奥马环素的抗菌活性、耐药性、药动学特性和临床疗效研究进展

王乐莹; 王义俊; 张莉

doi:10.6039/j.issn.1001-0408.2024.20.22

您当前的位置：

首页 >

文章列表页 >

奥马环素的抗菌活性、耐药性、药动学特性和临床疗效研究进展

综述 | 更新时间：2024-10-25

- 奥马环素的抗菌活性、耐药性、药动学特性和临床疗效研究进展
- Research progress on antibacterial activity， resistance， pharmacokinetics characteristics and clinical efficacy of omadacycline
- 中国药房 2024年35卷第20期页码：2571-2576
- 作者机构：
  
  南京医科大学第二附属医院药学部，南京　210011
- 作者简介：
  
  主管药师，硕士研究生。研究方向：临床药学（呼吸专业）。E-mail：763484026@qq.com
  主任药师，硕士生导师。研究方向：药事管理、临床药学。E-mail：efywyj@163.com
- 基金信息：
  
  “南京药学会——常州四药医院药学科研基金”资助项目(2023YX002)
- DOI：10.6039/j.issn.1001-0408.2024.20.22
  中图分类号： R978.1;R969.1
- 纸质出版日期：2024-10-30，
  
  收稿日期：2024-04-24，
  
  修回日期：2024-07-28，
- 稿件说明：
移动端阅览
王乐莹,王义俊,张莉.奥马环素的抗菌活性、耐药性、药动学特性和临床疗效研究进展 ^Δ[J].中国药房,2024,35(20):2571-2576.

WANG Leying,WANG Yijun,ZHANG Li.Research progress on antibacterial activity， resistance， pharmacokinetics characteristics and clinical efficacy of omadacycline[J].ZHONGGUO YAOFANG,2024,35(20):2571-2576.
王乐莹,王义俊,张莉.奥马环素的抗菌活性、耐药性、药动学特性和临床疗效研究进展 ^Δ[J].中国药房,2024,35(20):2571-2576. DOI： 10.6039/j.issn.1001-0408.2024.20.22.

WANG Leying,WANG Yijun,ZHANG Li.Research progress on antibacterial activity， resistance， pharmacokinetics characteristics and clinical efficacy of omadacycline[J].ZHONGGUO YAOFANG,2024,35(20):2571-2576. DOI： 10.6039/j.issn.1001-0408.2024.20.22.

摘要

由于病原体耐药形势日益严峻，经典抗菌药物疗效下降，使得社区获得性肺炎（CAP）的治疗难度逐渐增加。奥马环素于2021年12月在我国获批上市，批准用于成人社区获得性细菌性肺炎和急性细菌性皮肤及皮肤结构感染的治疗。本文在介绍CAP致病源耐药情况的基础上，系统综述了奥马环素的抗菌活性、耐药性、药动学特性以及临床疗效，发现其抗菌谱广、生物利用率高、安全性好，且药动学参数不受患者年龄、性别、肝肾功能、药物相互作用的影响，对多种耐药菌、产超广谱

-内酰胺酶革兰氏阴性菌、非典型病原体等均有效，可作为治疗CAP的治疗选择之一。但由于该药临床研究数据有限、临床实际应用时间较短，仍需更多临床研究综合评估奥马环素治疗肺部感染的有效性和安全性。

Abstract

Due to the increasingly severe situation of pathogen resistance， the efficacy of classical antibiotics has declined， and the difficulty of treating community-acquired pneumonia （CAP） has gradually increased. Omadacycline was approved for marketing in China in December 2021 and has been approved for treating community-acquired bacterial pneumonia and acute bacterial skin and skin structure infection in adults. Based on introducing the pathogen resistance of CAP， this article systematically reviews the antibacterial activity and resistance， pharmacokinetic characteristics， and clinical efficacy of omadacycline. It is found that its antibacterial spectrum is wide， its bioavailability is high， and its safety is good. Its pharmacokinetic parameters are not affected by the patients’ age， gender， liver and kidney function， or drug interactions， and it is effective against multiple drug-resistant bacteria， Gram-negative bacteria producing extended-spectrum

-lactases， atypical pathogens， etc. It can be used as one of the treatment options for CAP. However， due to limited clinical research data and the short clinical application time of the drug， more clinical studies are still needed to verify its efficacy as a monotherapy or in combination with

other antibiotics for severe pneumonia patients.

