1984 Volume 32 Issue Supplement2 Pages 575-587
In pharmacokinetic study, the absorption and excretion of TA-058 was studied in 4 healthy adult males by cross over method with CBPC as a control. Serum levels of the two drugs were similar except for their biological half lives. Namely, the half life (T½(β)) of TA-058 was 1.2 hr. and it was a little longer than that of CBPC, 0.8 hr. In the assessment on the penetration into human prostatic fluids, the mean level of TA-058 in prostatic fluids was 0.4 μg/ml (n=3) with the fluid/serum ratio of 0.009 at 1 hr. after single administration of 2 g.
Forty three patients (34 U.T.I. 7 gonococcal urethritis (GU) and 2 acute epididymitis) were treated with IA-058 at a dose of 1-4 g per day. Against 10 cases of simple U.T.I.(7 cystitis and 3 pyelonephritis), 100% cure rate was obtained. In complicated U.T.I., the efficacy rate was 54.2 % by the evaluation method of U.T.I. committee. In all of 7 GU, excellent results were gained. Satisfactory response was noticed in 2 acute epididymitis cases.
Concerning the in vitro activity on the clinical strains isolated from the treated cases, TA-058 had greater activity on the strains of E. coil, and gram positive cocci, such as S. faecalis and S.epidermidis, but less activity on P. aeruginosa.
There was no apparent untoward reaction except for one case of transient nausea. In the results of clinical laboratory values, slight elevation of s-GOT and s-GPT was observed in 4 cases and slight elevation of BUN in one case. No abnormal value was found in hematological studies.
It is concluded that TA-058, a new member of parenteral penicillins, is a safe, well tolerable antibiotic drug and clinically useful on the infections caused by E. coli, and other enteric rod bacteria, in addition to gram positive cocci.
