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赖右苯丙胺二甲磺酸盐:首个前体药物兴奋剂。

Lisdexamfetamine dimesylate: the first prodrug stimulant.

作者信息

Goodman David W

机构信息

Dr. Goodman is from the Adult Attention Deficit Disorder Center of Maryland, Johns Hopkins at Green Spring Station, Lutherville, Maryland; and Assistant Professor, Johns Hopkins University School of Medicine, Department of Psychiatry and Behavioral Sciences, Baltimore, Maryland.

出版信息

Psychiatry (Edgmont). 2007 Aug;4(8):39-45.

Abstract

Attention deficit hyperactivity disorder (ADHD) is one of the most common neurobehavioral disorders affecting children. The symptoms often persist into adolescence and adulthood, causing significant impairments. ADHD often remains undiagnosed and untreated, and because of its potential long-term impact, recognition, diagnosis, and management in children have become increasingly important. Education about ADHD and the available therapy options is important for both the patient and the caregiver to achieve more effective treatment. Efficacy and safety data on stimulant medications have provided evidence for their effectiveness in treating ADHD. Although they remain the first-line treatment, the need for multiple daily dosing and concerns about the general risk profile of stimulants have led to the development of new agents, including once-daily formulations that provide prolonged duration of action. However, pharmacokinetic variability of these formulations can result in inconsistent effects in some patients. The use of prodrug technology and the development of the only prodrug stimulant, lisdexamfetamine dimesylate (LDX), provide a promising treatment option for ADHD with an improved overdose potential risk profile when compared to d-amphetamine. This review of LDX, which presents the efficacy, safety, and pharmacokinetic profile of this new class of stimulant, is designed to help the physician better understand the clinical use of this agent in treating ADHD.

摘要

注意缺陷多动障碍(ADHD)是影响儿童的最常见神经行为障碍之一。这些症状常常持续到青少年期和成年期,造成严重损害。ADHD常常未被诊断和治疗,鉴于其潜在的长期影响,儿童期对该疾病的识别、诊断和管理变得越来越重要。对ADHD及现有治疗选择进行宣教,对患者及其照料者实现更有效的治疗很重要。关于兴奋剂药物的疗效和安全性数据已证明其治疗ADHD的有效性。尽管它们仍是一线治疗药物,但每日多次给药的需求以及对兴奋剂总体风险状况的担忧促使了新药物的研发,包括作用持续时间延长的每日一次剂型。然而,这些剂型的药代动力学变异性可能导致部分患者疗效不一致。前体药物技术的应用以及唯一的前体药物兴奋剂——二甲磺酸赖右苯丙胺(LDX)的研发,为ADHD提供了一种有前景的治疗选择,与右旋苯丙胺相比,其过量用药潜在风险状况有所改善。这篇关于LDX的综述介绍了这类新型兴奋剂的疗效、安全性和药代动力学特征,旨在帮助医生更好地了解该药物在治疗ADHD中的临床应用。

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