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伊維菌素：修订间差异

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== 在其他動物的用途 ==
== 在其他動物的用途 ==
伊維菌素对[[綿羊疥癬]]有高度治癒力。同時，它也能對抗[[羊痂恙蟲]]、[[綿羊蝨蠅]]、[[羊狂蠅]]的幼蟲及胃腸中大部分的[[線蟲]]和[[肺寄生蟲]]，且能控制[[綠頭蒼蠅]]的排泄物引起的[[蠅蛆病]]。使用在綿羊疥癬上時，最常用的剂型為長效型伊維菌素控制釋放膠囊。
伊維菌素对[[綿羊疥癬]]有高度治癒力。同時，它也能對抗[[羊痂恙蟲]]、[[綿羊蝨蠅]]、[[羊狂蠅]]的幼蟲及胃腸中大部分的[[線蟲]]和[[肺寄生蟲]]，且能控制[[綠頭蒼蠅]]的排泄物引起的[[蠅蛆病]]。使用在綿羊疥癬上時，最常用的剂型為長效型伊維菌素控制釋放膠囊。

== 研究 ==

伊维菌素在[[In vitro|体外]]对包括[[SARS-CoV-2]]在内的若干[[正单链RNA病毒]]有抗病毒作用。<ref>{{cite journal|vauthors=Heidary F, Gharebaghi R|date=September 2020|title=Ivermectin: a systematic review from antiviral effects to COVID-19 complementary regimen|journal=The Journal of Antibiotics|volume=73|issue=9|pages=593–602|doi=10.1038/s41429-020-0336-z|pmc=7290143|pmid=32533071}}</ref>后续研究发现本药在猴肾细胞对[[SARS-CoV-2]]的半抑制浓度为2.2–2.8μM。<ref name="Caly2020">{{cite journal | vauthors = Caly L, Druce JD, Catton MG, Jans DA, Wagstaff KM | title = The FDA-approved drug ivermectin inhibits the replication of SARS-CoV-2 in vitro | journal = Antiviral Research | volume = 178 | pages = 104787 | date = April 2020 | pmid = 32251768 | pmc = 7129059 | doi = 10.1016/j.antiviral.2020.104787 }}</ref><ref>{{cite journal|vauthors=Şimşek Yavuz S, Ünal S|date=April 2020|title=Antiviral treatment of COVID-19|journal=Turkish Journal of Medical Sciences|volume=50|issue=SI-1|pages=611–619|doi=10.3906/sag-2004-145|pmc=7195979|pmid=32293834|doi-access=free}}</ref>伊维菌素在人体内达到抗病毒作用所需剂量远高于人用最高批准剂量、亦超过可安全实现剂量。<ref name="Bray_2020">{{cite journal|vauthors=Bray M, Rayner C, Noël F, Jans D, Wagstaff K|date=June 2020|title=Ivermectin and COVID-19: A report in Antiviral Research, widespread interest, an FDA warning, two letters to the editor and the authors' responses|journal=Antiviral Research|volume=178|pages=104805|doi=10.1016/j.antiviral.2020.104805|pmc=7172803|pmid=32330482}}</ref><ref>{{cite journal |vauthors=López-Medina E, López P, Hurtado IC, Dávalos DM, Ramirez O, Martínez E, Díazgranados JA, Oñate JM, Chavarriaga H, Herrera S, Parra B |display-authors=6 |date=2021-03-04 |title=Effect of Ivermectin on Time to Resolution of Symptoms Among Adults With Mild COVID-19 |url=https://jamanetwork.com/journals/jama/fullarticle/2777389 |journal=JAMA |volume=325 |issue=14 |pages=1426–1435 |doi=10.1001/jama.2021.3071 |pmid=33662102 |pmc=7934083 |issn=0098-7484|pmc-embargo-date=September 4, 2021 }}</ref>本药通过抑制[[输入蛋白|输入蛋白α/β1]]的[[核运输]]达到抗病毒作用，在上述剂量下对宿主有毒。<ref>{{cite journal|vauthors=Yang SN, Atkinson SC, Wang C, Lee A, Bogoyevitch MA, Borg NA, Jans DA|date=May 2020|title=The broad spectrum antiviral ivermectin targets the host nuclear transport importin α/β1 heterodimer|url=http://dicyt.uto.edu.bo/observatorio/wp-content/uploads/2020/05/importin-alfa.pdf|journal=Antiviral Research|volume=177|pages=104760|doi=10.1016/j.antiviral.2020.104760|pmid=32135219}}</ref>因此现在缺乏展开本药COVID-19的临床检验的理由。<ref name="misleading-evidence" />

