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Emerging agents to combat complicated and resistant infections: focus on ceftobiprole

机译:新兴药物抗击复杂和耐药的感染:专注于头孢比普利

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Abstract: Antimicrobial resistance is a global concern. Over the past few years, considerable efforts and resources have been expended to detect, monitor, and understand at the basic level the many different facets of emerging and increasing resistance. Development of new antimicrobial agents has been matched by the development of new mechanisms of resistance by bacteria. Current antibiotics act at a variety of sites within the target bacteria, including the cross-linking enzymes in the cell wall, various ribosomal enzymes, nucleic acid polymerases, and folate synthesis. Ceftobiprole is a novel parenteral cephalosporin with high affinity for most penicillin-binding proteins, including the mecA product penicillin-binding protein 2a, rendering it active against methicillin-resistant staphylococci. Its in vitro activity against staphylococci and multiresistant pneumococci, combined with its Gram-negative spectrum comparable to that of other extended-spectrum cephalosporins, its stability against a wide range of beta-lactamases, and its pharmacokinetic and safety profiles make ceftobiprole an attractive and well tolerated new antimicrobial agent. The US Food and Drug Administration granted ceftobiprole medocaril fast-track status in 2003 for the treatment of complicated skin infections and skin structure infections due to methicillin-resistant staphylococci, and subsequently extended this to treatment of hospital-acquired pneumonia, including ventilator-associated pneumonia due to suspected or proven methicillin-resistant Staphylococcus aureus.
机译:摘要:耐药性是全球关注的问题。在过去的几年中,已经花费了大量的精力和资源来从根本上检测,监视和理解新出现和不断增加的抵抗的许多不同方面。新抗菌剂的开发与细菌耐药性新机制的开发相匹配。当前的抗生素作用于靶细菌内的多个位点,包括细胞壁中的交联酶,各种核糖体酶,核酸聚合酶和叶酸合成。 Ceftobiprole是一种新型肠胃外头孢菌素,对大多数青霉素结合蛋白(包括mecA产物青霉素结合蛋白2a)具有高度亲和力,使其对耐甲氧西林的葡萄球菌具有活性。它对葡萄球菌和多重耐药肺炎球菌的体外活性,与其他广谱头孢菌素相比,具有革兰氏阴性光谱,对多种β-内酰胺酶具有稳定性,其药代动力学和安全性使头孢比普利具有吸引力和良好的性能。耐受新的抗菌剂。美国食品药品监督管理局于2003年授予头孢比普利medocaril快速通道资格,用于治疗因耐甲氧西林的葡萄球菌引起的复杂皮肤感染和皮肤结构感染,随后将其扩展至医院获得性肺炎的治疗,包括呼吸机相关性肺炎由于怀疑或证明耐甲氧西林金黄色葡萄球菌。

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