Abstract: | The authors have carried out the laboratory and clinical studies of cefoperazone (CPZ). The results were as follows: The sensitivity was estimated by plate dilution method on 26 strains of S. aureus, E. coli and K. pneumoniae, 25 strains of P. aeruginosa, 14 strains of Salmonella sp. and 9 strains of GM resistant P. aeruginosa isolated from patients. The distribution of sensitivity of S. aureus was 1.56 approximately 25 mcg/ml and the peak of distribution was 3.13 mcg/ml. The growth of 96.2% of E. coli was inhibited at concentration of less than 12.5 mcg/ml. The growth of 50.0% of K. pneumoniae was inhibited at concentration of less than 6.25 mcg/ml. The peak of distribution of P. aeruginosa was 12.5 approximately 25 mcg/ml (GM sensitive) and 12.5 mcg/ml (GM resistant). CPZ was given by drip infusion for 30 minutes at a single dose of 25 mg/kg to 2 children, and by drip infusion for 60 minutes at a single dose of 46.9 mg/kg to a child. The serum mean level of CPZ was 127.5 +/- 8.5 mcg/ml at 30 minutes, 30.5 +/- 7.5 mcg/ml at 1 hour, 23.5 +/- 3.5 mcg/ml at 2 hours, 10.5 +/- 1.5 mcg/ml at 4 hours and 6.8 +/- 2.4 mcg/ml at 6 hours after administration at a single dose of 25 mg/kg, respectively. The serum level was 102.0 mcg/ml at 1 hour, 32 mcg/ml at 2 hours, 14.5 mcg/ml at 5 hours and 12.5 mcg/ml at 7 hours after administration at a single dose of 46.9 mg/kg. Half-life time was 92 minutes. The mean urinary excretion rate was 32.0 +/- 7.3% in the drip infusion for 30 minutes up to 8 hours after administration. CPZ was effective in 6 of 8 cases with pediatric bacterial infections. No side effects were observed except for 1 case with elevation of GOT. |