利右苯丙胺

化合物

利右苯丙胺INNlisdexamfetamine),也叫赖氨酸安非他命,品牌名VyvanseElvanse,中枢神经系统(CNS)兴奋剂右苯丙胺前体药物,为一种苯丙胺类英语substituted amphetamine苯乙胺衍生物,即右旋安非他命和赖氨酸形成的酰胺[4][5][6]该药品被用于治疗青少年及成年人的注意缺陷多动障碍(ADHD)以及成人的中重度暴食症,其给药方式为口服给药,药效通常在两个小时之内启动而能维持长达14个小时。[7]根据英国NCIE的意见,利右苯丙胺可作为二线药物,用于治疗在予足量哌甲酯6周后,在减少ADHD症状和相关损害方面没有获得足够的益处的6-17岁ADHD患者。[8]

利右苯丙胺
临床资料
其他名称Vyvanse
AHFS/Drugs.comMonograph
MedlinePlusa607047
核准状况
怀孕分级
依赖性身体依赖: 无
精神依赖: 中等
成瘾性中等
给药途径口服(胶囊
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度96.4%[1]
药物代谢起初由红血球水解
余下的代谢过程同安非他命#药物代谢动力学
药效起始时间英语Onset of action2小时[2][3]
生物半衰期≤1小时(前体药物分子)
9至11小时(右旋安非他命)
作用时间12 hours[2][3]
排泄途径肾脏:约2%
识别信息
  • (2S)-2,6-diamino-N-[(2S)-1-phenylpropan-2-yl]hexanamide
CAS号608137-32-2  checkY[IUPHAR]
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C15H25N3O
摩尔质量263.39 g·mol−1
3D模型(JSmol英语JSmol
  • O=C(N[C@H](Cc1ccccc1)C)[C@@H](N)CCCCN
  • InChI=1S/C15H25N3O/c1-12(11-13-7-3-2-4-8-13)18-15(19)14(17)9-5-6-10-16/h2-4,7-8,12,14H,5-6,9-11,16-17H2,1H3,(H,18,19)/t12-,14-/m0/s1 checkY
  • Key:VOBHXZCDAVEXEY-JSGCOSHPSA-N checkY
30毫克Vyvanse胶囊

赖右苯丙胺的常见副作用包括食欲不振、焦虑、腹泻、失眠、易怒和恶心。[9]

参考资料

编辑
  1. ^ Public Assessment Report Decentralised Procedure (PDF). Shire Pharmaceuticals Contracts Limited: 14. [2014-08-23]. (原始内容存档 (PDF)于2014-08-26). 
  2. ^ 2.0 2.1 Millichap JG. Chapter 9: Medications for ADHD. Millichap JG (编). Attention Deficit Hyperactivity Disorder Handbook: A Physician's Guide to ADHD 2nd. New York, USA: Springer. 2010: 112. ISBN 9781441913968.
    Table 9.2 Dextroamphetamine formulations of stimulant medication
    Dexedrine [Peak:2–3 h] [Duration:5–6 h] ...
    Adderall [Peak:2–3 h] [Duration:5–7 h]
    Dexedrine spansules [Peak:7–8 h] [Duration:12 h] ...
    Adderall XR [Peak:7–8 h] [Duration:12 h]
    Vyvanse [Peak:3–4 h] [Duration:12 h]
     
  3. ^ 3.0 3.1 Brams, Matthew; Mao, Alice R.; Doyle, Robert L. Onset of Efficacy of Long-Acting Psychostimulants in Pediatric Attention-Deficit/Hyperactivity Disorder. Postgraduate Medicine. 2008-01, 120 (3): 69–88. ISSN 0032-5481. PMID 18824827. doi:10.3810/pgm.2008.09.1909 (英语). Onset of efficacy was earliest for d-MPH-ER at 0.5 hours, followed by d, l-MPH-LA at 1 to 2 hours, MCD at 1.5 hours, d, l-MPH-OR at 1 to 2 hours, MAS-XR at 1.5 to 2 hours, MTS at 2 hours, and LDX at approximately 2 hours. ... MAS-XR, and LDX have a long duration of action at 12 hours postdose 
  4. ^ Details about INN Request 8690. extranet.who.int. [2024-06-07]. (原始内容存档于2024-06-07). 
  5. ^ Vyvanse Prescribing Information (PDF). United States Food and Drug Administration. Shire US Inc. January 2015 [2015-02-24]. (原始内容存档 (PDF)于2015-02-25). 
  6. ^ Heal, David J; Smith, Sharon L; Gosden, Jane; Nutt, David J. Amphetamine, past and present – a pharmacological and clinical perspective. Journal of Psychopharmacology. 2013-06, 27 (6): 479–496 [2022-05-09]. ISSN 0269-8811. PMC 3666194 . PMID 23539642. doi:10.1177/0269881113482532. (原始内容存档于2022-01-05) (英语). 
  7. ^ Lisdexamfetamine Monograph for Professionals. Drugs.com. [2024-06-07]. (原始内容存档于2024-06-19) (英语). 
  8. ^ Recommendations | Attention deficit hyperactivity disorder: diagnosis and management | Guidance | NICE. www.nice.org.uk. 2018-03-14 [2024-06-07]. (原始内容存档于2018-10-04). 
  9. ^ Lisdexamfetamine Monograph for Professionals. Drugs.com. [2024-11-14] (英语).