Department of Psychiatry, Washington University, St. Louis, MO 63301, USA.
CNS Spectr. 2010 May;15(5):315-25. doi: 10.1017/s1092852900027541.
Attention-deficit/hyperactivity disorder (ADHD) is a highly genetic neuropsychiatric disorder that can cause impairment at school, work, home, and in social relationships. Once considered a childhood disorder, as many as 65% of children with ADHD continue to exhibit symptoms into adulthood. While a mainstay of ADHD patient care, immediate-release stimulant use has been constrained by concerns about safety, tolerability, and issues related to nonmedical use and abuse. These concerns have prompted interest in developing modified versions or new delivery systems for stimulants. Prodrugs have been used in pharmaceutical development to optimize delivery of an active drug or to minimize toxicity. Prodrugs are pharmacologically inactive compounds that require in vivo conversion to release therapeutically active medications. Lisdexamfetamine dimesylate (LDX) is an inactive, water-soluble prodrug in which d-amphetamine is bonded to l-lysine, a naturally occurring amino acid. After oral ingestion, LDX is metabolized into l-lysine and active d-amphetamine. This review of LDX presents the efficacy, safety, and pharmacokinetic profile of this novel stimulant medication, and is intended to help clinicians understand its role in treating children and adults with ADHD.
注意缺陷多动障碍（ADHD）是一种高度遗传的神经精神疾病，可导致在学校、工作、家庭和社交关系中出现障碍。曾经被认为是一种儿童疾病，多达 65%的 ADHD 儿童在成年后仍表现出症状。尽管即时释放兴奋剂的使用是 ADHD 患者护理的主要手段，但由于对安全性、耐受性以及与非医疗用途和滥用相关的问题的担忧，其使用受到了限制。这些问题促使人们有兴趣开发改良版本或新的兴奋剂输送系统。前药在药物开发中被用于优化活性药物的递送或最小化毒性。前药是一种药理上无活性的化合物，需要在体内转化才能释放出具有治疗作用的药物。右苯丙胺赖氨酸盐（LDX）是一种无活性的水溶性前药，其中 d-苯丙胺与 l-赖氨酸结合，l-赖氨酸是一种天然存在的氨基酸。口服摄入后，LDX 代谢为 l-赖氨酸和活性 d-苯丙胺。本文对 LDX 的综述介绍了这种新型兴奋剂药物的疗效、安全性和药代动力学特征，旨在帮助临床医生了解其在治疗儿童和成人 ADHD 中的作用。
