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的抗抑郁药。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-羟色胺和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。
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] |
|
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] |
|
左旋米那普倫 | Fetzima | 成人重度抑郁障碍 | 5-HT:NA NE:NA D:NA |
|
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
- ^ 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.
- ^ 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.
- ^ 3.0 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.