Peck A W, Bye C E, Clubley M, Henson T, Riddington C
Br J Clin Pharmacol. 1979 May;7(5):469-78. doi: 10.1111/j.1365-2125.1979.tb00988.x.
The effects of bupropion, a potential antidepressant drug, has been investigated in twelve healthy subjects, (six men and six women) in a double-blind controlled, balanced study, and compared with dexamphetamine and amitriptyline. Analysis of variance was used to assess significance of differences with < 0.05 taken as significant. Bupropion 50 and 100 mg (HCl) failed to differ from lactose on any of the measures of performance tested. By contrast amitriptyline 25 mg (base) impaired auditory vigilance, tapping rate, and short term memory and prolonged auditory reaction time. Dexamphetamine 10 mg improved auditory vigilance and tapping rates and dexamphetamine 5 mg produced similar trends. Bupropion did not differ from lactose on heart rate, pupil size and salivary secretion. Amitriptyline produced miosis and dexamphetamine 10 mg mydriasis and increased heart rate. Dexamphetamine 10 mg increased systolic blood pressure (BP) when taken erect and supine. Supine systolic BP was increased, compared with lactose, after all treatments except bupropion 50 mg, possibly due to a spuriously low mean after lactose. These changes were not seen when standing and no changes ascribable to treatments were recorded in diastolic BP. No changes in the electroencephalogram (EEG) occurred after bupropion or dexamphetamine. Amitriptyline increased activity in the delta band (2.3-4 Hz) and decreased in the alpha band (7.5-13.5 Hz). Bupropion produced no changes in subjective ratings measured with visual analogue scales. Amitriptyline produced drowsiness, sedation and physical impairment, whereas dexamphetamine increased alertness and produced elation and increased sociability. No side effects could be ascribed to bupropion with any certainty. It was concluded that bupropion differs in its pharmacodynamic properties from both dexamphetamine and amitriptyline. At the doses examined the drug is devoid of stimulant and sedative properties. In addition, no cardiovascular or anticholinergic effects occurred and in view of these potential advantages over available antidepressant drugs, further clinical studies are in progress.
在一项双盲对照、均衡的研究中,对12名健康受试者(6名男性和6名女性)进行了潜在抗抑郁药物安非他酮的效果研究,并与右旋苯丙胺和阿米替林进行了比较。采用方差分析来评估差异的显著性,以P<0.05为有显著性差异。安非他酮50毫克和100毫克(盐酸盐)在任何一项测试的性能指标上与乳糖均无差异。相比之下,25毫克(碱基)的阿米替林损害了听觉警觉性、敲击速度和短期记忆,并延长了听觉反应时间。10毫克的右旋苯丙胺提高了听觉警觉性和敲击速度,5毫克的右旋苯丙胺也有类似趋势。安非他酮在心率、瞳孔大小和唾液分泌方面与乳糖无差异。阿米替林导致瞳孔缩小,10毫克的右旋苯丙胺导致瞳孔散大并使心率增加。10毫克的右旋苯丙胺在直立和仰卧时均使收缩压升高。除50毫克安非他酮外,所有治疗后仰卧收缩压均较乳糖组升高,这可能是由于乳糖组的平均血压异常低。站立时未观察到这些变化,舒张压未记录到可归因于治疗的变化。服用安非他酮或右旋苯丙胺后脑电图(EEG)无变化。阿米替林使δ波段(2.3 - 4赫兹)的活动增加,α波段(7.5 - 13.5赫兹)的活动减少。安非他酮用视觉模拟量表测量的主观评分无变化。阿米替林导致嗜睡、镇静和身体功能受损,而右旋苯丙胺提高了警觉性,产生欣快感并增加社交性。无法确定安非他酮有任何副作用。得出的结论是,安非他酮在药效学特性上与右旋苯丙胺和阿米替林均不同。在所研究的剂量下,该药物没有兴奋和镇静特性。此外,未出现心血管或抗胆碱能作用,鉴于其相对于现有抗抑郁药物的这些潜在优势,进一步的临床研究正在进行中。