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[奥匹哌醇更新内容]

[Update Opipramol].

作者信息

Gahr Maximilian, Hiemke Christoph, Connemann Bernhard J

机构信息

Klinik für Psychiatrie und Psychotherapie III, Universitätsklinikum Ulm.

Klinik für Psychiatrie und Psychotherapie, Universitätsklinikum Mainz.

出版信息

Fortschr Neurol Psychiatr. 2017 Mar;85(3):139-145. doi: 10.1055/s-0043-100762. Epub 2017 Mar 20.

Abstract

Opipramol was developed in the 1960s as an antidepressant and has chemical similarities with tricyclic antidepressants. Pharmacodynamic properties with absent reuptake inhibition of serotonin and noradrenaline and agonism at sigma receptors distinguish opipramol from tricyclics. Furthermore, antidepressive effects are smaller than the anxiolytic ones. The mechanism of action of opipramol is currently not sufficiently understood. Agonistic effects at sigma receptors have been linked with therapeutic effects. Excessive hepatic metabolism (primarily via CYP2D6) should be considered, particularly in patients with impaired hepatic function and polypharmacy. The available clinical data suggest good tolerability and safety within the approved dose range. Mild disturbances of vigilance and anticholinergic adverse events are the predominant side effects. In Germany, opipramol is approved for the treatment of somatoform disorders and generalized anxiety disorder, and there is sufficient evidence for the efficacy of opipramol in these disorders. The agent is still prescribed very often in Germany, yet plays a minor role in the clinical as well as scientific setting. In view of the limited availability of (pharmacologic) treatment options for generalized anxiety disorder and particularly somatoform disorders, opipramol should be considered in the treatment of these entities.

摘要

奥匹哌醇于20世纪60年代作为一种抗抑郁药被研发出来,与三环类抗抑郁药有化学相似性。奥匹哌醇与三环类药物的区别在于其不具备5-羟色胺和去甲肾上腺素再摄取抑制作用以及对σ受体的激动作用等药效学特性。此外,其抗抑郁作用小于抗焦虑作用。目前对奥匹哌醇的作用机制了解尚不充分。对σ受体的激动作用已被认为与治疗效果有关。应考虑到其肝代谢过度(主要通过CYP2D6)的情况,尤其是在肝功能受损和联合用药的患者中。现有临床数据表明在批准的剂量范围内其耐受性和安全性良好。主要的副作用是轻度的警觉性障碍和抗胆碱能不良事件。在德国,奥匹哌醇被批准用于治疗躯体形式障碍和广泛性焦虑症,且有充分证据证明其在这些疾病中的疗效。在德国,该药物的处方量仍然很大,但在临床和科研领域的作用较小。鉴于广泛性焦虑症尤其是躯体形式障碍的(药物)治疗选择有限,在治疗这些疾病时应考虑使用奥匹哌醇。

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