Temple University School of Pharmacy, Philadelphia, Pennsylvania.
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S1-S5. doi: 10.1093/cid/ciz394.
When tetracyclines were introduced in the 1940s, these antibiotics offered a broad spectrum of activity against multiple types of pathogens. However, their utility waned after the selection of tetracycline resistance in the pathogens against which they were effective. Omadacycline is a semisynthetic aminomethylcycline antibacterial derived from the tetracycline class of antibiotics that is unaffected by these resistance mechanisms. It has an appropriate spectrum of activity for community-acquired infections, including those caused by many resistant organisms. Omadacycline offers a well-tolerated treatment for acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia. Omadacycline has minimal known drug-drug interactions, and should be administered in a fasting state, avoiding dairy and cation-containing products for at least 4 hours after dosing. It does not require dose adjustments for sex, age, or hepatic or renal impairment, and has a safety profile similar to that of other oral tetracyclines. Because omadacycline can be administered effectively orally, it can help reduce hospitalization costs associated with intravenous antibiotic administration. This special supplement to Clinical Infectious Diseases offers an in-depth examination of omadacycline development, including discussions of pharmacokinetic and pharmacodynamic trials, spectrum of activity and preclinical data, early clinical trials, phase III clinical trials, and an integrated safety summary.
当四环素类药物在 20 世纪 40 年代问世时,这些抗生素对多种病原体具有广谱活性。然而,在针对有效病原体选择四环素耐药性后,它们的用途减少了。奥马环素是一种半合成的氨基甲基环素类抗菌药物,源自四环素类抗生素,不受这些耐药机制的影响。它具有适当的社区获得性感染谱,包括许多耐药菌引起的感染。奥马环素为急性细菌性皮肤和皮肤结构感染和社区获得性细菌性肺炎提供了一种耐受良好的治疗方法。奥马环素有很少已知的药物相互作用,应空腹给药,避免在给药后至少 4 小时内服用含乳制品和阳离子的产品。它不需要根据性别、年龄、肝或肾功能损害进行剂量调整,并且与其他口服四环素类药物的安全性特征相似。由于奥马环素可以有效地口服给药,因此可以帮助降低与静脉内抗生素给药相关的住院费用。这篇临床传染病的特刊深入探讨了奥马环素的开发,包括药代动力学和药效学试验、活性谱和临床前数据、早期临床试验、III 期临床试验以及综合安全性总结的讨论。