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苏沃雷生：修订间差异

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'''苏沃雷生'''，品牌名'''Belsomra'''，是一种[[食欲素受体拮抗剂]]，被用于治疗失眠症，主要用于入睡或睡眠维持困难的成年患者的治疗。<ref name=":0">{{Cite web|title=DailyMed - BELSOMRA- suvorexant tablet, film coated|url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e5b72731-1acb-45b7-9c13-290ad12d3951|access-date=2023-07-23|website=dailymed.nlm.nih.gov}}</ref><ref name=":1">{{Cite journal |last=Jacobson |first=Laura H. |last2=Callander |first2=Gabrielle E. |last3=Hoyer |first3=Daniel |date=2014-11 |title=Suvorexant for the treatment of insomnia |url=https://pubmed.ncbi.nlm.nih.gov/25318834/ |journal=Expert Review of Clinical Pharmacology |volume=7 |issue=6 |doi=10.1586/17512433.2014.966813 |issn=1751-2441 |pmid=25318834}}</ref><ref name=":2">{{Cite web|title=苏沃雷生[精二]_其他镇静催眠药_镇静药与催眠药_作用于神经系统的药物_湖南药事服务网|url=https://www.hnysfww.com/mobile/goods.php?id=733|access-date=2023-07-23|website=www.hnysfww.com}}</ref>苏沃雷生具有加速入睡、延长睡眠时间、减少半夜醒来次数以及提高睡眠质量的作用。<ref name=":0" /><ref name=":1" /><ref name=":3">{{Cite journal |last=Kuriyama |first=Akira |last2=Tabata |first2=Hiromitsu |date=2017-10 |title=Suvorexant for the treatment of primary insomnia: A systematic review and meta-analysis |url=https://pubmed.ncbi.nlm.nih.gov/28365447/ |journal=Sleep Medicine Reviews |volume=35 |doi=10.1016/j.smrv.2016.09.004 |issn=1532-2955 |pmid=28365447}}</ref>其药效中等，<ref>{{Cite web|title=Table 1: The Single Nucleotide Polymorphisms in cathepsin B protein mined from literature (PMID: 16492714).|url=http://dx.doi.org/10.7717/peerj.7425/table-1|access-date=2023-07-23|website=dx.doi.org}}</ref>与其他[[食欲素受体拮抗剂]]类似，但低于[[苯二氮䓬类|苯二氮卓类药物]]与[[Z-drugs|非苯二氮卓类药物]]。<ref>{{Cite journal |last=De Crescenzo |first=Franco |last2=D'Alò |first2=Gian Loreto |last3=Ostinelli |first3=Edoardo G |last4=Ciabattini |first4=Marco |last5=Di Franco |first5=Valeria |last6=Watanabe |first6=Norio |last7=Kurtulmus |first7=Ayse |last8=Tomlinson |first8=Anneka |last9=Mitrova |first9=Zuzana |last10=Foti |first10=Francesca |last11=Del Giovane |first11=Cinzia |date=2022-07 |title=Comparative effects of pharmacological interventions for the acute and long-term management of insomnia disorder in adults: a systematic review and network meta-analysis |url=https://linkinghub.elsevier.com/retrieve/pii/S0140673622008789 |journal=The Lancet |language=en |volume=400 |issue=10347 |doi=10.1016/S0140-6736(22)00878-9}}</ref>苏沃雷生的给药方式为口服给药。<ref name=":0" /><ref name=":1" /><ref name=":2" /><ref>{{Cite web|last=https://www.facebook.com/Drugscom|title=Generic Belsomra Availability|url=https://www.drugs.com/availability/generic-belsomra.html|access-date=2023-07-23|website=Drugs.com|language=en}}</ref>

