Laboratory and clinical studies of cefoperazone (CPZ), a new semisynthetic cephalosporin, were investigated and following results were obtained.
(1) Blood level: CPZ was given intravenous dose.of, 25mg/kg and50mg/kg to each3children.In the former, the blood level of15minutes after injection was194.2mcg/ml on average and the half life was106.2minutes.In the latter, the blood level was 320.0mcg/ml pn average and half life was 102.2minutes.
(2) Urinary concentration: In the cases of the dose of 25mg/kg, 35.9%of CPZ was recovered on average from the urine within6hours after injection, and the urinary concentration reached to 2,148.6mcg/ml (0-2 hours).And in the cases of the dose of 50mg/kg, dip recovery rate in urine was 43.6%, and the urinary concentration was 3,008.3mcg/ml.
(3) Cerebrospinal fluid level: CSF level was determined in a patient with bacterial meningitis by
S.pneumoniae. Ninety mg/kg of CPZ were given intravenous Injection.After 60 minutes CSF level was 3.35mcg/ml, and after 80 minutes the blood level was 192.0mcg/ml.
(4) Bacteriological evaluation: Against 164 strains isolated clinical specimens, the bacteriological evaluation on CPZ was performed in comparison with cefotaxime (CTX), cefazolin (CEZ) and piperacillin (PIPC) by inoculum size of 10
8 cells/ml.CPZ showed antibacterial.activity against Gram-negativebacteria almost similar to CTX and PIPC.
(5) Clinical results: CPZ was given48.3-360mg/kg/day (average146.1mg/kg/day) by intravenous route to46patients with various infection.The overall efficacy rate was 80.4%, The rate of bacteriological effectiveness was 78.9%in 19 cases.
(6) Side.effects: As side effects, diarrhea, fever, rash, urticaria, leukopenia, eosinophilia, elevation of GOT, GPT, and LDH were observed, but not seriously.
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