新lipoglycopeptides:比较dalbavancin复审,oritavancin telavancin。

文章的细节

引用
复制到剪贴板

Zhanel GG, Calic D, F施魏策尔,Zelenitsky年代,亚当·H Lagace-Wiens公关,鲁宾斯坦E,杜松子酒,贺朋的DJ, Karlowsky农协

新lipoglycopeptides:比较dalbavancin复审,oritavancin telavancin。

药。2010年5月7日,70 (7):859 - 86。doi: 10.2165 / 11534440-000000000-00000。

PubMed ID
20426497 (在PubMed
]
文摘

Dalbavancin, oritavancin和telavancin半合成lipoglycopeptides证明承诺治疗患者的多重耐药性菌株引起的感染的革兰氏阳性病原体。这些代理包含一个heptapeptide核心,常见糖肤,这使他们能够抑制转糖基作用和转肽作用(细胞壁合成)。修改heptapeptide核心导致不同的体外活动三个半合成lipoglycopeptides。所有三个lipoglycopeptides包含亲脂性的侧链,延长半衰期,帮助来锚定代理细胞膜,增加他们的活动对革兰氏阳性球菌。除了抑制细胞壁的合成,telavancin和oritavancin也能够破坏细菌细胞膜的完整性和膜透性增加;oritavancin还能抑制RNA合成。Enterococci展示VanA表型(耐万古霉素和teicoplanin)对dalbavancin和telavancin虽然oritavancin保留活动。Dalbavancin, oritavancin和telavancin展览活动反对VanB vancomycin-resistant enterococci。所有三个lipoglycopeptides证明有效的体外活性对金黄色葡萄球菌和葡萄球菌epidermidis meticillin不管他们的易感性,以及链球菌spp。dalbavancin和telavancin都积极反对vancomycin-intermediate金黄色葡萄球菌(签证),但显示可怜的活动与vancomycin-resistant金黄色葡萄球菌(VRSA)。Oritavancin签证和VRSA很活跃。 Telavancin displays greater activity against Clostridium spp. than dalbavancin, oritavancin or vancomycin. The half-life of dalbavancin ranges from 147 to 258 hours, which allows for once-weekly dosing, the half-life of oritavancin of 393 hours may allow for one dose per treatment course, while telavancin requires daily administration. Dalbavancin and telavancin exhibit concentration-dependent activity and AUC/MIC (area under the concentration-time curve to minimum inhibitory concentration ratio) is the pharmacodynamic parameter that best describes their activities. Oritavancin's activity is also considered concentration-dependent in vitro, while in vivo its activity has been described by both concentration and time-dependent models; however, AUC/MIC is the pharmacodynamic parameter that best describes its activity. Clinical trials involving patients with complicated skin and skin structure infections (cSSSIs) have demonstrated that all three agents are as efficacious as comparators. The most common adverse effects reported with dalbavancin use included nausea, diarrhoea and constipation, while injection site reactions, fever and diarrhoea were commonly observed with oritavancin therapy. Patients administered telavancin frequently reported nausea, taste disturbance and insomnia. To date, no drug-drug interactions have been identified for dalbavancin, oritavancin or telavancin. All three of these agents are promising alternatives for the treatment of cSSSIs in cases where more economical options such as vancomycin have been ineffective, in cases of reduced vancomycin susceptibility or resistance, or where vancomycin use has been associated with adverse events.

DrugBank数据引用了这篇文章

药物