右美沙芬：修订间差异

来自Hyacinth
跳转到导航 跳转到搜索
←上一编辑下一编辑→
删除的内容 添加的内容
可视化wikitext
草awa（留言 | 贡献）
行政员、​界面管理员、​管理员
2,521次编辑
小无编辑摘要
草awa（留言 | 贡献）
行政员、​界面管理员、​管理员
2,521次编辑
小无编辑摘要
第7行： 第7行：
}}
}}


'''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"/>
第64行： 第64行：


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:右美沙芬化学结构.png
化学数据
化学式C18H25NO
摩尔质量271.40 g·mol−1

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[1]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

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、肝肾功能不全患者及孕妇慎用。医疗剂量下可见头晕、头痛、嗜睡、易激动、嗳气、食欲缺乏、便秘、恶心、皮肤过敏等副作用，过量时可见神志不清、幻觉、支气管痉挛、呼吸抑制。[2]

药理学

右美沙芬及其代谢物结合的受体[3][4][5][6]
位点 DXM DXOTooltip 右啡烷 来源 参考
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-阿片受体 1,280
ND		 420
>1,000		 鼠
人类		 [4]
[7]
DORTooltip δ-阿片受体 11,500 34,700 鼠 [4]
KORTooltip κ-阿片受体 7,000 5,950 鼠 [4]
SERTTooltip 血清素转运体 23–40 401–484 鼠 [4]
NETTooltip 去甲肾上腺素转运体 ≥240 ≥340 鼠 [4]
DATTooltip 多巴胺转运体 >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 毒蕈碱乙酰胆碱受体 >1,000 100% at 1 μM 鼠 [4]
nAChRsTooltip 烟碱乙酰胆碱受体 700–8,900
(IC50)		 1,300–29,600
(IC50)		 鼠 [4]
VDSCsTooltip 电压依赖性钠通道 >50,000 (IC50) ND 鼠 [8][9]
除非另有说明，数值均为 Ki(nM)。该值越小则药物与该位点的结合越强。

右美沙芬通过MK-801/PCP位点非竞争性拮抗NMDA受体。[10]它还是血清素和去甲肾上腺素转运体抑制剂（SNRI）；是σ-1受体的激动剂；是烟碱乙酰胆碱受体的负变构调节剂；右美沙芬还是血清素1B/1D、组胺H1、α2-肾上腺素能和毒蕈碱乙酰胆碱受体的配体。[4][10]

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。[11]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。[12]

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。[13]

药物滥用

右美沙芬时常被滥用，其中属未成年中较为流行。[14]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。[1][15]但右美沙芬至今仍能在药店随意购买。[16]

参考文献

  1. ↑ 1.0 1.1 "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）". 国家药品监督管理局. 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(氢溴酸右美沙芬片)" (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. ↑ "右美沙芬滥用者的隐秘世界". 苏子涵 、李沁桦、刘汨. 2022-12-29. Retrieved 2024-02-11.
  15. ↑ "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）". 国家药品监督管理局. 2022-11-30. Retrieved 2024-02-11.
  16. ↑ "人民热评：右美沙芬被滥用，谁在顶风作案？". 人民网-观点频道. 2023-12-05日. Retrieved 2024-02-11. {{cite web}}: Check date values in: |date= (help)
检索自“https://www.hyacinthwiki.com/index.php?title=右美沙芬&oldid=2157”