有多人因服用本药马用浓缩剂住院；用药过度亦已导致死亡病例；死亡原因可能是本药与其他药物的相互作用。<ref name="fda-ivermectin"/>{{asof|2021|6|lc=yes}}，为解决原有小规模、低质量研究的不确定之处，美国和英国展开了大规模临床研究。<ref>{{cite news |publisher=BBC News |title=Covid: Ivermectin to be studied as possible treatment in UK |date=23 June 2021 |last1=Schraer |first1=Rachel |url=https://www.bbc.co.uk/news/health-57570377 |access-date=23 June 2021}}</ref><ref>{{cite web |title=COVID-19 Therapeutics Prioritized for Testing in Clinical Trials |url=https://www.nih.gov/research-training/medical-research-initiatives/activ/covid-19-therapeutics-prioritized-testing-clinical-trials#activ6 |website=National Institutes of Health |access-date=27 June 2021}}</ref>

众多对本药运用于[[COVID-19]]的研究有重大方法缺陷，证据水平因此很低。<ref name="misleading-evidence">{{cite journal |vauthors=Garegnani LI, Madrid E, Meza N |title=Misleading clinical evidence and systematic reviews on ivermectin for COVID-19 |journal=BMJ Evidence-Based Medicine |volume= |issue= |pages= |date=2021-04-22 |issn=2515-446X |pmid=33888547 |doi=10.1136/bmjebm-2021-111678 |url=https://ebm.bmj.com/content/early/2021/05/26/bmjebm-2021-111678 |doi-access=free}}</ref><ref>{{cite journal |vauthors=Bartoszko JJ, Siemieniuk RA, Kum E, Qasim A, Zeraatkar D, Ge L, Han MA, Sadeghirad B, Agarwal A, Agoritsas T, Chu DK, Couban R, Darzi AJ, Devji T, Ghadimi M, Honarmand K, Izcovich A, Khamis A, Lamontagne F, Loeb M, Marcucci M, McLeod SL, Motaghi S, Murthy S, Mustafa RA, Neary JD, Pardo-Hernandez H, Rada G, Rochwerg B, Switzer C, Tendal B, Thabane L, Vandvik PO, Vernooij RW, Viteri-García A, Wang Y, Yao L, Ye Z, Guyatt GH, Brignardello-Petersen R |title=Prophylaxis against covid-19: living systematic review and network meta-analysis |journal=BMJ |volume=373 |issue= |pages=n949 |date=April 2021 |pmid=33903131 |pmc=8073806 |doi=10.1136/bmj.n949 |type=Systematic review |display-authors=5}}</ref><ref>{{cite journal |vauthors=Roman YM, Burela PA, Pasupuleti V, Piscoya A, Vidal JE, Hernandez AV |title=Ivermectin for the treatment of COVID-19: A systematic review and meta-analysis of randomized controlled trials |journal=Clinical Infectious Diseases |url=https://academic.oup.com/cid/advance-article/doi/10.1093/cid/ciab591/6310839 |date=28 June 2021 |doi=10.1093/cid/ciab591 |pmid=34181716 |issn=1058-4838}}</ref>众多组织因此公开表示本药对于COVID-19有效的证据薄弱。2021年2月，本药的研发厂商[[默克药厂|默克]]发表声明表示目前没有本药对COVID-19有效的适当证据、以此目的使用本药亦相当危险。<ref name=dhg>{{cite web |url=https://sciencebasedmedicine.org/ivermectin-is-the-new-hydroxychloroquine/ |author=Gorski DH |title=Ivermectin is the new hydroxychloroquine |publisher=[[Science-Based Medicine]] |date=15 April 2021}}</ref><ref>{{cite web|date=4 February 2021|title=Merck Statement on Ivermectin use During the COVID-19 Pandemic|url=https://www.merck.com/news/merck-statement-on-ivermectin-use-during-the-covid-19-pandemic/|publisher=Merck}}</ref>美国[[国立卫生研究院 (美国)|国立卫生研究院]]COVID-19治疗指南表示本药证据极其有限，无法做出任何建议。<ref name="nih-iver-2021-01">{{cite web|date=14 January 2020|title=The COVID-19 Treatment Guidelines Panel's Statement on the Use of Ivermectin for the Treatment of COVID-19|url=https://www.covid19treatmentguidelines.nih.gov/statement-on-ivermectin/|publisher=National Institutes of Health}}</ref>英国全国COVID-19治疗咨询委员会认定本药用于COVID-19治疗的证据和可行性不足以进行下一步调查.<ref>{{cite journal |vauthors=Wadvalla BA |title=Covid-19: Ivermectin's politicisation is a warning sign for doctors turning to orphan treatments |journal=BMJ |volume=373 |issue= |pages=n747 |date=April 2021 |pmid=33795225 |doi=10.1136/bmj.n747 |s2cid=232484313 |url=|doi-access=free }}</ref>

