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选择性5-羟色胺再摄取抑制剂西酞普兰的临床及生化效应——抑郁症患者的剂量反应研究

Clinical and biochemical effects of citalopram, a selective 5-HT reuptake inhibitor--a dose-response study in depressed patients.

作者信息

Bjerkenstedt L, Edman G, Flyckt L, Hagenfeldt L, Sedvall G, Wiesel F A

出版信息

Psychopharmacology (Berl). 1985;87(3):253-9. doi: 10.1007/BF00432703.

Abstract

Citalopram is a bicyclic phtalane derivative. In animal experiments, citalopram has been demonstrated to possess a potent and highly selective inhibitory effect on serotonin reuptake. Several studies in man have indicated that citalopram given in daily doses of 40-60 mg has antidepressant properties and few side effects. The present double-blind study investigated the effects of three doses of citalopram (5 mg, 25 mg, and 50 mg) on depressive symptoms and various biochemical variables in 26 depressive patients. A significant reduction of the clinical ratings of depressive symptoms occurred at all dose levels. In endogenously depressed patients, a dose of 25 or 50 mg daily seemed to have the most pronounced antidepressive effect. The side effects were few and not related to dose level. A highly significant decrease in 5-HIAA in the CSF was found. MO-PEG in the CSF was also significantly decreased, while HVA in the CSF was increased. In addition, a significant decrease in the plasma concentrations of valine, leucine, tyrosine, and histidine was found. None of the biochemical effects was dose-dependent. The complex pattern of biochemical effects indicate that the amelioration of depressive symptoms might be related to effects of citalopram on central monoaminergic mechanisms and peripheral amino acid concentrations.

摘要

西酞普兰是一种双环邻苯二甲烷衍生物。在动物实验中,已证明西酞普兰对5-羟色胺再摄取具有强效且高度选择性的抑制作用。多项人体研究表明,每日服用40 - 60毫克西酞普兰具有抗抑郁特性且副作用较少。本双盲研究调查了三种剂量(5毫克、25毫克和50毫克)的西酞普兰对26名抑郁症患者抑郁症状及各种生化变量的影响。在所有剂量水平下,抑郁症状的临床评分均显著降低。在内源性抑郁症患者中,每日25毫克或50毫克的剂量似乎具有最显著的抗抑郁效果。副作用较少且与剂量水平无关。脑脊液中5-羟吲哚乙酸(5-HIAA)显著降低。脑脊液中的3-甲氧基-4-羟基苯乙二醇(MO-PEG)也显著降低,而脑脊液中的高香草酸(HVA)升高。此外,血浆中的缬氨酸、亮氨酸、酪氨酸和组氨酸浓度显著降低。这些生化效应均不呈剂量依赖性。生化效应的复杂模式表明,抑郁症状的改善可能与西酞普兰对中枢单胺能机制及外周氨基酸浓度的作用有关。

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