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头孢替坦在儿科的实验与临床评估

[Experimental and clinical evaluation of cefotetan in pediatrics].

作者信息

Iwata S, Iwasaki Y, Kanemitsu T, Tojo M, Jozaki K, Akita H, Kojima Y, Wakabayashi R, Sunakawa K, Osano M

出版信息

Jpn J Antibiot. 1983 Jun;36(6):1204-18.

PMID:6581327
Abstract

Preclinical studies were carried out on cefotetan (CTT), together with clinical studies in the field of pediatrics. The following results were obtained. A total of 114 clinical isolates that have been stored in the authors' department was employed to determine the minimum inhibitory concentrations (MICs) of CTT against various bacterial species. Against E. coli, Salmonella, K. pneumoniae and P. mirabilis, the MICs of CTT showed a peak at 0.78 micrograms/ml, and most of the strains were inhibited by a CTT concentration of 6.25 micrograms/ml or less. The MICs for S. marcescens strains showed a peak at 25 micrograms/ml, with 25% of the strains having MICs of 3.13 micrograms/ml or less, and 67% having MICs of 25 micrograms/ml or more. All of the P. aeruginosa strains had MICs of over 100 micrograms/ml. Against all of the tested strains of S. aureus, a Gram-positive bacterium, CTT showed MICs of 12.5 micrograms/ml or more, while all of the strains of S. faecalis were found to have MICs of over 100 micrograms/ml. CTT was administered intravenously to pediatric patients as a bolus injection, and then the concentration of the antibiotic in the serum was determined as a function of time. When the dosage rate was 10 mg/kg, the mean serum levels were as follows; 58.2 micrograms/ml at 30 minutes, 45.5 micrograms/ml at 1 hour, 33.6 micrograms/ml at 2 hours, 18.0 micrograms/ml at 4 hours and 11.7 micrograms/ml at 6 hours after the injection. The half-life of CTT in the serum at this dosage was thus 2.40 hours. Similarly, at a dosage rate of 20 mg/kg, the mean values at the various times were; 98.6 micrograms/ml at 30 minutes, 75.6 micrograms/ml at 1 hour, 57.8 micrograms/ml at 2 hours, 35.5 micrograms/ml at 4 hours and 23.2 micrograms/ml at 6 hours subsequent to the injection. The half-life of CTT in the serum in these cases was 2.73 hours. CTT was drip-infused intravenously over a period of 1 hour, and then the serum concentration of the drug was monitored with the passage of time. Subsequent to the administration of 10 mg/kg, the mean serum concentrations were as follows; 48.8 micrograms/ml at 30 minutes, 81.5 micrograms/ml at 1 hour, 42.2 micrograms/ml at 2 hours, 23.6 micrograms/ml at 4 hours and 14.8 micrograms/ml at 6 hours subsequent to the injection. The half-life of CTT in the serum after this intravenous drip infusion was thus 2.13 hours.(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

对头孢替坦(CTT)进行了临床前研究,并在儿科领域开展了临床研究。获得了以下结果。作者科室保存的114株临床分离株用于测定CTT对各种细菌的最低抑菌浓度(MIC)。对于大肠杆菌、沙门氏菌、肺炎克雷伯菌和奇异变形杆菌,CTT的MIC在0.78微克/毫升时出现峰值,大多数菌株在CTT浓度为6.25微克/毫升或更低时受到抑制。粘质沙雷氏菌菌株的MIC在25微克/毫升时出现峰值,25%的菌株MIC为3.13微克/毫升或更低,67%的菌株MIC为25微克/毫升或更高。所有铜绿假单胞菌菌株的MIC均超过100微克/毫升。对于革兰氏阳性菌金黄色葡萄球菌的所有测试菌株,CTT的MIC为12.5微克/毫升或更高,而所有粪肠球菌菌株的MIC均超过100微克/毫升。将CTT以静脉推注的方式给予儿科患者,然后测定血清中抗生素浓度随时间的变化。当给药速率为10毫克/千克时,平均血清水平如下:注射后30分钟为58.2微克/毫升,1小时为45.5微克/毫升,2小时为33.6微克/毫升,4小时为18.0微克/毫升,6小时为11.7微克/毫升。因此,在此剂量下CTT在血清中的半衰期为2.40小时。同样,当给药速率为20毫克/千克时,各时间点的平均值为:注射后30分钟为98.6微克/毫升,1小时为75.6微克/毫升,2小时为57.8微克/毫升,4小时为35.5微克/毫升,6小时为23.2微克/毫升。在这些情况下,CTT在血清中的半衰期为2.73小时。将CTT静脉滴注1小时,然后随着时间推移监测药物的血清浓度。给予10毫克/千克后,平均血清浓度如下:注射后30分钟为48.8微克/毫升,1小时为81.5微克/毫升,2小时为42.2微克/毫升,4小时为23.6微克/毫升,6小时为14.8微克/毫升。因此,这种静脉滴注后CTT在血清中的半衰期为2.13小时。(摘要截断于400字)

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