[[美国食品药品监督管理局]]（FDA）未批准本药在美国治疗任何病毒疾病、在欧洲亦未获准用于治疗COVID-19。<ref name="nih-iver-2021-01" /><ref name=ema/>
在审核本药相关证据后，[[欧洲药品管理局]]（EMA）表示目前数据不支持在良好设计的临床试验外使用本药。<ref name="ema">{{cite press release|publisher=[[European Medicines Agency]]|date=22 March 2021|url=https://www.ema.europa.eu/en/news/ema-advises-against-use-ivermectin-prevention-treatment-covid-19-outside-randomised-clinical-trials|title=EMA advises against use of ivermectin for the prevention or treatment of COVID-19 outside randomised clinical trials}}</ref>2021年3月，FDA及EMA皆发布指南表示不应使用本药治疗COVID-19。<ref name="fda-ivermectin">{{cite web | title=Why You Should Not Use Ivermectin to Treat or Prevent COVID-19 | website=U.S. [[Food and Drug Administration]] (FDA) | date=5 March 2021 | url=https://www.fda.gov/consumers/consumer-updates/why-you-should-not-use-ivermectin-treat-or-prevent-covid-19 | access-date=5 March 2021}}</ref><ref name=ema/>[[世界卫生组织]]亦表示本药除临床试验外不应用于治疗COVID-19。<ref>{{cite web |title=WHO advises that ivermectin only be used to treat COVID-19 within clinical trials |publisher=World Health Organisation |date=31 March 2021 |url=https://www.who.int/news-room/feature-stories/detail/who-advises-that-ivermectin-only-be-used-to-treat-covid-19-within-clinical-trials}}</ref>{{link-en|巴西国家卫生监督局|Brazilian Health Regulatory Agency}}、巴西传染病学会、巴西胸腔学会发布声明反对使用本药预防或治疗早期COVID-19。<ref name="PEBMED">{{cite web|last=Quintanilha|first=Dayana de Oliveira|date=2020-07-13|title=Anvisa se manifesta contra o uso da ivermectina na Covid-19|trans-title=Anvisa speaks out against the use of ivermectin in Covid-19|url=https://pebmed.com.br/anvisa-se-manifesta-contra-o-uso-da-ivermectina-na-covid-19|url-access=subscription|work=PEBMED|language=Portuguese}}</ref><ref name="SBI">{{cite web|date=2020-12-09|title=Atualizações e Recomendações sobre a Covid-19|trans-title=Updates and recommendations on Covid-19|url=https://infectologia.org.br/wp-content/uploads/2020/12/atualizacoes-e-recomendacoes-covid-19.pdf|publisher=Sociedade Brasileira de Infectologia|language=Portuguese}}</ref><ref name="SBPT">{{cite web|date=2021-01-17|title=Posicionamento da Sociedade Brasileira de Pneumologia e Tisiologia Sobre o Colapso em Manaus e Tratamento Preventivo e Precoce da Covid-19|trans-title=Brazilian Thoracic Society Position Statement on the Collapse in Manaus and the Preventive and Early Treatment of Covid-19|url=https://pebmed.com.br/anvisa-se-manifesta-contra-o-uso-da-ivermectina-na-covid-19/|access-date=2021-01-18|publisher=Sociedade Brasileira de Pneumologia e Tisiologia|language=Portuguese}}</ref>


== 參見 ==
== 參見 ==

2021年7月11日 (日) 01:43的版本

伊維菌素
臨床資料
懷孕分級
  • C
给药途径口服
ATC碼
藥物動力學數據
血漿蛋白結合率93%
药物代谢肝臟; CYP450
生物半衰期18小時
排泄途徑糞便; 尿液<1%
识别信息
  • Ivermectin（22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b）
CAS号70288-86-7  checkY
71827-03-7
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB配體ID
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.067.738 編輯維基數據鏈接
化学信息
化学式C48H74O14(22,23-dihydroavermectin B=1a)
C47H72O14(22,23-dihydroavermectin B=1b)
摩尔质量875.10 g/mol
维基百科中的醫學内容仅供参考，並不能視作專業意見。如需獲取醫療幫助或意見，请咨询专业人士。詳見醫學聲明。

