右美沙芬：修订间差异

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第7行： 第7行：
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'''右美沙芬'''（英文：Dextromethorphan），又名右甲吗喃，英文简称DM或DXM，是一种[[处方]]中枢性止咳药，它的氢溴酸盐（Dextromethorphan hydrobromide）常用于药品中，也就是常见的[[氢溴酸右美沙芬]]片或氢溴酸右美沙芬糖浆。主要用于[[干咳]]，通过抑制[[延髓]][[咳嗽中枢]]而发挥中枢性镇咳作用。
'''右美沙芬'''（英文：Dextromethorphan），又名右甲吗喃，英文简称DM或DXM，是一种[[处方]]<ref name="Rx-upgrade"></ref>中枢性止咳药，它的氢溴酸盐（Dextromethorphan hydrobromide）常用于药品中，也就是常见的氢溴酸右美沙芬片或氢溴酸右美沙芬糖浆。主要用于[[干咳]]而[[湿咳]]应慎用，通过抑制[[延髓]][[咳嗽中枢]]而发挥中枢性镇咳作用。


== 药品说明书 ==
== 药品说明书 ==
第16行： 第16行：
|+ 右美沙芬及其代谢物结合的受体<ref name="PDSP">{{cite web | title = PDSP K<sub>i</sub> Database | work = Psychoactive Drug Screening Program (PDSP)|author1-link=Bryan Roth | vauthors = Roth BL, Driscol J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | access-date = 14 August 2017 | url = https://pdsp.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=dextromethorphan&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}</ref><ref name="NguyenThomas2016">{{cite journal | vauthors = Nguyen L, Thomas KL, Lucke-Wold BP, Cavendish JZ, Crowe MS, Matsumoto RR | title = Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders | journal = Pharmacology & Therapeutics | volume = 159 | pages = 1–22 | date = March 2016 | pmid = 26826604 | doi = 10.1016/j.pharmthera.2016.01.016 }}</ref><ref name="pmid17689532">{{cite journal | vauthors = Werling LL, Keller A, Frank JG, Nuwayhid SJ | title = A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder | journal = Experimental Neurology | volume = 207 | issue = 2 | pages = 248–257 | date = October 2007 | pmid = 17689532 | doi = 10.1016/j.expneurol.2007.06.013 | s2cid = 38476281 }}</ref><ref name="pmid27139517">{{cite journal | vauthors = Taylor CP, Traynelis SF, Siffert J, Pope LE, Matsumoto RR | title = Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use | journal = Pharmacology & Therapeutics | volume = 164 | pages = 170–182 | date = August 2016 | pmid = 27139517 | doi = 10.1016/j.pharmthera.2016.04.010 | doi-access = free }}</ref>
|+ 右美沙芬及其代谢物结合的受体<ref name="PDSP">{{cite web | title = PDSP K<sub>i</sub> Database | work = Psychoactive Drug Screening Program (PDSP)|author1-link=Bryan Roth | vauthors = Roth BL, Driscol J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | access-date = 14 August 2017 | url = https://pdsp.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=dextromethorphan&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}</ref><ref name="NguyenThomas2016">{{cite journal | vauthors = Nguyen L, Thomas KL, Lucke-Wold BP, Cavendish JZ, Crowe MS, Matsumoto RR | title = Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders | journal = Pharmacology & Therapeutics | volume = 159 | pages = 1–22 | date = March 2016 | pmid = 26826604 | doi = 10.1016/j.pharmthera.2016.01.016 }}</ref><ref name="pmid17689532">{{cite journal | vauthors = Werling LL, Keller A, Frank JG, Nuwayhid SJ | title = A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder | journal = Experimental Neurology | volume = 207 | issue = 2 | pages = 248–257 | date = October 2007 | pmid = 17689532 | doi = 10.1016/j.expneurol.2007.06.013 | s2cid = 38476281 }}</ref><ref name="pmid27139517">{{cite journal | vauthors = Taylor CP, Traynelis SF, Siffert J, Pope LE, Matsumoto RR | title = Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use | journal = Pharmacology & Therapeutics | volume = 164 | pages = 170–182 | date = August 2016 | pmid = 27139517 | doi = 10.1016/j.pharmthera.2016.04.010 | doi-access = free }}</ref>
|-
|-
! 点位 !! {{abbr|DXM|右美沙芬}} !! {{abbrlink|DXO|右啡烷}} !! 来源 !! 参考
! 位点 !! {{abbr|DXM|右美沙芬}} !! {{abbrlink|DXO|右啡烷}} !! 来源 !! 参考
|-
|-
| [[NMDA受体|{{abbr|NMDAR|N-甲基-D-天冬氨酸受体}}<br/>(MK-801)]] || 2,120–8,945 || 486–906 || 鼠 || <ref name="NguyenThomas2016"/>
| [[NMDA受体|{{abbr|NMDAR|N-甲基-D-天冬氨酸受体}}<br/>(MK-801)]] || 2,120–8,945 || 486–906 || 鼠 || <ref name="NguyenThomas2016"/>
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右美沙芬的代谢物之一[[右啡烷]]作为比右美沙芬更强的NMDA拮抗剂，通常比右美沙芬更造成[[解离]]。<ref name="pmid10064839">{{cite journal | vauthors = Chou YC, Liao JF, Chang WY, Lin MF, Chen CF | title = Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan | journal = Brain Research | volume = 821 | issue = 2 | pages = 516–519 | date = March 1999 | pmid = 10064839 | doi = 10.1016/S0006-8993(99)01125-7 | s2cid = 22762264 }}</ref>而右美沙芬的另一种主要代谢物(+)-3-甲氧基吗啡喃的作用尚不完全明确。<ref>{{cite journal | vauthors = Schmider J, Greenblatt DJ, Fogelman SM, von Moltke LL, Shader RI | title = Metabolism of dextromethorphan in vitro: involvement of cytochromes P450 2D6 and 3A3/4, with a possible role of 2E1 | journal = Biopharmaceutics & Drug Disposition | volume = 18 | issue = 3 | pages = 227–240 | date = April 1997 | pmid = 9113345 | doi = 10.1002/(SICI)1099-081X(199704)18:3<227::AID-BDD18>3.0.CO;2-L | s2cid = 5638973 }}</ref>
右美沙芬的代谢物之一[[右啡烷]]作为比右美沙芬更强的NMDA拮抗剂，通常比右美沙芬更造成[[解离]]。<ref name="pmid10064839">{{cite journal | vauthors = Chou YC, Liao JF, Chang WY, Lin MF, Chen CF | title = Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan | journal = Brain Research | volume = 821 | issue = 2 | pages = 516–519 | date = March 1999 | pmid = 10064839 | doi = 10.1016/S0006-8993(99)01125-7 | s2cid = 22762264 }}</ref>而右美沙芬的另一种主要代谢物(+)-3-甲氧基吗啡喃的作用尚不完全明确。<ref>{{cite journal | vauthors = Schmider J, Greenblatt DJ, Fogelman SM, von Moltke LL, Shader RI | title = Metabolism of dextromethorphan in vitro: involvement of cytochromes P450 2D6 and 3A3/4, with a possible role of 2E1 | journal = Biopharmaceutics & Drug Disposition | volume = 18 | issue = 3 | pages = 227–240 | date = April 1997 | pmid = 9113345 | doi = 10.1002/(SICI)1099-081X(199704)18:3<227::AID-BDD18>3.0.CO;2-L | s2cid = 5638973 }}</ref>

