1984 Volume 32 Issue Supplement2 Pages 180-190
TA-058, a new parenteral penicillin, has been investigated to give following results.
1) Antibacterial activities
MICs of TA-058 against 220 strains of S. aureus, E. coli, P. aeruginosa and Proteus spp. isolated clinically was determined using plate dilution method inoculum size in 106 cells/ml. The peak of the minimum inhibitory concentration was 12.5μg/ml for S. aureus, 3.13 for E. coli, 0.78 forP. mirabilis, 3.13 for P. morganii, and 1.56 for P. aeruginosa.
2) Pharmacokinetics
Serum levels and urinary excretion of TA-058 after single intravenous injection of 2.0 g of the drug were measured in 6 healthy male volunteers.
The mean peak serum level of the drug, five minutes after injection was 263.3μg/ml, and 4.4μg/ml in serum was detected after 6 hours. The mean value of biological half life in serum was calculated 1.62 hours in β phase.
The mean urinary excretion rate was 76.1% within 6 hours. Although clinical laboratory tests were examined, no abnormal finding due to the drug was observed.
TA-058 was thought to be a good tolerable drug from this study.
3) Clinical results
Twenty four patients with various infectious diseases including sepsis, respiratory tract infections, bilary tract infections and urinary tract infections were treated with 2-4g daily dose of TA-058 for 5-15 days. Clinical effect was excellent in 11 cases, good in 7 cases, fair in 3 cases and poor in 3 cases. It was 75.0% of the efficacy rate of the drug.
As to the side effect, diarrhoea was occured in one patient, and no abnormal laboratory findings were noted.