伊維菌素（ivermectin）也稱為愛獲滅，是一種阿維菌素家族[1]有效抗多種寄生蟲的治療藥物[2]，其適用於治療頭蝨[1]、疥蟎引起的疥瘡[3]，蟠尾絲蟲症（河盲症）[4]，線蟲感染[5]，班氏絲蟲感染導致的象皮病等[6]。伊維菌素可以塗抹於皮膚或是口服，但應避免接觸眼睛[1]

常見的副作用包含眼睛紅癢，皮膚乾燥與灼燒感[1]。目前尚不清楚在孕期中使用是否安全，但是在哺乳期使用似乎尚可[7]。其作用機制是使增加無脊椎動物的細胞壁可透性，導致他們死亡。

伊維菌素發現於1975年，並在1981年列為藥物[6][8]。 它是世界卫生组织基本药物标准清单中的一部份，是基層健康衛生系統中非常重要的藥物[9]。一套治療流程需要的藥物售價約為0.12美金[10]，在美國約要價25到50美金[5]，在其他的動物身上，伊維菌素用於治療與預防犬心絲蟲等疾病[2]。

历史

伊維菌素这种高效低毒的药品由日本北里大学有機化學家大村智和默克藥廠默克治疗研究所的威廉·坎贝尔从阿维菌素提纯出来[11]，并于1981年被引入治疗[12]。2015年度的诺贝尔生理学或医学奖的一半联合授予坎贝尔和大村，理由是“这种衍生物从根本上降低了河盲症和淋巴丝虫病（“象皮病”）的发病率，以及有效对抗快速增加中的其他寄生虫疾病“[13]。

在其他動物的用途

伊維菌素对綿羊疥癬有高度治癒力。同時，它也能對抗羊痂恙蟲、綿羊蝨蠅、羊狂蠅的幼蟲及胃腸中大部分的線蟲和肺寄生蟲，且能控制綠頭蒼蠅的排泄物引起的蠅蛆病。使用在綿羊疥癬上時，最常用的剂型為長效型伊維菌素控制釋放膠囊。

研究

伊维菌素在体外对包括SARS-CoV-2在内的若干正单链RNA病毒有抗病毒作用。[14]后续研究发现本药在猴肾细胞对SARS-CoV-2的半抑制浓度为2.2–2.8μM。[15][16]伊维菌素在人体内达到抗病毒作用所需剂量远高于人用最高批准剂量、亦超过可安全实现剂量。[17][18]本药通过抑制输入蛋白α/β1的核运输达到抗病毒作用，在上述剂量下对宿主有毒。[19]因此现在缺乏展开本药COVID-19的临床检验的理由。[20]

有多人因服用本药马用浓缩剂住院；用药过度亦已导致死亡病例；死亡原因可能是本药与其他药物的相互作用。[21]截至2021年6月 (2021-06)，为解决原有小规模、低质量研究的不确定之处，美国和英国展开了大规模临床研究。[22][23]

众多对本药运用于COVID-19的研究有重大方法缺陷，证据水平因此很低。[20][24][25]众多组织因此公开表示本药对于COVID-19有效的证据薄弱。2021年2月，本药的研发厂商默克发表声明表示目前没有本药对COVID-19有效的适当证据、以此目的使用本药亦相当危险。[26][27]美国国立卫生研究院COVID-19治疗指南表示本药证据极其有限，无法做出任何建议。[28]英国全国COVID-19治疗咨询委员会认定本药用于COVID-19治疗的证据和可行性不足以进行下一步调查.[29]

美国食品药品监督管理局（FDA）未批准本药在美国治疗任何病毒疾病、在欧洲亦未获准用于治疗COVID-19。[28][30] 在审核本药相关证据后，欧洲药品管理局（EMA）表示目前数据不支持在良好设计的临床试验外使用本药。[30]2021年3月，FDA及EMA皆发布指南表示不应使用本药治疗COVID-19。[21][30]世界卫生组织亦表示本药除临床试验外不应用于治疗COVID-19。[31]巴西国家卫生监督局（英语：Brazilian Health Regulatory Agency）、巴西传染病学会、巴西胸腔学会发布声明反对使用本药预防或治疗早期COVID-19。[32][33][34]

