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Tigecycline.

机译:Tigecycline。

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摘要

Tigecycline is the first member of a new class of broad-spectrum antibacterials, the glycylcyclines, that has been specifically developed to overcome the two major mechanisms of tetracycline resistance (ribosomal protection and efflux). In vitro, tigecycline was active against a wide range of Gram-positive and -negative aerobic and anaerobic bacteria implicated in complicated skin and skin structure infections (cSSSIs) and complicated intra-abdominal infections (cIAIs). Intravenously administered tigecycline (recommended dosage regimen 100 mg initially, followed by 50 mg every 12 hours for 5-14 days) has been approved by the US FDA for the treatment of cSSSIs and cIAIs. In well designed, pivotal phase III studies, tigecycline monotherapy was noninferior to combination therapy with vancomycin 1 g plus aztreonam 2 g every 12 hours in hospitalised adult patients with cSSSIs (two trials; pooled clinical cure rates, 86.5% vs 88.6%) or broad-spectrum therapy with imipenem/cilastatin 200-500 mg/200-500 mg every 6 hours in hospitalised adult patients with cIAIs (two trials; pooled clinical cure rates, 86.1% vs 86.2%). Tigecycline was generally well tolerated in phase III studies; nausea, vomiting and diarrhoea were the most frequent adverse events in patients treated with tigecycline or an active comparator (vancomycin plus aztreonam or imipenem/cilastatin).
机译:Tigecycline是一类新的广谱抗菌剂,甘氨酰环素,专门开发用于克服四环素抗药性的两个主要机制(核糖体保护和外排)。在体外,替加环素对多种革兰氏阳性和阴性需氧和厌氧细菌具有活性,这些细菌与复杂的皮肤和皮肤结构感染(cSSSI)和复杂的腹腔内感染(cIAIs)有关。静脉注射替加环素(最初推荐剂量为100 mg,随后每12小时50 mg,持续5-14天)已获美国FDA批准用于治疗cSSSI和cIAI。在精心设计的关键性III期研究中,在住院的成年cSSSI患者中,替加环素单药治疗不低于万古霉素1 g加氨曲南2 g每12小时联合治疗(两项试验;合并临床治愈率86.5%vs 88.6%)或广泛在住院的cIAI成年患者中,每6小时使用亚胺培南/西司他丁200-500 mg / 200-500 mg进行广谱治疗(两项试验;合并临床治愈率分别为86.1%和86.2%)。在三期研究中,对Tigecycline的耐受性良好;替加环素或活性比较剂(万古霉素加氨曲南或亚胺培南/西司他丁)治疗的患者中,恶心,呕吐和腹泻是最常见的不良事件。

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