Nishimura T, Tabuki K, Takashima T, Takagi M
Jpn J Antibiot. 1984 Nov;37(11):2131-40.
The authors have carried out the laboratory and clinical studies of ceftriaxone (Ro 13-9904, CTRX) and obtained the following results. The antibacterial activities of CTRX against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, Citrobacter sp. and P. aeruginosa were measured by the agar dilution method with inoculum size of 10(6) cells/ml. The susceptibility distribution of S. aureus to CTRX ranged from 0.2 to 12.5 micrograms/ml, and the peak of distribution was 3.13 micrograms/ml. The peak of susceptibility distribution of E. coli and K. pneumoniae were 0.1 microgram/ml or lower, and the distribution of E. aerogenes and E. cloacae ranged from 0.1 to 100 micrograms/ml, Citrobacter sp. and S. marcescens, from 0.1 to 12.5 micrograms/ml and that of P. aeruginosa, from 0.39 to 100 micrograms/ml or more. For pharmacokinetic study, CTRX was given in a single dose of 10 mg/kg in 1 child and 20 mg/kg in 2 children by drip infusion for 1 hour. After drip infusion of CTRX in a single dose of 10 mg/kg, the peak serum level was 61.4 micrograms/ml on completion of the infusion, and 8.43 micrograms/ml at 12 hours. Half-life time was 4.6 hours. With drip infusion of CTRX in a single dose of 20 mg/kg, the peak serum level was 105.5 micrograms/ml on completion of the infusion, and 19.1 micrograms/ml at 12 hours. Half-life time was 8.7 hours. CTRX was effective all cases out of 8 cases with bacterial infection. No side effect was observed except for elevation of serum GOT in 2 cases and eosinophilia in 1 case.
作者进行了头孢曲松(Ro 13 - 9904,CTRX)的实验室和临床研究,并获得了以下结果。采用接种量为10(6)个细胞/ml的琼脂稀释法测定了CTRX对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌、阴沟肠杆菌、产气肠杆菌、粘质沙雷氏菌、柠檬酸杆菌属和铜绿假单胞菌临床分离株的抗菌活性。金黄色葡萄球菌对CTRX的敏感性分布范围为0.2至12.5微克/毫升,分布峰值为3.13微克/毫升。大肠杆菌和肺炎克雷伯菌的敏感性分布峰值为0.1微克/毫升或更低,产气肠杆菌和阴沟肠杆菌的分布范围为0.1至100微克/毫升,柠檬酸杆菌属和粘质沙雷氏菌为0.1至12.5微克/毫升,铜绿假单胞菌为0.39至100微克/毫升或更高。在药代动力学研究中,1名儿童以10毫克/千克的单剂量静脉滴注1小时给予CTRX,2名儿童以20毫克/千克的单剂量静脉滴注1小时给予CTRX。以10毫克/千克的单剂量静脉滴注CTRX后,输注结束时血清峰值水平为61.4微克/毫升,12小时时为8.43微克/毫升。半衰期为4.6小时。以20毫克/千克的单剂量静脉滴注CTRX时,输注结束时血清峰值水平为105.5微克/毫升,12小时时为19.1微克/毫升。半衰期为8.7小时。8例细菌感染病例中,CTRX对所有病例均有效。除2例血清谷草转氨酶升高和1例嗜酸性粒细胞增多外,未观察到副作用。