Retsema J A, English A R, Girard A E
Antimicrob Agents Chemother. 1980 Apr;17(4):615-22. doi: 10.1128/AAC.17.4.615.
CP-45,899 is a new, semisynthetic beta-lactamase inhibitor. When tested alone, CP-45,899 displayed only weak antibacterial activity, with the notable exception of its potent action against penicillin-susceptible and -resistant Neisseria gonorrhoeae. A combination of 3.12 microgram of CP-45,899 per ml with 3.12 microgram of ampicillin per ml, tested in broth cultures, inhibited ca. 90% of resistant Staphylococcus and Haemophilus influenzae strains; similar data were obtained in a variety of media. The same combination of CP-45,899 with ampicillin or penicillin G inhibited 90% of Bacteroides fragilis as interpreted from agar dilution minimal inhibitory concentrations. Inhibitory concentrations of CP-45,899-ampicillin were bactericidal against H. influenzae strains and were as bactericidal as nafcillin or cephalothin against S. aureus. Ampicillin-resistant S. aureus, H. influenzae, and B. fragilis strains did not develop resistance to CP-45,899-ampicillin when transferred as many as six passages in the presence of a sublethal concentration of the combination.
CP - 45,899是一种新型半合成β - 内酰胺酶抑制剂。单独测试时,CP - 45,899仅表现出微弱的抗菌活性,但对青霉素敏感和耐药的淋病奈瑟菌有显著的强效作用。在肉汤培养物中测试时,每毫升含3.12微克CP - 45,899与每毫升含3.12微克氨苄西林的组合,可抑制约90%的耐药葡萄球菌和流感嗜血杆菌菌株;在多种培养基中均获得了类似数据。从琼脂稀释最小抑菌浓度来看,CP - 45,899与氨苄西林或青霉素G的相同组合可抑制90%的脆弱拟杆菌。CP - 45,899 - 氨苄西林的抑菌浓度对流感嗜血杆菌菌株具有杀菌作用,对金黄色葡萄球菌的杀菌作用与萘夫西林或头孢噻吩相当。耐氨苄西林的金黄色葡萄球菌、流感嗜血杆菌和脆弱拟杆菌菌株在亚致死浓度的该组合存在下传代多达六次时,未对CP - 45,899 - 氨苄西林产生耐药性。