Cefsulodin (SCE-129, CFS), a new cephalosporin derivative developed by Takeda Chemical Industries LTD., was examined as to its in vitro activity against clinically isolated bacteria, its serum level and urinary excre tion rate in humans after intramuscular injection, tissue concentrations in rats as well as its effectiveness in clinical cases.
The results obtained were as follows:
1) Antibacterial activity: MIC of CFS against 50 strains of Pseudoinonas aeruginosa were 0.8 to 3.1μg/ml similar to those of Dibekacin and Gentamicin.
2) Serum levels in adult men: The drug showed a serum peak level as high as 13-23μg/ml one hour after 0.5g i.m. injection, being still detectable (1, 7-4.0 μg/ml) 6 hours after the administration.
3) Distribution in rat organs: The highest tissue concentration of CFS in rat organs aftei i.m. administration (10mg/kg) was found in kidneys, followed by blood, lung, spleen, liver and muscles.
4) Clinical trials: Six clinical cases with Pseudornonas infections (chr. bronchitis 1 UTI 3, and decubitus 2; all having underlying diseases) were treated with CFS 250-1, 000 mg/day i.m. Although the Pseudomonas infections of the five cases, except for one bronchitis case, well responded to the therapy, substitution of the pathogen by other organisms were commonly observed after the treatment. No adverse effects or abnormal laboratory findings caused by CFS were observed.
