Finch R G
Department of Microbial Diseases, University of Nottingham, City Hospital, England.
Drugs. 1996;51 Suppl 1:31-7. doi: 10.2165/00003495-199600511-00007.
Most Gram-positive organisms are highly susceptible to the streptogramin, quinupristin/dalfopristin (RP 59500; Synercid). Minimum inhibitory concentrations for 90% of isolates (MIC90) were < or = 1 mg/L for Staphylococcus aureus, S. epidermidis, S. haemolyticus, Streptococcus pneumoniae, S. pyogenes and Listeria monocytogenes. Importantly, quinupristin/dalfopristin shows similar activity against methicillin-susceptible and -resistant strains of S. aureus, and streptococci with benzylpenicillin (penicillin G)- or erythromycin-acquired resistance. Enterococci have varying susceptibility to quinupristin /dalfopristin, although most isolates tested are susceptible to the drug, including vancomycin-resistant and multiresistant Enterococcus faecium. E. faecalis are generally the least susceptible. Among the Gram-negative respiratory pathogens Moraxella catarrhalis is susceptible and Haemophilus influenzae is moderately susceptible to quinupristin/ dalfopristin; however, Enterobacteriaceae, Pseudomonas aeruginosa and Acinetobacter spp. are resistant. The drug is active against anaerobic organisms tested, including Clostridium perfringens, Lactobacillus spp., Bacteroides fragilis and Peptostreptococcus. Synergy has been demonstrated in vancomycin-resistant and multiresistant E. faecium, and methicillin-sensitive and -resistant S. aureus with the combination of vancomycin and quinupristin/ dalfopristin. Quinupristin/dalfopristin shows antibacterial activity in vivo in animal models of infection, including methicillin-sensitive and -resistant S. aureus infection in rabbits, S. aureus and S. pneumoniae in mice, and erythromycin-sensitive and -resistant viridans group streptococci infections in rats. The drug is rapidly bactericidal against Gram-positive organisms (with the exception of enterococci) at concentrations similar to or within 4-fold of the MIC, and it has a long postantibiotic effect both in vitro and in vivo.
大多数革兰氏阳性菌对链阳菌素、奎奴普丁/达福普汀（RP 59500；Synercid）高度敏感。金黄色葡萄球菌、表皮葡萄球菌、溶血葡萄球菌、肺炎链球菌、化脓性链球菌和单核细胞增生李斯特菌90%菌株的最低抑菌浓度（MIC90）≤1mg/L。重要的是，奎奴普丁/达福普汀对甲氧西林敏感和耐药的金黄色葡萄球菌菌株，以及对苄青霉素（青霉素G）或红霉素获得性耐药的链球菌显示出相似的活性。肠球菌对奎奴普丁/达福普汀的敏感性各不相同，尽管大多数测试菌株对该药物敏感，包括耐万古霉素和多重耐药的粪肠球菌。粪肠球菌通常最不敏感。在革兰氏阴性呼吸道病原体中，卡他莫拉菌敏感，流感嗜血杆菌对奎奴普丁/达福普汀中度敏感；然而，肠杆菌科、铜绿假单胞菌和不动杆菌属耐药。该药物对测试的厌氧菌有活性，包括产气荚膜梭菌、乳酸杆菌属、脆弱拟杆菌和消化链球菌。在耐万古霉素和多重耐药的粪肠球菌，以及甲氧西林敏感和耐药的金黄色葡萄球菌中，已证实万古霉素与奎奴普丁/达福普汀联合使用具有协同作用。奎奴普丁/达福普汀在动物感染模型中显示出体内抗菌活性，包括兔体内甲氧西林敏感和耐药的金黄色葡萄球菌感染、小鼠体内金黄色葡萄球菌和肺炎链球菌感染，以及大鼠体内对红霉素敏感和耐药的草绿色链球菌感染。该药物在与MIC相似或为其4倍以内的浓度下，对革兰氏阳性菌（肠球菌除外）具有快速杀菌作用，并且在体外和体内均具有较长的抗生素后效应。
