[Experimental and clinical studies on cefoperazone (author's transl)]

Experimental and clinical studies were conducted on a new synthetic cephalosporin antibiotic cefoperazone (CPZ). Antibacterial activity of CPZ against S. aureus, E. coli, Klebsiella sp., Proteus sp. and P. aeruginosa was compared with that of cefazolin (CEZ), cephalothin (CET), gentamicin (GM) and cefotaxime (CTX). Ordinary cephalosporin C antibiotics, CEZ and CET showed an excellent antibacterial activity against S. aureus, while CPZ showed a low MIC of 3.13 mcg/ml even 10(6)/ml inoculation. CPZ showed an antibacterial activity against Gram-negative bacteria such as E. coli, Klebsiella sp. and Proteus sp. Its activity was very similar to CTX and superior to CET and CEZ. CPZ showed the greatest activity against P. aeruginosa, i.e., 2 tubes greater than CTX. By intravenous injection, the peak of blood concentration of CPZ treated with 25 mg/kg was 42 mcg/ml (4 cases); in the case of 1 hr. drip infusion, the peak of blood concentration with same dose was 41.25 mcg/ml at the end of drip infusion. By both routes of administration, the half lives were noted to be as long as 101.4 and 84.8 minutes, respectively. The recovery rates (3 cases) in the urine were quite different: 60.8%, 22.6% and 76.8% at 6 hours after administration. The spinal fluid concentration of CPZ was about 5 mcg/ml in the acute stage during the first 5 days and the CSF/serum ratio was above 10%. Clinical evaluation of CPZ was performed in a total of 31 cases; 13 cases of respiratory tract infection, 8 cases of urinary tract infection, 2 cases of staphylococcal scalded skin syndrome, 2 cases of enterocolitis, 2 cases of septicemia and 4 cases of purulent meningitis. Of 31 cases, CPZ proved to be markedly effective or effective in 28 cases, an efficacy rate of 90.3%. CPZ was found to e ineffective in 1 case of pyothorax and 2 cases of septicemia. Of the two cases of septicemia, one who had been also suffering from ecthyma gangrenosum suspected to be caused by P. aeruginosa and died within 10 hours of admission. Therefore, it may be better to consider this case an unknown case. Side effects observed during the therapy were 1 case of rash and 1 case of a rise of BUN.