1984 Volume 32 Issue Supplement2 Pages 339-352
TA-058, a new derivative of amoxicillin recently developed by Tanabe Seiyaku Co., Ltd. was examined on its blood levels and urinary excretion rates in humans administered with the drug.
Some clinical trials were as follows;
1) In vitro antibacterial activity against bacteria isolated from human infection foci: MIC of the drug against S. aureus strains distributed from 0.4 to > 100μg/ml; while those resistant to apalcillin or piperacillin showed somewhat better sensitivity against TA-058.
Against E. coli, TA-058 showed similar activity to piperacillin, the MIC peak being located at O.8-6.2μg/ml. TA-058 was less active against P. aeruginosa and K. pneumoniae than piperacillin or apalcillin.
2) Blood levels and urinary excretion rates in human: The blood level of TA-058 in plasma after intravenous drip infusion of 500mg in 15 min. was 60μg/ml.
The urinary excretion rate of the antibiotic during six hours after administration was 78.8%.
3) Clinical trials: All of thirteen patients with various infections (pneumonia 7, acute bronchitis diffuse panbronchitis 1, and acute exacerbation of chronic bronchitis 3) responded at least fairly the treatment with TA-058 (2-4g/day, intravenous drip infusion, 6-11 days), excepting a case Candida in sputum and a case of diffuse panbronchitis by H. influenzae.
As to the side effects or abnormal laboratory findings attributable to the drug, only one out of the thirteen cases showed a transient elevation of S-GOT and S-GPT.
