Telithromycin:第一ketolide抗菌素。

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阮M,钟EP

Telithromycin:第一ketolide抗菌素。

其他。2005年8月,27 (8):1144 - 63。

PubMed ID

16199242 (在PubMed

]

文摘

背景:Telithromycin ketolide抗菌药物的是第一个获得美国食品和药物管理局(FDA)批准临床使用。批准用于治疗社区获得性肺炎(CAP),慢性支气管炎急性加重(AECB)和急性上颌窦炎(AMS)的成年人。目的:本文综述的作用机制、体外抗菌活性、药代动力学和药效学,临床疗效、安全、和telithromycin药物相互作用的状况。方法:相关研究发现通过搜索英文文献索引MEDLINE(1990 - 2005年3月)使用术语telithromycin和HMR 3647年,审查确定文章的引用列表,和准备的简报文件审查制造商telithromycin提交给FDA抗感染药物咨询委员会。一个搜索的摘要抗菌药物和化疗跨学科会议上(2001 - 2004)也进行了。结果:体外敏感性研究的结果表明,telithromycin提供投保的关键呼吸道病原体,典型和非典型。此外,telithromycin可能是有用的对肺炎链球菌和流感嗜血杆菌的耐多药菌株,无论beta-lactamase生产。在随机、双盲、比较试验(对阿莫西林、阿莫西林/ clavulanate,头孢呋辛axetil,克拉霉素,莫西沙星,或trovafloxacin), telithromycin有类似功效比较器的经验治疗帽(4)研究,AECB(研究),和AMS(研究)。Telithromycin给在800 mg QD(两个400毫克片剂)在社区获得性呼吸道感染(rti)。老年人不需要调整剂量,轻度至中度肾功能不全的患者,或肝功能不全的患者。 The majority of adverse events associated with telithromycin were mild to moderate, with gastrointestinal effects (diarrhea, nausea, vomiting) being the most commonly reported, followed by headache and dizziness. Telithromycin has been associated with elevations in hepatic transaminases and prolongation of the electrocardiographic QTc interval, although the significance of these findings is not known. Telithromycin is also a strong inhibitor of and substrate for the cytochrome P450 (CYP) 3A4 isozyme. Therefore, it is important to monitor for potential drug interactions with medications that prolong the QTc interval or are metabolized by the CYP system. CONCLUSIONS: Telithromycin appears to be a useful option for the empiric treatment of community-acquired RTIs in adults. It may be particularly useful in the outpatient setting in areas with high rates of penicillin- and macrolide-resistant S pneumoniae; it may also be an alternative agent for patients who are allergic to beta-lactams and live in areas with a high prevalence of multidrug-resistant S pneumoniae or for those who have failed to respond to beta-lactam- or macrolide-based therapy.

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药物酶

药物	酶	类	生物	药理作用	行动
Telithromycin	细胞色素P450 3 a4	蛋白质	人类	未知的	底物 抑制剂	细节