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首页> 外文期刊>CNS drug reviews >The selective norepinephrine reuptake inhibitor antidepressant reboxetine: pharmacological and clinical profile.
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The selective norepinephrine reuptake inhibitor antidepressant reboxetine: pharmacological and clinical profile.

机译：选择性去甲肾上腺素再摄取抑制剂抗抑郁药瑞波西汀：药理和临床概况。

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Reboxetine is the first commercially available norepinephrine reuptake inhibitor developed specifically as a first line therapy for major depressive disorder. In vitro and in vivo pharmacological studies indicated that reboxetine methanesulphonate has high affinity and selectivity for the human norepinephrine transporter over the serotonin and dopamine transporters. Pharmacological specificity is further demonstrated by the absence of affinity for 45 transmitter receptors and CNS targets. Pharmacokinetic studies demonstrated that reboxetine is suitable for twice daily administration (8-10 mg/day) and that it exhibits minimal drug-drug interactions. The starting dose of reboxetine should be reduced in the elderly, in patients with renal or hepatic impairment, or in patients receiving potent CYP3A inhibitors. A total of 20 phase II/III clinical studies comprising placebo-controlled, active comparator-controlled and open-label uncontrolled studies in both short-term and long-term treatment of major depression have been conducted. In the treatment of major depression, reboxetine was superior to placebo in 5 of 12 short- or long-term placebo-controlled studies and was comparable in efficacy to active comparators in 3 out of 3 active-controlled studies. Unlike conventional tricyclic antidepressants (TCAs), reboxetine had only minimal sedative and cardiovascular liabilities, probably due to increased pharmacological specificity of reboxetine as compared with TCAs. Unlike serotonin reuptake inhibitors, this selective and specific norepinephrine reuptake inhibitor demonstrated a distinct side-effect profile with diminishing sexual dysfunction and GI side effects. The availability of this agent has afforded patients suffering from major depressive disorder a new class of agents to combat the debilitating consequence of this psychiatric disease. The demonstrated pharmacological specificity of this compound has provided the psychopharmacology community with a tool to elucidate the role of norepinephrine in brainfunctions. Testing this agent in different animal models has enabled the exploration of the role of modulation of norepinephrine tone in the therapy of CNS disorders beyond depression.
机译：瑞波西汀是第一种专门作为重度抑郁症的一线疗法而开发的去甲肾上腺素再摄取抑制剂。体外和体内药理研究表明，瑞波西汀甲磺酸盐对人去甲肾上腺素转运蛋白具有比5-羟色胺和多巴胺转运蛋白高的亲和力和选择性。尚无对45个递质受体和CNS靶标的亲和力进一步证明了药理学特异性。药代动力学研究表明，瑞波西汀适合每日两次给药（8-10毫克/天），并且其药物与药物的相互作用最小。老年人，肾或肝功能不全患者或接受强效CYP3A抑制剂的患者应降低瑞波西汀的起始剂量。总共进行了20项II / III期临床研究，包括在重大抑郁症的短期和长期治疗中进行的安慰剂对照，活性比较剂对照和开放标签非对照研究。在重度抑郁症的治疗中，瑞波西汀在12项短期或长期安慰剂对照研究中有5项优于安慰剂，并且在3项主动对照研究中有3项与活性比较药物相当。与常规三环类抗抑郁药（TCA）不同，瑞波西汀的镇静和心血管作用极低，这可能是由于瑞波西汀的药理学特异性高于三氯乙酸。与5-羟色胺再摄取抑制剂不同，这种选择性和特异性去甲肾上腺素再摄取抑制剂表现出独特的副作用，并减少了性功能障碍和胃肠道副作用。这种药物的可获得性为患有严重抑郁症的患者提供了新型的药物来对抗这种精神疾病的虚弱后果。该化合物的已证实的药理学特异性为心理药理学界提供了阐明去甲肾上腺素在脑功能中作用的工具。在不同的动物模型中测试该药物可以探索去甲肾上腺素基调在抑郁症以外的中枢神经系统疾病中的作用。

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