Motohiro T, Aramaki M, Kawakami A, Tanaka K, Koga T, Shimada Y, Tomita N, Sakata Y, Fujimoto T, Nishiyama T
Jpn J Antibiot. 1985 Nov;38(11):3387-413.
Aztreonam (AZT), a new injectable monobactam antibiotic, was administered to 7 healthy male volunteers, aged 21-28 years (23 years, on average) and weighing 60.5-87.0 kg, (69.5 kg, on average) by one shot intravenous injection of 1,000 mg twice a day for 5 days. The effect of AZT on the fecal flora was studied 3 days before administration, on the day of the initiation, 3 and 5 days (end of the administration course) after the initiation, and 3, 5 and 10 days after the end of the administration. Fecal concentration of AZT was also studied. Also, fecal concentration and recovery rate of AZT in 4 healthy male volunteers aged 23-31 years (26 years, on average), weighing 59.5-70.5 kg (65.6 kg, on average) were measured by injecting 1,000 mg of AZT by intravenous injection only one time. Susceptibility of the bacteria isolated from the 7 cases receiving consecutive dosage to AZT, cefmetazole (CMZ), latamoxef (LMOX), cefoperazone (CPZ) and ceftazidime (CAZ) as well as side effect and laboratory values were examined with the following results. In the fecal flora, the population of Enterobacteriaceae on average was 10(7) cells/g feces on the day of the initiation and decreased by 2 logarithms to 10(5) cells/g 3 days after the initiation, 10(5) cells/g feces 5 days after the initiation with no bacterial isolation in 2 cases, 10(7) cells/g feces on 3 and 5 days after the end of administration respectively with recovery of the population to the average population on the day of the initiation. However, it increased 10 days after the end of administration with the population of 10(9) cells/g feces due to the isolation of one 10(10) cells/g feces, which was an increase by 2 logarithms as compared with average population before the administration. It was also higher than the average population 3 days before the initiation of administration. Temporal decrease or disappearance of the bacteria were noted by the administration of AZT. As to other cases of Gram-negative bacilli, Pseudomonas sp. was detected from only 2 cases 3 days before the initiation of administration and on the day of the initiation, but there was an increase to 4 and 5 cases 3 and 5 days after the initiation respectively. Number of isolation returned to 2 cases, 3, 5 and 10 days after the end of administration respectively and it was same as the number before the initiation of administration.(ABSTRACT TRUNCATED AT 400 WORDS)
氨曲南(AZT)是一种新型注射用单环β-内酰胺类抗生素,对7名年龄在21至28岁(平均23岁)、体重60.5至87.0千克(平均69.5千克)的健康男性志愿者,每日两次静脉注射1000毫克,共注射5天。在给药前3天、给药当天、给药开始后3天和5天(给药疗程结束时)以及给药结束后3天、5天和10天研究了AZT对粪便菌群的影响。还研究了AZT的粪便浓度。此外,对4名年龄在23至31岁(平均26岁)、体重59.5至70.5千克(平均65.6千克)的健康男性志愿者仅静脉注射1000毫克AZT后,测量了AZT的粪便浓度和回收率。对7例连续给药患者分离出的细菌对AZT、头孢美唑(CMZ)、拉氧头孢(LMOX)、头孢哌酮(CPZ)和头孢他啶(CAZ)的敏感性以及副作用和实验室值进行了检查,结果如下。在粪便菌群中,给药当天肠杆菌科平均数量为每克粪便10⁷个细胞,给药开始后3天减少2个对数至每克粪便10⁵个细胞,给药开始后5天为每克粪便10⁵个细胞,2例无细菌分离,给药结束后3天和5天分别为每克粪便10⁷个细胞,菌群数量恢复到给药当天的平均水平。然而,给药结束后10天增加,由于分离出一株每克粪便10¹⁰个细胞,菌群数量为每克粪便10⁹个细胞,与给药前平均水平相比增加了2个对数。也高于给药开始前3天的平均水平。给予AZT后可见细菌暂时减少或消失。至于其他革兰氏阴性杆菌病例,给药前3天和给药当天仅从2例中检测到假单胞菌属,但给药开始后3天和5天分别增加到4例和5例。给药结束后3天、5天和10天分离数量分别恢复到2例,与给药开始前数量相同。(摘要截断于400字)