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新型碳青霉烯类药物BO-2727的体外和体内抗菌活性

In vitro and in vivo antibacterial activities of BO-2727, a new carbapenem.

作者信息

Asahi Y, Miyazaki S, Yamaguchi K

机构信息

Department of Microbiology, Toho University School of Medicine, Tokyo, Japan.

出版信息

Antimicrob Agents Chemother. 1995 May;39(5):1030-7. doi: 10.1128/AAC.39.5.1030.

Abstract

BO-2727, a new injectable carbapenem, was evaluated for its in vitro and in vivo antibacterial activities in comparison with those of biapenem, meropenem, imipenem, cefpirome, and ceftazidime. BO-2727 had activity comparable to that of imipenem against methicillin-susceptible staphylococci and streptococci, with MICs at which 90% of strains tested (MIC90s) are inhibited being equal to 0.5 microgram/ml or less. Against methicillin-resistant staphylococci, BO-2727 was the most active among the antibiotics tested, with MIC90s ranging from 4 to 8 micrograms/ml. BO-2727 was highly active against members of the family Enterobacteriaceae, Haemophilus influenzae, and Moraxella catarrhalis, with MIC90s ranging from 0.006 to 2 micrograms/ml. BO-2727 was also highly active against Pseudomonas aeruginosa (imipenem-susceptible strains), for which the MIC90 was 2 micrograms/ml, which was lower than those of imipenem, cefpirome, and ceftazidime and comparable to those of biapenem and meropenem. Differences in activity between BO-2727 and the other carbapenems against imipenem-resistant P. aeruginosa were particularly striking (MIC90, 8 micrograms/ml). Furthermore, BO-2727 displayed a high degree of activity against many of the ceftazidime-, ciprofloxacin-, and/or gentamicin-resistant isolates of P. aeruginosa. The in vivo efficacy of BO-2727 against experimental septicemia caused by gram-positive and gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and imipenem-resistant P. aeruginosa, reflected its potent in vitro activity and high levels in plasma.

摘要

将新型注射用碳青霉烯类药物BO - 2727与比阿培南、美罗培南、亚胺培南、头孢匹罗和头孢他啶进行比较,评估其体外和体内抗菌活性。BO - 2727对甲氧西林敏感葡萄球菌和链球菌的活性与亚胺培南相当,90%受试菌株被抑制的最低抑菌浓度(MIC90)等于或低于0.5微克/毫升。对于耐甲氧西林葡萄球菌,BO - 2727在所测试的抗生素中活性最强,MIC90范围为4至8微克/毫升。BO - 2727对肠杆菌科细菌、流感嗜血杆菌和卡他莫拉菌具有高度活性,MIC90范围为0.006至2微克/毫升。BO - 2727对铜绿假单胞菌(亚胺培南敏感菌株)也具有高度活性,其MIC90为2微克/毫升,低于亚胺培南、头孢匹罗和头孢他啶,与比阿培南和美罗培南相当。BO - 2727与其他碳青霉烯类药物对耐亚胺培南铜绿假单胞菌的活性差异尤为显著(MIC90为8微克/毫升)。此外,BO - 2727对许多耐头孢他啶、环丙沙星和/或庆大霉素的铜绿假单胞菌分离株显示出高度活性。BO - 2727对由革兰氏阳性和革兰氏阴性细菌引起的实验性败血症,包括耐甲氧西林金黄色葡萄球菌和耐亚胺培南铜绿假单胞菌的体内疗效,反映了其强大的体外活性和血浆中的高浓度。

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