== 药代动力学 ==
右美沙芬在口服后大约15~30分钟内开始吸收，在2~3小时达到[[血药峰值]]，它的生物半衰期在代谢能力强的人身上大约为2~4小时，而代谢能力弱的人有可能到达24小时，大部分通过尿液排出。<ref name = MSR>{{cite web|title=Balminil DM, Benylin DM (dextromethorphan) dosing, indications, interactions, adverse effects, and more|work=Medscape Reference|publisher=WebMD|accessdate=2024-02-11|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>

== 药物滥用 ==
右美沙芬时常被滥用，其中属未成年中较为流行。<ref>{{cite web |url=https://new.qq.com/rain/a/20221229A04TJH00 |title=右美沙芬滥用者的隐秘世界 |publisher=苏子涵 、李沁桦、刘汨 |date=2022-12-29 |accessdate=2024-02-11 }}</ref>由于其被滥用的潜质，中国国家药监局在2021年12月16日将右美沙芬口服单方制从[[非处方药]]剂转换为[[处方药]]并随后实行[[网络禁售]]。<ref name="Rx-upgrade">{{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/yaopin/ypggtg/20211227162159192.html |accessdate=2024-02-11 |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><ref>{{cite web |url=https://www.nmpa.gov.cn/yaopin/ypggtg/20221130200847133.html |title=国家药监局关于发布药品网络销售禁止清单（第一版）的公告（2022年 第111号） |publisher=国家药品监督管理局 |date=2022-11-30 |accessdate=2024-02-11 }}</ref>但右美沙芬至今仍能在药店随意购买。<ref>{{cite web |url=http://opinion.people.com.cn/n1/2023/1205/c436867-40132522.html |title=人民热评：右美沙芬被滥用，谁在顶风作案？ |publisher=人民网-观点频道 |date=2023-12-05日 |accessdate=2024-02-11 }}</ref>