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苏沃雷生的副作用包括[[嗜睡症|嗜睡]]、[[頭暈|头晕]]、[[白天嗜睡]]和[[镇静]]、[[頭痛|头痛]]、[[頭暈|头晕]]、[[梦境异常]]、[[口乾|口干]]和次日驾驶能力受损。<ref name=":0" /><ref name=":3" /><ref name=":4">{{Cite journal |last=Sutton |first=Eliza |date=2015-11 |title=Profile of suvorexant in the management of insomnia |url=https://www.dovepress.com/profile-of-suvorexant-in-the-management-of-insomnia-peer-reviewed-article-DDDT |journal=Drug Design, Development and Therapy |language=en |doi=10.2147/DDDT.S73224 |issn=1177-8881 |pmc=PMC4651361 |pmid=26648692}}</ref>偶见[[睡眠瘫痪症|睡眠麻痹]]，[[做梦异常]]与[[梦游症|梦游]]等复杂睡眠行为与出现[[自杀意念]]。<ref name=":0" /><ref name=":1" /><ref name=":4" />服用这种药物似乎不会产生明显的[[藥物耐受性|药物耐受性]]、[[药物依赖]]、[[藥物戒斷|戒断症状]]和[[反弹现象]]。<ref name=":0" /><ref>{{Cite journal |last=Keks |first=Nicholas A. |last2=Hope |first2=Judy |last3=Keogh |first3=Simone |date=2017-12 |title=Suvorexant: scientifically interesting, utility uncertain |url=https://pubmed.ncbi.nlm.nih.gov/28994603/ |journal=Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists |volume=25 |issue=6 |doi=10.1177/1039856217734677 |issn=1440-1665 |pmid=28994603}}</ref><ref>{{Cite journal |last=Muehlan |first=Clemens |last2=Vaillant |first2=Cedric |last3=Zenklusen |first3=Isabelle |last4=Kraehenbuehl |first4=Stephan |last5=Dingemanse |first5=Jasper |date=2020-11-01 |title=Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders |url=https://www.tandfonline.com/doi/full/10.1080/17425255.2020.1817380 |journal=Expert Opinion on Drug Metabolism & Toxicology |language=en |volume=16 |issue=11 |doi=10.1080/17425255.2020.1817380 |issn=1742-5255}}</ref>苏沃雷生是一种[[双重食欲素受体激动剂]]（DORA），选择性拮抗[[食欲素1型受体]]（Ox1R）和[[食欲素2型受体]]（Ox2R）。<ref name=":1" />该药物的达峰时间为2至3小时，清除半衰期为12小时。<ref name=":0" /><ref name=":1" />与苯二氮卓类药物与非苯二氮卓类药物不同的是，苏沃雷生并不会与 GABA 受体发生相互作用，而是通过其特殊的药理学机制发挥作用。<ref name=":1" /><ref>{{Cite journal |last=Atkin |first=Tobias |last2=Comai |first2=Stefano |last3=Gobbi |first3=Gabriella |date=2018-04 |title=Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery |url=https://pubmed.ncbi.nlm.nih.gov/29487083/ |journal=Pharmacological Reviews |volume=70 |issue=2 |doi=10.1124/pr.117.014381 |issn=1521-0081 |pmid=29487083}}</ref>

