Laboratory and clinical studies on temafloxacin

The newly developed broad-spectrum fluoroquinolone, temafloxacin (TMFX), was evaluated in vitro and in vivo in comparison with ofloxacin (OFLX), ciprofloxacin (CPFX) and norfloxacin (NFLX). The results were as follows: 1. Antimicrobial activity: Minimal inhibitory concentrations (MICs) against 483 clinical isolates including 15 different species were determined by the microbroth dilution method. TMFX showed excellent antimicrobial activity against gram-positive bacteria in particular.The MIC values for 3 species of gram-positive bacteria were superior to those of the other quinolones tested except against Streptococcus pyogenes and Enterococcus faecalis, for which TMFX was equal to CPFX. The MIC values for gram-negative bacteria were below those of CPFX, especially for Morganella morganii, Citrobacter freundii, Proteus vulgaris and Pseudomonas aeruginosa. TMFX, however, showed equal activity to OFLX and NFLX against the other gram-negative bacteria. 2. TMFX concentrations in serum and sputum: TMFX was orally administered at a single dose of 300 mg to two patients with chronic lower respiratory diseases, and the concentrations in serum and sputum were measured by HPLC. The peak concentrations of TMFX in the serum and sputum of one patient were 2.98 and 3.38 μg/ml, respectively, and those of the other patient were 1.80 and 1.45 μg/ml, respectively. From these data, it was suggested that TMFX has good penetration into sputum. 3. Clinical efficacy and adverse reactions: Twenty-six patients with respiratory tract infections were treated with TMFX, and the overall efficacy rate was 76% (exellent in 2 cases, good in 17, fair in 5, poor in 1, and not evaluable in 1). Stomach discomfort was observed as a side effect in one patient. Although the elevation of GPT was observed in one case, leukopenia in 1 case and the elevation of GOT, GPT and ALP in 1 case, these abnormal laboratory findings were mild and improved rapidly after the completion of TMFX treatment.