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雷美替胺
化合物 / 维基百科,自由的 encyclopedia
雷美替胺,商品名柔速瑞(Rozerem),是可治疗因难以入睡而失眠的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]
![]() | 此条目可参照英语维基百科相应条目来扩充。 (2024年1月26日) |
Quick Facts 临床资料, 商品名(英语:Drug nomenclature) ...
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临床资料 | |
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商品名(英语:Drug nomenclature) | Rozerem, others |
其他名称 | TAK-375 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a605038 |
核准状况 | |
依赖性 | 低[1] |
给药途径 | 口服 |
ATC码 | |
法律规范状态 | |
法律规范 | |
药物动力学数据 | |
生物利用度 | 1.8%[2] |
血浆蛋白结合率 | 82%(大多为白蛋白)[2] |
药物代谢 | 肝(CYP1A2,少部分由CYP2C(英语:CYP2C)与CYP3A4代谢)[2] |
代谢产物 | 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] |
排泄途径 | 尿液84%[2] 粪便4%[2] |
识别信息 | |
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CAS号 | 196597-26-9 ![]() |
PubChem CID | |
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DrugBank |
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ChEMBL | |
CompTox Dashboard(英语:CompTox Chemicals Dashboard) (EPA) | |
ECHA InfoCard | 100.215.666 ![]() |
化学信息 | |
化学式 | C16H21NO2 |
摩尔质量 | 259.35 g·mol−1 |
3D模型(JSmol(英语:JSmol)) | |
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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]它是褪黑激素的结构类似物,也是褪黑激素受体1A(英语:MT1 receptor)和褪黑激素受体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]它不是苯二氮䓬类或非苯二氮䓬类药物(英语:Z-drug),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
- 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
.
- Rozerem- ramelteon tablet, film coated. DailyMed. 2018-12-28 [2020-04-13]. (原始内容存档于2021-03-26).
- 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.
- 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
.
- 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.
- 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.
- 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
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- 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.
- 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).