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首页> 外文期刊>The journal of clinical psychiatry >Serotonergic and noradrenergic reuptake inhibitors: prediction of clinical effects from in vitro potencies.
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Serotonergic and noradrenergic reuptake inhibitors: prediction of clinical effects from in vitro potencies.

机译：血清素能和去甲肾上腺素再摄取抑制剂：从体外效力预测临床效果。

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This article reviews the pharmacology of antidepressants, particularly focusing on those that act acutely by blocking the reuptake of norepinephrine (NE) and/or serotonin (5-HT). Such drugs have a very wide range of potencies, measured in vitro, to inhibit the reuptake of these biogenic amines. As a group, the selective serotonin reuptake inhibitors (SSRIs) are the most potent at inhibiting the reuptake of 5-HT. Some tricyclic antidepressants (TCAs), such as desipramine and nortriptyline, are much more potent at blocking NE reuptake than 5-HT reuptake, as is the new non-TCA drug reboxetine. Among SSRIs, paroxetine is most potent at blocking the reuptake of NE. When considering whether such potencies measured in vitro translate into pharmacologic effects clinically, it is necessary to know how much drug gets to its site of therapeutic action, presumably the brain. Most, but not all, antidepressants are extensively bound to plasma proteins, and this binding limits considerably the penetration of these drugs across the blood-brain barrier. The amount of drug present in the extracellular fluid (ECF) of brain approximates the non-protein-bound drug concentration in plasma. Comparison of the concentration of antidepressants in ECF with their potencies to inhibit the reuptake of 5-HT and/or NE reveals why some drugs block the reuptake of these biogenic amines in either a selective or nonselective manner. This analysis reveals that venlafaxine may be unique among antidepressants in having a dose-dependent nonselectivity; at low doses it acts primarily as an SSRI, but at higher doses it inhibits the reuptake of NE as well.
机译：本文综述了抗抑郁药的药理作用，特别关注那些通过阻断去甲肾上腺素（NE）和/或5-羟色胺（5-HT）的再摄取而发挥急性作用的药物。这类药物在体外测量具有非常广泛的效力，可以抑制这些生物胺的再摄取。作为一个整体，选择性5-羟色胺再摄取抑制剂（SSRIs）在抑制5-HT再摄取方面最有效。某些三环抗抑郁药（TCA），如地昔帕明和去甲替林，与新的非TCA药物瑞波西汀相比，在阻止NE再摄取方面比5-HT再摄取更有效。在SSRIs中，帕罗西汀最能阻止NE的再摄取。在考虑这种在体外测量的效力是否在临床上转化为药理作用时，有必要知道多少药物可以到达其治疗作用部位，大概是大脑。大多数（但不是全部）抗抑郁药广泛结合血浆蛋白，这种结合大大限制了这些药物穿过血脑屏障的渗透。脑细胞外液（ECF）中存在的药物量近似于血浆中非蛋白质结合的药物浓度。将ECF中抗抑郁药的浓度与其抑制5-HT和/或NE的再吸收能力进行比较，揭示了为什么某些药物以选择性或​​非选择性方式阻止这些生物胺的再吸收。该分析表明，文拉法辛在抗抑郁药中可能具有独特的剂量依赖性非选择性。在低剂量时，它主要起SSRI的作用，但在高剂量时，它也抑制NE的再摄取。

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