新フルオロキノロン薬balofloxacinのin vitro, in vivo抗菌作用  [in Japanese] In vitro and in vivo antibacterial activities of balofloxacin, a novel fluoroquinolone  [in Japanese]

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フルオロキノロン系広域抗菌薬balofloxacin (BLFX) の<I>in vitro</I>およびい<I>in vivo</I>抗菌作用を, ofloxacin (OFLX), ciprofloxacin (CPFX), tosunoxacin (TFLX), sparfloxacin (SPFX) およびlomefloxacin (LFLX) を対照薬に用いて評価した。BLFXは<I>in vitro</I>薬剤感受性試験においてグラム陰性菌からグラム陽性菌まで幅広い抗菌作用を示した。特にBLFXの臨床分離MRSAに対するMIC<SUB>90</SUB>値は8.0μg/mlと良好で, この値はSPFXのMIC<SUB>90</SUB>値の1/2倍であった。BLFXの臨床分離メチシリン感受性<I>Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae</I>および<I>Streptococcus pyogenes</I>に対するMIC<SUB>90</SUB>値は各々0.25, ≦0.063, ≦0.063および0, 125μg/mlであった。これらの値はCPFXおよびLFLX各値の1/2以下で, SPFXおよびTFLXの各値と同等であった。他のグラム陰性菌に対するBLFXのMIC値は比較キノロン薬の2倍から4倍であった。<BR>マウス全身感染モデルにおいてBLFXは<I>in vitro</I>の抗菌作用を反映した良好な治療効果を示した。BLFXは<I>S. pneumoniae</I> TMS-3を用いたマウス呼吸器感染 (肺炎モデル) 実験においてSPFXおよびTFLXと同等の優れた治療効果を示した。また, BLFXは<I>Escherichia coli</I> TMS-3を用いたマウス上行性尿路感染 (腎炎モデル) 実験において, OFLXと同等の治療効果を示した。BLFXをマウスに50mg/kg経口投与した場合の血清中, 肺内および腎内最高濃度は, 各々3.35±0.95μg/ml (投与15分後), 9.57±2.67μg/g (15分後) および11.64±2.43μg/g (30分後) であった。

Balofloxacin (BLFX), a new fluoroquinolone, was evaluated for its <I>in vitro</I> and <I>in vivo</I> antibacterial activities in comparison with those of ciprofloxacin (CPFX), lomefloxacin (LFLX), ofloxacin (OFLX), sparfloxacin (SPFX) and tosufloxacin (TFLX). BLFX showed <I>in vitro</I> antibacterial activity against both gram-positive and gram-negative bacteria. The MIC for 90% of methicillin-resistant <I>Staphylococcus aureus</I> (MRSA)(MIC<SUB>90</SUB>) was 8.0μg/ml, and was two-fold more active than SPFX. The MIC<SUB>90</SUB> for methicillinsusceptible <I>S. aureus, Staphylococcus epidermidis, Streptococcus pneumoniae</I> and <I>Streptococcus pyogenes</I> were 0.25, ≤0.063, ≤0.063 and 0.125μg/ml, respectively. These values indicate that the drug was two-fold or more active than CPFX and LFLX, but was similar in activity to SPFX and TFLX. Against other gramnegative bacteria, BLFX was 2-to more than 4-fold (in some cases) less active than the reference quinolones. In experimental septicemia, the <I>in vivo</I> activity of BLFX was reflected its <I>in vitro</I> antibacterial activity. In respiratory tract infections in mice with <I>S. pneumoniae</I> TMS-3, in which OFLX showed only slight effect, BLFX showed a therapeutic effect similar to SPFX and TFLX. BLFX showed almost the same activity as OFLX in mice with pyelonephritic infection due to <I>Escherichia coli</I> TMS-3. The peak levels of BLFX in murine serum, lungs and kidneys after a single oral administration of 50 mg/kg were 3.35±0.95μg/ml (15 min after administration), 9.57±2.67μg/g (15 min) and 11.64±2.43μg/g (30 min), respectively.

Journal

  • Japanese Journal of Chemotherapy

    Japanese Journal of Chemotherapy 43, 17-26, 1995-11-27

    Japanese Society of Chemotherapy

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