CHMOTHERAPY OF BILIARY TRACT INFECTIONS (XIX) WITH EXCRETION IN BILE AND ITS CLINICAL EFFECT USING A NEW ANTIBIOTIC, TA-058
1984 Volume 32 Issue Supplement2 Pages 502-513
Details
1984 Volume 32 Issue Supplement2 Pages 502-513
Biliary excretion and clinical efficacy in biliary tract infections of TA-058, a new penicillin antibiotic was reported that the antibacterial activity in vivo was more effective than in vitro, were studied and the following results were obtained.
1) Biliary concentration of TA-058 was compared with TIPC by crossover method. 1 g of each antibiotic was given intravenously to 2 patients who, had indwelling T-tubes. Both TA-058 and TIPC reached the peak biliary concentrations at 2 hours after their administrations. The peak biliary concentration of TA-058 and that of TIPC was 246.5μg/ml, 66.6μg/ml, respectively.
2) After i. v. administration of 1 g of TA-058, the mean concentration in gallbladder bile of 5 cases was 218.9μg/ml, and the mean concentration in the gallbladder tissues of 9 cases was 18.1μg/g.
3) TA-058, penicilloic acid and 5-epi-penicilloic acid were isolated and identified with highperformance liquid chromatographic (HPLC) method. Penicilloic acid and 5-epi-penicilloic acid were the metabolites of TA-058. The correlationship between chemical assay and bioassay results of the concentration of TA-058 in each bile was r=0.998.
The rates of the metabolites after i. v. administration of 1 g of TA-058 were 12.9-31.4%(average 24.6%), but after 3 weeks at -20°C conditions it showed an increase of about 30%.
4) TA-058 was administered intravenously at a dose of 1 g 2 times a day over 5-9 days in total of 22 cases including 11 cases of cholacystitis, 11 cases of cholangitis. The clinical results showed excellent in 3, good in 15, fair in 2, poor in 1 and unknown in 1 and the efficacy rate was 85.7%.
5) TA-058 was given to 38 cases including prophylactic use for postoperative infection, no side effects were observed.
