Lisdexamfetamine (LDX), a prodrug of d-amphetamine, is widely used in the pharmacological treatment of neuropsychiatric disorders such as attention-deficit/hyperactivity disorder (ADHD) and binge eating disorder (BED). Chemically, it consists of the amino acid lysine linked to d-amphetamine. Its enzymatic conversion to d-amphetamine sets the stage for a prolonged and controlled release, influencing its clinical profile and differentiating it from other stimulant medications. As a central nervous system stimulant, LDX primarily acts by increasing the release of neurotransmitters, particularly dopamine and noradrenaline, in the brain. Clinically, this enhanced availability of neurotransmitters is believed to contribute to improvements in attention, focus and impulse control in individuals with ADHD. The side effects of LDX include insomnia, decreased appetite, weight loss and xerostomia. This work reviews the pharmacological mechanisms, clinical applications and forensic considerations associated with its use. It is expected that clinicians, researchers and policymakers have a comprehensive understanding of the pharmacological and toxicological aspects of LDX.
Keywords: attention‐deficit/hyperactivity disorder; d‐amphetamine; lisdexamfetamine; pharmacodynamics; pharmacokinetics.
© 2025 The Author(s). Basic & Clinical Pharmacology & Toxicology published by John Wiley & Sons Ltd on behalf of Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).