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Introduction Lisdexamfetamine is an inactive prodrug of dexamfetamine, used for the second-line treatment of attention-deficit/hyperactivity disorder (ADHD) in children above the age of 6 years and up to adulthood, when response to previous methylphenidate treatment is considered clinically inadequate ( Following oral administration, lisdexamfetamine is rapidly taken up from the small intestine by active carrier-mediated transport, probably via peptide transporter 1 ( The dexamfetamine generated crosses the blood-brain barrier to access binding sites in the central nervous system and to exert therapeutic effects by increasing noradrenergic and dopaminergic neurotransmission ( After administration of lisdexamfetamine dimesylate in 50 mg incremental single doses ranging from 50 to 250 mg, it was found that the pharmacokinetic parameters of dexamfetamine are dose-proportional and predictable over a wide range of prodrug doses, with low intersubject and intrasubject variability ( 0.05)

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