右美沙芬：修订间差异
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{{Copy edit|time=2023-08-22T17:25:04+00:00}}
{{Expert needed|subject=药理学|time=2023-08-22T17:25:04+00:00}}
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{{medical}}
{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 470624518
| IUPAC_name = (4b''S'',8a''R'',9''S'')-3-Methoxy-11-methyl-6,7,8,8a,9,10-hexahydro-5''H''-9,4b-(epiminoethano)phenanthrene
| image = Dextromethorphan.svg
| image2 = Dextromethorphan-from-xtal-3D-balls-A.png
<!--Clinical data-->
| tradename = Robitussin, Delsym, DM, DexAlone, Duract
| Drugs.com = {{drugs.com|monograph|dextromethorphan-hydrochloride}}
| MedlinePlus = a682492
| pregnancy_AU = A
| pregnancy_US = C
| legal_status =
| legal_UK = GSL
| legal_AU = S2
| legal_US = OTC
| legal_CA = OTC
| legal_CN = [[第二类精神药品]] {{small|（单方制剂）}}
| routes_of_administration = [[口服]]
| dependency_liability = 低
<!--Pharmacokinetic data-->
| bioavailability = 11%<ref name="pmid15500572">{{cite journal |doi=10.1111/j.1365-2885.2004.00608.x |pmid=15500572 |title=Plasma profile and pharmacokinetics of dextromethorphan after intravenous and oral administration in healthy dogs |journal=Journal of Veterinary Pharmacology and Therapeutics |volume=27 |issue=5 |pages=337–41 |year=2004 |last1=Kukanich |first1=B. |last2=Papich |first2=M. G. }}</ref>
| metabolism = 經肝酶代謝，主由[[CYP2D6]]，次則由[[CYP3A4]]與[[CYP3A5]]
| elimination_half-life = 2-4 hours (extensive metabolisers); 24 hours (poor metabolisers)<ref name = MSR>{{cite web|title=Balminil DM, Benylin DM (dextromethorphan) dosing, indications, interactions, adverse effects, and more|work=Medscape Reference|publisher=WebMD|accessdate=2014-04-15|url=http://reference.medscape.com/drug/balminil-dm-benylin-dm-dextromethorphan-343401#showall|archive-date=2019-03-31|archive-url=https://web.archive.org/web/20190331154154/https://reference.medscape.com/drug/balminil-dm-benylin-dm-dextromethorphan-343401#showall|dead-url=no}}</ref>
| excretion = [[肾脏]]
<!--Identifiers-->
| IUPHAR_ligand = 6953
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 125-71-3
| ATC_prefix = R05
| ATC_suffix = DA09
| PubChem = 15978238
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00514
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 13109865
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 7355X3ROTS
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D03742
| ChEBI_Ref = {{ebicite|changed|EBI}}
| ChEBI = 4470
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 52440
<!--Chemical data-->
| C=18 | H=25 | N=1 | O=1
| smiles = CN1CC[C@@]23CCCC[C@@H]2[C@@H]1Cc4c3cc(cc4)OC
| InChI = 1/C18H25NO/c1-19-10-9-18-8-4-3-5-15(18)17(19)11-13-6-7-14(20-2)12-16(13)18/h6-7,12,15,17H,3-5,8-11H2,1-2H3/t15-,17+,18+/m1/s1
| InChIKey = MKXZASYAUGDDCJ-NJAFHUGGBD
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C18H25NO/c1-19-10-9-18-8-4-3-5-15(18)17(19)11-13-6-7-14(20-2)12-16(13)18/h6-7,12,15,17H,3-5,8-11H2,1-2H3/t15-,17+,18+/m1/s1
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = MKXZASYAUGDDCJ-NJAFHUGGSA-N
| melting_point = 111
}}
'''右美沙芬'''（Dextromethorphan），又名'''右甲嗎喃'''，英文簡稱DM或DXM，是一種鎮咳藥物，它的[[氫溴酸鹽]]（Dextromethorphan hydrobromide）常用於藥品中。
