Providence Care Centre-Mental Health Services, Kingston, ON, Canada.
Psychopharmacology (Berl). 2009 Nov;207(1):27-34. doi: 10.1007/s00213-009-1633-1. Epub 2009 Aug 7.
Citalopram, a selective serotonin reuptake inhibitor, is used as a neuroendocrine probe in human subjects to assess serotonin function as reflected in prolactin and plasma cortisol release. Citalopram is a racemic mixture of equal proportions of the S(+) and R(-) enantiomers. Inhibition of serotonin reuptake and, consequently, antidepressant activity is associated, almost exclusively, with the S(+) enantiomer ("escitalopram"). Studies in animal models indicate that the presence of the R(-) isomer may interfere with the serotonin reuptake activity of escitalopram. The current study compared the neuroendocrine effects of citalopram and escitalopram in healthy human volunteers.
Plasma cortisol and prolactin levels following a single oral dose of citalopram (40 mg) or escitalopram (20 mg) were compared in samples taken every 15-30 min over a period of 240 min. Plasma citalopram concentration was determined at the same intervals.
Escitalopram and citalopram caused equivalent increases in plasma cortisol and prolactin. The administration of dexamethasone prior to the escitalopram challenge blocked the evoked increase in cortisol.
This is the first study to prove that a single dose of escitalopram acts centrally and not peripherally, providing further support of the use of oral escitalopram as a probe for brain serotonergic function.
西酞普兰是一种选择性 5-羟色胺再摄取抑制剂,被用作人体神经内分泌探针,以评估反映在催乳素和血浆皮质醇释放中的 5-羟色胺功能。西酞普兰是 S(+)和 R(-)对映体等比例的外消旋混合物。5-羟色胺再摄取的抑制作用,进而抗抑郁作用,几乎完全与 S(+)对映体(“艾司西酞普兰”)相关。动物模型研究表明,R(-)对映体的存在可能会干扰艾司西酞普兰的 5-羟色胺再摄取活性。本研究比较了西酞普兰和艾司西酞普兰在健康人类志愿者中的神经内分泌效应。
在 240 分钟的时间内,每隔 15-30 分钟采集一次样本,比较单次口服西酞普兰(40mg)或艾司西酞普兰(20mg)后血浆皮质醇和催乳素水平。同时在相同的时间间隔内测定血浆西酞普兰浓度。
艾司西酞普兰和西酞普兰引起血浆皮质醇和催乳素的同等增加。在艾司西酞普兰挑战前给予地塞米松可阻断皮质醇的诱发增加。
这是第一项证明单剂量艾司西酞普兰作用于中枢而不是外周的研究,进一步支持了口服艾司西酞普兰作为脑 5-羟色胺能功能探针的应用。