== 参考文献 ==
== 参考文献 ==

2024年2月12日 (一) 00:00的版本

右美沙芬
文件:右美沙芬化學結構.png
化學數據
化學式C18H25NO
摩爾質量271.40 g·mol−1

右美沙芬（英文：Dextromethorphan），又名右甲嗎喃，英文簡稱DM或DXM，是一種處方[1]中樞性止咳藥，它的氫溴酸鹽（Dextromethorphan hydrobromide）常用於藥品中，也就是常見的氫溴酸右美沙芬片或氫溴酸右美沙芬糖漿。主要用於乾咳而濕咳應慎用，通過抑制延髓咳嗽中樞而發揮中樞性鎮咳作用。

藥品說明書

右美沙芬片每片15mg，成人口服一次1～2片，一日3～4次。哮喘、痰多、肝腎功能不全患者及孕婦慎用。醫療劑量下可見頭暈、頭痛、嗜睡、易激動、噯氣、食慾缺乏、便秘、噁心、皮膚過敏等副作用，過量時可見神志不清、幻覺、支氣管痙攣、呼吸抑制。[2]

藥理學

右美沙芬及其代謝物結合的受體[3][4][5][6]
位點 DXM DXOTooltip 右啡烷 來源 參考
NMDAR
(MK-801)		 2,120–8,945 486–906 鼠 [4]
σ1 142–652 118–481 老鼠 [4]
σ2 11,060–22,864 11,325–15,582 鼠 [4]
MORTooltip μ-阿片受體 1,280
ND		 420
>1,000		 鼠
人類		 [4]
[7]
DORTooltip δ-阿片受體 11,500 34,700 鼠 [4]
KORTooltip κ-阿片受體 7,000 5,950 鼠 [4]
SERTTooltip 血清素轉運體 23–40 401–484 鼠 [4]
NETTooltip 去甲腎上腺素轉運體 ≥240 ≥340 鼠 [4]
DATTooltip 多巴胺轉運體 >1,000 >1,000 鼠 [4]
5-HT1A >1,000 >1,000 鼠 [4]
5-HT1B/1D 61% at 1 μM 54% at 1 μM 鼠 [4]
5-HT2A >1,000 >1,000 鼠 [4]
α1 >1,000 >1,000 鼠 [4]
α2 60% at 1 μM >1,000 鼠 [4]
β >1,000 35% at 1 μM 鼠 [4]
D2 >1,000 >1,000 鼠 [4]
H1 >1,000 95% at 1 μM 鼠 [4]
mAChRsTooltip 毒蕈鹼乙醯膽鹼受體 >1,000 100% at 1 μM 鼠 [4]
nAChRsTooltip 菸鹼乙醯膽鹼受體 700–8,900
(IC50)		 1,300–29,600
(IC50)		 鼠 [4]
VDSCsTooltip 電壓依賴性鈉通道 >50,000 (IC50) ND 鼠 [8][9]
除非另有說明，數值均為 Ki(nM)。該值越小則藥物與該位點的結合越強。

右美沙芬通過MK-801/PCP位點非競爭性拮抗NMDA受體。[10]它還是血清素和去甲腎上腺素轉運體抑制劑（SNRI）；是σ-1受體的激動劑；是菸鹼乙醯膽鹼受體的負變構調節劑；右美沙芬還是血清素1B/1D、組胺H1、α2-腎上腺素能和毒蕈鹼乙醯膽鹼受體的配體。[4][10]

右美沙芬的代謝物之一右啡烷作為比右美沙芬更強的NMDA拮抗劑，通常比右美沙芬更造成解離。[11]而右美沙芬的另一種主要代謝物(+)-3-甲氧基嗎啡喃的作用尚不完全明確。[12]

藥代動力學

右美沙芬在口服後大約15~30分鐘內開始吸收，在2~3小時達到血藥峰值，它的生物半衰期在代謝能力強的人身上大約為2~4小時，而代謝能力弱的人有可能到達24小時，大部分通過尿液排出。[13]

藥物濫用

右美沙芬時常被濫用，其中屬未成年中較為流行。[14]由於其被濫用的潛質，中國國家藥監局在2021年12月16日將右美沙芬口服單方制從非處方藥劑轉換為處方藥並隨後實行網絡禁售。[1][15]但右美沙芬至今仍能在藥店隨意購買。[16]

