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吗氯贝胺。其药理特性与治疗用途的最新进展。

Moclobemide. An update of its pharmacological properties and therapeutic use.

作者信息

Fulton B, Benfield P

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1996 Sep;52(3):450-74. doi: 10.2165/00003495-199652030-00013.

Abstract

Unlike older monoamine oxidase inhibitors, which irreversibly and nonselectively bind monoamine oxidase (MAO), moclobemide is a reversible and selective inhibitor of the MAO-A isozyme. Moclobemide only weakly potentiates the pressor response induced by tyramine or other indirectly acting sympathomimetics; therefore, there is no need to avoid dietary tyramine or over-the-counter decongestants with moclobemide as there is with older MAO inhibitors. Recent clinical trials and meta-analyses have confirmed the efficacy of moclobemide in the treatment of depressive disorders. Moclobemide has been shown to have similar efficacy to tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs) and nonselective, irreversible MAO inhibitors. Long term follow-up studies of 6 to 12 months' duration have demonstrated that the antidepressant efficacy of moclobemide is maintained. Moclobemide, given alone or in combination with another antidepressant, has shown some efficacy in patients with refractory depression; however, comparative trials are required to confirm these findings. Data are also available to show clinical efficacy of moclobemide in the management of social phobia. Comparative studies have established that moclobemide is better tolerated at therapeutic dosages and has less toxicity in overdose than TCAs and nonselective, irreversible MAO inhibitors. Moclobemide lacks the anticholinergic, sedative and cardiovascular effects associated with many of the older antidepressants. Compared with SSRIs, moclobemide has a similar overall tolerability, although it tends to cause fewer gastrointestinal effects than the SSRIs and has not been reported to interfere with sexual function. In summary, recent data which confirm and extend its comparative therapeutic efficacy and low potential for adverse effects have established moclobemide as an effective treatment in depressive disorders. The drug is also effective in patients with a primary diagnosis of social phobia. Its lack of adverse anticholinergic, cardiovascular, cognitive and psychomotor effects makes moclobemide a particularly useful option in the elderly or patients with cardiac disease.

摘要

与不可逆且非选择性结合单胺氧化酶(MAO)的老式单胺氧化酶抑制剂不同,吗氯贝胺是MAO - A同工酶的可逆性选择性抑制剂。吗氯贝胺仅微弱增强酪胺或其他间接作用拟交感神经药诱导的升压反应;因此,与老式MAO抑制剂不同,使用吗氯贝胺时无需避免饮食中的酪胺或非处方减充血剂。近期的临床试验和荟萃分析已证实吗氯贝胺在治疗抑郁症方面的疗效。已表明吗氯贝胺与三环类抗抑郁药(TCA)、选择性5-羟色胺再摄取抑制剂(SSRI)及非选择性、不可逆MAO抑制剂具有相似疗效。为期6至12个月的长期随访研究表明,吗氯贝胺的抗抑郁疗效得以维持。吗氯贝胺单独使用或与另一种抗抑郁药联合使用,在难治性抑郁症患者中已显示出一定疗效;然而,需要进行对比试验来证实这些发现。也有数据表明吗氯贝胺在社交恐惧症治疗中具有临床疗效。对比研究证实,与TCA及非选择性、不可逆MAO抑制剂相比,吗氯贝胺在治疗剂量下耐受性更好,过量使用时毒性更低。吗氯贝胺缺乏许多老式抗抑郁药所具有的抗胆碱能、镇静及心血管作用。与SSRI相比,吗氯贝胺总体耐受性相似,尽管其引起的胃肠道效应往往比SSRI少,且未被报道会干扰性功能。总之,近期证实并扩展其对比治疗疗效及低不良反应可能性的数据已确立吗氯贝胺为抑郁症的有效治疗药物。该药物对初步诊断为社交恐惧症的患者也有效。其缺乏不良抗胆碱能、心血管、认知及精神运动效应,使吗氯贝胺成为老年患者或心脏病患者特别有用的选择。

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