Departments of Psychiatry and of Neuroscience and Physiology, State University of New York (SUNY) Upstate Medical University, Syracuse, NY, United States; K.G. Jebsen Centre for Research on Neuropsychiatric Disorders, University of Bergen, Bergen, Norway.
Neurosci Biobehav Rev. 2018 Apr;87:255-270. doi: 10.1016/j.neubiorev.2018.02.001. Epub 2018 Feb 8.
Psychostimulants, including amphetamines and methylphenidate, are first-line pharmacotherapies for individuals with attention-deficit/hyperactivity disorder (ADHD). This review aims to educate physicians regarding differences in pharmacology and mechanisms of action between amphetamine and methylphenidate, thus enhancing physician understanding of psychostimulants and their use in managing individuals with ADHD who may have comorbid psychiatric conditions. A systematic literature review of PubMed was conducted in April 2017, focusing on cellular- and brain system-level effects of amphetamine and methylphenidate. The primary pharmacologic effect of both amphetamine and methylphenidate is to increase central dopamine and norepinephrine activity, which impacts executive and attentional function. Amphetamine actions include dopamine and norepinephrine transporter inhibition, vesicular monoamine transporter 2 (VMAT-2) inhibition, and monoamine oxidase activity inhibition. Methylphenidate actions include dopamine and norepinephrine transporter inhibition, agonist activity at the serotonin type 1A receptor, and redistribution of the VMAT-2. There is also evidence for interactions with glutamate and opioid systems. Clinical implications of these actions in individuals with ADHD with comorbid depression, anxiety, substance use disorder, and sleep disturbances are discussed.
精神兴奋剂，包括苯丙胺和哌醋甲酯，是治疗注意力缺陷/多动障碍（ADHD）患者的一线药物治疗方法。本综述旨在教育医生了解苯丙胺和哌醋甲酯在药理学和作用机制方面的差异，从而增强医生对精神兴奋剂的理解及其在治疗可能伴有精神共病的 ADHD 患者中的应用。2017 年 4 月，我们对 PubMed 进行了系统的文献回顾，重点关注苯丙胺和哌醋甲酯对细胞和大脑系统水平的影响。两者的主要药理作用是增加中枢多巴胺和去甲肾上腺素的活性，从而影响执行和注意力功能。苯丙胺的作用包括多巴胺和去甲肾上腺素转运体抑制、囊泡单胺转运体 2（VMAT-2）抑制和单胺氧化酶活性抑制。哌醋甲酯的作用包括多巴胺和去甲肾上腺素转运体抑制、5-羟色胺 1A 受体激动剂活性和 VMAT-2 的再分布。还有证据表明其与谷氨酸和阿片样物质系统相互作用。讨论了这些作用在伴有抑郁、焦虑、物质使用障碍和睡眠障碍的 ADHD 患者中的临床意义。
