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舒巴坦/头孢哌酮在儿科领域的基础与临床研究

[Fundamental and clinical studies of sulbactam/cefoperazone in the pediatric field].

作者信息

Iwata S, Sato Y, Iwasaki Y, Hayano S, Wakabayashi R, Kojima Y, Akita H, Sunakawa K, Oikawa T, Osano M

出版信息

Jpn J Antibiot. 1984 Oct;37(10):1831-45.

PMID:6094863
Abstract

Fundamental and clinical studies were carried out on sulbactam/cefoperazone (SBT/CPZ) in the field of pediatrics. The following results were obtained: A total of 185 clinical isolates that had been stocked at our department was employed to determine the minimum inhibitory concentrations (MICs) of SBT/CPZ against various bacterial species. SBT/CPZ showed strong antibacterial potency against E. coli, Salmonella, Klebsiella and P. mirabilis, and relatively strong potency against S. marcescens, P. aeruginosa and S. aureus. Antibacterial potency of SBT/CPZ was stronger than that of CPZ alone against E. coli, and it also showed strong activity against strains of Salmonella, S. marcescens and S. aureus, moderately or highly resistant to CPZ. SBT/CPZ was administered by intravenous bolus infusion to pediatric patients to determine the serum concentrations of SBT and CPZ. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were as follows; 17.8 micrograms/ml, 40.7 micrograms/ml at 15 minutes and 0.3 microgram/ml at 6 hours, respectively. The half-lives of SBT and CPZ in the serum were 1.05 hours and 1.76 hours, respectively. Similarly, at a dose of 20 mg/kg the mean serum levels of SBT and CPZ were; 31.9 micrograms/ml, 81.0 micrograms/ml at 15 minutes and 0.5 microgram/ml, 6.1 micrograms/ml at 6 hours, and the half-lives were 1.00 hour and 1.72 hours, respectively. At a dose of 40 mg/kg, only 1 case was determined. The serum levels of SBT and CPZ were 34.4 micrograms/ml, 74.8 micrograms/ml at 30 minutes and 0.2 microgram/ml at 6 hours, and the half-lives were 0.78 hour and 1.38 hours, respectively. SBT/CPZ was drip-infused intravenously over a period of 1 hour, and the serum concentrations of SBT and CPZ were determined. At the dose of 10 mg/kg or 20 mg/kg, the peak serum levels of SBT and CPZ were observed at 1 hour or at the end of drip infusion. At a dose of 10 mg/kg the mean serum levels of SBT and CPZ were 14.4 micrograms/ml, 33.7 micrograms/ml at 1 hour and 1.4 micrograms/ml, 4.6 micrograms/ml at 7 hours, respectively. The half-lives was 1.86 hours for SBT and 2.23 hours for CPZ, respectively. Similarly at a dose of 20 mg/kg, the mean serum levels of SBT and CPZ were, 22.2 micrograms/ml, 34.6 micrograms/ml at 1 hour and 0.5 microgram/ml, 2.8 micrograms/ml at 7 hours, and the half-lives was 1.17 hours and 1.75 hours, respectively. The urinary recovery rate was determined for the 6 hours period after administration.(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

在儿科领域开展了舒巴坦/头孢哌酮(SBT/CPZ)的基础和临床研究。获得了以下结果:使用本科室保存的185株临床分离菌来测定SBT/CPZ对各种细菌的最低抑菌浓度(MIC)。SBT/CPZ对大肠杆菌、沙门氏菌、克雷伯菌和奇异变形杆菌显示出强大的抗菌效力,对粘质沙雷氏菌、铜绿假单胞菌和金黄色葡萄球菌显示出相对较强的效力。SBT/CPZ对大肠杆菌的抗菌效力强于单独使用头孢哌酮(CPZ),并且对CPZ中度或高度耐药的沙门氏菌、粘质沙雷氏菌和金黄色葡萄球菌菌株也显示出强大活性。对儿科患者静脉推注SBT/CPZ以测定SBT和CPZ的血清浓度。在剂量为10mg/kg时,SBT和CPZ的平均血清水平如下:15分钟时分别为17.8微克/毫升、40.7微克/毫升,6小时时分别为0.3微克/毫升。SBT和CPZ在血清中的半衰期分别为1.05小时和1.76小时。同样,在剂量为20mg/kg时,SBT和CPZ的平均血清水平为:15分钟时分别为31.9微克/毫升、81.0微克/毫升,6小时时分别为0.5微克/毫升、6.1微克/毫升,半衰期分别为1.00小时和1.72小时。在剂量为40mg/kg时,仅测定了1例。SBT和CPZ的血清水平在30分钟时分别为34.4微克/毫升、74.8微克/毫升,6小时时为0.2微克/毫升。半衰期分别为0.78小时和1.38小时。SBT/CPZ静脉滴注1小时,然后测定SBT和CPZ的血清浓度。在剂量为10mg/kg或20mg/kg时,SBT和CPZ的血清峰值水平在1小时或滴注结束时观察到。在剂量为10mg/kg时,SBT和CPZ的平均血清水平在1小时时分别为14.4微克/毫升、33.7微克/毫升,7小时时分别为1.4微克/毫升、4.6微克/毫升。SBT的半衰期为1.86小时,CPZ的半衰期为2.23小时。同样,在剂量为20mg/kg时,SBT和CPZ的平均血清水平在1小时时分别为22.2微克/毫升、34.6微克/毫升,7小时时分别为0.5微克/毫升、2.8微克/毫升,半衰期分别为1.17小时和1.75小时。测定给药后6小时的尿回收率。(摘要截取自400字)

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