Abstract
1. Minimum inhibitory concentrations (MICs) of levofloxacin (LVFX, DR-3355), ofloxacin (OFLX), tosufloxacin (TFLX), norfloxacin (NFLX) were determined, with an inoculum size of 106 cfu/ml, against 122 strains of Staphylococcus aureus isolated from lesions of skin infections. LVFX showed most frequent MIC values of 0.20μg/ml. OFLX, TFLX, and NFLX showed most frequent MIC values of 0.39μg/ml, ≤0.05μg/ml and 0.78μg/ml, respectively.
2. Serum and skin levels of LVFX after oral administration (10mg/kg, fasting) were determined in rats. Serum levels were 1.79, 1.29, 0.60, 0.43 and 0.18μg/ml, and corresponding skin levels were 1.63, 1.77, 1.04, 0.87 and 0.64μg/g (wet weight) at 0.5, 1, 2, 4 and 8 hours after administration (n=5), respectively.
3. LVFX was used clinically in 43 cases at doses of 200-300 mg divided into 2 or 3 doses, and evaluated for final overall clinical efficacy in 41 cases. Cure was observed in 21 cases, remarkable improvement in 13 cases, improvement in 4 cases, unchanged in 1 case, aggravation in 1 case, and remarkable aggravation in 1 case. Diarrhea was obseved in 2 cases, diffuse erythema with feverishness in 1 case and slight dyspnea in 1 case. Transient slight eosinophilia, elevation of Al-P, anemia and leukopenia were observed.
