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SOME BIOLOGICAL PROPERTIES OF CEPHALOSPORIN C AND A DERIVATIVE
Author(s) -
JAGO M.,
HEATLEY N. G.
Publication year - 1961
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1961.tb00310.x
Subject(s) - cephalosporin , cephalosporin antibiotic , microbiology and biotechnology , pyridinium , antibiotics , chemistry , urine , pyridine , pharmacology , cephalosporin c , medicine , biology , biochemistry , medicinal chemistry
Some biological properties of cephalosporin C and of a pyridinium derivative, “cephalosporin C A (pyridine),” were examined. Staphylococci, both penicillinase‐producing and non‐penicillinase‐producing, and some other bacteria tested, were inhibited by 60 to 125 μg cephalosporin C/ml., and 5 to 20 μg cephalosporin C A (pyridine)/ml. The ratio of the activity of the two antibiotics varied for different organisms. Resistance developed slowly on repeated subculture of penicillinase‐producing staphylococci in presence of either antibiotic. The minimum inhibitory concentration of cephalosporin C A (pyridine) upon penicillinase‐producing staphylococci increased 4 to 8‐fold with a 500‐fold increase in inoculum size; with cephalosporin C there was a 2‐fold increase. Their activity was not reduced by serum. Both substances were non‐toxic. They were excreted quantitatively in the urine when given intravenously or subcutaneously to mice. After oral administration less than 5% of the dose was excreted. Cephalosporin C A (pyridine) was about 8 times more active than cephalosporin C in protecting mice from an experimental streptococcal infection, nine doses of 6.25 mg/kg affording complete protection.