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奥马环素:一种现代化的四环素类药物。

Omadacycline: A Modernized Tetracycline.

机构信息

Temple University School of Pharmacy, Philadelphia, Pennsylvania.

出版信息

Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S1-S5. doi: 10.1093/cid/ciz394.

DOI:10.1093/cid/ciz394
PMID:31367739
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6669280/
Abstract

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.

摘要

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。

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Omadacycline: A Modernized Tetracycline.奥马环素:一种现代化的四环素类药物。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S1-S5. doi: 10.1093/cid/ciz394.
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An Integrated Safety Summary of Omadacycline, a Novel Aminomethylcycline Antibiotic.奥马环素的综合安全性总结,一种新型氨甲基环素抗生素。
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Future Microbiol. 2016 Oct;11:1421-1434. doi: 10.2217/fmb-2016-0100. Epub 2016 Aug 19.

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本文引用的文献

1
Pharmacokinetics and Pharmacodynamics of Oral and Intravenous Omadacycline.口服和静脉注射奥马环素的药代动力学和药效学。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S16-S22. doi: 10.1093/cid/ciz309.
2
Microbiology and Preclinical Review of Omadacycline.奥马环素的微生物学与临床前评价。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S6-S15. doi: 10.1093/cid/ciz395.
3
Omadacycline for Acute Bacterial Skin and Skin Structure Infections.口服多西环素治疗急性细菌性皮肤和皮肤结构感染。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S23-S32. doi: 10.1093/cid/ciz396.
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Early Clinical Response in Community-acquired Bacterial Pneumonia: From Clinical Endpoint to Clinical Practice.社区获得性细菌性肺炎的早期临床应答:从临床终点到临床实践。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S33-S39. doi: 10.1093/cid/ciz397.
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An Integrated Safety Summary of Omadacycline, a Novel Aminomethylcycline Antibiotic.奥马环素的综合安全性总结,一种新型氨甲基环素抗生素。
Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S40-S47. doi: 10.1093/cid/ciz398.
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Omadacycline for Community-Acquired Bacterial Pneumonia.奥马环素治疗社区获得性细菌性肺炎。
N Engl J Med. 2019 Feb 7;380(6):517-527. doi: 10.1056/NEJMoa1800201.
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Omadacycline for Acute Bacterial Skin and Skin-Structure Infections.口服多西环素治疗急性细菌性皮肤和皮肤结构感染。
N Engl J Med. 2019 Feb 7;380(6):528-538. doi: 10.1056/NEJMoa1800170.
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The role of omadacycline in skin and soft tissue infections.奥马环素在皮肤和软组织感染中的作用。
Curr Opin Infect Dis. 2018 Apr;31(2):148-154. doi: 10.1097/QCO.0000000000000429.
9
Pharmacokinetics and Safety of Omadacycline in Subjects with Impaired Renal Function.奥马环素在肾功能损害受试者中的药代动力学和安全性。
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.02057-17. Print 2018 Feb.
10
Comparison of Omadacycline and Tigecycline Pharmacokinetics in the Plasma, Epithelial Lining Fluid, and Alveolar Cells of Healthy Adult Subjects.比较奥马环素和替加环素在健康成年受试者血浆、上皮衬液和肺泡细胞中的药代动力学。
Antimicrob Agents Chemother. 2017 Aug 24;61(9). doi: 10.1128/AAC.01135-17. Print 2017 Sep.