1984 Volume 32 Issue Supplement2 Pages 686-697
MIC of TA-058 and AMPC against 210 strains of GNR including each 30 strains of E. coli, K pneumoniae, P. mirabilis, P. vulgaris, Enterobacter, S. marcescens and P. aeruginosa isolated from U. T. I. were measured by agar dilution method with inocutum size of 108/ml and 106/ml. Antibicterial, activity of TA-058 against E. coli showed two peaks of MIC distribution at 3.13μg/ml and higher than 100μg/ml. Antibacterial activities of TA-058 seemed to be one fold stronger than AMPC. Both drugs did not demonstrate strong activity against K pneurnoniae and P. mirabilis. Nevertheless, TA-058 was, a little superior than AMPC. P. vulgaris, Enterobacter and S. marcescens seemed to be resistant to both drugs. P. aeruginosa was not sensitive to this drug with 108/ml inoculum size but 19 out of 28 strains (67.896) distributed from 3.13μg/ml to 50 with 106 /ml inoculation.
Bolus injection of 2 g of TA-058 and SBPC was administered to 4 male healthy volunteers by cross-over method. Serum peak level was obtained 5 minutes after the injection, 148.3μg/ml for TA-058 and 202.5μg/ml for SBPC. Serum half-life of fl-phase of the drug was 1.5 hours, which was a little longer than that of SBPC. AUC of the two drugs ranged 191.2μg/ml·hr. and 219.1μg/ml·hr., respectively. trinary excretion rate of TA-058 and SBPC until 6 hours was measured as much as 81. 1% and 82.6%, respectively. Maximum urinary concentration was recorded at the first 1 hour urine, 16, 675μg/ml for TA-058 and 9, 875μg/ml for SBPC. TA-058 was administered to 22 patients with chronic U. T. I. I to 4g daily for 5 days. Overall clinical efficacy according to the 2 nd criterion recommended by Japanese U. T. I. committee was evaluated excellent in 6, moderate in 7 and poor in 9 cases, counting 59.1% of effectiveness rate.
Five strains of S.faicalis and a few of K. pneurnoniae, P. aeruginosa, E. coli, S. marcescens and other bacteria were cleared from the urine after the treatment.
No adverse subjective effect and abnormal clinical laboratory test were observed with this regimen.