[[美國食品及藥物管理局]]在1958年批准右美沙芬可不需醫生處方而作為鎮咳藥發售。當時最廣泛使用的咳藥[[可待因]]有被濫用的可能性，也可成癮
== 藥物效應動力學 ==
第32行 ⟶ 第70行：
服用治療劑量後，右美沙芬在[[中樞神經系統]]作用，抑制咳嗽，卻不抑制[[纖毛]]活動。右美沙芬在腸胃被迅速吸收，在口服後15至60分鐘內可發揮藥效。口服後藥力可維持大約3至8小時。
成人口服用量大約是每6至8小時服30毫克，或依醫師指示。
== 臨床藥理學 ==
口服後，右美沙芬迅速從腸胃吸收，進入血管及穿過[[腦血管障壁]]。初次進入[[肝門靜脈]]後，部份右美沙芬被代謝成另一有藥效的代謝物[[右啡烷]]
許多藥物（包括[[抗抑鬱藥]]）是CYP2D6的強效抑制劑，如果同時服用這些藥物及右美沙芬，可能產生藥物間的相互作用，曾有因此致死的事例報告。
== 歷史 ==
右美沙芬獲批的{{US patent|2,676,177}}
目前在台灣有商品販售的藥，就屬由美商[[惠氏藥廠]]所生產的「諾比舒咳」。而該商品又細分兩種：「咳嗽液」和「祛痰液」。只有咳嗽液含有右美沙芬。
==
{{Main|右美沙芬的娛樂用途}}
尽管成瘾度相较于可待因等鸦片类止咳药物更低，右美沙芬仍有药物滥用的危险。长期大剂量的服用可能导致毛细血管脆化，组织易出血，增加创伤的程度。
=== 中国大陆 ===
在[[中国大陆]]，滥用者常常将药物整板吞下或整瓶一饮而尽并配上[[可乐]]或其他含有[[咖啡因]]的饮料以求兴奋效果<ref>{{cite news|title=沈摧毁“小泰”江浙入辽渠道抓39人|url=http://liaoning.lnd.com.cn/htm/2016-04/27/content_4409676.htm|agency=辽宁新闻|date=2016-04-27|language=zh-cn|access-date=2016-08-14|archive-url=https://web.archive.org/web/20170111083519/http://liaoning.lnd.com.cn/htm/2016-04/27/content_4409676.htm|archive-date=2017-01-11|dead-url=yes}}</ref>。一些媒体称其为“[[可待因]]第二”<ref>{{cite news|title=止咳水严禁违法销售滥用成瘾 替代品现身|url=http://finance.sina.com.cn/consume/20150107/101921242916.shtml|agency=[[新浪]]|date=2015-01-07|language=zh-cn|accessdate=2016-08-14|archive-date=2016-08-22|archive-url=https://web.archive.org/web/20160822131148/http://finance.sina.com.cn/consume/20150107/101921242916.shtml|dead-url=no}}</ref>。由于可能的药物滥用风险等因素，中国[[国家药品监督管理局]]已于2021年12月将所有氢溴酸右美沙芬口服单方制剂由原先的甲类[[非处方药]]改为[[处方药]]，并要求生产企业修订说明书，删除“长期服用无成瘾性和耐受性”等类似表述<ref>{{cite news |title=国家药监局关于氢溴酸右美沙芬口服单方制剂转换为处方药的公告（2021年第151号） |url=https://www.nmpa.gov.cn/directory/web/nmpa/xxgk/ggtg/qtggtg/20211227162159192.html |accessdate=2022-02-15 |publisher=国家药品监督管理局 |date=2021-12-16 |archive-date=2022-02-15 |archive-url=https://web.archive.org/web/20220215013414/https://www.nmpa.gov.cn/directory/web/nmpa/xxgk/ggtg/qtggtg/20211227162159192.html |dead-url=no }}</ref>。不过，即使在网络禁售后，在一些相对小众的电商平台上也还能购得。<ref>{{Cite web|author=魏倩|date=2023-02-16|editor=周蕾|title=深陷困境的年轻人，嗑“镇咳药”成瘾|url=https://www.lifeweek.com.cn/h5/article/detail.do?artId=191298|access-date=2023-04-15|website=[[三联生活周刊]]|publisher=三联数字刊|language=zh-CN|archive-date=2023-04-19|archive-url=https://web.archive.org/web/20230419150741/https://www.lifeweek.com.cn/h5/article/detail.do?artId=191298|dead-url=no}}</ref>
2024年5月7日，国家药监局等三部门公告，将右美沙芬列入第二类精神药品目录，自当年7月1日起施行。<ref>{{Cite web |title=国家药监局 公安部 国家卫生健康委关于调整精神药品目录的公告（2024年第54号） |url=https://www.nmpa.gov.cn/xxgk/ggtg/ypggtg/ypqtggtg/20240507084000186.html |website=国家药品监督管理局 |date=2024-05-07}}</ref>按照规定，第二类精神药品处方量一般不超过7天，处方需保存2年备查。同时，这也意味着在中国大陆非法制造、运输、贩卖右美沙芬将被视作制造、贩运毒品。
=== 美国 ===
[[美国食品药品监督管理局]]专家委员会因右美沙芬有被滥用的潜在风险，曾考虑将右美沙芬列入处方药范畴，但在2010年9月投票反对该建议，称缺乏将其列为处方药可以遏制滥用的证据。<ref>{{Cite web|date=2010-09-15|title=Cough Medications Should Stay As Over-The-Counter Drugs, FDA Panel Recommends|url=https://www.medicalnewstoday.com/articles/201227|access-date=2023-04-15|website=www.medicalnewstoday.com|language=en|archive-date=2023-04-19|archive-url=https://web.archive.org/web/20230419122455/https://www.medicalnewstoday.com/articles/201227|dead-url=no}}</ref>一些州已限制右美沙芬的销售只限于成年人或实施其他限制购买的措施，类似于伪麻黄碱的限制。截至2012年1月1日，[[加利福尼亚州|加州]]禁止向未成年人销售右美沙芬，[[俄勒冈州]]从2018年1月1日起实行相同政策，除非有医生处方。