Motohiro T, Tanaka K, Koga T, Shimada Y, Tomita N, Sakata Y, Fujimoto T, Nishiyama T, Kuda N, Ishimoto K
Jpn J Antibiot. 1985 Oct;38(10):2770-96.
Ceftriaxone (CTRX), a newly developed antibiotic agent, was administered at 1,000 mg intravenously twice a day for 5 days to 7 healthy volunteers aged 21 to 26, weighing 61 to 79 kg (mean: 67.7 kg). The fecal bacterial flora was examined and the fecal level of CTRX was determined before, on 3 and 5 days after starting the administration, and on 3, 5 and 10 days after terminating the administration. At the same time, various bacteria isolated from the collected fecal specimens were studied for the sensitivity to CTRX, CEZ, CMZ and CTX. Adverse reactions and influence on various clinical laboratory parameters of CTRX were also examined. The results were as follows. Fecal bacterial flora: Enterobacteriaceae was at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) before starting the administration. The bacteria were detected from none of the 7 subjects on 5 days after starting the administration and on 3 days after terminating the administration. On 10 days after terminating the administration, the bacteria were detected in 6 out of 7 subjects at the level of 10(3) to 10(7) cells/g (mean: 10(7) cells/g). The level was the same as before starting the administration as a whole, but it had not been recovered to the initial level in any individual subject. With regard to other Gram-negative bacilli, P. aeruginosa which was isolated from none of the 7 subjects before starting the administration was detected at the level of 10(2) to 10(6) cells/g in 1 or 2 subjects on 3 days after starting, and on 3, 5 and 10 days after terminating the administration. Concerning Gram-positive bacteria, Staphylococcus sp. was isolated at the level of 10(3) to 10(4) cells/g in 3 subjects before starting the administration. The detection rate was decreased after starting the administration; it was detected in 2 and 1 subjects on 3 and 5 days after starting the administration, respectively, and in 1 subject on 3 days after terminating the administration. Then the detection rate was gradually increased; i.e., in 3 and 5 subjects on 5 and 10 days after terminating the administration, respectively. The level became gradually higher from on 5 days after terminating the administration than before starting the administration. Enterococcus sp. was isolated at the level of 10(5) to 10(8) cells/g (mean: 10(7) cells/g) in all of the 7 subjects before starting the administration. It was was detected in 1 and 4 subjects on 3 and 5 days, respectively, after starting the administration.(ABSTRACT TRUNCATED AT 400 WORDS)
头孢曲松(CTRX)是一种新开发的抗生素,对7名年龄在21至26岁、体重61至79千克(平均67.7千克)的健康志愿者,每天静脉注射1000毫克,每日两次,共5天。在给药前、给药开始后3天和5天以及给药结束后3天、5天和10天,检查粪便细菌菌群并测定粪便中CTRX的水平。同时,对从收集的粪便标本中分离出的各种细菌进行了对CTRX、头孢唑啉(CEZ)、头孢美唑(CMZ)和头孢噻肟(CTX)的敏感性研究。还检查了CTRX的不良反应及其对各种临床实验室参数的影响。结果如下。粪便细菌菌群:给药开始前,肠杆菌科细菌水平为10⁵至10⁸个/克(平均10⁷个/克)。给药开始后5天和给药结束后3天,7名受试者中均未检测到该细菌。给药结束后10天,7名受试者中有6名检测到该细菌,水平为10³至10⁷个/克(平均10⁷个/克)。总体水平与给药开始前相同,但任何个体受试者均未恢复到初始水平。关于其他革兰氏阴性杆菌,给药开始前7名受试者中均未分离出的铜绿假单胞菌,在给药开始后3天,有1或2名受试者检测到,水平为10²至10⁶个/克,在给药结束后3天、5天和10天也有检测到。关于革兰氏阳性菌,给药开始前,有3名受试者分离出葡萄球菌,水平为10³至10⁴个/克。给药开始后检出率下降;给药开始后3天和5天,分别有2名和1名受试者检测到,给药结束后3天有1名受试者检测到。然后检出率逐渐增加;即给药结束后5天和10天,分别有3名和5名受试者检测到。从给药结束后5天起,其水平逐渐高于给药开始前。给药开始前,所有7名受试者中均分离出肠球菌,水平为10⁵至10⁸个/克(平均10⁷个/克)。给药开始后3天和5天,分别有1名和4名受试者检测到。(摘要截短至400字)