Iwai N, Taneda Y, Shibata M, Mizoguchi F, Nakamura H, Katayama M
Jpn J Antibiot. 1985 Nov;38(11):3273-84.
Fundamental and clinical studies on aztreonam (AZT), a new monobactam antibiotic, were performed in the pediatric field. The MICs of AZT were assessed against the clinically isolated strains in the pediatric infections. AZT showed an excellent antibacterial activity against Gram-negative bacteria, i.e., against E. coli (20 strains), K. pneumoniae (9), P. mirabilis (16), P. vulgaris (5), P. aeruginosa (10), S. typhimurium (4) and H. influenzae (11); the MICs of AZT against the above strains were less than 0.39 microgram/ml, 0.10 microgram/ml, 0.024 microgram/ml, 0.024 microgram/ml, 6.25 micrograms/ml, 0.10 microgram/ml and 0.10 microgram/ml, respectively. However, antibacterial activity of AZT against Gram-positive bacteria was inferior to that against Gram-negative bacteria, i.e., against the strains of S. aureus (16) and S. pyogenes (4), those MICs were more than 400 micrograms/ml and 3.13 micrograms/ml, respectively. Serum concentrations and urinary excretion of AZT were measured in 2 children aged 7 and 11 years after a single intravenous injection at the dose of 20 mg/kg. The mean serum concentration of AZT followed by the injection 62.5 micrograms/ml at 1/4 hour, 28.5 micrograms/ml at 1/2 hour, 16.5 micrograms/ml at 1 hour, 12.0 micrograms/ml at 2 hours, 3.6 micrograms/ml at 4 hours and 1.1 micrograms/ml at 6 hours, respectively. The mean half-life (beta-phase) was 1.24 hours. The mean urinary concentrations after the injection were 5,000 micrograms/ml in 0-2 hours, 1,650 micrograms/ml in 2-4 hours and 611 micrograms/ml in 4-6 hours and the mean urinary recovery rate up to 6 hours was 61.2%. These results in our studies were considered to be comparable with those reported in adults. In our clinical studies, AZT was administered to a total of 14 cases, i.e., acute pneumonia (4 cases), acute pyelonephritis (4), acute enteritis (5) and acute sppurative cholangitis (1). Clinical effect of AZT was excellent or good in 13 cases except fair in 1 case with acute enteritis and the efficacy rate (excellent and good) was 92.9%. With regard to bacteriological effect, all the strains of H. influenzae (3), E. coli (2), P. mirabilis (1) and P. vulgaris (1) were eradicated, but, S. typhimurium (4) was not eradicated. Neither side effect nor abnormal laboratory findings were observed during the study.
对新型单环β-内酰胺类抗生素氨曲南（AZT）进行了儿科领域的基础和临床研究。评估了AZT对儿科感染临床分离菌株的最低抑菌浓度（MIC）。AZT对革兰氏阴性菌显示出优异的抗菌活性，即针对大肠杆菌（20株）、肺炎克雷伯菌（9株）、奇异变形杆菌（16株）、普通变形杆菌（5株）、铜绿假单胞菌（10株）、鼠伤寒沙门氏菌（4株）和流感嗜血杆菌（11株）；AZT对上述菌株的MIC分别小于0.39微克/毫升、0.10微克/毫升、0.024微克/毫升、0.024微克/毫升、6.25微克/毫升、0.10微克/毫升和0.10微克/毫升。然而，AZT对革兰氏阳性菌的抗菌活性低于对革兰氏阴性菌，即针对金黄色葡萄球菌（16株）和化脓性链球菌（4株），其MIC分别大于400微克/毫升和3.13微克/毫升。对2名7岁和11岁儿童单次静脉注射20毫克/千克剂量的AZT后，测定了其血清浓度和尿排泄情况。注射后AZT的平均血清浓度在1/4小时为62.5微克/毫升，1/2小时为28.5微克/毫升，1小时为16.5微克/毫升，2小时为12.0微克/毫升，4小时为3.6微克/毫升，6小时为1.1微克/毫升。平均半衰期（β期）为1.24小时。注射后的平均尿浓度在0 - 2小时为5000微克/毫升，2 - 4小时为1650微克/毫升，4 - 6小时为611微克/毫升，至6小时的平均尿回收率为61.2%。我们研究中的这些结果被认为与成人报道的结果相当。在我们的临床研究中，共对14例患者使用了AZT，即急性肺炎（4例）、急性肾盂肾炎（4例）、急性肠炎（5例）和急性化脓性胆管炎（1例）。除1例急性肠炎患者效果一般外，AZT的临床效果在13例患者中为优或良，有效率（优和良）为92.9%。关于细菌学效果，所有流感嗜血杆菌（3株）、大肠杆菌（2株）、奇异变形杆菌（1株）和普通变形杆菌（1株）菌株均被根除，但鼠伤寒沙门氏菌（4株）未被根除。研究期间未观察到副作用或实验室检查异常。
