcus luteus DNA gyrase by norfloxacin and 10 other quinolone carboxylic acids. Antimicrob Agents Chemother. 1986 Apr;29(4):598–601. doi: 10.1128/aac.29.4.598. [DOI] [PMC free article] [PubMed] [Google Scholar]
