FUNDAMENTAL STUDIES ON TA-058
SENSITIVITY OF THE CLINICAL ISOLATES AND PASSAGE OF THE DRUG INTO THE CEREBROSPINAL FLUID IN STAPHYLOCOCCAL MENINGITIS IN RABBITS
1984 Volume 32 Issue Supplement2 Pages 73-76
Details
1984 Volume 32 Issue Supplement2 Pages 73-76
A new penicillin, TA-058, was evaluated in regard to MICs to 220 strains of various clinical isolates and passage into the cerebrospinal fluid (CSF) in experimental stapylococcal meningitis in rabbits, and the following results were obtained.
1) Antibacterial activity of the drug was slightly more active than ABPC against E. coli, Salmonella and P. mirabilis, however it showed cross-resistance against about 50% of E. coli isolates, those MICs were>100μg/ml and TA-058 was less active than ABPC against S. aureus. Both TA-058 and ABPC were scarcely active against Klebsiella and indole (+) Proteus, whereas few strains of Enterobacter, Citrobacter and S. marcescens was susceptible to ≤6. 25μg/ml of TA-058 only and also in P. aeruginosa few strains were susceptible to 25-100μg/ml of the drug.
2) With experimental staphylococcal meningitis in rabbits, concentration of TA-058 in the CSF was more higher than ABPC, since TA-058 maintained well absorbed in serum.
But a CSF/serum ratio of maximum concentration and AUC up to 2 hours was 4.84 % and 10.1%, respectively, then these values were lower than those of ABPC which had already been reported. However, TA-058 was recorded highest value in both T1/2 of CSF concentration and CSF/serum ratio compared with all other penicillins.
Based on-above results, it was suggested that TA-058 is a novel antibiotic in pharmacokinetically.
