Laboratory and clinical studies on temafloxacin

We performed laboratory and clinical studies on temafloxacin (TMFX), a new oral pyridonecarboxylic acid, with the following results. 1) Minimal inhibitory concentrations (MIC) of TMFX were measured for 242 clinical isolates of 12 species, and compared with those of ciprofloxacin (CPFX), ofloxacin (OFLX) and enoxacin (ENX). The MIC values of TMFX against gram-positive cocci and Acinetobacter calcoaceticus were equal to those of CPFX, but superior to those of OFLX and ENX. In contrast, those of TMFX against gram-negative bacteria were inferior to those of CPFX, but equal to those of OFLX. Those of TMFX against Proteus spp. were less than those of the other three quinolones. 2) Effects of cimetidine (H₂-blocker) on absorption and excretion of TMFX were investigated in five healthy male volunteers. The time of the maximum TMFX concentration (Tmax) was delayed and the 12h-cumulative urinary recovery rates were decreased by cimetidine, but other data were not influenced. 3) The clinical efficacy of TMFX was evaluated in a total 33 patients; 6 with pneumonia, 1 with pneumonia and cystitis, 8 with acute bronchitis, 1 with acute bronchitis and an infected decubitus ulcer, 4 with chronic bronchitis, 1 with infected pulmonary infarction, 3 with pharyngitis and laryngitis, 1 with acute pharyngitis and cystitis, 6 with cystitis, 1 with bacillary dysentery and 1 with acute lymphadenitis. The patients were given a daily dose of 150~300 mg, b.i.d. or t.i.d. for 2~37 days. The clinical response was excellent in 9 cases, good in 22 cases, fair in 2 cases and poor in 3 cases, the efficacy rate being 86.1 %. Bacteriologically, 14 of 16 strains isolated from respiratory tract infections and 8 of 9 strains isolated from urinary tract infections were eradicated by treatment with TMFX. The side effects observed in 3 cases were vomiting/epigastralgia, fever/headache and general fatigue. Elevations of GOT and GPT were observed in a case.