Lloyld L. Gregory School of Pharmacy, Palm Beach Atlantic University, West Palm Beach, FL, USA.
Regis University School of Pharmacy, Denver, CO, USA.
Ann Pharmacother. 2020 Dec;54(12):1203-1214. doi: 10.1177/1060028020932521. Epub 2020 Jun 4.
To review the pharmacology, microbiology, efficacy, and safety of lefamulin.
A literature search was performed using PubMed and Google Scholar (2010 to end-April 2020) with the search terms and . Other resources included abstracts presented at recent conferences, prescribing information, and the manufacturer's and Food and Drug Administration websites.
All relevant English-language articles of studies assessing the efficacy and safety of lefamulin were included.
Lefamulin is a pleuromutilin antibiotic with activity against , and atypical bacteria. Lefamulin, given at the dose of 150 mg intravenously or 600 mg orally on an empty stomach every 12 hours for 5 to 7 days, was proven noninferior to moxifloxacin for the treatment of community-acquired bacterial pneumonia (CABP). Common adverse reactions include injection site reactions, hepatic enzyme elevation, gastrointestinal upset, hypokalemia, insomnia, and headache. Lefamulin is associated with QT prolongation, and concomitant use with CYP3A substrates that prolong the QT interval is contraindicated. Lefamulin may cause fetal harm.
Lefamulin is a novel antibiotic with a unique mechanism of action. It represents an alternative option to β-lactams and macrolides in the treatment of adults with CABP and an alternative option to amoxicillin and doxycycline in the outpatient setting given the rise in resistance to macrolides and safety concerns with fluoroquinolones. Nausea, vomiting, and diarrhea may limit the tolerability of the oral formulation.
Lefamulin is the first systemic pleuromutilin antibiotic that has proven safe and effective for adults with CABP.
综述莱福米汀的药理学、微生物学、疗效和安全性。
使用 PubMed 和 Google Scholar（2010 年至 2020 年 4 月底）进行文献检索，检索词为 和 。其他资源包括最近会议上提交的摘要、说明书以及制造商和美国食品和药物管理局的网站。
所有评估莱福米汀疗效和安全性的相关英文文章均被纳入。
莱福米汀是一种截短侧耳素类抗生素，对 和非典型细菌具有活性。莱福米汀，静脉内给予 150mg 或空腹时口服 600mg，每 12 小时一次，连用 5 至 7 天，与莫西沙星治疗社区获得性细菌性肺炎（CABP）的疗效相当。常见不良反应包括注射部位反应、肝酶升高、胃肠道不适、低钾血症、失眠和头痛。莱福米汀与 CYP3A 底物相关联，后者会延长 QT 间期，因此禁止同时使用，因为会引起 QT 延长。莱福米汀可能会对胎儿造成伤害。
莱福米汀是一种具有独特作用机制的新型抗生素。它代表了治疗成人 CABP 的β-内酰胺类和大环内酯类抗生素的替代选择，在门诊环境下，鉴于大环内酯类抗生素耐药性的增加以及对氟喹诺酮类药物安全性的担忧，它也是阿莫西林和多西环素的替代选择。恶心、呕吐和腹泻可能会限制口服制剂的耐受性。
莱福米汀是第一个经证实对成人 CABP 安全有效的全身性截短侧耳素类抗生素。
