1984 Volume 32 Issue Supplement2 Pages 706-716
TA-058, a newly developed penicillin, was evaluated id the field of obstetrics and gynecology, and the following results were obtained.
1) The antibacterial activity was determined in 15 species (70 strains) of clinical isolates. The sensitivity destribution ranged from 1.56 to 3.13 μg/ml in 27.2 % and 30 % with over 100 μg/ml.
2) As to the pharmacokinetics, concentration in serum was 34.7 μg/ml at 30 minutes after intravenous injection of 1 g. The half-life in serum estimated to be 78 minutes, and AUC was 64.6 μg/ml·hr. The urinary recovery rate was 58.1 % in 6 hours.
3) The tissue penetration of TA-058 in uterine artery serum, uterine and adnexal tissues after intravenous injection of 1 g were determined and pharmacokinetic analysis was performed. The peak serum concentration (Cmax) in uterine artery serum was 24.4 μg/ml and the half-life (T1/2 (β)) was 56.8 min. Cmax in each tissues were 10. 6-16.5 μg/g, Tmax were 42.9-52.6 min. and half-life (T1/2 (β)) were 45.2-55.3 min. The area under the curve (AUC) was 74.5 μg/mlμhr. in serum and were 25.8-41.4 μg/mlμhr. in each tissues. Penetration of TA-058 into intrapelvic genital organs was found to be good.
4) Rapid transference of TA-058 into the umbilical cord serum and amniotic fluid was observed after an intravenous injection of 1 g, and those levels were about 25-30 % of the mother's serum level.
5) Distribution of TA-058 into mother's milk after an intravenous injection of 1 g in puerperants was low.
6) TA-058 was administered intravenously to 10 cases of gynecoobstetrical infections with daily dose of 2-3 g. The good clinical responses were assessed in 9 cases and few side effects were observed. As for the laboratory findings, a little elevation of transaminase was observed in one case. These results indicates that TA-058 is a useful drug in the field of obstetrics and gynecology.
