Iwata S, Yamamoto K, Isohata E, Kin Y, Yokota T, Kusumoto Y, Sato Y, Akita H, Nanri S, Oikawa T
Department of Pediatrics, Kasumigaura National Hospital.
Jpn J Antibiot. 1994 Dec;47(12):1668-84.
Biapenem (L-627), a novel injectable carbapenem antibiotic, was studied with regard to its effect on mice inoculated with four types of bacteria and on the intestinal flora of pediatric patients. L-627 was given i.m., 40 mg/kg once daily for 5 consecutive days, to mice inoculated enterically with four types of bacteria (Escherichia coli, Enterococcus faecalis, Bacteroides fragilis, and Bifidobacterium breve). Except for a mild decrease in E. coli, there were no major fluctuations in viable bacterial counts in the feces during the treatment. Five children with bacterial infections (3 boys and 2 girls; ages: 1 month to 7 years and 7 months; body weights 4.62-21.8 kg) were given L-627 at 6.0 to 11.7 mg/kg 3 times daily for 7 to 11 days. Among aerobes, although Enterobacteriaceae such as E. coli tended to decrease remarkably in all patients, there was no major change in Enterococcus. Consequently, total aerobe counts did not change significantly in any patient. Among anaerobes, Bifidobacterium, Bacteroides, and Eubacterium, which are the predominant organisms in infants, decreased remarkably in some patients. One of the patients showed a marked decrease in total anaerobe count associated with a change in fecal characteristics (diarrhea). Glucose nonfermenting Gram-negative bacilli or fungi did not become predominant organisms in any patient. Recovery from these changes in the intestinal flora was noted promptly after terminating L-627 treatment. L-627 was detected in the feces of 4 patients during treatment. The fecal concentration ranged from 0.24 to 2.22 micrograms/g. Clostridium difficile was not detected in any patient. Although C. difficile D-1 antigen was observed in 2 patients, it bore no relationship to fecal properties. The results indicated that L-627 had relatively few effects on the intestinal flora compared to other new beta-lactam antibiotics.
比阿培南(L-627)是一种新型注射用碳青霉烯类抗生素,研究了其对接种四种细菌的小鼠以及儿科患者肠道菌群的影响。给经肠道接种四种细菌(大肠杆菌、粪肠球菌、脆弱拟杆菌和短双歧杆菌)的小鼠肌肉注射L-627,剂量为40mg/kg,每日1次,连续5天。除大肠杆菌略有减少外,治疗期间粪便中活菌数无明显波动。5例细菌感染患儿(3男2女;年龄:1个月至7岁7个月;体重4.62-21.8kg),给予L-627,剂量为6.0至11.7mg/kg,每日3次,共7至11天。在需氧菌中,虽然所有患者的大肠杆菌等肠杆菌科细菌均有明显减少趋势,但肠球菌无明显变化。因此,所有患者的需氧菌总数均无明显变化。在厌氧菌中,婴儿肠道中的主要菌群双歧杆菌、拟杆菌和真杆菌在部分患者中明显减少。其中1例患者粪便性状改变(腹泻),厌氧菌总数明显减少。葡萄糖非发酵革兰阴性杆菌或真菌在任何患者中均未成为优势菌。停用L-627治疗后,肠道菌群的这些变化迅速恢复。治疗期间,4例患者的粪便中检测到L-627。粪便浓度范围为0.24至2.22μg/g。所有患者均未检测到艰难梭菌。虽然2例患者检测到艰难梭菌D-1抗原,但与粪便性状无关。结果表明,与其他新型β-内酰胺类抗生素相比,L-627对肠道菌群的影响相对较小。