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5-羟色胺和去甲肾上腺素再摄取抑制剂

5-羟色胺和去甲肾上腺素再摄取抑制剂(英語:SNRIs, Serotonin–norepinephrine reuptake inhibitors),是一种用来治疗重度抑郁症和其他精神障碍抗抑郁药。SNRI有时候也用来治疗焦虑症强迫症多动症,慢性神经性疼痛,躯体化障碍,纤维肌痛综合征和缓解更年期症状。

SNRI是高效的5-羟色胺去甲肾上腺素再摄取抑制剂。[1]已知这些神经递质在控制情绪时发挥着重要的作用。 SNRI比使用更广泛但只能单独作用于5-羟色胺的选择性5-羟色胺再摄取抑制剂(SSRI)作用更多。

Timeline-SNRIs-2010
已批准的SNRI时间线图
活性成分 药品名称 治疗用途 受体亲和力
(Ki, nm)
结构
文拉法辛(Venlafaxine) 怡诺思(Efexor) 重性抑郁障碍,包括对其他治疗没反应的患者,广泛性焦虑症慢性疼痛综合症[2] 5-HT:7.8
NE:1920
D:6050 [3]
米那普仑(Milnacipran) Savella, Ixel, Dalcipran, Toledomin 纤维肌痛综合征及其并发症,重度抑郁障碍[4] 5-HT:8.4
NE:22
D:>100000[3]
Milnacipran
Milnacipran
度洛西汀(Duloxetine) Cymbalta, Ariclaim, Xeristar, Yentreve 重度抑郁障碍和纤维肌痛综合征[5] 5-HT:0.07
NE:1.2
D:230[3]
Duloxetine
Duloxetine
左旋米那普倫 Fetzima 成人重度抑郁障碍 5-HT:NA
NE:NA
D:NA
Levomilnacipran
Levomilnacipran
去甲文拉法辛(Desvenlafaxine) Pristiq 成人重度抑郁障碍[6] 5-HT:61.4
NE:2953
D:NA
西布曲明(Sibutramine) Meridia, Reductil 肥胖[7] 5-HT:298
NE:5451
D:943

5-HT: 5-羟色胺- NE: 去甲肾上腺素- D: 多巴胺- NA: 不可用

引用

  1. ^ Cashman, JR; Ghirmai, S. Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorganic & Medicinal Chemistry. 2009, 17 (19): 6890–7. PMID 19740668. doi:10.1016/j.bmc.2009.08.025. 
  2. ^ Gutierrez, MA; Stimmel, GL; Aiso, JY. Venlafaxine: A 2003 update. Clinical Therapeutics. 2003, 25 (8): 2138–54. PMID 14512125. doi:10.1016/s0149-2918(03)80210-2. 
  3. ^ 3.0 3.1 3.2 Stahl, SM; Grady, MM; Moret, C; Briley, M. SNRIs: Their pharmacology, clinical efficacy, and tolerability in comparison with other classes of antidepressants. CNS Spectrums. 2005, 10 (9): 732–47. PMID 16142213. 
  4. ^ Morishita, Shigeru; Arita, Seizaburo. The clinical use of milnacipran for depression. European Psychiatry. 2003, 18 (1): 34–5. PMID 12648895. doi:10.1016/S0924-9338(02)00003-2. 
  5. ^ Hunziker, ME; Suehs, BT; Bettinger, TL; Crismon, ML. Duloxetine hydrochloride: A new dual-acting medication for the treatment of major depressive disorder. Clinical Therapeutics. 2005, 27 (8): 1126–43. PMID 16199241. doi:10.1016/j.clinthera.2005.08.010. 
  6. ^ Perry, R; Cassagnol, M. Desvenlafaxine: A new serotonin-norepinephrine reuptake inhibitor for the treatment of adults with major depressive disorder. Clinical Therapeutics. 2009, 31 (1): 1374–404. PMID 19698900. doi:10.1016/j.clinthera.2009.07.012. 
  7. ^ Luque, CA; Rey, JA. The discovery and status of sibutramine as an anti-obesity drug. European Journal of Pharmacology. 2002, 440 (2–3): 119–28. PMID 12007530. doi:10.1016/S0014-2999(02)01423-1. 
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