Citron D M, Merriam C V, Tyrrell K L, Warren Y A, Fernandez H, Goldstein E J C
R M Alden Research Laboratory, Santa Monica, California 90404, USA.
Antimicrob Agents Chemother. 2003 Jul;47(7):2334-8. doi: 10.1128/AAC.47.7.2334-2338.2003.
By using an agar dilution method, the in vitro activities of ramoplanin, teicoplanin, vancomycin, linezolid, and five other agents were determined against 300 gram-positive and 54 gram-negative strains of intestinal anaerobes. Ramoplanin was active at <or=2 microg/ml against 287 of 300 (95.7%) gram-positive organisms, including 18 strains of Clostridium difficile for which MICs of ramoplanin were 0.25 to 0.5 microg/ml; for 3 of these, linezolid MICs were 8 to 16 micro g/ml. Nineteen Clostridium innocuum strains for which the vancomycin MIC at which 90% of strains were inhibited was 16 microg/ml were susceptible to ramoplanin at 0.06 to 0.25 microg/ml and to teicoplanin at 0.125 to 1.0 microg/ml. All strains of Eubacterium, Actinomyces, Propionibacterium, and Peptostreptococcus spp. were inhibited by <or=0.25 microg of ramoplanin per ml and <or=1 microg of vancomycin per ml. Ramoplanin was also active at <or=4 microg/ml against 15 of 22 of the Prevotella and Porphyromonas strains tested, but ramoplanin MICs for all 31 strains of the Bacteroides fragilis group, the Fusobacterium mortiferum-Fusobacterium varium group, and Veillonella spp. were >or=256 microg/ml. Ramoplanin displays excellent activity against C. difficile and other gram-positive enteric anaerobes, including vancomycin-resistant strains; however, it has poor activity against most gram-negative anaerobes and thus potentially has a lesser effect on the ecological balance of normal fecal flora.
采用琼脂稀释法,测定了雷莫拉宁、替考拉宁、万古霉素、利奈唑胺及其他5种药物对300株革兰氏阳性和54株革兰氏阴性肠道厌氧菌的体外活性。雷莫拉宁对300株革兰氏阳性菌中的287株(95.7%)在≤2μg/ml时具有活性,包括18株艰难梭菌,其雷莫拉宁的最低抑菌浓度(MIC)为0.25至0.5μg/ml;其中3株,利奈唑胺的MIC为8至16μg/ml。19株无害梭菌菌株,其90%菌株被抑制时的万古霉素MIC为16μg/ml,对雷莫拉宁敏感,MIC为0.06至0.25μg/ml,对替考拉宁敏感,MIC为0.125至1.0μg/ml。所有真杆菌属、放线菌属、丙酸杆菌属和消化链球菌属菌株均被每毫升≤0.25μg的雷莫拉宁和每毫升≤1μg的万古霉素所抑制。雷莫拉宁对所测试的22株普雷沃菌属和卟啉单胞菌属菌株中的15株在≤4μg/ml时也具有活性,但对所有31株脆弱拟杆菌群、死亡梭杆菌-多变梭杆菌群和韦荣球菌属菌株的雷莫拉宁MIC均≥256μg/ml。雷莫拉宁对艰难梭菌和其他革兰氏阳性肠道厌氧菌(包括耐万古霉素菌株)显示出优异的活性;然而,它对大多数革兰氏阴性厌氧菌活性较差,因此对正常粪便菌群的生态平衡可能影响较小。