Swanson J M, Volkow N D
Department of Pediatrics, University of California at Irvine, 19722 MacArthur Boulevard, Irvine, CA 92697-4480, USA.
Behav Brain Res. 2002 Mar 10;130(1-2):73-8. doi: 10.1016/s0166-4328(01)00433-8.
In the USA, the stimulant drug methylphenidate (MPH) is used to treat a large number (2 million or more per year) of children with Attention Deficit Hyperactivity Disorder (ADHD). Although the US FDA approved MPH in the 1960s, the pharmacokinetic (PK) properties of serum concentrations of MPH in children with ADHD were not described until the 1980s, and then in only a few cases. Recently, information from drug development programs have increased our knowledge about the serum PK and some pharmacodynamic (PD) characteristics of MPH in ADHD children, and studies based on positron emission tomograpy (PET) in adult volunteers have provided new knowledge about the PK properties of MPH at the primary site of action in the brain. We will review these two topics and use this new information to evaluate the mechanisms of action of MPH.
在美国，刺激性药物哌甲酯（MPH）被用于治疗大量（每年200万或更多）患有注意力缺陷多动障碍（ADHD）的儿童。尽管美国食品药品监督管理局（FDA）在20世纪60年代就批准了MPH，但直到20世纪80年代才开始描述ADHD儿童血清中MPH浓度的药代动力学（PK）特性，而且当时仅涉及少数病例。最近，药物研发项目提供的信息增加了我们对ADHD儿童中MPH血清PK及一些药效学（PD）特性的了解，并且基于正电子发射断层扫描（PET）对成年志愿者进行的研究，为MPH在大脑主要作用部位的PK特性提供了新知识。我们将回顾这两个主题，并利用这些新信息来评估MPH的作用机制。
