02051nas a2200325 4500000000100000008004100001260001300042653001200055653002700067653001100094653001500105653001200120653000900132653002400141653003200165653001800197653004500215653002400260653003100284653003200315653001400347100001400361700001100375700001200386245010400398300001100502490000700513520119100520022001401711 1991 d c1991 Sep10aAnimals10aDisease Models, Animal10aFemale10aFleroxacin10aleprosy10aMice10aMice, Inbred BALB C10aMicrobial Sensitivity Tests10aMycobacterium10aMycobacterium Infections, Nontuberculous10aMycobacterium avium10aMycobacterium tuberculosis10aNontuberculous Mycobacteria10aOfloxacin1 aTomioka H1 aSato K1 aSaito H00aComparative in vitro and in vivo activity of fleroxacin and ofloxacin against various mycobacteria. a176-800 v723 a
In vitro antimicrobial activity of fleroxacin (6,8- difluoro-1-(2-fluoroethyl)-1, 4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid) and ofloxacin against representative pathogenic mycobacteria was evaluated by the agar dilution method, using 7H11 agar medium. Fleroxacin showed appreciable antimicrobial activity against Mycobacterium tuberculosis (MIC90 = 6.25 mg/l), M. kansasii (MIC90 = 3.13 mg/l), and M. fortuitum (MIC90 = 6.25 mg/l), whereas M. marinum, M. scrofulaceum, M. avium, M. intracellulare, and M. chelonae were highly resistant to the agent. The activity of fleroxacin was comparable to that of ofloxacin. Fleroxacin showed antimicrobial activity against M. intracellulare phagocytosed in murine peritoneal macrophages at a concentration of 10 mg/l in the culture medium, but its activity was considerably lower than that of ofloxacin. On the other hand, the therapeutic activity of fleroxacin against M. fortuitum infection induced in mice was higher than that of ofloxacin. Neither fleroxacin nor ofloxacin was efficacious against M. intracellulare infection. Fleroxacin significantly depressed the growth of M. leprae in the mouse footpad.
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