Barry A L, Jones R N, Thornsberry C, Ayers L W, Kundargi R
Diagn Microbiol Infect Dis. 1985 Mar;3(2):93-104. doi: 10.1016/0732-8893(85)90017-3.
In vitro studies with imipenem (N-formimidoyl thienamycin or MK0787) were performed with 8481 clinical isolates in three separate medical centers. More extensive comparative studies were also performed with 605 representative isolates, comparing imipenem to six other beta-lactams. Although the newer beta-lactams were often more active against susceptible species, imipenem demonstrated the broadest spectrum of antibacterial activity, with MIC 90s less than or equal to 4.0 micrograms/ml for all species tested except Pseudomonas maltophilia and P. cepacia. Imipenem was very active against all streptococci and staphylococci, in contrast to the third-generation cephalosporins. There was no evidence of cross-resistance between imipenem and the cephalosporins or penicillins. Resistance to hydrolysis by seven beta-lactamase preparations was documented for imipenem, cefotaxime, and moxalactam. Like many other beta-lactams, imipenem inhibited the Type I beta-lactamase produced by Enterobacter cloacae. Other beta-lactamases from gram-negative bacilli were also inhibited by high concentrations of imipenem.
在三个不同的医学中心,对8481株临床分离菌进行了亚胺培南(N-甲酰亚胺基硫霉素或MK0787)的体外研究。还对605株代表性分离菌进行了更广泛的比较研究,将亚胺培南与其他六种β-内酰胺类药物进行比较。虽然新型β-内酰胺类药物通常对敏感菌的活性更强,但亚胺培南显示出最广谱的抗菌活性,除嗜麦芽窄食单胞菌和洋葱伯克霍尔德菌外,所有测试菌的MIC90均小于或等于4.0微克/毫升。与第三代头孢菌素不同,亚胺培南对所有链球菌和葡萄球菌都非常有效。没有证据表明亚胺培南与头孢菌素或青霉素之间存在交叉耐药性。已证明亚胺培南、头孢噻肟和莫西沙星对七种β-内酰胺酶制剂的水解具有抗性。与许多其他β-内酰胺类药物一样,亚胺培南可抑制阴沟肠杆菌产生的I型β-内酰胺酶。高浓度的亚胺培南也可抑制革兰氏阴性杆菌产生的其他β-内酰胺酶。