Department of Pharmacotherapy and Translational Research, College of Pharmacy, University of Florida, Gainesville, FL 32610-0486, USA; Center for Pharmacogenomics and Precision Medicine, College of Pharmacy, University of Florida, Gainesville, FL 32610-0486, USA.
Department of Pharmacotherapy and Translational Research, College of Pharmacy, University of Florida, Gainesville, FL 32610-0486, USA.
Child Adolesc Psychiatr Clin N Am. 2022 Jul;31(3):393-416. doi: 10.1016/j.chc.2022.03.003. Epub 2022 May 11.
The psychostimulants-amphetamine and methylphenidate-have been in clinical use for well more than 60 years. In general, both stimulants are rapidly absorbed with relatively poor bioavailability and short half-lives. The pharmacokinetics of both stimulants are generally linear and dose proportional although substantial interindividual variability in pharmacokinetics is in evidence. Amphetamine (AMP) is highly metabolized by several oxidative enzymes forming multiple metabolites while methylphenidate (MPH) is primarily metabolized by hydrolysis to the inactive metabolite ritalinic acid. At present, pharmacogenomic testing as an aid to guide dosing and personalized treatment cannot be recommended for either agent. Few pharmacokinetically based drug-drug interactions (DDIs) have been documented for either stimulant.
苯丙胺类兴奋剂——苯丙胺和哌甲酯——在临床上已经使用了 60 多年。一般来说，这两种兴奋剂吸收迅速，但生物利用度相对较差，半衰期短。这两种兴奋剂的药代动力学通常呈线性和剂量比例，尽管药代动力学存在显著的个体间变异性。苯丙胺（AMP）被多种氧化酶高度代谢，形成多种代谢物，而哌甲酯（MPH）主要通过水解转化为无活性的代谢物利他林酸。目前，作为指导剂量和个体化治疗辅助手段的药物基因组学检测不能推荐用于这两种药物。只有少数基于药代动力学的药物-药物相互作用（DDI）被记录下来。
