1984 Volume 32 Issue Supplement2 Pages 642-652
Fundamental and clinical studies of TA-058 were performed and transfer of TA-058 into prostatic tissue was also scrutinized.
The following results were obtained;
1) Minimum inhibitory concentration of TA-058 was determined by plate dilution method on strains isolated from urinary tract infections. Antibacterial activities of TA-058 were markedly strong against P. mirabilis, moderately strong against E. coli and slightly weak K pneurnoniae, P. gulgaris and P.aeruginosa. However, S.marcescens was resistanoe to TA-058. As compaired with other penicillin derivatives, TA-058 was weaker than PIPC but equal or slightly strong than ABPC or CBPC in antibacterial activities.
2) Transfer of TA-058 into prostatic tissue to 13 patients with prostatectomy examined. Maximum concentration of TA-058 was observed 61. 5±28.5μg/g at 30 minutes after one shot intravenous administration of 2 g and still maintained 19.0±7.1μg/g at two hours after administration. Judging from its favorable tranfer into the prostatic tissue and MICs against clinically isolated S. aureus, S. faecalis, S epidermidis and P. mirabilis, TA-058 seemed to be clinically useful in the treatment of prostatic infections.
3) Twenty three cases with complicated urinary tract infections were treated with TA-058 and evaluated clinically by the criteria of U. T. I. committee. The group of 2 g daily (21 cases) resulted 28.5% of effective rate, whereas the group_of 4 g daily (2 cases) resulted 100% of effective rate. Bacteriologically, TA-058 showed superior antibacterial activities against gram-positive bacteria, Enterobacter, E. coli and P. mirabilis. 22 out of 34 strains were eradicated (eradicated rate: 64.7%). No noteworthy side effects attributable to TA-058 were observed.
