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奎奴普丁/达福普汀对甲氧西林敏感和耐药金黄色葡萄球菌的体外抗菌活性综述。

A review of in-vitro antibacterial activity of quinupristin/dalfopristin against methicillin-susceptible and -resistant Staphylococcus aureus.

作者信息

Low D E, Nadler H L

机构信息

Department of Microbiology, Mount Sinai Hospital, Toronto, Ontario, Canada.

出版信息

J Antimicrob Chemother. 1997 May;39 Suppl A:53-8. doi: 10.1093/jac/39.suppl_1.53.

Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) presently represents approximately 30% of clinical isolates of S. aureus in the USA. Many strains are additionally resistant to erythromycin, 15- and 16-membered macrolides (e.g. azithromycin, spiramycin), clindamycin, aminoglycosides and/or quinolones. A review of the literature shows that quinupristin/dalfopristin, a semisynthetic derivative of pristinamycin, exhibits good in-vitro activity against methicillin-sensitive S. aureus and MRSA (mean MIC90 0.25-1.0 and 0.5-2.0 mg/L, respectively). Its in-vitro bacteriostatic activity is also unaffected by resistance phenotypes for erythromycin, ciprofloxacin, rifampicin or gentamicin. Among erythromycin-resistant MRSA strains, those with constitutive (macrolide and lincosamide) resistance are only 2-fold less sensitive as strains with inducible (14- and 15-membered macrolide only) resistance (MICs 0.5-1.0 and 0.25-1.0 mg/L, respectively). Quinupristin/dalfopristin is at least as active as vancomycin and more active than ciprofloxacin and erythromycin against MRSA. It generally has a more rapid bactericidal action than vancomycin and oxacillin against many strains of MRSA. The bactericidal activity of quinupristin/dalfopristin may be affected by macrolide resistance phenotype: S. aureus strains susceptible or inducibly resistant to macrolides are killed within 6 h, whereas a number of strains constitutively resistant to macrolides remain viable after 12 h. The clinical significance of this laboratory phenomenon requires investigation, possibly in additional animal models of infection.

摘要

耐甲氧西林金黄色葡萄球菌(MRSA)目前在美国金黄色葡萄球菌临床分离株中约占30%。许多菌株还对红霉素、15和16元大环内酯类(如阿奇霉素、螺旋霉素)、克林霉素、氨基糖苷类和/或喹诺酮类耐药。文献综述表明,普那霉素的半合成衍生物奎奴普丁/达福普汀对甲氧西林敏感金黄色葡萄球菌和MRSA具有良好的体外活性(平均MIC90分别为0.25 - 1.0和0.5 - 2.0mg/L)。其体外抑菌活性也不受红霉素、环丙沙星、利福平或庆大霉素耐药表型的影响。在耐红霉素的MRSA菌株中,具有组成型(大环内酯类和林可酰胺类)耐药性的菌株比具有诱导型(仅14和15元大环内酯类)耐药性的菌株敏感性仅低2倍(MIC分别为0.5 - 1.0和0.25 - 1.0mg/L)。奎奴普丁/达福普汀对MRSA的活性至少与万古霉素相当,且比对环丙沙星和红霉素更具活性。与万古霉素和苯唑西林相比,它对许多MRSA菌株通常具有更快的杀菌作用。奎奴普丁/达福普汀的杀菌活性可能受大环内酯类耐药表型的影响:对大环内酯类敏感或诱导耐药的金黄色葡萄球菌菌株在6小时内被杀灭,而一些对大环内酯类组成型耐药的菌株在12小时后仍存活。这一实验室现象的临床意义需要进一步研究,可能需要在更多的动物感染模型中进行。

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