Neu H C, Labthavikul P
Antimicrob Agents Chemother. 1982 Jan;21(1):180-7. doi: 10.1128/AAC.21.1.180.
The in vitro activity of N-formimidoyl thienamycin was determined against 800 gram-positive and gram-negative aerobic and anaerobic bacteria and compared with the activity of cefoxitin, cefazolin, cefamandole, cefotaxime, moxalactam, ampicillin, cefoperazone, and gentamicin. N-Formimidoyl thienamycin inhibited the majority of organisms at concentrations below 1 microgram/ml. It inhibited methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis, and Streptococcus faecalis. It inhibited beta-lactamase-producing Haemophilus influenzae and Neisseria gonorrhoeae. Unlike other new beta-lactams, it inhibited Listeria. Escherichia coli, Klebsiella pneumoniae, enterobacters, Serratia, indole-positive Proteus, Acinetobacter, Pseudomonas aeruginosa, and Bacteroides resistant to other agents were inhibited. There was minimal effect of inoculum size and aerobic versus anaerobic conditions, and serum had no effect on activity. Most minimal bactericidal concentrations were two- or fourfold greater than the minimal inhibitory concentration. N-Formimidoyl thienamycin showed partial synergy with aminoglycosides against S. aureus, S. faecalis, and many Pseudomonas and Enterobacteriaceae. It was not hydrolyzed by plasmid-mediated and chromosomal beta-lactamases.
测定了N-甲酰亚胺硫霉素对800株革兰氏阳性和革兰氏阴性需氧及厌氧菌的体外活性,并与头孢西丁、头孢唑林、头孢孟多、头孢噻肟、莫西沙星、氨苄西林、头孢哌酮和庆大霉素的活性进行了比较。N-甲酰亚胺硫霉素在浓度低于1微克/毫升时能抑制大多数菌株。它能抑制耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌和粪肠球菌。它能抑制产β-内酰胺酶的流感嗜血杆菌和淋病奈瑟菌。与其他新型β-内酰胺类药物不同,它能抑制李斯特菌。对其他药物耐药的大肠杆菌、肺炎克雷伯菌、肠杆菌、沙雷菌、吲哚阳性变形杆菌、不动杆菌、铜绿假单胞菌和拟杆菌均受到抑制。接种量大小以及需氧与厌氧条件对其影响极小,血清对其活性也无影响。大多数最小杀菌浓度比最小抑菌浓度高两倍或四倍。N-甲酰亚胺硫霉素与氨基糖苷类药物对金黄色葡萄球菌、粪肠球菌以及许多假单胞菌和肠杆菌科细菌表现出部分协同作用。它不会被质粒介导的和染色体β-内酰胺酶水解。