Roncero Carlos, Álvarez F Javier
Department of Psychiatry, Outpatient Drug Clinic, Vall d'Hebron University Hospital-Barcelona Pubic Health Agency (ASPB), Passeig Vall d'Hebron, 119-129, E-08035 Barcelona, Spain.
Expert Rev Neurother. 2014 Aug;14(8):849-65. doi: 10.1586/14737175.2014.932691. Epub 2014 Jun 20.
Lisdexamfetamine dimesylate (LDX) is a long-acting oral prodrug stimulant. It is inactive until enzymatically hydrolyzed in the blood to active D-amphetamine. The pharmacological action of this compound involves blocking norepinephrine (NE) and dopamine reuptake into presynaptic neurons and promoting the release of NE and dopamine into the extraneuronal space. LDX has been approved for treating ADHD, which is the most common psychiatric disorder in children and adolescents. Also, LDX has been proposed for other psychiatric conditions related with dopaminergic and NE CNS. LDX is the first long-acting oral prodrug indicated for the treatment of ADHD in children (6-12 years), adolescents (13-17 years) and in adults in the USA and Canada, whereas, in Europe, LDX is licensed in several countries for the treatment of children and adolescents with ADHD who have had a clinically inadequate response to methylphenidate. This article covers the most important pharmacological aspects of LDX as well as data on the efficacy, tolerability and safety of this long-acting amphetamine prodrug collected from clinical studies recently published in the literature.
赖右苯丙胺二甲磺酸盐（LDX）是一种长效口服前体药物兴奋剂。在血液中被酶水解为活性D-苯丙胺之前，它是无活性的。该化合物的药理作用包括阻断去甲肾上腺素（NE）和多巴胺重新摄取到突触前神经元中，并促进NE和多巴胺释放到神经元外间隙。LDX已被批准用于治疗注意缺陷多动障碍（ADHD），这是儿童和青少年中最常见的精神疾病。此外，LDX也被提议用于治疗与多巴胺能和NE中枢神经系统相关的其他精神疾病。在美国和加拿大，LDX是首个被批准用于治疗6至12岁儿童、13至17岁青少年及成人ADHD的长效口服前体药物；而在欧洲，多个国家已批准LDX用于治疗对哌甲酯临床反应不佳的ADHD儿童和青少年。本文涵盖了LDX最重要的药理学方面，以及从近期文献发表的临床研究中收集到的关于这种长效苯丙胺前体药物的疗效、耐受性和安全性的数据。
