Lisdexamfetamine: chemistry, pharmacodynamics, pharmacokinetics, and clinical efficacy, safety, and tolerability in the treatment of binge eating disorder
Abstract
Introduction The indications for lisdexamfetamine (LDX), a central nervous system stimulant, were recently expanded to include treatment of moderate to severe binge eating disorder (BED). Areas covered: This review aims to describe the chemistry and pharmacology of LDX, as well as the clinical trials investigating the efficacy and safety of this medication for the management of BED. Expert opinion: LDX is the first medication with United States Food and Drug Administration approval for the treatment of BED. It is an inactive prodrug of d-amphetamine that extends the half-life of d-amphetamine to allow for once daily dosing. D-amphetamine acts primarily to increase the concentrations of synaptic dopamine and norepinephrine. Metabolism of LDX to d-amphetamine occurs when peptidases in red blood cells cleave the covalent bond between d-amphetamine and l-lysine. D-amphetamine is then further metabolized by CYP2D6. Excretion is primarily through renal mechanisms. In clinical trials, LDX demonstrated statistical and clinical superiority over placebo in reducing binge eating days per week at doses of 50 and 70 mg daily. Commonly reported side effects of LDX include dry mouth, insomnia, weight loss, and headache, and its use should be avoided in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart arrhythmia or coronary artery disease. As with all CNS stimulants, risk of abuse needs to be assessed prior to prescribing.
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Lisdexamfetamine is a prodrug approved for ADHD and binge eating disorder treatment.
“Lisdexamfetamine, the first prodrug approved for ADHD (16, 17) and binge eating disorder (18) treatment, is synthesized by covalently linking d-amphetamine to the amino acid l-lysine (19).”
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“Pivotal trials One Phase II [49], and two Phase III [50], 11–12 week randomized controlled trials in patients with moderate to severe BED.”
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Absorption of lisdexamfetamine dimesylate and its enzymatic conversion to d-amphetamine
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Jian-min, C., Zhi-yuan, W., Shi-xuan, W., Rui, S., Ning, W., & Jin, L. (2022) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2022.885574 · Cited by 7 · see citing works
- Authors
- Ward, K., & Citrome, L.
- Affiliations
- University of Michigan (US)
- New York Medical College (US)
- Corresponding author
- Citrome, Leslie
- Venue
- Expert Opinion on Drug Metabolism & Toxicology
- Publisher
- Informa UK Limited
- Published
- 2018-01-04
- Volume
- 14
- Issue
- 2
- Pages
- 229-238
- ISSN
- 1742-5255 (ISSN-L)
- 1744-7607
- OpenAlex
- W2777742400
- Cited by
- 32
- References
- 11
- Citations by year
- 2026: 3 · 2025: 1 · 2024: 4 · 2023: 3 · 2022: 4 · 2021: 4 · 2020: 8 · 2019: 5
- FWCI
- 4.40
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Opinion on Drug Metabolism & Toxicology (publishedVersion)
- PubMed (publishedVersion)
- Touro Scholar (Touro College) (submittedVersion)
- Topics
- Social Sciences › Psychology › Clinical Psychology › Eating Disorders and Behaviors
- Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Keywords
- lisdexamfetamine, binge eating disorder, d-amphetamine, prodrugs, psychostimulants, pharmacokinetics, pharmacodynamics, drug metabolism, CYP2D6, dopamine, norepinephrine, drug safety, abuse risk, FDA approval
- MeSH terms
- Lisdexamfetamine Dimesylate, Central Nervous System Stimulants, Animals, Drug Administration Schedule, Half-Life, Humans, Methyldopa, Norepinephrine, Prodrugs, Severity of Illness Index, Binge-Eating Disorder
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