关键词

奥马环素社区获得性肺炎抗菌活性药动学特性临床疗效

Keywords

community-acquired pneumoniaantibacterial activitypharmacokinetic characteristicsclinical efficacy

references

QIN T，ZHOU H J，REN H Y，et al. Incidence，etiology，and environmental risk factors of community-acquired pneumonia requiring hospitalization in China：a 3-year，prospective，age-stratified，multicenter case-control study[J]. Open Forum Infect Dis，2021，8（11）：ofab499.

DURÃES F，SOUSA E. Omadacycline：a newly approved antibacterial from the class of tetracyclines[J]. Pharmaceuticals，2019，12（2）：63.

中华医学会，中华医学会杂志社，中华医学会全科医学分会，等. 成人社区获得性肺炎基层诊疗指南：2018年[J]. 中华全科医师杂志，2019，18（2）：117-126.

Chinese Medical Association，Chinese Medical Journals Publishing House Co.，Ltd.，General Practice Branch of Chinese Medical Association，etc. Guideline for primary care of adult community acquired pneumonia：2018[J]. Chin J Gen Pract，2019，18（2）：117-126.

全国细菌耐药监测网. CHINET 2023年全年细菌耐药监测结果[EB/OL].（2024-03-05）[2024-08-22]. https：//www.chinets.com/Content/File/CHINET%202023%E5%B9%- B4%E7%BB%86%E8%8F%8C%E8%80%90%E8%- 8D%AF%E7%9B%91%E6%B5%8B%E7%BB%93%- E6%9E%9C.pdfhttps://www.chinets.com/Content/File/CHINET%202023%E5%B9%-B4%E7%BB%86%E8%8F%8C%E8%80%90%E8%-8D%AF%E7%9B%91%E6%B5%8B%E7%BB%93%-E6%9E%9C.pdf.

China Antimicrobial Resistance Surveillance System. CHINET 2023 annual bacterial resistance monitoring results[EB/OL].（2024-03-05）[2024-08-22]. https：//www.chinets.com/Content/File/CHINET%202023%E5%B9%- B4%E7%BB%86%E8%8F%8C%E8%80%90%E8%- 8D%AF%E7%9B%91%E6%B5%8B%E7%BB%93%- E6%9E%9C.pdfhttps://www.chinets.com/Content/File/CHINET%202023%E5%B9%-B4%E7%BB%86%E8%8F%8C%E8%80%90%E8%-8D%AF%E7%9B%91%E6%B5%8B%E7%BB%93%-E6%9E%9C.pdf.

王潜，杨菊华，陈乡，等. 基于宏基因组二代测序的儿童肺炎支原体耐药基因位点分析[J]. 中华儿科杂志，2024，62（5）：457-461.

WANG Q，YANG J H，CHEN X，et al. Metagenomic next-generation sequencing-based retrospective investigation of the drug resistance sites of Mycoplasma pneumoniae in children[J]. Chin J Pediatr，2024，62（5）：457-461.

DRAPER M P，WEIR S，MACONE A，et al. Mechanism of action of the novel aminomethylcycline antibiotic omadacycline[J]. Antimicrob Agents Chemother，2014，58（3）：1279-1283.

BURGOS R M，RODVOLD K A. Omadacycline：a novel aminomethylcycline[J]. Infect Drug Resist，2019，12：1895-1915.

HUBAND M D，PFALLER M A，SHORTRIDGE D，et al. Surveillance of omadacycline activity tested against clinical isolates from the United States and Europe：results from the SENTRY antimicrobial surveillance programme，2017[J]. J Glob Antimicrob Resist，2019，19：56-63.

US Food and Drug Administration. Omadacycline injection and oral products：FDA identified breakpoints for omadacycline[EB/OL].（2022-06-06）[2024-05-28].https：//www.fda.gov/drugs/development-resources/omadacycline-injection-and-oral-productshttps://www.fda.gov/drugs/development-resources/omadacycline-injection-and-oral-products.

WAITES K B，CRABB D M，LIU Y，et al. In vitro activities of omadacycline（PTK 0796）and other antimicrobial agents against human Mycoplasmas and Ureaplasmas[J]. Antimicrob Agents Chemother，2016，60（12）：7502-7504.

KOHLHOFF S A，HUERTA N，HAMMERSCHLAG M R. In vitro activity of omadacycline against Chlamydia pneumoniae[J]. Antimicrob Agents Chemother，2019，63（2）：e01907-e01918.

