In vitro and in vivo antibacterial activity of temafloxacin

概要

論文の詳細を見る
In vitro and in vivo antibacterial activity of temafloxacin (TMFX), a new fluoroquinolone, was compared with that of ciprofloxacin (CPFX), ofloxacin (OFLX), and norfloxacin (NFLX). The results are summarized as follows: 1) The potency of TMFX against gram-positive aerobic bacteria was higher or comparable to that of CPFX, OFLX and NFLX. 2) TMFX was less active than CPFX against most gram-negative enteric bacteria and Pseudomonas species, but was generally as active as OFLX and NFLX, except against Proteus species and Morganella morganii. 3) TMFX showed bactericidal action at concentrations near the MIC against a variety of bacteria. 4) The activity of TMFX was unaffected by different media, inoculum sizes, and horse serum, but decreased under acidic conditions and in the presence of magnesium ion. 5) TMFX yielded low-frequency mutation rates, the same as other fluoroquinolones. 6) TMFX strongly inhibited the supercoiling activity of DNA gyrase purified from Escherichia coli. 7) The in vivo efficacy of TMFX after oral administration was higher or comparable to that of CPFX against Staphylococcus aureus, E. coli and Pseudomonas aeruginosa systemic infection models.
公益社団法人日本化学療法学会の論文