{{Drugbox|drug_name=苏沃雷生
{{Drugbox|drug_name=苏沃雷生
| Verifiedfields = verified
| Verifiedfields = verified
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| legal_AU_comment = <ref>{{cite web | title=Prescription medicines: registration of new chemical entities in Australia, 2016 | website=Therapeutic Goods Administration (TGA) | date=21 June 2022 | url=https://www.tga.gov.au/prescription-medicines-registration-new-chemical-entities-australia-2016 | access-date=10 April 2023}}</ref>
| legal_AU_comment = <ref>{{cite web | title=Prescription medicines: registration of new chemical entities in Australia, 2016 | website=Therapeutic Goods Administration (TGA) | date=21 June 2022 | url=https://www.tga.gov.au/prescription-medicines-registration-new-chemical-entities-australia-2016 | access-date=10 April 2023}}</ref>
| legal_US=Schedule IV}}
| legal_US=Schedule IV}}
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'''苏沃雷生'''，品牌名'''Belsomra'''，是一种[[食欲素受体拮抗剂]]，被用于治疗失眠症，主要用于入睡或睡眠维持困难的成年患者的治疗。<ref name=":0">{{Cite web|title=DailyMed - BELSOMRA- suvorexant tablet, film coated|url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e5b72731-1acb-45b7-9c13-290ad12d3951|access-date=2023-07-23|website=dailymed.nlm.nih.gov}}</ref><ref name=":1">{{Cite journal |last=Jacobson |first=Laura H. |last2=Callander |first2=Gabrielle E. |last3=Hoyer |first3=Daniel |date=2014-11 |title=Suvorexant for the treatment of insomnia |url=https://pubmed.ncbi.nlm.nih.gov/25318834/ |journal=Expert Review of Clinical Pharmacology |volume=7 |issue=6 |doi=10.1586/17512433.2014.966813 |issn=1751-2441 |pmid=25318834}}</ref><ref name=":2">{{Cite web|title=苏沃雷生[精二]_其他镇静催眠药_镇静药与催眠药_作用于神经系统的药物_湖南药事服务网|url=https://www.hnysfww.com/mobile/goods.php?id=733|access-date=2023-07-23|website=www.hnysfww.com}}</ref>苏沃雷生具有加速入睡、延长睡眠时间、减少半夜醒来次数以及提高睡眠质量的作用。<ref name=":0" /><ref name=":1" /><ref name=":3">{{Cite journal |last=Kuriyama |first=Akira |last2=Tabata |first2=Hiromitsu |date=2017-10 |title=Suvorexant for the treatment of primary insomnia: A systematic review and meta-analysis |url=https://pubmed.ncbi.nlm.nih.gov/28365447/ |journal=Sleep Medicine Reviews |volume=35 |doi=10.1016/j.smrv.2016.09.004 |issn=1532-2955 |pmid=28365447}}</ref>其药效中等，<ref>{{Cite web|title=Table 1: The Single Nucleotide Polymorphisms in cathepsin B protein mined from literature (PMID: 16492714).|url=http://dx.doi.org/10.7717/peerj.7425/table-1|access-date=2023-07-23|website=dx.doi.org}}</ref>与其他[[食欲素受体拮抗剂]]类似，但低于[[苯二氮䓬类|苯二氮卓类药物]]与[[Z-drugs|非苯二氮卓类药物]]。<ref>{{Cite journal |last=De Crescenzo |first=Franco |last2=D'Alò |first2=Gian Loreto |last3=Ostinelli |first3=Edoardo G |last4=Ciabattini |first4=Marco |last5=Di Franco |first5=Valeria |last6=Watanabe |first6=Norio |last7=Kurtulmus |first7=Ayse |last8=Tomlinson |first8=Anneka |last9=Mitrova |first9=Zuzana |last10=Foti |first10=Francesca |last11=Del Giovane |first11=Cinzia |date=2022-07 |title=Comparative effects of pharmacological interventions for the acute and long-term management of insomnia disorder in adults: a systematic review and network meta-analysis |url=https://linkinghub.elsevier.com/retrieve/pii/S0140673622008789 |journal=The Lancet |language=en |volume=400 |issue=10347 |doi=10.1016/S0140-6736(22)00878-9}}</ref>苏沃雷生的给药方式为口服给药。<ref name=":0" /><ref name=":1" /><ref name=":2" /><ref>{{Cite web|last=https://www.facebook.com/Drugscom|title=Generic Belsomra Availability|url=https://www.drugs.com/availability/generic-belsomra.html|access-date=2023-07-23|website=Drugs.com|language=en}}</ref>

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苏沃雷生的副作用包括[[嗜睡症|嗜睡]]、[[頭暈|头晕]]、[[白天嗜睡]]和[[镇静]]、[[頭痛|头痛]]、[[頭暈|头晕]]、[[梦境异常]]、[[口乾|口干]]和次日驾驶能力受损。<ref name=":0" /><ref name=":3" /><ref name=":4">{{Cite journal |last=Sutton |first=Eliza |date=2015-11 |title=Profile of suvorexant in the management of insomnia |url=https://www.dovepress.com/profile-of-suvorexant-in-the-management-of-insomnia-peer-reviewed-article-DDDT |journal=Drug Design, Development and Therapy |language=en |doi=10.2147/DDDT.S73224 |issn=1177-8881 |pmc=PMC4651361 |pmid=26648692}}</ref>偶见[[睡眠瘫痪症|睡眠麻痹]]，[[做梦异常]]与[[梦游症|梦游]]等复杂睡眠行为与出现[[自杀意念]]。<ref name=":0" /><ref name=":1" /><ref name=":4" />服用这种药物似乎不会产生明显的[[藥物耐受性|药物耐受性]]、[[药物依赖]]、[[藥物戒斷|戒断症状]]和[[反弹现象]]。<ref name=":0" /><ref>{{Cite journal |last=Keks |first=Nicholas A. |last2=Hope |first2=Judy |last3=Keogh |first3=Simone |date=2017-12 |title=Suvorexant: scientifically interesting, utility uncertain |url=https://pubmed.ncbi.nlm.nih.gov/28994603/ |journal=Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists |volume=25 |issue=6 |doi=10.1177/1039856217734677 |issn=1440-1665 |pmid=28994603}}</ref><ref>{{Cite journal |last=Muehlan |first=Clemens |last2=Vaillant |first2=Cedric |last3=Zenklusen |first3=Isabelle |last4=Kraehenbuehl |first4=Stephan |last5=Dingemanse |first5=Jasper |date=2020-11-01 |title=Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders |url=https://www.tandfonline.com/doi/full/10.1080/17425255.2020.1817380 |journal=Expert Opinion on Drug Metabolism & Toxicology |language=en |volume=16 |issue=11 |doi=10.1080/17425255.2020.1817380 |issn=1742-5255}}</ref>苏沃雷生是一种[[双重食欲素受体激动剂]]（DORA），选择性拮抗[[食欲素1型受体]]（Ox1R）和[[食欲素2型受体]]（Ox2R）。<ref name=":1" />该药物的达峰时间为2至3小时，清除半衰期为12小时。<ref name=":0" /><ref name=":1" />与苯二氮卓类药物与非苯二氮卓类药物不同的是，苏沃雷生并不会与 GABA 受体发生相互作用，而是通过其特殊的药理学机制发挥作用。<ref name=":1" /><ref>{{Cite journal |last=Atkin |first=Tobias |last2=Comai |first2=Stefano |last3=Gobbi |first3=Gabriella |date=2018-04 |title=Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery |url=https://pubmed.ncbi.nlm.nih.gov/29487083/ |journal=Pharmacological Reviews |volume=70 |issue=2 |doi=10.1124/pr.117.014381 |issn=1521-0081 |pmid=29487083}}</ref>

