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舒马曲普坦

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舒马曲普坦
Sumatriptan molecule
臨床資料
商品名英语Drug nomenclatureImitrex, Imigran ,Treximet
AHFS/Drugs.comMonograph
核准狀況
懷孕分級
  • C
给药途径tablet, subcutaneous injection, nasal spray
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度15% (oral)/ 96% (s.c)
血漿蛋白結合率14%-21%
药物代谢MAO
生物半衰期2.5 hours
排泄途徑60% urine; 40% feces
识别信息
  • 1-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]- N-methyl-methanesulfonamide
CAS号103628-46-2  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.130.518 編輯維基數據鏈接
化学信息
化学式C14H21N3O2S
摩尔质量295.40 g·mol−1
3D模型(JSmol英语JSmol
  • O=S(=O)(NC)Cc1cc2c(cc1)ncc2CCN(C)C
  • InChI=1S/C14H21N3O2S/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3/h4-5,8-9,15-16H,6-7,10H2,1-3H3 checkY
  • Key:KQKPFRSPSRPDEB-UHFFFAOYSA-N checkY

舒马曲普坦[1]INN:sumatriptan)又译舒马普坦舒马曲坦 ,是一种曲普坦类药物(triptans)[2][3][4],为血清素 5-HT1B/1D/1F 受体激动剂[5][6],用于缓解偏頭痛丛集性头痛[7]。曲普坦类选择性作用于颅内血管和三叉神经的感觉纤维,造成血管收缩和抑制三叉神经活性[8][9]

在结构上,舒马曲普坦和蟾毒色胺5-甲氧基二甲基色胺一样是一种生物碱——二甲基色胺DMT)的衍生物,其特点是二甲基N-乙酰基团连在吲哚环的5号位C上[10]

许多制药工厂都有生产舒马曲普坦,并以不同商品名出售,比如舒马普坦(Sumatriptan)、英明格(Imigran)、Imitrex、Treximet等等。

参考文献

[编辑]
  1. ^ 黄世杰.舒马曲普坦鼻粉剂用于治疗有或无预兆的偏头痛[J].国际药学研究杂志, 2016, 43(2):1.DOI:CNKI:SUN:GWYZ.0.2016-02-027.
  2. ^ 中国医师协会神经内科医师分会,中国研究型医院学会头痛与感觉障碍专业委员会,董钊,等.中国偏头痛诊治指南(2022版)[J].中国疼痛医学杂志, 2022, 28(12):881-898. [1]
  3. ^ Jerry W. Swanson; Manjit Matharu. Migraine Management. Elsevier. 2024: 24. ISBN 9780128234815. 
  4. ^ Tepper SJ, Jenkins A, Henriksen C, Dai F, Atkinson J, Abraham L, Gendolla A. A comparison of the persistence of acute treatment with rimegepant versus oral triptans in patients with migraine: A retrospective analysis of US claims data. Cephalalgia. 2025 Jul;45(7):3331024251352849. doi: 10.1177/03331024251352849. Epub 2025 Jul 27. PMID: 40717449.
  5. ^ Syed YY. Sumatriptan/Naproxen Sodium: A Review in Migraine. Drugs. January 2016, 76 (1): 111–121. PMID 26628293. S2CID 25060147. doi:10.1007/s40265-015-0521-8. 
  6. ^ Rubio-Beltrán E, Labastida-Ramírez A, Villalón CM, MaassenVanDenBrink A. Is selective 5-HT1F receptor agonism an entity apart from that of the triptans in antimigraine therapy?. Pharmacol Ther. June 2018, 186: 88–97. PMID 29352859. doi:10.1016/j.pharmthera.2018.01.005. hdl:1765/104159可免费查阅. 
  7. ^ Derry CJ, Derry S, Moore RA. Sumatriptan (all routes of administration) for acute migraine attacks in adults - overview of Cochrane reviews. The Cochrane Database of Systematic Reviews. May 2014, 2014 (5): CD009108. PMC 6469574可免费查阅. PMID 24865446. doi:10.1002/14651858.CD009108.pub2. 
  8. ^ Gawel MJ. The new triptans. Can J Clin Pharmacol. 1999 Autumn;6 Suppl A:20A-4A. PMID: 10494008.
  9. ^ Tepper SJ, Rapoport AM, Sheftell FD. Mechanisms of action of the 5-HT1B/1D receptor agonists. Arch Neurol. 2002 Jul;59(7):1084-8. doi: 10.1001/archneur.59.7.1084. PMID: 12117355.
  10. ^ The presence of the sulfonamide group in the molecule does not make sumatriptan a "sulfa drug", since it does not have any anti-microbial properties.