小児科領域における Cefbtetan の基礎的・臨床的検討

: Preclinical and clinical studies were carried out on cefotetan (CTT), a new synthetic cephamycin antibacterial agent. The results are described below. Antibacterial activity The minimum inhibitory concentrations (MICs) of CTT, CEZ, CTM and CMZ were determined against clinical isolates of S. aureus, E. coli, K. pneumoniae and P. mirabilis. To CTT S. aureus, showed its sensitivity peak (in the graphic plot of the MIC distribution) at a concentration range of 3.13-6.25 micrograms/ml when a 100-fold dilution of the pathological specimen was employed as the inoculum. These results were inferior to those with CEZ and CTM by 2-4 concentration tubes. The CTT results were also about 2 tubes inferior to the results with CMZ, which is a cephamycin antibiotic. On the other hand, CTT was found to show very strong antibacterial activity against Gram-negative rods. For example, the sensitivity peak of E. coli, occurred at an antibiotic concentration of less than or equal to 0.1-0.2 microgram/ml, regardless of whether the inoculum was the undiluted pathological specimen or the 100-fold dilution thereof. Similar results were obtained in relation to the K. pneumoniae strains: at a CTT concentration of less than or equal to 0.1 microgram/ml, suppression of growth was achieved in 74% of the strains when the inocula were the undiluted specimens, and 86% when the inocula were the 100-fold dilutions thereof. In addition, against P. mirabilis, when the inoculum consisted of the undiluted pathological specimen the MIC peak for CTT occurred at a concentration range of 0.39-0.78 microgram/ml, whereas the peak occurred at 0.2-0.39 microgram/ml when the bacterial inoculum was the 100-fold dilution of the collected specimen. In contrast, CTM showed slightly stronger antibacterial activity than CTT in relation to P. mirabilis; that is, its MIC peak occurred at less than or equal to 0.1-0.2 microgram/ml when the inoculum was the undiluted pathological specimen, and at less than or equal to 0.1 microgram/ml when the bacterial inoculum was the 100-fold dilution. Otherwise, against these 3 species of bacteria, CTT yielded results which were clearly superior to those achieved with the other 3 antibiotics. Absorption and excretion CTT was administered to children at a dosage of 10 mg/kg and 20 mg/kg as a one-shot intravenous injection or as a 1-hour intravenous drip infusion. Thereafter, the serum concentration of the antibiotic was monitored and it excretion rate in the urine was also determined.(ABSTRACT TRUNCATED AT 400 WORDS)