1984 Volume 32 Issue Supplement2 Pages 374-389
Laboratory and clinical studies were performed on TA-058, a new semisynthetic penicillin antibiotic, and results were follows.
1) Antimicrobial activities
MICs of TA-058 against clinical isolates from our clinic were determined. With the inoculum size of 106cells/ml, percentages of strains susceptible to 12.5μg/ml or less were S.aureus 89%, S.faecalis 86%, E.coli 37%, K.pneumoniae 0%, Enterobacter sp. 63%, S.marcescens 4%, Proteus sp. 79%, P.aeruginosa 8%. Antimicrobial activities agaist Gram-positive cocci were inferior to AMPC, but its activities againt Gram-negative bacilli were superior to AMPC.
2) Serum levels and urinary excretion rates
Three healthy adults were bolusly injected with 2g of TA-058, and mean serum levels of TA-058 were 283.3μg/ml at the end of the injection, 3.3μg/ml after 6 hours. Pharmacokinetic parameters calculated with these data were T1/2 (β) 1.3hr., AUC 202μg/ml·hr. Urinary excretion rates were 66 % during 6 hours. In a case of chronic renal failure, urinary excretion rate was very small and T1/2 (β) was lengthened.
3) Clinical efficacy
Nine patients with pneumonia, 3 with bronchitis, 1 with pulmonary tuberculosis, 7 with cystitis, 4 with pyelonephritis, 3 with bacteremia, 1 with meningitis, 1 with arthritis, and 1 with perianal abscess were treated with TA-058 daily at a dose of 1-8 g for 3-55 days. Clinical responses were excellent in 2 cases, good in 16, fair in 4, poor in 6, and unknown in 2 cases. Its efficacy rates were 54.5% in RTI, 72.7% in UTI, and 66.7% in other cases. One patient complained of vascular pain on the first trial of TA-058. GOT, GPT elevation was observed in 2 patients and ALP elevation in a case, who had previously liver damages.
