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苏沃雷生:修订间差异

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2023年7月23日 (日) 12:15的版本

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。[1][2][3]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。[1][2][4]其药效中等,[5]与其他食欲素受体拮抗剂类似,但低于苯二氮卓类药物非苯二氮卓类药物[6]苏沃雷生的给药方式为口服给药。[1][2][3][7]

苏沃雷生的副作用包括嗜睡头晕白天嗜睡镇静头痛头晕梦境异常口干和次日驾驶能力受损。[1][4][8]偶见睡眠麻痹做梦异常梦游等复杂睡眠行为与出现自杀意念[1][2][8]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反弹现象[1][9][10]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)。[2]该药物的达峰时间为2至3小时,清除半衰期为12小时。[1][2]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。[2][11]

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
成癮性
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
  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 DailyMed - BELSOMRA- suvorexant tablet, film coated. dailymed.nlm.nih.gov. [2023-07-23]. 
  2. ^ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 Jacobson, Laura H.; Callander, Gabrielle E.; Hoyer, Daniel. Suvorexant for the treatment of insomnia. Expert Review of Clinical Pharmacology. 2014-11, 7 (6). ISSN 1751-2441. PMID 25318834. doi:10.1586/17512433.2014.966813. 
  3. ^ 3.0 3.1 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. www.hnysfww.com. [2023-07-23]. 
  4. ^ 4.0 4.1 Kuriyama, Akira; Tabata, Hiromitsu. Suvorexant for the treatment of primary insomnia: A systematic review and meta-analysis. Sleep Medicine Reviews. 2017-10, 35. ISSN 1532-2955. PMID 28365447. doi:10.1016/j.smrv.2016.09.004. 
  5. ^ Table 1: The Single Nucleotide Polymorphisms in cathepsin B protein mined from literature (PMID: 16492714).. dx.doi.org. [2023-07-23]. 
  6. ^ De Crescenzo, Franco; D'Alò, Gian Loreto; Ostinelli, Edoardo G; Ciabattini, Marco; Di Franco, Valeria; Watanabe, Norio; Kurtulmus, Ayse; Tomlinson, Anneka; Mitrova, Zuzana; Foti, Francesca; Del Giovane, Cinzia. Comparative effects of pharmacological interventions for the acute and long-term management of insomnia disorder in adults: a systematic review and network meta-analysis. The Lancet. 2022-07, 400 (10347). doi:10.1016/S0140-6736(22)00878-9 (英语). 
  7. ^ https://www.facebook.com/Drugscom. Generic Belsomra Availability. Drugs.com. [2023-07-23] (英语). 
  8. ^ 8.0 8.1 Sutton, Eliza. Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy. 2015-11. ISSN 1177-8881. PMC 4651361可免费查阅. PMID 26648692. doi:10.2147/DDDT.S73224 (英语). 
  9. ^ Keks, Nicholas A.; Hope, Judy; Keogh, Simone. Suvorexant: scientifically interesting, utility uncertain. Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists. 2017-12, 25 (6). ISSN 1440-1665. PMID 28994603. doi:10.1177/1039856217734677. 
  10. ^ Muehlan, Clemens; Vaillant, Cedric; Zenklusen, Isabelle; Kraehenbuehl, Stephan; Dingemanse, Jasper. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opinion on Drug Metabolism & Toxicology. 2020-11-01, 16 (11). ISSN 1742-5255. doi:10.1080/17425255.2020.1817380 (英语). 
  11. ^ Atkin, Tobias; Comai, Stefano; Gobbi, Gabriella. Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery. Pharmacological Reviews. 2018-04, 70 (2). ISSN 1521-0081. PMID 29487083. doi:10.1124/pr.117.014381. 
  12. ^ cite web | title=Prescription medicines: registration of new chemical entities in Australia, 2016 | website=Therapeutic Goods Administration (TGA) | date=21 June 2022 |}
  13. ^ Prescription medicines: registration of new chemical entities in Australia, 2016. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023].