度洛西汀

度洛西汀(英語:,商品名为欣百达奥思平,是一种5-羟色胺和去甲肾上腺素再摄取抑制剂(SNRI),由礼来研发。度洛西汀常用来治疗重性抑郁障碍广泛性焦虑症纤维肌痛、各种躯体不适[1][2][3]度洛西汀常作为治疗躯体化障碍的首选药物。

度洛西汀
系统(IUPAC)命名名称
(+)-(S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(thiophen-2-yl)propan-1-amine
临床数据
商品名Cymbalta
Drugs.comMonograph
MedlinePlusa604030
医疗法规
妊娠分级
  • AU: B3
  • US: C (不排除有风险的可能)
给药途径Oral
合法狀態
合法状态
  • AU: 限医生处方 (S4)
  • CA: 处方药(-only)
  • UK: 处方药(-only) (POM)
  • US: 处方药(-only)
药代动力学数据
生物利用度~ 50% (32%至80%)
蛋白结合度~ 95%
代谢肝脏, 两种P450酶, CYP2D6CYP1A2
生物半衰期12.1 小时
排泄70% 尿液, 20% 粪便
识别
CAS注册号116539-59-4(free base)  N
136434-34-9盐酸盐
ATC代码N06AX21
PubChemCID 60835
IUPHAR/BPS202
DrugBankDB00476 
ChemSpider54822 
UNIIO5TNM5N07U 
KEGGD07880 
ChEBICHEBI:36795 
ChEMBLCHEMBL1175 
PDB配体ID29E (PDBe, RCSB PDB)
化学
化学式C18H19NOS
摩尔质量297.41456 g/mol

引用

  1. . Monograph. The American Society of Health-System Pharmacists. [2015-02-26].
  2. National Institute for Health and Clinical Excellence. Clinical guideline 96: Neuropathic pain - pharmacological management. London, 2010.
  3. Bril V, England J, Franklin GM; 等. . Neurology. 2011, Online (20): 1758–65. PMC 3100130. PMID 21482920. doi:10.1212/WNL.0b013e3182166ebe.
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