Review of the Pharmacology and Clinical Profile of Bupropion, an Antidepressant and Tobacco Use Cessation Agent

Linda P. Dwoskin, Anthony S. Rauhut, Kelley A. King-Pospisil, Michael T. Bardo
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引用次数: 249

Abstract

Bupropion hydrochloride ((±)-2-tert-butylamino)-3′-chloropropiophenone · HCl) is a nonselective inhibitor of the dopamine transporter (DAT) and the norepinephrine transporter (NET) and is also an antagonist at neuronal nicotinic acetylcholine receptors (nAChRs). In animal models used commonly to screen for antidepressant activity, bupropion shows a positive response. Also using animal models, bupropion has been shown to attenuate nicotine-induced unconditioned behaviors, to share or enhance discriminative stimulus properties of nicotine and to have a complex effect on nicotine self-administration, i.e., low doses augmenting nicotine self-administration and high doses attenuating self-administration. Current studies show that bupropion facilitates the acquisition of nicotine conditioned place preference in rats, further suggesting that bupropion enhances the rewarding properties of nicotine. Bupropion has been shown to attenuate the expression of nicotine withdrawal symptoms in both animal models and human subjects. With respect to relapse, current studies show that bupropion attenuates nicotine-induced reinstatement in rats, but large individual differences are apparent. Clinically, bupropion is used as a treatment for two indications, as an antidepressant, the indication for which it was developed, and as a tobacco use cessation agent. In clinical trials, bupropion is being tested as a candidate treatment for psychostimulant drug abuse, attention-deficit hyperactivity disorder (ADHD) and obesity. Bupropion is available in three bioequivalent oral formulations, immediate release (IR), sustained release (SR), and extended release (XL). Extensive hepatic metabolism of bupropion produces three pharmacologically active metabolites, which may contribute to its clinical profile.

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抗抑郁和戒烟药物安非他酮的药理学和临床研究综述
盐酸安非他酮((±)-2-叔丁基氨基)-3′-氯丙烯酮·HCl)是多巴胺转运体(DAT)和去甲肾上腺素转运体(NET)的非选择性抑制剂,也是神经元烟碱乙酰胆碱受体(nAChRs)的拮抗剂。在通常用于筛选抗抑郁药物活性的动物模型中,安非他酮显示出积极的反应。同样在动物模型中,安非他酮已被证明可以减弱尼古丁诱导的无条件行为,分享或增强尼古丁的鉴别刺激特性,并对尼古丁自我给药产生复杂的影响,即低剂量增加尼古丁自我给药,高剂量减弱尼古丁自我给药。目前的研究表明,安非他酮促进大鼠尼古丁条件位置偏好的获得,进一步表明安非他酮增强了尼古丁的奖励特性。安非他酮已被证明在动物模型和人类受试者中都能减轻尼古丁戒断症状的表达。关于复发,目前的研究表明,安非他酮在大鼠中减弱尼古丁诱导的恢复,但很大的个体差异是明显的。临床上,安非他酮被用作两种适应症的治疗,一种是抗抑郁药,它被开发的适应症,另一种是戒烟剂。在临床试验中,安非他酮被用作治疗精神兴奋剂滥用、注意力缺陷多动障碍(ADHD)和肥胖的候选药物。安非他酮有三种生物等效口服制剂,即立即释放(IR)、缓释(SR)和缓释(XL)。安非他酮广泛的肝脏代谢产生三种药理活性代谢物,这可能有助于其临床表现。
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