Lisdexamfetamine: A pharmacokinetic review
Abstract
Lisdexamfetamine (LDX) is a d-amphetamine (d-AMPH) pro-drug used to treat Attention Deficit and Hyperactivity Disorder (ADHD) and Binge Eating Disorder (BED) symptoms. The in vivo pharmacodynamics of LDX is the same as that of its active product d-AMPH, although there are a few qualitative and quantitative differences due to pharmacokinetics. Due to the specific pharmacokinetics of the long-acting stimulants, this article revises the pharmacokinetic studies on LDX, the newest amphetamine pro-drug. The Medline/Pubmed, Science Direct and Biblioteca Virtual em Saúde (Lilacs and Ibecs) (2007-2016) databases were searched for articles and their list of references. As for basic pharmacokinetics studies, since LDX is a newly developed medication, there are few results concerning biotransformation, distribution and the use of different biological matrices for analysis. This is the first robust review on this topic, gathering data from all clinical pharmacokinetics studies available in the literature. The particular pharmacokinetics of LDX plays a major role in studying this pro-drug, since this knowledge was essential to understand some reports on clinical effects in literature, e.g. the small likelihood of reducing the effect by interactions, the effect of long duration use and the still questionable reduction of the potential for abuse. In general the already well-known pharmacokinetic properties of amphetamine make LDX relatively predictable, simplifying the use of LDX in clinical…
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Levels of d-amphetamine are proportional to the LDX dose, exhibiting low intraindividual and interindividual variability.
“Levels of d-amphetamine are proportional to the LDX dose, exhibiting low intraindividual and interindividual variability.”
From Review of Lisdexamfetamine Dimesylate in Adults With Attention-Deficit/Hyperactivity Disorder (2017) · cites this paper as [19]
Both LDX and d-amphetamine are renally eliminated and are not dialyzable.
“Both LDX and d-amphetamine are renally eliminated and are not dialyzable”
From Review of Lisdexamfetamine Dimesylate in Adults With Attention-Deficit/Hyperactivity Disorder (2017) · cites this paper as [19]
Long-term release of LDX results in a homogeneous action, allowing for a similar effect noted 90 minutes to 14 hours after administration.
“The long-term release of the drug results in a homogeneous action, allowing for a similar effect noted 90 minutes to 14 hours after administration.”
From Review of Lisdexamfetamine Dimesylate in Adults With Attention-Deficit/Hyperactivity Disorder (2017) · cites this paper as [18]
Cites
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ADHD and the Prefrontal Cortex
Arnsten, A. F. T. (2009) · The Journal of Pediatrics · doi:10.1016/j.jpeds.2009.01.018 · Cited by 220 · see citing works
Absorption of lisdexamfetamine dimesylate and its enzymatic conversion to d-amphetamine
Pennick (2010) · Neuropsychiatric Disease and Treatment · doi:10.2147/ndt.s9749 · Cited by 170 · see citing works
Multiple daily-dose pharmacokinetics of lisdexamfetamine dimesylate in healthy adult volunteers
Krishnan, S. M., & Stark, J. G. (2008) · Current Medical Research and Opinion · doi:10.1185/030079908x242737 · Cited by 55 · see citing works
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Lisdexamfetamine Dimesylate: A New Therapeutic Option for Attention-Deficit Hyperactivity Disorder
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Review of Lisdexamfetamine Dimesylate in Adults With Attention-Deficit/Hyperactivity Disorder
Najib, J., Wimer, D., Zeng, J., Lam, K. W., Romanyak, N., Paige Morgan, E., & Thadavila, A. (2017) · Journal of Central Nervous System Disease · doi:10.1177/1179573517728090 · Cited by 17 · see citing works
- Authors
- Comiran, E., Kessler, F. H., Fröehlich, P. E., & Limberger, R. P.
- Affiliations
- Universidade Federal do Rio Grande do Sul (BR)
- Corresponding author
- Comiran, Eloisa
- Venue
- European Journal of Pharmaceutical Sciences
- Publisher
- Elsevier BV
- Published
- 2016-06
- Volume
- 89
- Pages
- 172-179
- ISSN
- 0928-0987 (ISSN-L)
- OpenAlex
- W2392555149
- Cited by
- 31
- References
- 7
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 5 · 2023: 2 · 2022: 2 · 2021: 3 · 2020: 2 · 2019: 1 · 2018: 2 · 2017: 6 · 2016: 2
- FWCI
- 0.53
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmaceutical Sciences (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (Capes)
- Fundo de Incentivo à Pesquisa e Eventos
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Attention Deficit Hyperactivity Disorder
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Keywords
- lisdexamfetamine, pharmacokinetics, attention deficit hyperactivity disorder, binge eating disorder, long-acting stimulants, biotransformation, drug distribution, biological matrices, drug interactions, abuse liability
- MeSH terms
- Lisdexamfetamine Dimesylate, Attention Deficit Disorder with Hyperactivity, Biotransformation, Humans, Prodrugs
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