评估疗效的临床研究的结果,安全性和耐受性的米氮平治疗抑郁症患者。
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福西特J,巴尔金RL
评估疗效的临床研究的结果,安全性和耐受性的米氮平治疗抑郁症患者。
J影响Disord。1998年12月,51 (3):267 - 85。
- PubMed ID
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10333982 (在PubMed]
- 文摘
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米氮平是一种突触前α2拮抗剂,具有双重作用通过增加去甲羟色胺神经传递。羟色胺神经传递的增强是专门通过5-HT1受体介导,因为米氮平是突触后血清素激活的5-HT2 5-HT3拮抗剂。此外,米氮平只有弱5-HT1受体亲和力,有很弱毒蕈碱的抗胆碱能和组胺拮抗剂(H1)属性。由于其独特的药效学特性,米氮平是一种有效、安全、良好的抗抑郁药物医疗设备。米氮平是口服后从胃肠道吸收,并广泛在肝脏代谢四通过脱甲基和羟基化代谢产物,其次是葡糖苷酸接合。的非结合的desmethyl代谢物比母体化合物药物不活跃。米氮平缺乏auto-induction肝同功酶。虽然米氮平是P450酶同功酶的底物1 a2, 2 d6和3 a4,体外研究表明,这不是一个有效的抑制剂或任何这些酶的诱导物。米氮平一直在评估全球临床发展项目涉及大约4500名患者。控制临床试验涉及近2800 mirtazapine-treated病人已经证明了复合moderate-to-serve抑郁症的治疗是有效的。 Mirtazapine was consistently superior to placebo, and equivalent in efficacy to the tricyclic antidepressants amitriptyline, doxepin and clomipramine, but with an improved tolerability profile. Mirtazapine has shown a rapid onset of action in patients with predominantly severe depressive illness in a comparative study against fluoxetine. Mirtazapine has a unique tolerability profile, since the specific postsynaptic 5-HT2 and 5-HT3 receptor blockade of mirtazapine provides early antidepressant effects without causing unwanted serotonin-related side-effects. Transient somnolence, hyperphagia and weight gain are the most commonly reported adverse events, which may be attributed to the antihistaminic (H1) activity of mirtazapine at low doses. Somnolence, the most commonly reported side-effect, appears to be less frequent at higher dosages. Mirtazapine also demonstrates important anxiolytic and sleep-improving effects, which may be related to its pharmacodynamic properties. In addition, mirtazapine does not appear to be associated with sexual dysfunction. Mirtazapine has shown no significant cardiovascular adverse effects at multiples of 7 to 22 times the maximum recommended dose. Mirtazapine is a unique addition to the antidepressant armamentarium as first-line therapy in patients with major depression and symptoms of anxiety/agitation or anxiety/somatization or complaints of insomnia and as a useful alternative in depressed patients who do not adequately respond to or are intolerant of tricyclic antidepressants or serotonin-specific reuptake inhibitors.
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