Nakazawa S, Sato H, Narita A, Matsumoto K, Suzuki H, Nakazawa S, Chikaoka H, Kamigaki M, Koido R, Nakada Y
Jpn J Antibiot. 1985 Nov;38(11):3239-62.
The fundamental and clinical studies of aztreonam (AZT) were performed. The results were as follows: The MICs of AZT for E. coli and Salmonella sp. which were recently isolated in the pediatric field were less than 0.78 micrograms/ml. AZT also was effective against ABPC/PIPC-resistant bacteria. The MIC of AZT for V. parahaemolyticus was less than 1.56 micrograms/ml. The peak serum levels of AZT which were occurred just after the 1 hour drip infusion of 10-30 mg/kg were 60.5-136.8 micrograms/ml, and at 6 hours after infusion the serum levels were 1.3-6.1 micrograms/ml; therefore, the dose response was proved. The mean half-lives (T 1/2) were between 1.21 and 1.36 hours. The excretion rates in urine up to 6 hours after intravenous drip infusion were between 32.7 and 77.5%. The ratio of the cerebrospinal fluid concentration to serum in the child with purulent meningitis was 3.5% at 1 hour after the intravenous injection at the dose of 69 mg/kg, and the ratios of the subdural fluid levels to serum were 31.3-37.5%. The levels of AZT into the feces by the multiple dosage were 0-840 micrograms/g. Twenty-five pediatric patients with acute infections had been treated by intravenous injection or drip infusion at the doses of 49-120 mg/kg/day (almost 50-100 mg/kg/day) for 4 to 13 days. The efficacy rate of excellent + good was 84% and that of excellent + good + fair was 96%. The efficacy rate of excellent + good was 100% in all cases with upper/lower respiratory tract infection, bronchopneumonia, and acute urinary tract infection caused by Gram-negative rods. The clinical efficacy was observed in all cases with acute bacterial enteritis. Although AZT was clinically effective against Salmonella enteritis, bacteriological efficacy on the causative organisms was not observed in some cases. Although AZT was bacteriologically effective in 1 patient with typhoid, it did not alleviated fever. AZT showed activity to 9 strains isolated from the culture of throat swab, urine and feces. No side effects were clinically observed in all cases, while slight elevations of laboratory findings were observed in 4 cases.
进行了氨曲南(AZT)的基础和临床研究。结果如下:AZT对儿科领域近期分离出的大肠杆菌和沙门氏菌属的最低抑菌浓度(MIC)小于0.78微克/毫升。AZT对氨苄青霉素/哌拉西林耐药菌也有效。AZT对副溶血性弧菌的MIC小于1.56微克/毫升。在静脉滴注10 - 30毫克/千克1小时后即刻出现的AZT血清峰值水平为60.5 - 136.8微克/毫升,输注后6小时血清水平为1.3 - 6.1微克/毫升;因此,证明了剂量反应关系。平均半衰期(T1/2)在1.21至1.36小时之间。静脉滴注后6小时内尿液排泄率在32.7%至77.5%之间。在剂量为69毫克/千克静脉注射1小时后,化脓性脑膜炎患儿脑脊液浓度与血清浓度之比为3.5%,硬膜下液水平与血清水平之比为31.3% - 37.5%。多次给药后AZT在粪便中的水平为0 - 840微克/克。25例急性感染的儿科患者接受了静脉注射或滴注治疗,剂量为49 - 120毫克/千克/天(几乎为50 - 100毫克/千克/天),疗程为4至13天。优 + 良的有效率为84%,优 + 良 + 中的有效率为96%。在所有由革兰氏阴性杆菌引起的上/下呼吸道感染、支气管肺炎和急性尿路感染病例中,优 + 良的有效率为100%。在所有急性细菌性肠炎病例中均观察到临床疗效。虽然AZT对沙门氏菌肠炎临床有效,但在某些病例中未观察到对病原体的细菌学疗效。虽然AZT对1例伤寒患者有细菌学疗效,但未减轻发热症状。AZT对从咽拭子、尿液和粪便培养物中分离出的9株菌株有活性。所有病例临床均未观察到副作用,而4例观察到实验室检查结果略有升高。