Eliopoulos G M, Wennersten C, Reiszner E, Moellering R C
Antimicrob Agents Chemother. 1987 Aug;31(8):1188-93. doi: 10.1128/AAC.31.8.1188.
The in vitro activity of a new penem antimicrobial agent, CGP 31608, was compared with those of imipenem, SCH 34343, and several other antimicrobial agents against approximately 600 bacterial isolates. CGP 31608 was active against gram-positive organisms, including methicillin-susceptible Staphylococcus aureus (MIC for 90% of the isolates [MIC90], 0.25 microgram/ml) and penicillin-susceptible streptococci (MIC90s, less than or equal to 2 micrograms/ml). Penicillin-resistant streptococci (including enterococci) and methicillin-resistant S. aureus were more resistant to the penem. Activities of CGP 31608 against members of the family Enterobacteriaceae were remarkably uniform, with MIC90s of 8 to 16 micrograms/ml. CGP 31608 was at least as active as imipenem and ceftazidime and more active than piperacillin against Pseudomonas aeruginosa. Drug activity was not influenced by the presence of any of 10 plasmid-mediated beta-lactamases. Against strains of Serratia marcescens, Enterobacter cloacae, and P. aeruginosa with derepressible chromosomally mediated beta-lactamases, the presence of cefoxitin did not induce increased resistance to CGP 31608. The new drug was also active against anaerobes (MIC90s, 0.25 to 8 micrograms/ml), Haemophilus influenzae (MIC90s, 0.5 to 1.0 micrograms/ml), and Legionella spp. (MIC90, 2 micrograms/ml). CGP 31608 showed an antibacterial spectrum similar to those of imipenem and SCH 34343 (except that the latter is not active against P. aeruginosa) but was generally less potent than these drugs. However, CGP 31608 demonstrated more activity (MIC90) than imipenem against P. aeruginosa, Pseudomonas cepacia, and methicillin-resistant Staphylococcus epidermidis and S. aureus.
将新型青霉烯类抗菌剂CGP 31608的体外活性与亚胺培南、SCH 34343及其他几种抗菌剂针对约600株细菌分离株的活性进行了比较。CGP 31608对革兰氏阳性菌有活性,包括对甲氧西林敏感的金黄色葡萄球菌(90%分离株的MIC[MIC90]为0.25微克/毫升)和对青霉素敏感的链球菌(MIC90s小于或等于2微克/毫升)。耐青霉素链球菌(包括肠球菌)和耐甲氧西林金黄色葡萄球菌对该青霉烯类更具耐药性。CGP 31608对肠杆菌科成员的活性非常一致,MIC90s为8至16微克/毫升。CGP 31608对铜绿假单胞菌的活性至少与亚胺培南和头孢他啶相当,且比哌拉西林更具活性。药物活性不受10种质粒介导的β-内酰胺酶中任何一种的影响。对于具有可去阻遏的染色体介导β-内酰胺酶的粘质沙雷氏菌、阴沟肠杆菌和铜绿假单胞菌菌株,头孢西丁的存在并未诱导对CGP 31608的耐药性增加。这种新药对厌氧菌(MIC90s为0.25至8微克/毫升)、流感嗜血杆菌(MIC90s为0.5至1.0微克/毫升)和军团菌属(MIC90为2微克/毫升)也有活性。CGP 31608显示出与亚胺培南和SCH 34343相似的抗菌谱(后者对铜绿假单胞菌无活性除外),但总体效力低于这些药物。然而,CGP 31608对铜绿假单胞菌、洋葱伯克霍尔德菌以及耐甲氧西林表皮葡萄球菌和金黄色葡萄球菌的活性(MIC90)高于亚胺培南。