1984 Volume 32 Issue Supplement2 Pages 239-252
The antimicrobial activity, absorption, excretion and clinical effects on TA-058 were investigated and the following results were obtained.
1) Antimicrobial activity
The antimicrobial activities of TA-058 against the following clinically isolated organisms, i. e. E. coil, K. pneumoniae, Enterobacter sp., C. freundii, indole-positive Proteus sp., P.mirabilis and P aeruginosa, were 1-2 steps higher than ampicillin, carbenicillin and ticarcillin to E. coil, K. pneumoniae, Enterobacter sp., C. freundii, P. mirabilis and P. aeruginosa, while 2 steps lower than piperacillin to those organisms.
2) Serum levels
The serum levels of TA-058 in healthy adult volunteers after intravenous injection in a single dose of 1, 000 mg attained to 94μg/ml within 5 min. and 20 μg/ml within 1 hr. after the injection. When TA-058 was administered in combination with probenecid to the same volunteers, serum levels were almost similar to those when TA-058 was administered alone.
3) Urinary excretion
The maximum urinary concentration of TA-058 reached to 1, 900-4, 600μg/ml, and within 8 hours after TA-058 injection, 74.3 % of the drug was recovered in average from the urine.
4) Clinical results
TA-058 was administered in 3 cases of urinary tract infections who had chronic renal diseases. The results were 2 good and 1 poor. No side effect was observed.
