Motohiro T, Yoshinaga Y, Sasaki H, Aramaki M, Oda K, Kawakami A, Tanaka K, Koga T, Shimada Y, Tomita S
Department of Pediatrics, School of Medicine, Kurume University.
Jpn J Antibiot. 1990 Feb;43(2):285-317.
Rokitamycin, a newly developed macrolide antibiotic was orally administered to 7 healthy male volunteers (22-25 years) for 7 consecutive days to study changes in bacterial flora and concentrations of the drug in feces, and to observe adverse reactions and laboratory test parameters. A dose of 200 mg (2 tablets: 100 mg/tablet) was given 3 times daily before meals and the fecal studies were done on the 5 days before administration (adm.) [b.a.], at the time of administration (0), and the 3rd, 5th, 7th (the final day of treatment) days during adm. [u.a.] and the 3rd, 5th, 10th, 20th, 30th days after adm. [a.a.]. The results obtained are summarized as follows. 1. Obvious changes in mean populations of total aerobes and enterobacteriaceae were not found. In changes of each bacteria of enterobacteriaceae, Escherichia coli was not observed in cases from initial day of treatment to the 3rd day a.a. Cases from which Citrobacter sp. was isolated tended to increase after 3 days u.a. and gradually decrease after 3 days a.a. Among Gram-negative bacilli, cases where isolation of Pseudomonas sp. was observed increased temporarily on the 3rd u.a., Gram-positive cocci did not show particular patterns of changes. No changes in mean count of total anaerobes were observed during the course of the experiment. Among individual anaerobes, numbers of Lactobacillus and Peptococcaceae decreased slightly from the 3rd day u.a. and returned on the 5th day a.a. 2. Clostridium difficile D-1 toxin was detected in feces at amounts approximately 500 ng/g in 2 cases each on 20th and 30th day a.a., with 1 incidence occurring in the same person on the 2 separate days. 3. The drug was detected in all 7 cases on the 3rd, 5th and 7th days u.a., and in 1 cases each on the 5th and the 30th day a.a. The mean peak level was 315.5 micrograms/g on the 7th day u.a. The reason for the detection of the drug in feces in 1 case on the 30th day a.a. at a value of 5.90 micrograms/g was not clear. 4. Adverse reactions and abnormal laboratory test results due to this drug were not observed in any cases.
罗他霉素是一种新开发的大环内酯类抗生素，连续7天口服给予7名健康男性志愿者（22 - 25岁），以研究菌群变化和粪便中药物浓度，并观察不良反应及实验室检查指标。剂量为200mg（2片：每片100mg），每日3次，饭前服用，粪便研究在给药前5天（基础值）、给药时（0）、给药期间第3、5、7天（治疗最后一天）（用药后）以及给药后第3、5、10、20、30天（用药后）进行。所得结果总结如下。1. 需氧菌总数和肠杆菌科的平均菌数未见明显变化。在肠杆菌科各细菌的变化中，从治疗首日至用药后第3天，未观察到大肠杆菌。分离出柠檬酸杆菌属的病例在用药后3天趋于增加，用药后3天逐渐减少。在革兰氏阴性杆菌中，观察到铜绿假单胞菌分离的病例在用药后第3天暂时增加，革兰氏阳性球菌未显示出特定变化模式。实验过程中总厌氧菌平均计数未见变化。在个体厌氧菌中，乳酸杆菌和消化球菌数量从用药后第3天开始略有下降，用药后第5天恢复。2. 在用药后第20天和第30天，各有2例粪便中检测到艰难梭菌D - 1毒素，含量约为500ng/g，1例在2个不同日期出现在同一人身上。3. 在用药后第3、5和7天，所有7例均检测到药物，用药后第5天和第30天各有1例检测到。用药后第7天平均峰值水平为315.5微克/克。用药后第30天1例粪便中检测到药物，值为5.90微克/克，原因不明。4. 未观察到因该药物引起的不良反应和实验室检查异常结果。
