Catchpole C R, Wise R, Thornber D, Andrews J M
Department of Microbiology, Dudley Road Hospital, Birmingham, United Kingdom.
Antimicrob Agents Chemother. 1992 Sep;36(9):1928-34. doi: 10.1128/AAC.36.9.1928.
The in vitro activity of L-627, a new parenterally administered carbapenem, was compared with those of imipenem, meropenem, FCE 22101 (a penem), ceftazidime, and ceftriaxone. L-627 was active against members of the family Enterobacteriaceae (MIC for 90% of strains tested [MIC90] ranging from 0.03 to 4 micrograms/ml). L-627 displayed activity equal to that of meropenem against Pseudomonas aeruginosa (MIC90, 2 micrograms/ml), although, as with other carbapenems, the antipseudomonal activity was reduced against D2-deficient strains. Staphylococci and streptococci were susceptible (MIC90 of 1.0 micrograms/ml for Staphylococcus aureus and 0.015 micrograms/ml for group A streptococci). L-627 also had activity against anaerobic bacteria (MIC90, 2.0 micrograms/ml for Bacteroides fragilis). Neisseria gonorrhoeae and Neisseria meningitidis were highly susceptible (MIC90, 0.06 micrograms/ml), and against the common respiratory pathogens (Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella catarrhalis), the MIC90s were less than or equal to 2.0 micrograms/ml. The protein binding of L-627 ranged from 13.8 to 22%, depending on the concentration. The presence of human serum had little effect on the MIC or MBC of L-627. These results suggest that L-627 merits further study in the treatment of infections caused by a wide range of pathogens.
将新型胃肠外给药碳青霉烯类药物L - 627的体外活性与亚胺培南、美罗培南、FCE 22101(一种青霉烯类药物)、头孢他啶和头孢曲松进行了比较。L - 627对肠杆菌科细菌有活性(90%受试菌株的最低抑菌浓度[MIC90]为0.03至4微克/毫升)。L - 627对铜绿假单胞菌的活性与美罗培南相当(MIC90为2微克/毫升),不过与其他碳青霉烯类药物一样,对D2缺陷菌株的抗假单胞菌活性降低。葡萄球菌和链球菌敏感(金黄色葡萄球菌的MIC90为1.0微克/毫升,A组链球菌的MIC90为0.015微克/毫升)。L - 627对厌氧菌也有活性(脆弱拟杆菌的MIC90为2.0微克/毫升)。淋病奈瑟菌和脑膜炎奈瑟菌高度敏感(MIC90为0.06微克/毫升),对于常见呼吸道病原体(流感嗜血杆菌、肺炎链球菌和卡他莫拉菌),MIC90小于或等于2.0微克/毫升。L - 627的蛋白结合率在13.8%至22%之间,取决于浓度。人血清的存在对L - 627的MIC或MBC影响很小。这些结果表明,L - 627在治疗由多种病原体引起的感染方面值得进一步研究。