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新型抗耐甲氧西林药物左氧氟沙星的临床、药理学及抗菌谱比较评估:在医院感染和社区感染中的治疗作用

A comparative assessment of clinical, pharmacological and antimicrobial profile of novel anti-methicillin-resistant agent levonadifloxacin: Therapeutic role in nosocomial and community infections.

作者信息

Bakthavatchalam Yamuna Devi, Rao Shoma Vinay, Isaac Barney, Manesh Abi, Nambi Senthur, Swaminathan Subramanian, Nagvekar Vasanth, Nangia Vivek, John Peter Victor, Veeraraghavan Balaji

机构信息

Department of Clinical Microbiology, Christian Medical College, Vellore, Tamil Nadu, India.

Department of Critical Care Unit, Christian Medical College, Vellore, Tamil Nadu, India.

出版信息

Indian J Med Microbiol. 2019 Oct-Dec;37(4):478-487. doi: 10.4103/ijmm.IJMM_20_34.

DOI:10.4103/ijmm.IJMM_20_34
PMID:32436868
Abstract

Staphylococcus aureus is of significant clinical concern in both community- and hospital-onset infections. The key to the success of S. aureus as a pathogen is its ability to swiftly develop antimicrobial resistance. Methicillin-resistant S. aureus (MRSA) is not only resistant to nearly all beta-lactams but also demonstrates resistance to several classes of antibiotics. A high prevalence of MRSA is seen across worldwide. For many decades, vancomycin remained as gold standard antibiotic for the treatment of MRSA infections. In the past decades, linezolid, daptomycin, ceftaroline and telavancin received regulatory approval for the treatment of infections caused by resistant Gram-positive pathogens. Although these drugs may offer some advantages over vancomycin, they also have significant limitations. These includes vancomycin's slow bactericidal activity, poor lung penetration and nephrotxicity;linezolid therapy induced myelosuppression and high cost of daptomycin greatly limits their clinical use. Moreover, daptomycin also gets inactivated by lung naturally occurring surfactants. Thus, currently available therapeutic options are unable to provide safe and efficacious treatment for those patients suffering from hospital-acquired pneumonia, bloodstream infections (BSIs), bone and joint infections and diabetic foot infections (DFI). An unmet need also exists for a safe and efficacious oral option for switch-over convenience and community treatment. Herein, the review is intended to describe the supporting role of anti-staphylococcal antibiotics used in the management of S. aureus infections with a special reference to levonadifloxacin. Levonadifloxacin and its prodrug alalevonadifloxacin are novel benzoquinolizine subclass of quinolone with broad-spectrum of anti-MRSA activity. It has been recently approved for the treatment of complicated skin and soft-tissue infection as well as concurrent bacteraemia and DFI in India.

摘要

金黄色葡萄球菌在社区获得性感染和医院获得性感染中均引起了临床的高度关注。金黄色葡萄球菌作为病原体成功的关键在于其迅速产生抗菌耐药性的能力。耐甲氧西林金黄色葡萄球菌(MRSA)不仅对几乎所有β-内酰胺类抗生素耐药,还对几类抗生素表现出抗性。MRSA在全球范围内普遍存在。几十年来,万古霉素一直是治疗MRSA感染的金标准抗生素。在过去几十年中,利奈唑胺、达托霉素、头孢洛林和替加环素获得了监管批准,用于治疗由耐药革兰氏阳性病原体引起的感染。尽管这些药物可能比万古霉素有一些优势,但它们也有显著的局限性。这些局限性包括万古霉素杀菌活性缓慢、肺部穿透性差和肾毒性;利奈唑胺治疗引起的骨髓抑制以及达托霉素的高成本极大地限制了它们的临床应用。此外,达托霉素也会被肺中天然存在的表面活性剂灭活。因此,目前可用的治疗选择无法为那些患有医院获得性肺炎、血流感染(BSIs)、骨和关节感染以及糖尿病足感染(DFI)的患者提供安全有效的治疗。对于安全有效的口服选择以实现转换便利性和社区治疗,也存在未满足的需求。在此,本综述旨在描述抗葡萄球菌抗生素在金黄色葡萄球菌感染管理中的支持作用,特别提及左氧氟沙星。左氧氟沙星及其前药阿拉左氧氟沙星是喹诺酮类的新型苯并喹嗪亚类,具有广谱抗MRSA活性。它最近在印度被批准用于治疗复杂性皮肤和软组织感染以及并发菌血症和DFI。

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