Moclobemide:治疗和临床研究使用。

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Moclobemide:治疗和临床研究使用。

中枢神经系统药物启2003弹簧;9 (1):97 - 140。doi: 10.1111 / j.1527-3458.2003.tb00245.x。

PubMed ID

12595913 (在PubMed

]

文摘

Moclobemide monoamine-oxidase-A的可逆抑制剂(裂缝)和被广泛评价治疗大范围的抑郁症和焦虑症的广泛研究。几乎所有的荟萃分析和最比较研究表明,急性抑郁症这种药物比安慰剂更有效的管理和有效的三环(或一些杂环)抗抑郁药物或选择性5 -羟色胺再摄取抑制剂(SSRIs)。有越来越多的证据表明,moclobemide不次于其他抗抑郁药治疗抑郁症的子类型,如心境恶劣,内生(单极和双极),反应性,非典型,激动,弱智抑郁与其他抗抑郁药有限的证据表明moclobemide一致的长期疗效。然而,更多的控制研究需要解决这个问题。双相抑郁患者患狂躁症的风险似乎不与其他抗抑郁药与moclobemide高于。有效治疗剂量范围moclobemide在大多数急性期试验是300到600毫克,分成2到3剂量。虽然一个对照试验和一个长期开放研究发现moclobemide是有效的在社交恐惧症,随后三个对照试验显示没有影响或少健壮的效果与高剂量的趋势(600 - 900 mg / d)更有效。两个对比试验证明moclobemide一样有效氟西汀和氯丙咪嗪患者患有恐慌症。安慰剂对照试验的迹象,然而,仍然缺乏。moclobemide的血浆浓度之间的关系及其治疗效果不明显,但与不良事件被发现正相关。 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.

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药物

Moclobemide

药物靶点

药物	目标	类	生物	药理作用	行动
Moclobemide	胺氧化酶(flavin-containing) 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tyramine-containing食物和补品。避免过度消费的酪胺(< 100毫克)。含有酪胺的食物包括酸奶、奶酪岁成熟的香蕉,酒,和酵母面包。