Wise R, Andrews J M, Danks G
Antimicrob Agents Chemother. 1983 Dec;24(6):909-14. doi: 10.1128/AAC.24.6.909.
The in vitro activity of FCE 22101, a new semisynthetic penem derivative, was compared with that of ceftriaxone, moxalactam, imipenem (formerly imipemide, N-formimidoyl thienamycin, or MK 0787), cefuroxime, ceftazidime, and other beta-lactams, when appropriate, against 472 recent isolates and known beta-lactam-resistant strains. The minimum inhibitory concentrations of FCE 22101 against 90% of the members of the family Enterobacteriaceae, Haemophilus influenzae, Staphylococcus aureus, Lancefield group D streptococci, and Bacteroides spp. were between 0.5 and 4 micrograms/ml. Methicillin-resistant strains of Staphylococcus aureus were susceptible. Ninety percent of the Neisseria gonorrhoeae and Streptococcus pneumoniae strains were susceptible to 0.25 microgram of FCE 22101 per ml. Pseudomonas aeruginosa strains were resistant to FCE 22101 (minimum inhibitory concentration, greater than 128 micrograms/ml). The susceptibility of known, characterized beta-lactamase-producing strains of the Enterobacteriaceae suggested that FCE 22101 is resistant to many beta-lactamases. Generally, FCE 22101 was slightly less active than imipenem, moxalactam, ceftriaxone, and ceftazidime against members of the Enterobacteriaceae and considerably more active than the cephalosporins (including moxalactam) against Staphylococcus aureus. The human serum protein binding of FCE 22101 was about 40%, and human serum had little effect on the activity.
将新型半合成青霉烯衍生物FCE 22101的体外活性与头孢曲松、莫西沙星、亚胺培南(原亚胺培米、N-甲酰亚胺硫霉素或MK 0787)、头孢呋辛、头孢他啶以及其他β-内酰胺类药物(适当时)针对472株近期分离株和已知的β-内酰胺耐药菌株进行了比较。FCE 22101对90%的肠杆菌科细菌、流感嗜血杆菌、金黄色葡萄球菌、D群链球菌和拟杆菌属成员的最低抑菌浓度在0.5至4微克/毫升之间。耐甲氧西林金黄色葡萄球菌菌株敏感。90%的淋病奈瑟菌和肺炎链球菌菌株对每毫升0.25微克的FCE 22101敏感。铜绿假单胞菌菌株对FCE 22101耐药(最低抑菌浓度大于128微克/毫升)。对已知的、已鉴定的产β-内酰胺酶的肠杆菌科菌株的敏感性表明FCE 22101对许多β-内酰胺酶耐药。一般来说,FCE 22101对肠杆菌科细菌的活性略低于亚胺培南、莫西沙星头孢曲松和头孢他啶,而对金黄色葡萄球菌的活性比对头孢菌素类(包括莫西沙星)强得多。FCE 22101与人血清蛋白的结合率约为40%,人血清对其活性影响很小。