參見

参考资料

  1. ^ 1.0 1.1 1.2 1.3 Ivermectin. The American Society of Health-System Pharmacists. [Jan 2016]. （原始内容存档于2016-01-03）. 
  2. ^ 2.0 2.1 Saunders Handbook of Veterinary Drugs: Small and Large Animal 4. Elsevier Health Sciences. 2015: 420 [2016-01-24]. ISBN 9780323244862. （原始内容存档于2016-01-31）. 
  3. ^ Panahi, Y; Poursaleh, Z; Goldust, M. The efficacy of topical and oral ivermectin in the treatment of human scabies.. Annals of parasitology. 2015, 61 (1): 11–6. PMID 25911032. 
  4. ^ Sneader, Walter. Drug Discovery a History.. Chichester: John Wiley & Sons. 2005: 333 [2016-01-24]. ISBN 9780470015520. （原始内容存档于2016-01-31）. 
  5. ^ 5.0 5.1 Hamilton, Richard J. Tarascon pocket pharmacopoeia : 2014 deluxe lab-pocket edition 15th edition. Sudbury: Jones & Bartlett Learning. 2014: 422 [2016-01-24]. ISBN 9781284053999. （原始内容存档于2016-01-31）. 
  6. ^ 6.0 6.1 Mehlhorn, Heinz. Encyclopedia of parasitology 3rd ed. Berlin: Springer. 2008: 646 [2016-01-24]. ISBN 9783540489948. （原始内容存档于2016-01-31）. 
  7. ^ Ivermectin Levels and Effects while Breastfeeding. [2016-01-16]. （原始内容存档于2016-01-01）. 
  8. ^ Vercruysse, edited by J.; Rew, R.S. Macrocyclic lactones in antiparasitic therapy. Oxon, UK: CABI Pub. 2002: Preface [2016-01-24]. ISBN 9780851998404. （原始内容存档于2016-01-31）. 
  9. ^ WHO Model List of Essential Medicines (PDF). World Health Organization. October 2013 [2014-04-22]. （原始内容存档 (PDF)于2014-04-23）. 
  10. ^ Ivermectin. International Drug Price Indicator Guide. [2016-01-16]. [永久失效連結]
  11. ^ Fisher MH, Mrozik H. The chemistry and pharmacology of avermectins. Annu. Rev. Pharmacol. Toxicol. 1992, 32: 537–53. PMID 1605577. doi:10.1146/annurev.pa.32.040192.002541. 
  12. ^ W. C. CAMPBELL; R. W. BURG, , M. H. FISHER, and , R. A. DYBAS. The Discovery of Ivermectin and Other Avermectins. American Chemical Society: 5–20. 1984-06-26. ISBN 9780841210837.  |chapter=被忽略 (帮助)
  13. ^ The Nobel Prize in Physiology or Medicine 2015. Nobel Foundation. [2020-05-06]. 
  14. ^ Heidary F, Gharebaghi R. Ivermectin: a systematic review from antiviral effects to COVID-19 complementary regimen. The Journal of Antibiotics. September 2020, 73 (9): 593–602. PMC 7290143 可免费查阅. PMID 32533071. doi:10.1038/s41429-020-0336-z. 
  15. ^ Caly L, Druce JD, Catton MG, Jans DA, Wagstaff KM. The FDA-approved drug ivermectin inhibits the replication of SARS-CoV-2 in vitro. Antiviral Research. April 2020, 178: 104787. PMC 7129059 可免费查阅. PMID 32251768. doi:10.1016/j.antiviral.2020.104787. 
  16. ^ Şimşek Yavuz S, Ünal S. Antiviral treatment of COVID-19. Turkish Journal of Medical Sciences. April 2020, 50 (SI-1): 611–619. PMC 7195979 可免费查阅. PMID 32293834. doi:10.3906/sag-2004-145 可免费查阅. 
  17. ^ Bray M, Rayner C, Noël F, Jans D, Wagstaff K. Ivermectin and COVID-19: A report in Antiviral Research, widespread interest, an FDA warning, two letters to the editor and the authors' responses. Antiviral Research. June 2020, 178: 104805. PMC 7172803 可免费查阅. PMID 32330482. doi:10.1016/j.antiviral.2020.104805. 
  18. ^ López-Medina E, López P, Hurtado IC, Dávalos DM, Ramirez O, Martínez E, et al. Effect of Ivermectin on Time to Resolution of Symptoms Among Adults With Mild COVID-19. JAMA. 2021-03-04, 325 (14): 1426–1435. ISSN 0098-7484. PMC 7934083 可免费查阅. PMID 33662102. doi:10.1001/jama.2021.3071.  已忽略未知参数|pmc-embargo-date= (帮助)
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规范控制数据库：各地 編輯維基數據鏈接
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