苏沃雷生的药物研发始于2006年，<ref>{{Cite journal |last=Preskorn |first=Sheldon H. |date=2014-11 |title=CNS Drug Development: Lessons from the Development of Ondansetron, Aprepitant, Ramelteon, Varenicline, Lorcaserin, and Suvorexant. Part I |url=https://journals.lww.com/practicalpsychiatry/Abstract/2014/11000/CNS_Drug_Development__Lessons_from_the_Development.6.aspx |journal=Journal of Psychiatric Practice® |language=en-US |volume=20 |issue=6 |doi=10.1097/01.pra.0000456594.66363.6f |issn=1527-4160}}</ref>并于2014年上市。<ref name=":0" />由于其潜在的滥用可能性，<ref name=":0" /><ref>{{Cite journal |last=Citrome |first=L. |date=2014-12 |title=Suvorexant for insomnia: a systematic review of the efficacy and safety profile for this newly approved hypnotic - what is the number needed to treat, number needed to harm and likelihood to be helped or harmed? |url=https://onlinelibrary.wiley.com/doi/10.1111/ijcp.12568 |journal=International Journal of Clinical Practice |language=en |volume=68 |issue=12 |doi=10.1111/ijcp.12568}}</ref>该药物在中国大陆被列为[[二类精神药品|第二类精神药品]]，<ref>{{Cite web|last=郝瑀然|title=国家药监局 公安部 国家卫生健康委关于调整麻醉药品和精神药品目录的公告_国务院部门文件_中国政府网|url=https://www.gov.cn/zhengce/zhengceku/2023-04/23/content_5752773.htm|access-date=2023-07-23|website=www.gov.cn}}</ref>在美国则被列为附表 IV 管控物质。<ref>{{Cite web|title=Federal Register :: Request Access|url=https://unblock.federalregister.gov/|access-date=2023-07-23|website=unblock.federalregister.gov}}</ref>在其他地方，如澳大利亚，苏沃雷生仅为处方药物而不受到管制。苏沃雷生暂无仿制药可用。<ref>{{Cite web|last=https://www.facebook.com/Drugscom|title=Generic Belsomra Availability|url=https://www.drugs.com/availability/generic-belsomra.html|access-date=2023-07-23|website=Drugs.com|language=en}}</ref><ref>{{Cite journal |last=Janto |first=Kayla |last2=Prichard |first2=J. Roxanne |last3=Pusalavidyasagar |first3=Snigdha |date=2018-08-15 |title=An Update on Dual Orexin Receptor Antagonists and Their Potential Role in Insomnia Therapeutics |url=http://jcsm.aasm.org/doi/10.5664/jcsm.7282 |journal=Journal of Clinical Sleep Medicine |language=en |volume=14 |issue=08 |doi=10.5664/jcsm.7282 |issn=1550-9389 |pmc=PMC6086961 |pmid=30092886}}</ref><ref>{{Cite journal |last=Janto |first=Kayla |last2=Prichard |first2=J. Roxanne |last3=Pusalavidyasagar |first3=Snigdha |date=2018-08-15 |title=An Update on Dual Orexin Receptor Antagonists and Their Potential Role in Insomnia Therapeutics |url=http://jcsm.aasm.org/doi/10.5664/jcsm.7282 |journal=Journal of Clinical Sleep Medicine |language=en |volume=14 |issue=08 |doi=10.5664/jcsm.7282 |issn=1550-9389 |pmc=PMC6086961 |pmid=30092886}}</ref>除苏沃雷生外，其他食欲素受体拮抗剂如[[达利雷生]]与[[莱博雷生]]亦已上市。<ref>{{Cite journal |last=Jacobson |first=Laura H. |last2=Hoyer |first2=Daniel |last3=Lecea |first3=Luis |date=2022-05 |title=Hypocretins (orexins): The ultimate translational neuropeptides |url=https://onlinelibrary.wiley.com/doi/10.1111/joim.13406 |journal=Journal of Internal Medicine |language=en |volume=291 |issue=5 |doi=10.1111/joim.13406 |issn=0954-6820}}</ref><ref>{{Cite journal |last=Markham |first=Anthony |date=2022-04 |title=Daridorexant: First Approval |url=https://link.springer.com/10.1007/s40265-022-01699-y |journal=Drugs |language=en |volume=82 |issue=5 |doi=10.1007/s40265-022-01699-y |issn=0012-6667 |pmc=PMC9042981 |pmid=35298826}}</ref>

