Iwata S, Yamada K, Kin Y, Yokota T, Kusumoto Y, Sato Y, Akita H, Nanri S, Oikawa T, Sunakawa K
Department of Pediatrics, Kasumigaura National Hospital.
Jpn J Antibiot. 1988 Dec;41(12):2012-34.
Effects of sultamicillin (SBTPC) fine granules, a new oral beta-lactam antibiotic, on the intestinal bacterial flora were studied in tetra-contaminated mice and in pediatric patients. SBTPC was administered at a dose of 100 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of organisms: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. In all of the 4 species, bacterial populations in feces were markedly reduced on days 4 to 5 after the start of the treatment. Subjects in the pediatric study were 5 children with bacterial infections (4 boys and 1 girl) at ages from 1 year 3 months to 10 years 8 months and with their body weight ranging from 11.8 kg to 35.0 kg. SBTPC fine granule was administered at a dose of 10 mg/kg 3 to 4 times a day for 4 to 7 days. Although there were some variations in the fecal bacterial flora noticed among these subjects during the treatment, populations of main aerobes and anaerobes such as Enterobacteriaceae, Enterococcus, Bacteroides and Bifidobacterium decreased markedly in all cases. These decreases were more pronounced for anaerobes and total numbers of anaerobes were markedly reduced in all cases. Glucose non-fermenting Gram-negative rods and fungi tended to increase with administration of SBTPC fine granule. Although these changes tended to return to pre-dosing state after the cessation of the treatment with SBTPC fine granule, attention must be paid to possible occurrences of diarrhea, superinfection or bleeding tendency when treatment with the drug is continued for a long period of time. Fecal concentrations of both ampicillin and sulbactam during SBTPC fine granule treatment showed relatively high values except 1 sample with a high beta-lactamase activity in feces. These high concentrations suggest the possibility of biliary excretion of absorbed drugs and the possibility of hydrolysis of SBTPC in the intestine due to high pH. Fecal concentrations of the drug also appeared to be closely related to beta-lactamase activity in feces.
研究了新型口服β-内酰胺抗生素舒他西林(SBTPC)细颗粒对四联感染小鼠和儿科患者肠道菌群的影响。以100mg/kg的剂量每天给感染4种不同生物体(大肠杆菌、粪肠球菌、脆弱拟杆菌和短双歧杆菌)的小鼠连续5天每日给药一次SBTPC。在治疗开始后的第4至5天,所有4种物种的粪便细菌数量均显著减少。儿科研究的受试者为5名细菌感染儿童(4名男孩和1名女孩),年龄在1岁3个月至10岁8个月之间,体重在11.8kg至35.0kg之间。以10mg/kg的剂量每天3至4次给SBTPC细颗粒给药4至7天。尽管在治疗期间这些受试者的粪便菌群存在一些差异,但所有病例中肠杆菌科、肠球菌、拟杆菌和双歧杆菌等主要需氧菌和厌氧菌数量均显著减少。厌氧菌的减少更为明显,所有病例中厌氧菌总数均显著减少。葡萄糖非发酵革兰氏阴性杆菌和真菌在使用SBTPC细颗粒给药后有增加趋势。尽管在停止使用SBTPC细颗粒治疗后这些变化倾向于恢复到给药前状态,但当长期持续使用该药物治疗时,必须注意可能出现的腹泻、二重感染或出血倾向。除1份粪便中β-内酰胺酶活性高的样本外,SBTPC细颗粒治疗期间氨苄西林和舒巴坦的粪便浓度均显示出相对较高的值。这些高浓度表明吸收的药物可能经胆汁排泄,也表明由于肠道pH值高,SBTPC在肠道中可能被水解。药物的粪便浓度似乎也与粪便中的β-内酰胺酶活性密切相关。