1984 Volume 32 Issue Supplement2 Pages 621-636
Fundamental and clinical studies on TA-058, a new injectable penicillin derivative, were performed, and following results were obtained.
1) Antibacterial activities
Antibacterial activities against clinically isolated 8 spieces were investigated, and approximately TA-058 displayed near equal activity in MICs comparison with CBPC, but slightly less activity than PIPC.
2) Serum levels and urinary excretions
Serum levels and urinary excretions of TA-058 after i. v. drip infusion of 1, 000 mg were determined in 3 male healthy adult volunteers.
When comparison of infusion time for 1 hr. and for 2 hr. was examined in this trial, in the former case the peak serum concentration was 60.7μg/ml, while in the latter case 31.5μg/ml. Similarly the peak urinary concentration showed value of 2, 809.6 μg/ml and 3, 709.1 μg/ml. respectively.
Urinary recovery rate was 76.1% and 77.0% within 24 hr. after administration.
3) Clinical evaluations TA-058 was treated in 10 cases of acute simple cystitis and 45 cases of complicated urinary tract infections (UTI). The cure rate for acute simple cystitis was 100% and for complicated UTI was 38%.
The rate of bacteria eradication in acute simple cystitis was 100%, and that of in complicated UTI was 63%.
As for side effects (total subjects: 65 cases), a slight anaphylactoid shock was observed in one case, however the symptom was immediately recovered by fluid therapy. Laboratory findings showed elevation of transaminases in two cases.
