奥利万星治疗急性细菌性皮肤和皮肤结构感染:基于证据的综述。

Core Evidence Pub Date : 2015-02-11 eCollection Date: 2015-01-01 DOI:10.2147/CE.S51284
Joumana Kmeid, Zeina A Kanafani
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引用次数: 9

摘要

革兰氏阳性菌对万古霉素和替柯planin等糖肽类抗生素的耐药性的出现,促使了对该类第二代药物的研究。Oritavancin是一种新型的第二代半合成脂糖肽,具有抑制细胞壁合成和破坏细胞膜的两种作用机制。与其他糖肽相比,这种双重作用机制增加了奥利塔万素对万古霉素耐药革兰氏阳性细菌的活性。Oritavancin对革兰氏阳性细菌具有浓度依赖性和快速的杀菌活性,特别是肠球菌,与万古霉素和替柯planin相反,它们表现出抑菌活性。它的半衰期很长,约为195.4小时,可以被肝脏和肾脏缓慢清除,每天服用一次。Oritavancin已经在I期和II期临床试验中证明了初步的安全性和有效性。最近,在一项大型III期随机双盲临床试验中,它的疗效优于万古霉素。迄今为止,不良事件是轻微和有限的,最常见的是给药部位投诉,头痛和恶心。奥利塔万星似乎是万古霉素的一种有前途的抗微生物替代品,对对万古霉素耐药的葡萄球菌和肠球菌具有额外的活性,而且给药方式更方便。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Oritavancin for the treatment of acute bacterial skin and skin structure infections: an evidence-based review.

The emergence of resistance to glycopeptide antibiotics such as vancomycin and teicoplanin among Gram-positive bacteria has spurred the search for second-generation drugs of this class. Oritavancin, a promising novel, second-generation, semisynthetic lipoglycopeptide, is distinguished by two mechanisms of action: inhibition of cell wall synthesis and disruption of the cell membrane. This dual mechanism of action has increased the activity of oritavancin against vancomycin-resistant Gram-positive bacteria compared to other glycopeptides. Oritavancin has a concentration-dependent and rapid bactericidal activity against Gram-positive bacteria, particularly enterococci, contrary to vancomycin and teicoplanin, which exhibit bacteriostatic activity. It has a long half-life of about 195.4 hours and is slowly eliminated by the liver and kidneys, allowing once-daily dosing. Oritavancin has demonstrated preliminary safety and efficacy in Phase I and Phase II clinical trials. It was recently shown to be noninferior to vancomycin in a large Phase III randomized, double-blind clinical trial. To date, adverse events have been mild and limited, the most common being administration site complaints, headache, and nausea. Oritavancin appears to be a promising antimicrobial alternative to vancomycin with additional activity against Staphylococcus and Enterococcus isolates resistant to vancomycin and a more convenient way of administration.

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Core Evidence
Core Evidence PHARMACOLOGY & PHARMACY-
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期刊介绍: Core Evidence evaluates the evidence underlying the potential place in therapy of drugs throughout their development lifecycle from preclinical to postlaunch. The focus of each review is to evaluate the case for a new drug or class in outcome terms in specific indications and patient groups The emerging evidence on new drugs is reviewed at key stages of development and evaluated against unmet needs
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