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艾司氯胺酮

维基百科，自由的百科全书
艾司氯胺酮
臨床資料
商品名（英语：Drug nomenclature）Spravato, Ketanest, Spravado, others
其他名稱(S)-Ketamine; S(+)-Ketamine; JNJ-54135419
AHFS/Drugs.comMonograph
MedlinePlusa619017
核准狀況
懷孕分級
成癮性中等[4]
给药途径鼻腔给药, 靜脈注射[5]
藥物類別NMDA受体拮抗剂; 抗抑郁药; 全身麻醉药; 解离剂; 镇痛药
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度鼻內: 30–50%
生物半衰期5 小時
识别信息
  • (S)-2-(2-chlorophenyl)-2-(methylamino)cyclohexanone
CAS号33643-46-8  checkY
33643-47-9  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.242.065 編輯維基數據鏈接
化学信息
化学式C13H16ClNO
摩尔质量237.73 g·mol−1
3D模型（JSmol（英语：JSmol））
  • CN[C@]1(c2ccccc2Cl)CCCCC1=O
  • InChI=1S/C13H16ClNO/c1-15-13(9-5-4-8-12(13)16)10-6-2-3-7-11(10)14/h2-3,6-7,15H,4-5,8-9H2,1H3/t13-/m0/s1 ☒N
  • Key:YQEZLKZALYSWHR-ZDUSSCGKSA-N ☒N

艾司氯胺酮（INN：Esketamine）用于治療難治型抑鬱症（英语：Treatment-resistant depression）或伴有急性自殺意念的抑鬱症[12] [13]。然而，似乎不如氯胺酮有效[14]。也可用在麻醉和止痛[15]。有鼻腔喷雾剂或静脉注射剂等不同劑型[12] [15]。治療抑郁症時，疗效通常在 24 小时内显现[12]。

常见副作用包括解離、头晕、镇静、头痛、焦虑、呕吐和血压升高[12]。其他副作用包括可能發生物質濫用[13]。该化合物是氯胺酮的S (+)对映异构体[16]。不建议哺乳期使用[17]。它是一種NMDA受体拮抗剂，能阻断 N-甲基-D-天冬氨酸（NMDA）受体透過發揮作用[12]。

艾司氯胺酮于 1997 年在德国取得醫療使用許可[18] [19]。之後于 2019 年在美国和欧洲取得醫療使用許可[16] [20]。已有學名藥流通於市[21]。

参考文獻

[编辑]
  1. ^ 1.0 1.1 Spravato. Therapeutic Goods Administration (TGA). 17 March 2021 [8 September 2021]. （原始内容存档于9 September 2021）. 
  2. ^ 2.0 2.1 AusPAR: Esketamine hydrochloride. Therapeutic Goods Administration (TGA). 24 May 2021 [8 September 2021]. （原始内容存档于9 September 2021）. 
  3. ^ Updates to the Prescribing Medicines in Pregnancy database. Therapeutic Goods Administration (TGA). 12 May 2022 [13 May 2022]. （原始内容存档于3 April 2022）. 
  4. ^ Orsolini L, Salvi V, Volpe U. Craving and addictive potential of esketamine as side effects?. Expert Opinion on Drug Safety. June 2022, 21 (6): 803–812. PMID 35509224. doi:10.1080/14740338.2022.2071422. 
  5. ^ Himmelseher S, Pfenninger E. [The clinical use of S-(+)-ketamine--a determination of its place]. Anästhesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie. December 1998, 33 (12): 764–70. PMID 9893910. S2CID 259981872. doi:10.1055/s-2007-994851 （德语）. 
  6. ^ Regulatory Decision Summary - Spravato -. Health Canada. 23 October 2014 [5 June 2022]. （原始内容存档于6 June 2022）. 
  7. ^ Spravato 28 mg nasal spray, solution - Summary of Product Characteristics (SmPC). (emc). [24 November 2020]. （原始内容存档于28 August 2021）. 
  8. ^ Vesierra 25 mg/ml solution for injection/infusion - Summary of Product Characteristics (SmPC). (emc). 21 February 2020 [24 November 2020]. （原始内容存档于21 April 2021）. 
  9. ^ Spravato- esketamine hydrochloride solution. DailyMed. 6 August 2020 [26 September 2020]. （原始内容存档于18 March 2021）. 
  10. ^ Spravato EPAR. European Medicines Agency (EMA). 16 October 2019 [24 November 2020]. （原始内容存档于23 November 2020）. 
  11. ^ 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）. 31 March 2023 (4 April 2023) [16 August 2023]. （原始内容存档于3 August 2023） （巴西葡萄牙语）. 
  12. ^ 12.0 12.1 12.2 12.3 12.4 Esketamine Monograph for Professionals. Drugs.com. [23 July 2021]. （原始内容存档于23 January 2021） （英语）. 
  13. ^ 13.0 13.1 Spravato- esketamine hydrochloride solution. DailyMed. 6 August 2020 [26 September 2020]. （原始内容存档于18 March 2021）. 
  14. ^ Bahji, A; Vazquez, GH; Zarate CA, Jr. Erratum to "Comparative efficacy of racemic ketamine and esketamine for depression: a systematic review and meta-analysis" [Journal of Affective Disorders 278C (2021) 542-555].. Journal of affective disorders. 15 February 2021, 281: 1001. PMID 33229028. doi:10.1016/j.jad.2020.11.103. 
  15. ^ 15.0 15.1 BNF 80. BMJ Group and the Pharmaceutical Press. September 2020 - March 2021: 1411. ISBN 978-0-85711-369-6. 
  16. ^ 16.0 16.1 Commissioner, Office of the. FDA approves new nasal spray medication for treatment-resistant depression; available only at a certified doctor’s office or clinic. FDA. 24 March 2020 [23 July 2021]. （原始内容存档于23 July 2021） （英语）. 
  17. ^ Esketamine. Drugs and Lactation Database (LactMed) [Internet]. 2019. PMID 31038855. 
  18. ^ Roche, Victoria; Zito, William S.; Lemke, Thomas; Williams, David A. Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. 29 July 2019: PT1423 [23 July 2021]. ISBN 978-1-4963-8587-1. （原始内容存档于28 August 2021） （英语）. 
  19. ^ Himmelseher S, Pfenninger E. [The clinical use of S-(+)-ketamine--a determination of its place]. Anasthesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie. December 1998, 33 (12): 764–70. PMID 9893910. doi:10.1055/s-2007-994851. 
  20. ^ Spravato. [23 July 2021]. （原始内容存档于23 November 2020）. 
  21. ^ Ferrier, I. Nicol; Waite, Jonathan. The ECT Handbook. Cambridge University Press. 4 July 2019: 150 [23 July 2021]. ISBN 978-1-911623-16-8. （原始内容存档于29 August 2021） （英语）. 


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