<I>In vitro</I> and <I>in vivo</I> antimicrobial activities of a new quinolone antimicrobial drug, gatifloxacin

DOI 3 Citations 11 References
  • Aoki Koji
    Department of Microbiology, School of Medicine, Toho University
  • Miyazaki Shuichi
    Department of Microbiology, School of Medicine, Toho University
  • Tsuji Akiyoshi
    Department of Microbiology, School of Medicine, Toho University
  • Kaneko Yasuko
    Department of Microbiology, School of Medicine, Toho University
  • Yamaguchi Keizo
    Department of Microbiology, School of Medicine, Toho University
  • Goto Sachiko
    Department of Microbiology, School of Medicine, Toho University

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  • 新キノロン系抗菌薬gatifloxacinの<I>in vitro</I>及び<I>in vivo</I>抗菌作用

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Abstract

The in vitro and in vivo antimicrobial activities of a new quinolone antimicrobial agent, gatifloxacin (GFLX), were examined and compared with those of sparfloxacin (SPFX), tosufloxacin (TFLX), ciprofloxacin (CPFX), and ofloxacin (OFLX).<BR>GFLX had a broad antimicrobial spectrum, and its antimicrobial activity against Staphylococcus (including methicillin-resistant Staphylococcus aureus subsp. aureus (MRSA)), Streptococcus, and Enterococcus was higher than that of CPFX and OFLX, and almost equal to that of SPFX and TFLX. Against members of the family Enterobacteriaceae and glucose-nonfermentative Gram-negative rods (except for Pseudomonas aeruginosa), the antimicrobial activity of GFLX was the same as that of SPFX, TFLX, CPFX, and OFLX. The activity of GFLX for P.aeruginosa was similar to that of SPFX and OFLX. The antibacterial effect of GFLX against Bacteroides fragilis was the most active among all the drugs tested.<BR>The therapeutic effects of GFLX in a mouse systemic infection model were almost equal to those of SPFX against S.aureus subsp.aureus Smith, Streptococcus pneumoniae TMS3, Escherichia coli C11, and Pseudomonas aeruginosa E7. In a transnasal pulmonary infection model using S.pneumoniae TMS3 as the infective strain, the therapeutic effect of GFLX was superior to that of CPFX and OFLX.<BR>Peak levels of GFLX in murine serum, lungs, and kidneys after a single oral administration of 50 mg/kg were 3.86±0.61μg/mL (15min after administration), 7.80±6.58μg/g (2 hours) and 16.49±4.69μg/g (30 min), respectively.The peak concentration of GFLX was less than that of OFLX except in kidneys, but 2-6 times higher than that of CPFX and TFLX and equal to that of SPFX. The excellent therapeutic effects of GFLX can be attributed to its potent antibacterial activity and favorable tissue distribution.

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