== 医疗用途 ==
苏沃雷生的适应症为成人[[失眠症]]，主要用于入睡与睡眠维持困难的治疗。<ref name=":0" /><ref name=":1" /><ref name=":2" />

2023年7月23日 (日) 13:27的版本

苏沃雷生
臨床資料
其他名稱MK-4305; MK4305
AHFS/Drugs.comMonograph
MedlinePlusa614046
核准狀況
依賴性低
成癮性低
给药途径口服
藥物類別（英语：Drug class）食欲素受体激动剂; 催眠药; 镇定剂
ATC碼
法律規範狀態
法律規範
识别信息
  • [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone
CAS号1030377-33-3  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.210.546 編輯維基數據鏈接
化学信息
化学式C23H23ClN6O2
摩尔质量450.93 g·mol−1
3D模型（JSmol（英语：JSmol））
  • C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl
  • InChI=1S/C23H23ClN6O2/c1-15-3-5-20(30-25-8-9-26-30)18(13-15)22(31)29-12-11-28(10-7-16(29)2)23-27-19-14-17(24)4-6-21(19)32-23/h3-6,8-9,13-14,16H,7,10-12H2,1-2H3/t16-/m1/s1 checkY
  • Key:JYTNQNCOQXFQPK-MRXNPFEDSA-N checkY

苏沃雷生，品牌名Belsomra，是一种食欲素受体拮抗剂，被用于治疗失眠症，主要用于入睡或睡眠维持困难的成年患者的治疗。[3][4][5]苏沃雷生具有加速入睡、延长睡眠时间、减少半夜醒来次数以及提高睡眠质量的作用。[3][4][6]其药效中等，[7]与其他食欲素受体拮抗剂类似，但低于苯二氮卓类药物与非苯二氮卓类药物。[8]苏沃雷生的给药方式为口服给药。[3][4][5][9]

苏沃雷生的副作用包括嗜睡、头晕、白天嗜睡和镇静、头痛、头晕、梦境异常、口干和次日驾驶能力受损。[3][6][10]偶见睡眠麻痹，做梦异常与梦游等复杂睡眠行为与出现自杀意念。[3][4][10]服用这种药物似乎不会产生明显的药物耐受性、药物依赖、戒断症状和反弹现象。[3][11][12]苏沃雷生是一种双重食欲素受体激动剂（DORA），选择性拮抗食欲素1型受体（Ox1R）和食欲素2型受体（Ox2R）。[4]该药物的达峰时间为2至3小时，清除半衰期为12小时。[3][4]与苯二氮卓类药物与非苯二氮卓类药物不同的是，苏沃雷生并不会与 GABA 受体发生相互作用，而是通过其特殊的药理学机制发挥作用。[4][13]

苏沃雷生的药物研发始于2006年，[14]并于2014年上市。[3]由于其潜在的滥用可能性，[3][15]该药物在中国大陆被列为第二类精神药品，[16]在美国则被列为附表 IV 管控物质。[17]在其他地方，如澳大利亚，苏沃雷生仅为处方药物而不受到管制。苏沃雷生暂无仿制药可用。[18][19][20]除苏沃雷生外，其他食欲素受体拮抗剂如达利雷生与莱博雷生亦已上市。[21][22]

医疗用途

苏沃雷生的适应症为成人失眠症，主要用于入睡与睡眠维持困难的治疗。[3][4][5]

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