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[喹硫平治疗双相情感障碍]

[Quetiapin in bipolar disorders].

作者信息

Sümegi András

机构信息

Vas Megyei Markusovszky Kórház, Pszichiátriai Centrum.

出版信息

Neuropsychopharmacol Hung. 2008 Dec;10(5):281-91.

Abstract

Atypical antipsychotics are now widely used in the acute and long-term treatment in bipolar disorder. The role of atypical antipsychotics as acute agents, add-on medications; or as primary mood stabilizers in different phases of bipolar disorder is an important current research tendency. However, in bipolar disorder the mostly used indication of quetiapine is the management of acute manic phases, clinical data and the actual research results suggest that it may have both antidepressant and long-term antimanic effects. Quetiapine enhances the transmission of the central serotonergic networks, by its high antagonistic affinity for 5-HT(2A) and partial agonistic activity for the 5-HT(1A) receptors. The 5HT(1A) partial agonism causes an increase in the dopaminergic neurotransmission of the prefrontal cortex, and also, the affinity for the alpha 2-adrenoceptor brings a relative increase in extracellular noradrenergic release an tone in the prefrontal cortex. Latest research shows that quetiapine's main, active, human plasma metabolite, N-desalkyl quetiapine (norquetiapine), has a high inhibition affinity for the noradrenergic transporter. These data suggest that comparing to other atypical antipsychotics, norquetiapine may have a relatively strong antidepressant potential. Modifying the dopaminergic transmission by quetiapine's D2 receptor blocking activity results indirect mediating the cAMP-PKA and the arrestin-Akt-GSK-3 intracellular signal transduction pathways, which process may explain its long-term antimanic and mood stabilizing capability. Quetiapine's activity on nerve growth factors, histamine H1 receptor, proinflammatory networks may take an important additional part in its efficacy in bipolar depression. Its very fast dissociation from the D2 receptor is an important pharmakokinetic parameter for managing the optimal quetiapine dose in the daily clinical practice. This review tries to organize the actual information on quetiapine's multiplex activity in bipolar disorder.

摘要

非典型抗精神病药物目前广泛应用于双相情感障碍的急性期和长期治疗。非典型抗精神病药物作为急性期药物、辅助用药或双相情感障碍不同阶段的主要心境稳定剂,是当前重要的研究趋势。然而,在双相情感障碍中,喹硫平最常用的适应证是急性躁狂相的管理,临床数据和实际研究结果表明它可能具有抗抑郁和长期抗躁狂作用。喹硫平通过对5-HT(2A)具有高拮抗亲和力以及对5-HT(1A)受体具有部分激动活性,增强中枢5-羟色胺能网络的传递。5HT(1A)部分激动作用导致前额叶皮质多巴胺能神经传递增加,并且其对α2-肾上腺素能受体的亲和力使前额叶皮质细胞外去甲肾上腺素释放和张力相对增加。最新研究表明,喹硫平的主要活性人体血浆代谢物N-去烷基喹硫平(去甲喹硫平)对去甲肾上腺素能转运体具有高抑制亲和力。这些数据表明,与其他非典型抗精神病药物相比,去甲喹硫平可能具有相对较强的抗抑郁潜力。喹硫平的D2受体阻断活性改变多巴胺能传递,间接介导cAMP-PKA和抑制蛋白-Akt-GSK-3细胞内信号转导途径,这一过程可能解释其长期抗躁狂和心境稳定能力。喹硫平对神经生长因子、组胺H1受体、促炎网络的作用可能在其双相抑郁疗效中起重要的附加作用。其从D2受体的快速解离是在日常临床实践中管理最佳喹硫平剂量的重要药代动力学参数。本综述试图整理关于喹硫平在双相情感障碍中多重活性的实际信息。

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