乙琥胺

化合物

乙琥胺是治疗失神性癫痫英语Absence seizure的口服药物[4]。可以单独使用,也可以与其他抗癫痫药品英语Anticonvulsant(如:丙戊酸)并用[4]

Ethosuximide
临床资料
商品名英语Drug nomenclatureZarontin, others
AHFS/Drugs.comMonograph
MedlinePlusa682327
核准状况
怀孕分级
  • : D
给药途径口服(胶囊剂, 溶液)
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度93%[2]
药物代谢肝脏 (CYP3A4, CYP2E1英语CYP2E1)
生物半衰期53 小时
排泄途径 (20%)
识别信息
  • (RS)-3-Ethyl-3-methyl-pyrrolidine-2,5-dione
CAS号77-67-8  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.000.954 编辑维基数据链接
化学信息
化学式C7H11NO2
摩尔质量141.17 g·mol−1
3D模型(JSmol英语JSmol
手性外消旋体
熔点64至65 °C(147至149 °F)
  • O=C1NC(=O)CC1(C)CC
  • InChI=1S/C7H11NO2/c1-3-7(2)4-5(9)8-6(7)10/h3-4H2,1-2H3,(H,8,9,10) checkY
  • Key:HAPOVYFOVVWLRS-UHFFFAOYSA-N checkY

副作用一般很小[5]。常见的副作用包括食欲不振、腹痛、腹泻和疲倦[4]。严重的副作用包括自杀想法英语Suicidal ideation血球减少英语Cytopenia红斑狼疮[4] [5]。目前写的怀孕期或 3 岁以下的安全仍不清楚[4]。乙琥胺属于丁二酰亚胺类药物。确定的作用机转并不清楚[4]

乙琥胺于 1960 年在美国取得医疗许可[4]。名列世界卫生组织基本药物标准清单[6]。已有学名药流通于市[4]。截至 2004 年,世界上大多数地区都已普遍可得[7]。但至 2019 年,由于美国的统一定价英语Price fixing或价格操纵的问题,这个药物在许多国家的取得都受到限制[8] [9] [10]

参见

编辑


参考文献

编辑
  1. ^ List of nationally authorised medicinal products (PDF). European Medicines Agency. 
  2. ^ Patsalos PN. Properties of antiepileptic drugs in the treatment of idiopathic generalized epilepsies. Epilepsia. November 2005,. 46 Suppl 9 (s9): 140–8. PMID 16302888. S2CID 19462889. doi:10.1111/j.1528-1167.2005.00326.x . 
  3. ^ Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União英语Diário Oficial da União. 2023-03-31 (2023-04-04) [2023-08-16]. (原始内容存档于2023-08-03) (巴西葡萄牙语). 
  4. ^ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 4.7 Ethosuximide. The American Society of Health-System Pharmacists. [8 December 2016]. (原始内容存档于21 December 2016). 
  5. ^ 5.0 5.1 World Health Organization. WHO Model Formulary 2008. World Health Organization. 2009: 69, 74–75. ISBN 9789241547659. 
  6. ^ World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO. 
  7. ^ Shorvon, Simon; Perucca, Emilio; Fish, David; Dodson, W. E. The Treatment of Epilepsy. John Wiley & Sons. 2004: 147 [2020-03-30]. ISBN 978-0-470-75245-6. (原始内容存档于2021-08-28) (英语). 
  8. ^ Hempel, Georg. Methods of Therapeutic Drug Monitoring Including Pharmacogenetics. Elsevier. 2019: 241 [2020-04-05]. ISBN 978-0-444-64067-3. (原始内容存档于2021-08-28) (英语). 
  9. ^ Attorney General Tong leads 44-state coalition in antitrust lawsuit against Teva Pharmaceuticals, 19 other generic drug manufacturers, 15 individuals in conspiracy to fix prices and allocate markets for more than 100 different generic drugs (新闻稿). Office of the Attorney General of the State of Connecticut. 12 May 2019 [5 April 2020]. (原始内容存档于20 April 2020). 
  10. ^ States sue generic drug makers, claiming a conspiracy to fix prices. consumeraffairs.com. 14 May 2019 [5 April 2020]. (原始内容存档于25 April 2020) (英语).