雷美替胺

化合物
(重定向自柔速瑞

雷美替胺,商品名柔速瑞(Rozerem),是可治疗因难以入睡而失眠褪黑激素受体激动剂英语melatonin agonist[2][4]它可减少入睡所需的时间,但临床益处较少。[5]它是口服药。[2]

雷美替胺
臨床資料
商品名英语Drug nomenclatureRozerem, others
其他名稱TAK-375
AHFS/Drugs.comMonograph
MedlinePlusa605038
核准狀況
依賴性[1]
给药途径口服
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度1.8%[2]
血漿蛋白結合率82%(大多为白蛋白[2]
药物代谢CYP1A2,少部分由CYP2C英语CYP2CCYP3A4代谢)[2]
代謝產物M-II(活性代谢产物[2]
生物半衰期雷美替胺:1–2.6小时[2]
M-II:2–5小时[2][3]
排泄途徑尿液84%[2]
粪便4%[2]
识别信息
  • (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]
    furan-8-yl)ethyl]propionamide
CAS号196597-26-9  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.215.666 編輯維基數據鏈接
化学信息
化学式C16H21NO2
摩尔质量259.35 g·mol−1
3D模型(JSmol英语JSmol
  • CCC(=O)NCC[C@@H]1CCc2ccc3c(c21)CCO3
  • InChI=1S/C16H21NO2/c1-2-15(18)17-9-7-12-4-3-11-5-6-14-13(16(11)12)8-10-19-14/h5-6,12H,2-4,7-10H2,1H3,(H,17,18)/t12-/m1/s1 checkY
  • Key:YLXDSYKOBKBWJQ-GFCCVEGCSA-N checkY

雷美替胺的副作用包括昏睡头晕疲劳恶心、失眠加剧、激素水平改变。[2]它是褪黑激素结构类似物,也是褪黑激素受体1A英语MT1 receptor褪黑激素受体1B英语MT2 receptor的选择性激动剂[2]雷美替胺的生物半衰期和药效持续时间都比褪黑激素长。[6]它不是苯二氮䓬类非苯二氮䓬类药物,不作用于GABA受体,有独特的作用机制[2][7]

雷美替胺于2002年发现,[8]2005年获批用于医药。[9]

参考资料

  1. ^ Kim, HK; Yang, KI. Melatonin and melatonergic drugs in sleep disorders.. Translational and clinical pharmacology. December 2022, 30 (4): 163–171. PMC 9810491 . PMID 36632077. doi:10.12793/tcp.2022.30.e21 . 
  2. ^ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 2.11 2.12 2.13 Rozerem- ramelteon tablet, film coated. DailyMed. 2018-12-28 [2020-04-13]. (原始内容存档于2021-03-26). 
  3. ^ Karim A, Tolbert D, Cao C. Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. Journal of Clinical Pharmacology. February 2006, 46 (2): 140–148. PMID 16432265. S2CID 38171735. doi:10.1177/0091270005283461. 
  4. ^ Neubauer DN. A review of ramelteon in the treatment of sleep disorders. Neuropsychiatric Disease and Treatment. February 2008, 4 (1): 69–79. PMC 2515902 . PMID 18728808. doi:10.2147/ndt.s483 . 
  5. ^ Kuriyama A, Honda M, Hayashino Y. Ramelteon for the treatment of insomnia in adults: a systematic review and meta-analysis. Sleep Medicine. April 2014, 15 (4): 385–392. PMID 24656909. doi:10.1016/j.sleep.2013.11.788. 
  6. ^ Hardeland R, Poeggeler B, Srinivasan V, Trakht I, Pandi-Perumal SR, Cardinali DP. Melatonergic drugs in clinical practice. Arzneimittel-Forschung. 2008, 58 (1): 1–10. PMID 18368944. S2CID 38857779. doi:10.1055/s-0031-1296459. 
  7. ^ Atkin T, Comai S, Gobbi G. Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery. Pharmacological Reviews. April 2018, 70 (2): 197–245. PMID 29487083. S2CID 3578916. doi:10.1124/pr.117.014381 . 
  8. ^ Uchikawa O, Fukatsu K, Tokunoh R, Kawada M, Matsumoto K, Imai Y, et al. Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists. Journal of Medicinal Chemistry. September 2002, 45 (19): 4222–4239. PMID 12213063. doi:10.1021/jm0201159. 
  9. ^ Drug Approval Package: Rozerem (Ramelteon) NDA #021782. U.S. Food and Drug Administration (FDA). 2005-10-20 [2020-04-13]. (原始内容存档于2021-03-31). 

外部链接

  • Ramelteon. Drug Information Portal. U.S. National Library of Medicine. [2024-01-26]. (原始内容存档于2019-06-28).