氯贝胺:治疗用途和临床研究。

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氯贝胺:治疗用途和临床研究。

中华神经外科杂志，2003 Spring;9(1):97-140。doi: 10.1111 / j.1527-3458.2003.tb00245.x。

PubMed ID

12595913 (PubMed视图

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摘要

莫氯贝胺是一种可逆性单胺氧化酶- a (RIMA)抑制剂，已广泛用于治疗各种抑郁症，在焦虑症中研究较少。几乎所有荟萃分析和大多数比较研究都表明，在抑郁症的急性治疗中，该药比安慰剂更有效，与三环(或一些杂环)抗抑郁药或选择性血清素再摄取抑制剂(SSRIs)一样有效。越来越多的证据表明，在治疗抑郁症亚型，如心境恶劣、内源性(单极性和双极性)、反应性、非典型、激动和迟发性抑郁症方面，氯贝胺并不不如其他抗抑郁药，因为与其他抗抑郁药相比，有限的证据表明，氯贝胺具有一致的长期疗效。然而，需要更多的对照研究来解决这个问题。对于双相抑郁症患者来说，使用氯贝胺出现躁狂的风险似乎并不比使用其他抗抑郁药高。在大多数急性期试验中，氯贝胺的有效治疗剂量范围为300 - 600 mg，分为2 - 3次。虽然一项对照试验和一项长期开放标签研究发现莫氯贝胺对社交恐惧症有效，但随后的三项对照试验显示要么没有效果，要么效果不佳，倾向于高剂量(600 - 900毫克/天)更有效。两项比较试验表明，莫氯贝胺对患有恐慌症的患者与氟西汀或氯丙咪嗪一样有效。然而，这一适应症的安慰剂对照试验仍然缺乏。氯贝胺的血药浓度与其疗效之间的关系不明显，但与不良事件呈正相关。 Dizziness, nausea and insomnia occurred more frequently on moclobemide than on placebo. Due to negligible anticholinergic and antihistaminic actions, moclobemide has been better tolerated than tri- or heterocyclic antidepressants. Gastrointestinal side effects and, especially, sexual dysfunction were much less frequent with moclobemide than with SSRIs. Unlike irreversible MAO-inhibitors, moclobemide has a negligible propensity to induce hypertensive crisis after ingestion of tyramine-rich food ("cheese-reaction"). Therefore, dietary restrictions are not as strict. However, with moclobemide doses above 900 mg/d the risk of interaction with ingested tyramine might become clinically relevant. After multiple dosing the oral bioavailability of moclobemide reaches almost 100%. At therapeutic doses, moclobemide lacks significant negative effects on psychomotor performance, cognitive function or cardiovascular system. Due to the relative freedom from these side effects, moclobemide is particularly attractive in the treatment of elderly patients. Moclobemide is a substrate of CYP2C19. Although it acts as an inhibitor of CYP1A2, CYP2C19, and CYP2D6, relatively few clinically important drug interactions involving moclobemide have been reported. It is relatively safe even in overdose. The drug has a short plasma elimination half-life that allows switching to an alternative agent within 24 h. Since it is well tolerated, therapeutic doses can often be reached rapidly upon onset of treatment. Steady-state plasma levels are reached approximately at one week following dose adjustment. Patients with renal dysfunction require no dose reduction in contrast to patients with severe hepatic impairment. Cases of refractory depression might improve with a combination of moclobemide with other antidepressants, such as clomipramine or a SSRI. Since this combination has rarely been associated with a potentially lethal serotonin syndrome, it requires lower entry doses, a slower dose titration and a more careful monitoring of patients. Combination therapy with moclobemide and other serotonergic agents, or opioids, should be undertaken with caution, although no serious adverse events have been published with therapeutic doses of moclobemide to date. On the basis of animal data the combined use of moclobemide with pethidine or dextropropoxyphene should be avoided. There is no evidence that moclobemide would increase body weight or produce seizures. Some preclinical data suggest that moclobemide may have anticonvulsant property.

引用本文的药物库数据

药物

Moclobemide

药物靶点

药物	目标	种类	生物	药理作用	行动
Moclobemide	胺氧化酶[含黄素]B	蛋白质	人类	未知的	拮抗剂	细节
Moclobemide	单胺氧化酶(蛋白质组)	蛋白质组	人类	未知的	拮抗剂	细节

食物相互作用

药物	交互
Moclobemide	避免含有酪胺的食物和补充剂。避免过量摄入酪胺(<100毫克)。含有酪胺的食物包括酸奶、陈年奶酪、熟透的香蕉、葡萄酒和酸面包。