1981 Volume 34 Issue 12 Pages 1634-1646
The authors have carried out the laboratory and clinical studies of cefroxadine (CXD), and obtained the fbllowing results.
The antibacterial activities of CXD were measured by plate dilution method on 26clinical isolates of S. aureus, E.coliand K.pneumoniae.
CXD inhibited the growth of all strains of S.aureus at concentrations less than 6.25 μg/ml, and the peak of activity distribution was obtained at 3.13μg/ml with an inoculum size of 106cells/ml. And the peak sensitivity distribution of, E.coli was obtained at 6.25μg/ml. The growth of all strains of K. pneumoniae was inhibited at concentrations of less than 25μg/ml.
Phagocytosis was determined by QulE's method. In the presence of CXD, phagocytosis of human PMNs was not enhanced to E.coli and K. pneumoniae.
For pharmacokinetic study, CXD was given orally at a single dose of 10mg/kg to 3 children befbre and after meals. The serum levels of CXD on fasting were 14.2μg/ml, 11.0μg/ml, 4.0μg/ml and 0.57 μg/ml at 0.5, 1, 2, 4 hours after administration respectively, and the level at6hours was not detectable. Half-1ife was 0.65hours.
The serum levels of CXD after meals were 3.9μg/ml, 5.3μg/ml, 5.3μg/ml, 2.4μg/ml and 0.42 μg/ml at 0.5, 1, 2, 4, 6hours after administration respectively, but at 8 hours it was not detectable. Half-1ife was 0.95hours.
The 8-hour urinary excretion rates on fasting and non fasting were 89.4%, 89.0% respectively.
CXD was given to 31 cases with tonsillitis, 4 with bronchitis, 1with impetigo, 3 with cervicallymphadenitis, 7 with U. T. I, totalling 46. A daily dose of CXD 400-1, 500mg was given for 4-14 days.
Clinical results obtained were good and excellent responses in 43/46 (93.5%) cases.
No side effects were observed except for lcase with elevation of GOT, 2 cascs with elevation of GOT and GPT and 1case with eosinophilia.