SHOEN C，BENAROCH D，SKLANEY M，et al. In vitro activities of omadacycline against rapidly growing Mycobacteria[J]. Antimicrob Agents Chemother，2019，63（5）：e02518-e02522.

STAPERT L，WOLFE C，SHINABARGER D，et al. In vitro activities of omadacycline and comparators against anaerobic bacteria[J]. Antimicrob Agents Chemother，2018，62（4）：e00018-e00047.

WATKINS R R，DERESINSKI S. Omadacycline：a novel tetracycline derivative with oral and intravenous formulations[J]. Clin Infect Dis，2019，69（5）：890-896.

LEPAK A J，ZHAO M，MARCHILLO K，et al. In vivo pharmacodynamic evaluation of omadacycline（PTK 0796）against Streptococcus pneumoniae in the murine pneumonia model[J]. Antimicrob Agents Chemother，2017，61（5）：e02316-e02368.

LEPAK A J，ZHAO M，MARCHILLO K，et al. In vivo pharmacodynamics of omadacycline against Staphylococcus aureus in the neutropenic murine thigh infection model[J]. Antimicrob Agents Chemother，2019，63（7）：e00624-e00619.

MACONE A B，CARUSO B K，LEAHY R G，et al. In vitro and in vivo antibacterial activities of omadacycline， a novel aminomethylcycline[J]. Antimicrob Agents Chemother，2014，58（2）：1127-1135.

ENDERMANN R，LADEL C H，BROETZ-OESTERHELT H，et al.BAY 73-7388，novel aminomethylcyclinea，is highly active in vivo in a murine model of Pneumococcal pneumonia[EB/OL].[2024-08-16].https：//api.semanticscholar.org/CorpusID：4489448https://api.semanticscholar.org/CorpusID:4489448.

KARLOWSKY J A，STEENBERGEN J，ZHANEL G G. Microbiology and preclinical review of omadacycline[J]. Clin Infect Dis，2019，69（Suppl. 1）：S6-S15.

STEENBERGEN J，TANAKA S K，MILLER L L，et al. In vitro and in vivo activity of omadacycline against two biothreat pathogens，Bacillus anthracis and Yersinia pestis[J]. Antimicrob Agents Chemother，2017，61（5）：e02416-e02434.

HONEYMAN L，ISMAIL M，NELSON M L，et al. Structure-activity relationship of the aminomethylcyclines and the discovery of omadacycline[J]. Antimicrob Agents Chemother，2015，59（11）：7044-7053.

YANG W R，MOORE I F，KOTEVA K P，et al. TetX is a flavin-dependent monooxygenase conferring resistance to tetracycline antibiotics[J]. J Biol Chem，2004，279（50）：52346-52352.

叶卓幸，汤燕君，何璐茜，等. 四环素类抗生素耐药研究进展：质粒介导的替加环素耐药机制[J]. 生态毒理学报，2022，17（4）：122-140.

YE Z X，TANG Y J，HE L X，et al. Mechanisms of tetra-cycline resistance：plasmid-mediated tigecycline resistance[J]. Asian J Ecotoxicol，2022，17（4）：122-140.

MOORE I F，HUGHES D W，WRIGHT G D. Tigecycline is modified by the flavin-dependent monooxygenase TetX[J]. Biochemistry，2005，44（35）：11829-11835.

CHEN C，CUI C Y，ZHANG Y，et al. Emergence of mobile tigecycline resistance mechanism in Escherichia coli strains from migratory birds in China[J]. Emerg Microbes Infect，2019，8（1）：1219-1222.

HE T，WANG R，LIU D J，et al. Emergence of plasmid-mediated high-level tigecycline resistance genes in animals and humans[J]. Nat Microbiol，2019，4（9）：1450-1456.

TANAKA S K，VILLANO S. In vitro and in vivo assessments of cardiovascular effects with omadacycline[J]. Antimicrob Agents Chemother，2016，60（9）：5247-5253.

GOTFRIED M H，HORN K，GARRITY-RYAN L，et al. Comparison of omadacycline and tigecycline pharmacokinetics in the plasma，epithelial lining fluid，and alveolar cells of healthy adult subjects[J]. Antimicrob Agents Chemother，2017，61（9）：e01117-e01135.

BUNDRANT L A，TZANIS E，GARRITY-RYAN L，et al. Safety and pharmacokinetics of the aminomethylcycline antibiotic omadacycline administered to healthy subjects in oral multiple-dose regimens[J]. Antimicrob Agents Chemother，2018，62（2）：e01417-e01487.

