Raghavan Murugan, Linden Peter K
Department of Internal Medicine, Conemaugh Memorial Medical Center Hospital, Johnstown, Pennsylvania, USA.
Drugs. 2004;64(15):1621-42. doi: 10.2165/00003495-200464150-00002.
In recent years, serious skin and soft tissue infections (SSTIs) caused by multidrug resistant pathogens have become more common. While the majority of SSTIs are caused by Staphylococcus aureus or beta-haemolytic streptococci that are methicillin/oxacillin susceptible, the emergence of methicillin-resistant and vancomycin-resistant community-acquired and nosocomial Gram-positive pathogens has created a need for different therapeutic agents, such as linezolid, quinupristin/dalfopristin, daptomycin, and newer generation carbapenems and fluoroquinolones. This review focuses on agents presently in clinical development for the treatment of SSTIs caused by Gram-positive pathogens such as staphylococci, streptococci and enterococci including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE). Newer-generation carbapenems, such as meropenem and ertapenem, are characterised by a broad-spectrum of activity against Gram-positive and -negative aerobes and anaerobes, and are resistant to hydrolysis by many beta-lactamases. Current-generation fluoroquinolones, such as levofloxacin, moxifloxacin and gatifloxacin, have demonstrated better eradication rates for S. aureus than conventional penicillin and cephalosporins. These antimicrobial agents can be used to treat methicillin-susceptible staphylococcal and streptococcal strains. Oxazolidinones, streptogramin combinations and cyclic lipopeptides have novel mechanisms of action and have been studied in several multinational phase III clinical trials in the treatment of complicated and uncomplicated SSTIs. They possess a broad spectrum of activity against multidrug-resistant pathogens, including MRSA and VRE. Linezolid has been shown to be active against a wide variety of community-acquired and nosocomial antimicrobial-resistant pathogens with comparability to vancomycin, as well as resulting in reduced lengths of hospital stay. Cyclic lipopeptides such as daptomycin have a unique mechanism of action by disruption of bacterial membrane electric potentials with less likelihood for development of cross-resistance. Daptomycin has recently been US FDA approved for the treatment of complicated SSTI. However, rapid development of resistance to some of these newer agents has already been reported and this trend magnifies the importance of further need for effective antimicrobial agents. Several investigational agents, such as dalbavancin, oritavancin and tigecycline, are in advanced stages of development and are likely to proceed to licensing in the next few years. With their long half-lives, these agents have an advantage of less frequent dose administration with more rapid bactericidal activity and less likelihood for development of resistance. However, because of their proven activity against highly resistant organisms, these antibacterial agents should be reserved only for life-threatening situations and/or when resistant pathogens are suspected. Rational antimicrobial use coupled with awareness of infection control measures is paramount to avert the emergence of multidrug-resistant organisms.
近年来,由多重耐药病原体引起的严重皮肤和软组织感染(SSTIs)变得更加常见。虽然大多数SSTIs是由对甲氧西林/苯唑西林敏感的金黄色葡萄球菌或β-溶血性链球菌引起的,但耐甲氧西林和耐万古霉素的社区获得性和医院内革兰氏阳性病原体的出现,使得需要不同的治疗药物,如利奈唑胺、奎奴普丁/达福普汀、达托霉素以及新一代碳青霉烯类和氟喹诺酮类药物。本综述聚焦于目前正在临床开发中用于治疗由革兰氏阳性病原体(如葡萄球菌、链球菌和肠球菌,包括耐甲氧西林金黄色葡萄球菌(MRSA)和耐万古霉素肠球菌(VRE))引起的SSTIs的药物。新一代碳青霉烯类药物,如美罗培南和厄他培南,具有对革兰氏阳性和阴性需氧菌及厌氧菌的广谱活性,并且对许多β-内酰胺酶具有抗水解能力。目前一代的氟喹诺酮类药物,如左氧氟沙星、莫西沙星和加替沙星,已显示出比传统青霉素和头孢菌素对金黄色葡萄球菌有更好的根除率。这些抗菌药物可用于治疗对甲氧西林敏感的葡萄球菌和链球菌菌株。恶唑烷酮类、链阳菌素组合和环脂肽具有新颖的作用机制,并已在多项跨国III期临床试验中用于治疗复杂性和非复杂性SSTIs。它们对包括MRSA和VRE在内的多重耐药病原体具有广谱活性。利奈唑胺已被证明对多种社区获得性和医院内抗菌耐药病原体具有活性,与万古霉素相当,还能缩短住院时间。环脂肽如达托霉素具有独特的作用机制,通过破坏细菌膜电位,产生交叉耐药的可能性较小。达托霉素最近已获美国食品药品监督管理局(FDA)批准用于治疗复杂性SSTI。然而,已经有报道称对其中一些新型药物的耐药性迅速发展,这种趋势凸显了进一步需要有效抗菌药物的重要性。几种研究性药物,如达巴万星、奥利万星和替加环素,正处于开发的后期阶段,可能在未来几年获得许可。由于它们的半衰期长,这些药物具有给药频率较低、杀菌活性更快且产生耐药性的可能性较小的优势。然而,由于它们对高度耐药菌已证实的活性,这些抗菌药物应仅保留用于危及生命的情况和/或怀疑有耐药病原体时。合理使用抗菌药物并提高对感染控制措施的认识对于避免多重耐药菌的出现至关重要。