參考文獻

  1. ↑ 1.0 1.1 "國家藥監局關於氫溴酸右美沙芬口服單方製劑轉換為處方藥的公告（2021年第151號）". 國家藥品監督管理局. 2021-12-16. Archived from the original on 2022-02-15. Retrieved 2024-02-11. {{cite news}}: Unknown parameter |dead-url= ignored (|url-status= suggested) (help)
  2. ↑ "右美沙芬片(氫溴酸右美沙芬片)" (in 中文). Retrieved 2024-01-04.
  3. ↑ Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
  4. ↑ 4.00 4.01 4.02 4.03 4.04 4.05 4.06 4.07 4.08 4.09 4.10 4.11 4.12 4.13 4.14 4.15 4.16 4.17 4.18 4.19 4.20 Nguyen L, Thomas KL, Lucke-Wold BP, Cavendish JZ, Crowe MS, Matsumoto RR (March 2016). "Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders". Pharmacology & Therapeutics. 159: 1–22. doi:10.1016/j.pharmthera.2016.01.016. PMID 26826604.
  5. ↑ Werling LL, Keller A, Frank JG, Nuwayhid SJ (October 2007). "A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder". Experimental Neurology. 207 (2): 248–257. doi:10.1016/j.expneurol.2007.06.013. PMID 17689532. S2CID 38476281.
  6. ↑ Taylor CP, Traynelis SF, Siffert J, Pope LE, Matsumoto RR (August 2016). "Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use". Pharmacology & Therapeutics. 164: 170–182. doi:10.1016/j.pharmthera.2016.04.010. PMID 27139517.
  7. ↑ Raynor K, Kong H, Mestek A, Bye LS, Tian M, Liu J, et al. (January 1995). "Characterization of the cloned human mu opioid receptor". The Journal of Pharmacology and Experimental Therapeutics. 272 (1): 423–428. PMID 7815359.
  8. ↑ Lee JH, Shin EJ, Jeong SM, Lee BH, Yoon IS, Lee JH, et al. (June 2007). "Effects of dextrorotatory morphinans on brain Na+ channels expressed in Xenopus oocytes". European Journal of Pharmacology. 564 (1–3): 7–17. doi:10.1016/j.ejphar.2007.01.088. PMID 17346698.
  9. ↑ Gao XF, Yao JJ, He YL, Hu C, Mei YA (2012). "Sigma-1 receptor agonists directly inhibit Nav1.2/1.4 channels". PLOS ONE. 7 (11): e49384. Bibcode:2012PLoSO...749384G. doi:10.1371/journal.pone.0049384. PMC 3489664. PMID 23139844.
  10. ↑ 10.0 10.1 Burns JM, Boyer EW (2013). "Antitussives and substance abuse". Substance Abuse and Rehabilitation. 4: 75–82. doi:10.2147/SAR.S36761. PMC 3931656. PMID 24648790.
  11. ↑ Chou YC, Liao JF, Chang WY, Lin MF, Chen CF (March 1999). "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan". Brain Research. 821 (2): 516–519. doi:10.1016/S0006-8993(99)01125-7. PMID 10064839. S2CID 22762264.
  12. ↑ Schmider J, Greenblatt DJ, Fogelman SM, von Moltke LL, Shader RI (April 1997). "Metabolism of dextromethorphan in vitro: involvement of cytochromes P450 2D6 and 3A3/4, with a possible role of 2E1". Biopharmaceutics & Drug Disposition. 18 (3): 227–240. doi:10.1002/(SICI)1099-081X(199704)18:3<227::AID-BDD18>3.0.CO;2-L. PMID 9113345. S2CID 5638973.
  13. ↑ "Balminil DM, Benylin DM (dextromethorphan) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 2019-03-31. Retrieved 2024-02-11. {{cite web}}: Unknown parameter |dead-url= ignored (|url-status= suggested) (help)
  14. ↑ "右美沙芬濫用者的隱秘世界". 蘇子涵 、李沁樺、劉汨. 2022-12-29. Retrieved 2024-02-11.
  15. ↑ "國家藥監局關於發布藥品網絡銷售禁止清單（第一版）的公告（2022年 第111號）". 國家藥品監督管理局. 2022-11-30. Retrieved 2024-02-11.
  16. ↑ "人民熱評：右美沙芬被濫用，誰在頂風作案？". 人民網-觀點頻道. 2023-12-05日. Retrieved 2024-02-11. {{cite web}}: Check date values in: |date= (help)
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