<ref name="urlwww.leginfo.ca.gov">{{cite web|title=Senate Bill No. 514|url=http://www.leginfo.ca.gov/pub/11-12/bill/sen/sb_0501-0550/sb_514_bill_20110831_chaptered.pdf|url-status=live|archive-url=https://web.archive.org/web/20180308012049/http://www.leginfo.ca.gov/pub/11-12/bill/sen/sb_0501-0550/sb_514_bill_20110831_chaptered.pdf|archive-date=2018-03-08|work=An act to add Sections 11110 and 11111 to the Health and Safety Code, relating to nonprescription drugs.|publisher=State of California, Legislative Counsel}}</ref>
=== 印尼 ===
截至2014年，印尼是世界上唯一一个即使有处方也禁止单一成分右美沙芬的国家<ref>{{cite web|date=2014-05-22|title=BPOM Tetap Batalkan Izin Edar Obat Dekstrometorfan|trans-title=BPOM Still Cancels Dextromethorphan Drug Distribution Permit|url=http://nasional.news.viva.co.id/news/read/506418-bpom-tetap-batalkan-izin-edar-obat-dekstrometorfan|archive-url=https://web.archive.org/web/20150528120821/http://nasional.news.viva.co.id/news/read/506418-bpom-tetap-batalkan-izin-edar-obat-dekstrometorfan|archive-date=2015-05-28|work=VIVAnews|language=id}}</ref>，违规者可能会受到法律制裁。{{Link-id|药物和食品控制局|Badan Pengawas Obat dan Makanan}}（BPOM）禁止销售单一成分右美沙芬药品，无论是否有处方；[[印度尼西亚国家禁毒局|国家禁毒局]]甚至威胁要撤销仍然存有右美沙芬的药店和药房的许可证，并通知警方进行[[刑事起訴|刑事起诉]]。<ref>{{Cite web|title=SINDOnews {{!}} Berita Daerah Dan Provinsi Di Indonesia|url=http://daerah.sindonews.com/read/878465/21/bnn-ancam-tutup-apotek-penjual-dextromethorphan-1404129585%5B%5D|access-date=2017-12-10|website=daerah.sindonews.com|language=id}} {{Dead link|date=2018-03}}</ref>由于这一规定，已有130种药品被撤出市场，但含有多成分右美沙芬的药品仍为非处方药。<ref>{{Cite web|title=Pimpinan dan Apoteker Penanggung Jawab|url=http://www.pom.go.id/files/edaran_dektrome_2013.pdf|archive-url=https://web.archive.org/web/20170810021225/http://www.pom.go.id/files/edaran_dektrome_2013.pdf|archive-date=2017-08-10}}</ref><ref>{{Cite web|title=Badan Pengawas Obat dan Makanan - Republik Indonesia|url=http://www.pom.go.id/new/index.php/view/pers/231/Penjelasan-Terkait-Produk-Obat-Batuk-yang-Beredar--dan--Mengandung-Bahan-Dekstrometorfan-Tunggal-.html|archive-url=https://web.archive.org/web/20170203184008/http://www.pom.go.id/new/index.php/view/pers/231/Penjelasan-Terkait-Produk-Obat-Batuk-yang-Beredar--dan--Mengandung-Bahan-Dekstrometorfan-Tunggal-.html|archive-date=2017-02-03|access-date=2017-12-10|website=www.pom.go.id|language=en-US}}</ref>
== 參考文獻 ==
{{reflist}}
==參見==
*[[对乙酰氨基酚]]
==外部連結==
* [http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Dextromethorphan U.S. National Library of Medicine: Drug Information Portal - Dextromethorphan]{{Wayback|url=http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Dextromethorphan |date=20130513032715 }}
* [https://web.archive.org/web/20101125083631/http://treatmentsclerosis.com/index.php/drugs-meds/nuedexta Nuedexta (dextromethorphan hydrobromide and quinidine sulfate): Prescribing Information (Original Approval Date FDA: October 29, 2010)]
{{Drug use}}
{{Hallucinogens}}
{{Sigmaergics}}
{{规范控制}}
[[Category:合成阿片样物质]]
[[Category:镇咳药]]
[[Category:解离性药物]]
[[Category:吗喃类]]
[[Category:
[[Category:Σ激动剂]]
[[Category:血清素
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[[Category:安乐药]]
[[Category:芳香醚]]
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