In vitro and in vivo activities of sparfloxacin and reference drugs againstChlamydia pneumoniae |
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Authors: | Rinzo Soejima Yoshihito Niki Toshio Kishimoto Naoyuki Miyashita Yoshifumi Kubota Katsuhisa Nakata |
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Affiliation: | (1) Department of Medical Social Work, Kawasaki University of Medical Welfare, 701-01 Okayama, Japan;(2) Division of Respiratory Diseases, Department of Medicine, Kawasaki Medical School, Okayama, Japan;(3) Discovery Research Laboratories II, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan |
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Abstract: | The activities of sparfloxacin and reference drugs againstChlamydia pneumoniae were compared by using in vitro and in vivo methods. The minimum inhibitory concentration (MIC) (μg/ml) ranges of sparfloxacin, levofloxacin, tosufloxacin, grepafloxacin, AM-1155, DU-6859a, clarithromycin, azithromycin, and minocycline for sixC. pneumoniae strains (two standard and four clinical strains) were 0.031 to 0.063, 0.25 to 0.5, 0.063 to 0.125, 0.063 to 0.125, 0.063 to 0.125, 0.031 to 0.063, 0.016 to 0.031, 0.125 to 0.25, and 0.016 to 0.031, respectively. The in vitro potency of sparfloxacin againstC. pneumoniae was similar to that of clarithromycin, minocycline, and DU-6859a, and higher than that of the other fluoroquinolones and azithromycin. Fatal pneumonia was induced in cyclophosphamide-treated leukopenic mice by intranasal inoculation withC. pneumoniae KKpn-2. Infiltration of the lung by neutrophils and lymphocytes was confirmed by histopathologic examination. Oral treatment with the various antichlamydial agents was given for seven days; sparfloxacin and minocycline had the lowest ED50 (effective treatment dose in 50% of the mice; given as mg/kg per dose) (1.11 each), followed by DU-6859a (1.92), tosufloxacin (2.09), grepafloxacin (2.41), clarithromycin and azithromycin (2.48 each), AM-1155 (2.77), and levofloxacin (>10). These results suggest that sparfloxacin may be an effective agent forC. pneumoniae infection in humans. |
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Keywords: | Chlamydia pneumoniae sparfloxacin fluoroquinolone leukopenic infection |
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