Abstract
Grepafloxacin (GPFX) was studied basically and clinically with the following results:
In the basic study, the MICs of GPFX on gram-positive bacilli (GPB; methicillin-susceptible Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Enterococcus faecalis) and gram-negative bacilli (GNB; Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Acinetobacter calcoaceticus, Moraxella catarrhalis, Haemophilus influenzae) were compared with those of other new quinolone antibacterial drugs (ofloxacin, ciprofloxacin, tosufloxacin, sparfloxacin), clavulanic acid/amoxicillin, cefixime, and cefteram pivoxil. The MICs of GPFX on GPB ranged from ≤0.05-1.56μg/ml with the MIC90 below 0.78μg/ml, indicating excellent antibacterial activity. On the other hand, the MICs of GPFX on GNB ranged from ≤0.05-3.13 except for ≤0.05-12.5μg/ml for E.coli and 0.2-100μg/ml for P.aeruginosa, and the effect of GPFX was almost equal or inferior to those of other control drugs. The MIC90 were all below 0.78μg/ml except for 25μg/ml for P.aeruginosa, indicating a superior effect.
In the clinical study, GPFX was administered to 20 patients with respiratory infections at a dose of 150mg once or twice a day for 3-7 days. The result was remarkably effective in 6 cases, effective in 8, slightly effective in 3, and ineffective in 3 (efficacy rate: 70%). As for adverse reactions, thirst and constipation were observed in 1 case each, but disappeared spontaneously after withdrawal. No abnormal laboratory changes were observed throughout this study. Thus GPFX was confirmed to be a very safe, useful drug.
