Nishimura T, Takashima T, Hiromatsu K, Tabuki K, Takagi M
Jpn J Antibiot. 1983 Jun;36(6):1301-12.
The authors have carried out the laboratory and clinical studies of cefotetan (CTT), and obtained the following results. The antibacterial activities of CTT were measured by the plate dilution method against the clinical isolates of S. aureus, E. coli, K. pneumoniae, S. marcescens and Salmonella sp. The susceptibility distribution of S. aureus to CTT was at concentration of 6.25-12.5 micrograms/ml and the peak of that was obtained at 6.25 micrograms/ml with an inoculum size of 10(6) cells/ml. And the peaks of susceptibility distribution of E. coli and K. pneumoniae to CTT were obtained at less than 0.1 microgram/ml respectively, and that of S. marcescens was obtained at 6.25-12.5 micrograms/ml with an inoculum size of 10(6) cells/ml. The growth of all strains of Salmonella sp. was inhibited at concentration of less than 0.1 microgram/ml. As for pharmacokinetic study, CTT was given by intravenous bolus injection and drip infusion for 30 minutes at a single dose of 20 mg/kg. After intravenous bolus injection of 20 mg/kg of CTT, the mean peak serum level was 175.0 +/- 7.0 micrograms/ml at 15 minutes after injection, and half-life time was 3.53 hours. After 30 minutes drip infusion of 20 mg/kg of CTT, the mean serum concentration was 106.0 +/- 6.0 micrograms/ml at end of infusion, half-life time was 2.41 hours. The mean urinary excretion rates were 49.4% and 64.2% up to 8 hours after drip and bolus injection of 20 mg/kg of CTT, respectively. CTT was given 15 cases with bacterial infection. Daily doses of CTT were from 15.0 to 107.0 mg/kg. Clinical results obtained were excellent and good responses in 12 of 15 cases (80.0%). No side effects were obtained except for 2 cases with elevation of GOT and GPT, and 1 case with eosinophilia.
作者进行了头孢替坦(CTT)的实验室和临床研究,获得了以下结果。采用平板稀释法测定CTT对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌、粘质沙雷氏菌和沙门氏菌临床分离株的抗菌活性。金黄色葡萄球菌对CTT的敏感性分布在浓度为6.25 - 12.5微克/毫升,接种量为10(6)个细胞/毫升时,在6.25微克/毫升处达到峰值。大肠杆菌和肺炎克雷伯菌对CTT的敏感性分布峰值分别在低于0.1微克/毫升时获得,粘质沙雷氏菌在接种量为10(6)个细胞/毫升时,在6.25 - 12.5微克/毫升处达到峰值。所有沙门氏菌菌株在浓度低于0.1微克/毫升时生长受到抑制。关于药代动力学研究,以20毫克/千克的单剂量通过静脉推注和30分钟静脉滴注给予CTT。静脉推注20毫克/千克CTT后,注射后15分钟时平均血清峰值水平为175.0±7.0微克/毫升,半衰期为3.53小时。以20毫克/千克CTT进行30分钟静脉滴注后,滴注结束时平均血清浓度为106.0±6.0微克/毫升,半衰期为2.41小时。分别在以20毫克/千克CTT进行滴注和推注后8小时内,平均尿排泄率分别为49.4%和64.2%。对15例细菌感染患者给予CTT。CTT的日剂量为15.0至107.0毫克/千克。15例中有12例(80.0%)临床结果为优或良。除2例谷草转氨酶(GOT)和谷丙转氨酶(GPT)升高以及1例嗜酸性粒细胞增多外,未观察到副作用。