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Lisdexamfetamine

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Abstract

  • ▲ Lisdexamfetamine is an amphetamine prodrug, comprising an l-lysine amino acid covalently bonded to dextroamphetamine (d-amphetamine). Lisdexamfetamine is approved in the US for the treatment of attention-deficit hyperactivity disorder in children aged 6–12 years.

  • ▲ Lisdexamfetamine is a therapeutically inactive molecule. After oral ingestion, lisdexamfetamine is hydrolyzed to l-lysine, a naturally occurring essential amino acid, and active d-amphetamine, which is responsible for the activity of the drug.

  • ▲ Ina well designed pharmacodynamic study in adult stimulant abusers, 50 or 100mg doses of oral lisdexamfetamine had less likability than d-amphetamine 40mg, suggesting a reduced abuse potential.

  • ▲ Through rate-limited hydrolysis in the body, l-lysine is cleaved, gradually releasing pharmacologically active d-amphetamine. The pharmacokinetics of lisdexamfetamine suggest a reduced potential for abuse.

  • ▲ In two well designed trials in children aged 6–12 years with attention-deficit hyperactivity disorder (ADHD), the efficacy of lisdexamfetamine was superior to that of placebo in improving symptoms associated with ADHD.

  • ▲ Adverse events with lisdexamfetamine were, in general, mild to moderate in severity and consistent with those commonly reported with amphetamine.

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Notes

  1. The use of trade names is for product identification purposes only and does not imply endorsement.

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Correspondence to Stephanie K. A. Blick.

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Blick, S.K.A., Keating, G.M. Lisdexamfetamine. Pediatr-Drugs 9, 129–135 (2007). https://doi.org/10.2165/00148581-200709020-00007

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