Fass R J, Helsel V L
Antimicrob Agents Chemother. 1986 Sep;30(3):429-34. doi: 10.1128/AAC.30.3.429.
The in vitro activities of two new oral cephalosporins, Ro 19-5247 and Ro 15-8074, were compared with the in vitro activities of cefuroxime, cefaclor, amoxicillin-clavulanate, trimethoprim-sulfamethoxazole (TMP-SMZ), and doxycycline against a variety of bacterial species. MIC50s (MICs required to inhibit 50% of strains) of Ro 19-5247 were less than or equal to 0.13 micrograms/ml for streptococci (except Streptococcus faecalis) and Haemophilus influenzae; 0.25 to 2 micrograms/ml for most strains of Enterobacteriaceae, Aeromonas hydrophila, Branhamella catarrhalis, and gram-positive anaerobic bacteria; and 1 to 8 micrograms/ml for methicillin-susceptible staphylococci. MIC50s of Ro 15-8074 were similar to those of Ro 19-5247, except that gram-positive aerobes and anaerobes were less susceptible. Both Ro 19-5247 and Ro 15-8074 had greater in vitro activity against strains of Enterobacteriaceae than did comparative beta-lactams and doxycycline; TMP-SMZ had the broadest spectrum of activity against these organisms. None of the cephalosporins were active against methicillin-resistant staphylococci, S. faecalis, most nonfermenters, or Bacteroides sp. Inoculum size variations affected MICs in a species-dependent manner for beta-lactams and unpredictably for TMP-SMZ but had little effect for doxycycline. Bactericidal activity was consistent with beta-lactams, inconsistent with TMP-SMZ, and uncommon with doxycycline.
将两种新型口服头孢菌素Ro 19 - 5247和Ro 15 - 8074的体外活性,与头孢呋辛、头孢克洛、阿莫西林 - 克拉维酸、甲氧苄啶 - 磺胺甲恶唑(TMP - SMZ)及多西环素针对多种细菌的体外活性进行了比较。Ro 19 - 5247对链球菌(粪肠球菌除外)和流感嗜血杆菌的MIC50(抑制50%菌株所需的MIC)小于或等于0.13微克/毫升;对大多数肠杆菌科菌株、嗜水气单胞菌、卡他布兰汉菌和革兰氏阳性厌氧菌为0.25至2微克/毫升;对甲氧西林敏感葡萄球菌为1至8微克/毫升。Ro 15 - 8074的MIC50与Ro 19 - 5247相似,只是革兰氏阳性需氧菌和厌氧菌的敏感性较低。Ro 19 - 5247和Ro 15 - 8074对肠杆菌科菌株的体外活性均强于对照β - 内酰胺类药物和多西环素;TMP - SMZ对这些菌的抗菌谱最广。这些头孢菌素对耐甲氧西林葡萄球菌、粪肠球菌、大多数非发酵菌或拟杆菌属均无活性。接种量的变化对β - 内酰胺类药物的MIC有菌种依赖性影响,对TMP - SMZ的影响不可预测,但对多西环素影响很小。杀菌活性与β - 内酰胺类药物相符,与TMP - SMZ不符,多西环素则少见。