Stahl精神药理学精要

1、1会计学Stahl精神药理学精要精神药理学精要影响选择抗抑郁药的相关因素主要抗抑郁药的作用机理疗效和不良反应特点和潜在优缺点5、2、3、4、1、 抗抑郁药使用现状 2021-12-143n各种所谓的“功能性疾病”中普遍应用美国成年人使用抗抑郁药约为1988年3倍抗抗郁药超过降压药成为美国最大的一类处方药2008年；抗抑郁药使用量增加了48%；2006年年1995-2002年2021-12-1452021-12-1462021-12-1472021-12-1482021-12-1492021-12-1410In addition to serotonin reuptake inhibition,

2、fluoxetine has norepinephrine reuptakeinhibition (NRI), CYP450 2D6 and 3A4inhibition, and serotonin 2C antagonistactions (5HT2C). Fluoxetines activatingeffects may be due to its actions atserotonin 2C receptors. Norepinephrinereuptake inhibition may be clinicallyrelevant only at very high doses.2021

3、-12-14112021-12-1412In addition to serotonin reuptake inhibition(SRI), paroxetine has mild anticholinergicactions (Ml), which can be calming orpossibly sedating, weak norepinephrinereuptake inhibition (NRI), which maycontribute to further antidepressantactions, and inhibition of the enzymenitric oxi

4、de synthetase (NOS), which maycontribute to sexual dysfunction. Paroxetine is also a potent inhibitor ofCYP450 2D6.2021-12-1413乳腺癌等疾病合并多种用药者2021-12-1414Fluvoxamines secondary propertiesinclude actions at sigma 1 receptors,which may be anxiolytic as well asbeneficial for psychotic depression, and inh

5、ibition of CYP450 1A2 and 3A4.2021-12-14152021-12-1416Sertraline: an SSRI with dopamine transporter (DAT) inhibitionSertraline has dopamine reuptakeinhibition (DRI) and sigma 1 receptorbinding in addition to serotonin reuptakeinhibition (SRI). The clinical relevance ofsertralines DRI is unknown, alt

6、hough itmay improve energy, motivation, andconcentration. Its sigma properties maycontribute to anxiolytic actions and mayalso be helpful in patients with psychoticdepression.2021-12-14172021-12-1418Citalopram consistsof two enantiomers, R and S.The R enantiomer has weakantihistamine properties and

7、isa weak inhibitor of CYP4502D6.2021-12-14192021-12-14202021-12-14212021-12-14222021-12-14232021-12-1424Venlafaxine inhibits reuptake of bothserotonin (SRI) and norepinephrine(NRI), thus combining two therapeuticmechanisms in one agent. Venlafaxinesserotonergic actions are present at lowdoses, while

8、 its noradrenergic actionsare progressively enhanced as doseincreases.2021-12-14252021-12-1426bupropion2021-12-14272021-12-1428Reboxetine and atomoxetine are two antidepressants that have selective actions at the norepinephrine reuptake inhibitor (NRI).2021-12-14292021-12-1430NaSSAMirtazapine is som

9、etimes called anoradrenergic and specificserotonergic antidepressant(NaSSA). Its primary therapeutic action is alpha 2antagonism, as shown in Figures 12-51 through 12-54. It also blocks threeserotonin (5HT) receptors: 5HT2A, 5HT2C, and 5HT3.Finally, it blocks histamine 1(HI) receptors.2021-12-143120

10、21-12-14322021-12-14332021-12-14352021-12-1436In addition to serotonin reuptake inhibition,fluoxetine has norepinephrine reuptakeinhibition (NRI), CYP450 2D6 and 3A4inhibition, and serotonin 2C antagonistactions (5HT2C). Fluoxetines activatingeffects may be due to its actions atserotonin 2C receptor

11、s. Norepinephrinereuptake inhibition may be clinicallyrelevant only at very high doses.2021-12-1437In addition to serotonin reuptake inhibition(SRI), paroxetine has mild anticholinergicactions (Ml), which can be calming orpossibly sedating, weak norepinephrinereuptake inhibition (NRI), which maycontribute to further antidepressantactions, an