In vitro anti-Legionella pneumophila activity of tosufloxacin and its therapeutic effect on experimental Legionella pneumonia in guinea pigs.

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  • Ｔｏｓｕｆｌｏｘａｃｉｎのｉｎ　ｖｉｔｒｏ抗Ｌｅｇｉｏｎｅｌｌａ　ｐｎｅｕｍｏｐｈｉｌａ活性およびモルモット実験的肺炎に対する治療効果

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Abstract

We evaluated in vitro and in vivo anti-Legionella pneumophila activity of tosufloxacin (TFLX). The MIC range of TFLX was 0.002-0.0078μg mL and its MIC50 and MIC900.0039μg mL. The MIC90 of TFLX against clinical isolates of L. pneumophila was 16-fold higher than that of rifampicin (RFP), equal to that of sparfloxacin, gatifloxacin and clarithromycin, and 14-to 164-fold lower than those of levofloxacin, ciprofloxacin, moxifloxacin, azithromycin (AZM) and erythromycin. TFLX showed clear bactericidal activity against L. pneumophila ATCC 33152 in macrophages from guinea pigs at a concentration of 16 times MIC, but RFP and AZM did not exhibited bactericidal activity even at 64 times MIC. The doses of 1.25mg kg and 2.5mg kg of TFLX completely protected guinea pigs from death due to pneumonia caused by L. pneumophila. The 80% and 20% of animals treated with 1.25mg and 2.5mg kg of AZM, and the 20% of animals treated with 1.25mg kg of RFP died. Viable cell counts in lungs after TFLX treatment were significantly fewer than in non treated control. The area under the curve of the concentration in lungs for TFLX was equal to that for RFP and smaller than that for AZM.

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