TZANIS E，MANLEY A，VILLANO S，et al. Effect of food on the bioavailability of omadacycline in healthy participants[J]. J Clin Pharmacol，2017，57（3）：321-327.

RODVOLD K A，PAI M P. Pharmacokinetics and pharmacodynamics of oral and intravenous omadacycline[J]. Clin Infect Dis，2019，69（Suppl. 1）：S16-S22.

TANAKA S K，TZANIS E，VILLANO S. Effect of age and gender on the pharmacokinetics of oral and Ⅳ omadacycline，a new class of aminomethylcyclines[C]//European Society of Clinical Microbiology and Infectious Diseases. Program and Abstracts of the 26th European Congress of Clinical Microbiology and Infectious Diseases. Basel，Switzerland：Congress of the European Society of Clinical Microbiology and Infection Disease，2016：P1318.

BERG J K，TZANIS E，GARRITY-RYAN L，et al. Pharmacokinetics and safety of omadacycline in subjects with impaired renal function[J]. Antimicrob Agents Chemother，2018，62（2）：e02017-e02057.

CORNELY O A，FILE T M，Jr，GARRITY-RYAN L，et al. Safety and efficacy of omadacycline for treatment of community-acquired bacterial pneumonia and acute bacterial skin and skin structure infections in patients with mild-to-moderate renal impairment[J]. Int J Antimicrob Agents，2021，57（2）：106263.

ZHANEL G G，ESQUIVEL J，ZELENITSKY S，et al. Omadacycline：a novel oral and intravenous aminomethylcycline antibiotic agent[J]. Drugs，2020，80（3）：285-313.

HUNT T L，TZANIS E，BAI S，et al. The effect of verapamil，a P-gp inhibitor，on the pharmacokinetics，safety，and tolerability of omadacycline in healthy adults：a phase Ⅰ，open-label，single-sequence study[J]. Eur J Drug Metab Pharmacokinet，2021，46（1）：85-92.

STETS R，POPESCU M，GONONG J R，et al. Omadacycline for community-acquired bacterial pneumonia[J]. N Engl J Med，2019，380（6）：517-527.

LIN F，HE R，YU B，et al. Omadacycline for treatment of acute bacterial infections：a meta-analysis of phase Ⅱ/Ⅲ trials[J]. BMC Infect Dis，2023，23（1）：232.

史海燕，胡英，黄建荣，等. 奥马环素对比美罗培南联合利奈唑胺治疗肺部感染：一项真实世界队列研究[J]. 中华临床感染病杂志，2023，16（3）：210-214.

SHI H Y，HU Y，HUANG J R，et al. Comparison of omada-cycline and meropenem plus linezolid in treatment of pulmonary infection：a real-world cohort study[J]. Chin J Clin Infect Dis，2023，16（3）：210-214.

程文斌，陈晔. 奥马环素治疗鹦鹉热衣原体肺炎1例[J]. 中国现代医生，2023，61（18）：140-142.

CHENG W B，CHEN Y. A case of pneumonia treated with omacycline[J]. China Mod Dr，2023，61（18）：140-142.

FANG C Q，XU L M，TAN J R，et al. Omadacycline for the treatment of severe Chlamydia psittaci pneumonia complicated with multiple organ failure：a case report[J]. Infect Drug Resist，2022，15：5831-5838.

WANG J，DONG S Y，FANG M J，et al. Omadacycline for the treatment of severe Chlamydia psittaci pneumonia complicated with guillain-barre syndrome[J]. Infect Drug Resist，2024，17：81-87.

XU L M，FANG C Q. Case report：omadacycline in the treatment of macrolide-unresponsive Mycoplasma pneumoniae pneumonia in an adolescent patient[J]. Front Cell Infect Microbiol，2023，13：1244398.

浏览量

下载量

CSCD

文章被引用时，请邮件提醒。

提交

工具集

关联资源

甲状腺相关眼病患者接受激素治疗后的临床疗效及生活质量评估

前列舒宁胶囊治疗慢性前列腺炎的临床疗效观察

丹参穴位注射配合梅花针叩刺治疗带状疱疹的疗效观察Δ

依达拉奉减轻颈动脉支架置入术老年患者脑血管痉挛的疗效观察

泮托拉唑联合血凝酶治疗上消化道出血的临床观察