Bactericidal Activities of Methoxyfluoroquinolones Gatifloxacin and Moxifloxacin against Aerobic and Anaerobic Respiratory Pathogens in Serum

Abstract

ABSTRACT Gatifloxacin (Bristol-Myers Squibb) and moxifloxacin (Bayer) are new methoxyfluoroquinolones with broad-spectrum activity against aerobic and anaerobic pathogens of the respiratory tract. In this investigation, we analyzed the bactericidal activity in serum over time of these antimicrobials against three aerobic ( Streptococcus pneumoniae, Haemophilus influenzae, and Staphylococcus aureus ) and four anaerobic ( Peptostreptococcus micros, Peptostreptococcus magnus, Fusobacterium nucleatum, and Prevotella melaninogenica ) bacteria associated with respiratory tract infections. Serum samples were obtained from 11 healthy male subjects following a single 400-mg oral dose of gatifloxacin and moxifloxacin. These samples were collected prior to and at 2, 6, 12, and 24 h after the dose of each drug. Gatifloxacin exhibited bactericidal activity for a median of 12 h against Streptococcus pneumoniae (MIC = 0.5 μg/ml), Peptostreptococcus micros (MIC = 0.25 μg/ml), and F. nucleatum (MIC = 0.5 μg/ml) and 24 h against H. influenzae (MIC = 0.03 μg/ml), Staphylococcus aureus (MIC = 0.125 μg/ml), Peptostreptococcus magnus (MIC = 0.125 μg/ml), and Prevotella melaninogenica (MIC = 0.5 μg/ml). Moxifloxacin exhibited bactericidal activity for a median of 24 h against Streptococcus pneumoniae (MIC = 0.125 μg/ml), H. influenzae (MIC = 0.015 μg/ml), Staphylococcus aureus (MIC = 0.06 μg/ml), F. nucleatum (MIC = 0.5 μg/ml), Prevotella melaninogenica (MIC =0.5 μg/ml), Peptostreptococcus magnus (MIC = 0.125 μg/ml), and Peptostreptococcus micros (MIC = 0.25 μg/ml). The results from this pharmacodynamic study suggest that these fluoroquinolones would have prolonged killing activity against these organisms in vivo and may have clinical utility in the treatment of mixed aerobic-anaerobic respiratory tract infections.