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[新型抗生素——停滞不前还是取得进展]

[New antibiotics - standstill or progress].

作者信息

Rademacher J, Welte T

机构信息

Klinik für Pneumologie, Medizinische Hochschule Hannover, Carl-Neuberg-Straße 1, 306125, Hannover, Deutschland.

出版信息

Med Klin Intensivmed Notfmed. 2017 Apr;112(3):206-213. doi: 10.1007/s00063-017-0271-3. Epub 2017 Mar 17.

DOI:10.1007/s00063-017-0271-3
PMID:28314920
Abstract

The development of resistance to antibiotics has been ignored for a long time. But nowadays, increasing resistance is an important topic. For a decade no new antibiotics had been developed and it is not possible to quickly close this gap of new resistance and no new drugs. This work presents six new antibiotics (ceftaroline, ceftobiprole, solithromycin, tedizolid, ceftolozane/tazobactam, ceftazidime/avibactam). In part, only expert opinions are given due to lack of study results.The two 5th generation cephalosporins ceftaroline and ceftobiprole have beside their equivalent efficacy to ceftriaxone (ceftaroline) and cefipim (ceftobiprole) high activity against MRSA. The fluoroketolide solithromycin should help against macrolide-resistant pathogens and has been shown to be noninferior to the fluorochinolones. The oxazolidinone tedizolid is effective against linezolid-resistant MRSA. The two cephalosporins ceftolozane/tazobactam and ceftazidime/avibactam are not only effective against gram-negative pathogens, but they have a very broad spectrum. Due to the efficacy against extended-spectrum β‑lactamases, they can relieve the selection pressure of the carbapenems. We benefit from all new antibiotics which can take the selection pressure from other often used antibiotics. The increasing number of resistant gram-negative pathogens worldwide is alarming. Thus, focusing on the development of new drugs is extremely important.

摘要

抗生素耐药性的发展长期以来一直被忽视。但如今,耐药性不断增加已成为一个重要话题。十年来一直没有研发出新的抗生素,而且不可能迅速填补新耐药性与无新药之间的差距。这项工作介绍了六种新型抗生素(头孢洛林、头孢托罗、索利霉素、特地唑胺、头孢洛扎/他唑巴坦、头孢他啶/阿维巴坦)。部分内容由于缺乏研究结果仅给出了专家意见。两种第五代头孢菌素头孢洛林和头孢托罗除了对头孢曲松(头孢洛林)和头孢吡肟(头孢托罗)具有等效疗效外,对耐甲氧西林金黄色葡萄球菌(MRSA)也有高活性。氟代酮内酯索利霉素应有助于对抗大环内酯类耐药病原体,并且已被证明不劣于氟喹诺酮类药物。恶唑烷酮特地唑胺对耐利奈唑胺的MRSA有效。两种头孢菌素头孢洛扎/他唑巴坦和头孢他啶/阿维巴坦不仅对革兰氏阴性病原体有效,而且具有非常广泛的抗菌谱。由于对超广谱β-内酰胺酶有效,它们可以减轻碳青霉烯类药物的选择压力。我们受益于所有能够减轻其他常用抗生素选择压力的新型抗生素。全球范围内耐革兰氏阴性病原体数量的增加令人担忧。因此,专注于新药研发极其重要。

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Efficacy and Safety of Ceftazidime-Avibactam Plus Metronidazole Versus Meropenem in the Treatment of Complicated Intra-abdominal Infection: Results From a Randomized, Controlled, Double-Blind, Phase 3 Program.头孢他啶-阿维巴坦联合甲硝唑与美罗培南治疗复杂性腹腔内感染的疗效和安全性:一项随机、对照、双盲、3期研究的结果
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含罗丹宁部分的 N-芳基磺酰基吲哚类似物作为抗菌剂的合成及生物活性评价
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