1980 Volume 28 Issue Supplement6 Pages 307-315
Basic and clinical studies on cefoperazone (CPZ, T-1551), a new broad spectrum cephalosporin derivative with 2, 3-dioxopiperazine, were carried out and the following results were obtained.
1) The MIC value distribution of CPZ was examined by plate dilution method against 200 clinical isolates of Pseudomonas aeruginosa. The peaks of susceptibility distribution of CPZ at inoculum size of 108 CFU/ml and 106CFU/ml were 12.5μg/ml and 6.25μg/ml, respectively. These results were similar to those of piperacillin.
2) The serum level and half-life of CPZ were measured following drip intravenous infusion of 1 and 2g doses for 1 hour. The mean peak level at the end of administration was 130μg/ml, ranged from 95μg/ml to 200μg/ml and the serum level after 2g administration was twice as high as those of 1g. The mean serum half-life was 2.36 hour and the mean urinary recovery within 6 hour was 20.5±1.9%, respectively. In 2 patients with obstructive jaundice due to pancreatic cancer, the biliary levels of CPZ following intravenous administration of 1 g were studied. The biliary level after 6 hour obtained was 106 μg/ml in 1 case, however, in other case was below assay limit.
3) Nineteen patients with various infections (6 respiratory, 4 biliary and 7 urinary tract infections and 2 other infections) were treated with CPZ in daily doses of 2 to 4g for 7 to 16 days. The majority of them were in advanced age and 10 patients had underlying diseases such as diabetes. GNR were mainly isolated 23 out of 29 strains, which were composed of each 4 of E. coli, Klebsiella and Pseudomonas and others. Clinical responses were excellent in 9 cases, good in 8 and fair in 2. The effective rate was 89.5%.
As to the side effect, a rash was observed in 1 case. The elevations of ALP and transaminase were observed in 2 cases. One case accompanied with rash was thought to be due to the drug administration, however, another case seems to have no direct correlation with the drug. Also, a slight decrease in RBC, Ht and Hb in 2 cases was thought to he not associated with the drug administration. It is concluded that CPZ was useful to the treatment of various infections due to GNR.
