Huang David B, DuPont Herbert L
Department of Medicine, Baylor College of Medicine, Houston, TX, USA.
J Infect. 2005 Feb;50(2):97-106. doi: 10.1016/j.jinf.2004.05.019.
Rifaximin is a poorly absorbed rifamycin antimicrobial drug with in vitro activity against Gram-positive, Gram-negative and anaerobic bacteria. The minimal concentration that inhibits 90% of strains of bacterial pathogens (MIC90) ranges between 32 and 64 microg/ml. Less than 1% of the drug is absorbed after oral administration. After three days of therapy, the average fecal level of this drug is 8000 microg/g of stool. Selection of resistant mutants, a problem with the related rifampin, appears to be unusual with rifaximin. Rifaximin shortens the duration of travelers' diarrhea and non-dysenteric diarrheal illness due to enterotoxigenic, enteroaggregative E. coli and Shigella sonnei without major alteration of aerobic fecal flora and without important side effects. The drug has been successfully used in preliminary studies of small bowel bacterial overgrowth syndrome and hepatic encephalopathy. To explain the beneficial effect of the drug on bacterial diarrhea without change in colonic flora or high rates of pathogen eradication, rifaximin may be more active against pathogens in the small bowel rather than the colon and/or the drug may alter the virulence of enteric pathogens in addition to organism inhibition.
利福昔明是一种吸收较差的利福霉素类抗菌药物,对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有体外活性。抑制90%的细菌病原体菌株的最低浓度(MIC90)在32至64微克/毫升之间。口服给药后,该药物的吸收率低于1%。治疗三天后,该药物在粪便中的平均水平为8000微克/克粪便。与相关的利福平一样,利福昔明出现耐药突变体的情况似乎并不常见。利福昔明可缩短由产肠毒素性、肠集聚性大肠杆菌和宋内志贺菌引起的旅行者腹泻和非痢疾性腹泻疾病的病程,且不会对需氧粪便菌群产生重大改变,也无重要副作用。该药物已成功用于小肠细菌过度生长综合征和肝性脑病的初步研究。为了解释该药物对细菌性腹泻有有益作用但不改变结肠菌群或病原体根除率高的原因,利福昔明可能对小肠中的病原体更具活性,而不是对结肠,和/或该药物除了抑制微生物外,还可能改变肠道病原体的毒力。