Kinney J L
Clin Pharm. 1985 Nov-Dec;4(6):625-36.
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage, and formulary recommendations for nomifensine maleate are reviewed. Nomifensine is a potent inhibitor of norepinephrine but has little effect on serotonin. It is unique in that it is a potent reuptake inhibitor of dopamine. Nomifensine is rapidly and completely absorbed and is widely distributed throughout the body. The major route of elimination is through the kidneys. Because of its short half-life and resultant lack of accumulation, nomifensine is usually given in divided doses. Nomifensine is approved for the treatment of depression. In clinical trials with imipramine, amitriptyline, nortriptyline, maprotiline, and various investigational antidepressant drugs, it has been found to be as effective as the standard antidepressant agents. In general, nomifensine has been well tolerated by patients and has caused few side effects. It also has not been associated with serious toxic effects in overdose situations. The usual effective dose of nomifensine maleate is 100-200 mg daily given in divided doses. It appears to be a good choice for patients with profoundly retarded depression and for those who cannot tolerate the side effects of traditional antidepressant drugs. Nomifensine should not be used alone in patients with schizoaffective disorders or in patients with agitated depression. Nomifensine is a safe and effective antidepressant with a fairly unique pharmacological profile. Because the drug is relatively safe and causes little sedation, it may offer substantial advantages over the more traditional antidepressants and should be considered for formulary addition.
本文综述了马来酸诺米芬辛的药理学、药代动力学、临床疗效、不良反应、药物相互作用、剂量及处方建议。诺米芬辛是去甲肾上腺素的强效抑制剂,但对血清素影响较小。其独特之处在于它是多巴胺的强效再摄取抑制剂。诺米芬辛吸收迅速且完全,广泛分布于全身。主要消除途径是通过肾脏。由于其半衰期短且无蓄积现象,诺米芬辛通常分剂量给药。诺米芬辛被批准用于治疗抑郁症。在与丙咪嗪、阿米替林、去甲替林、马普替林及各种研究性抗抑郁药物的临床试验中,发现它与标准抗抑郁药效果相当。总体而言,患者对诺米芬辛耐受性良好,副作用较少。在过量用药情况下也未发现严重毒性作用。马来酸诺米芬辛的常用有效剂量为每日100 - 200毫克,分剂量给药。对于重度迟发性抑郁症患者以及不能耐受传统抗抑郁药副作用的患者,它似乎是一个不错的选择。诺米芬辛不应单独用于分裂情感性障碍患者或伴有激越性抑郁的患者。诺米芬辛是一种安全有效的抗抑郁药,具有相当独特的药理学特性。由于该药物相对安全且几乎不引起镇静作用,与更传统的抗抑郁药相比可能具有显著优势,应考虑将其添加到处方集。