Cited by 70Attention Deficit Hyperactivity DisorderNeurotransmitter Receptor Influence on BehaviorNeuroscience and Neuropharmacology Research

The DOI matches its Crossref record; 218 of the 222 references it cites were found in a registry or an index; 129 of the 328 sources its claims cite were checked for support.

Molecular Characterisation of the Mechanism of Action of Stimulant Drugs Lisdexamfetamine and Methylphenidate on ADHD Neurobiology: A Review

Open access

Abstract

Attention-deficit/hyperactivity disorder (ADHD) is a common childhood-onset neurodevelopmental disorder characterised by persistent inattention, hyperactivity and impulsivity. Moreover, ADHD is commonly associated with other comorbid diseases (depression, anxiety, bipolar disorder, etc.). The ADHD symptomatology interferes with subject function and development. The treatment of ADHD requires a multidisciplinary approach based on a combination of non-pharmacological and pharmacological treatments with the aim of ameliorating the symptomatology; among first-line pharmacological treatments are stimulants [such as methylphenidate (MPH) and lisdexamfetamine dimesylate (LDX)]. In this review we explored recent ADHD- and stimulants-related literature, with the aim of compiling available descriptions of molecular pathways altered in ADHD, and molecular mechanisms of current first-line stimulants MPH and LDX. While conducting the narrative review, we applied structured search strategies covering PubMed/MEDLINE database and performed handsearching of reference lists on the results of those searches. The aetiology and pathophysiology of ADHD are incompletely understood; both genetic and environmental factors have been associated with the disorder and its grade of burden, and also the relationship between the molecular mechanisms of pharmacological treatments and their clinical implications. The lack of comprehensive understanding of the underlying molecular pathology makes both the diagnosis and treatment difficult. Few published studies evaluating molecular data on the mechanism of action (MoA) of MPH and LDX on ADHD are available and most of them are based on animal models. Further studies are necessary to improve the knowledge of ADHD pathophysiology and how the MoAs of MPH and LDX differentially modulate ADHD pathophysiology and control ADHD symptomatology.

Overview

AI snapshot

Written from the paper’s full text.

TL;DR

This narrative review compiles molecular pathways implicated in ADHD and the mechanisms of methylphenidate (MPH) and lisdexamfetamine dimesylate (LDX), finding that both increase dopamine/norepinephrine signalling via DAT/NET inhibition but LDX has more reported targets. Evidence is limited and largely from animal models, so how their mechanisms differentially modulate ADHD pathophysiology remains uncertain.

Key findings

  • ADHD is associated with neurotransmitter imbalance, neuroinflammation/defective immunoregulation, circadian system dysfunction, and altered neural viability/neurodegeneration; reported prevalence is around 4–12% in children and 2.5–5% in adults, with heritability estimates of 60–90% in twin studies versus 10–28% from SNP analysis and environmental factors estimated at 20–30%.
  • MPH directly inhibits DAT (SLC6A3) and NET (SLC6A2) and agonizes HTR1A (3 targets), whereas LDX directly activates TAAR1 and inhibits SLC18A2, DAT, NET, SERT, MAOA, and MAOB (7 targets); both activate DRD1, DRD5, ADRA2A, ADRA2B and induce TNF, while LDX also modulates IL-4, IL-6, and IL-10.
  • MPH has broader reported drug-induced changes including apoptosis/neural viability proteins (BCL2, BAX, CASP3, CYC1), circadian-related CREB1, and pro-inflammatory TNFα/IL-1β; LDX has oxidative stress effects via decreased CAT, GSH-Px, and SOD and a possible anti-inflammatory IL-4/IL-10 profile.
  • Few data are available on neuroinflammation/immunoregulation and circadian effects for both drugs; no evidence was found on whether LDX improves circadian rhythm in ADHD.

Methods

  • Narrative review, not a formal systematic review, using structured PubMed/MEDLINE searches plus handsearching of reference lists and PubMed “related articles.”
  • One search (January 2020) covered ADHD molecular pathophysiology reviews; another (April 2020) covered molecular/mechanism terms for stimulant drugs using generic and commercial names, with results contextualised for clinical implications.
  • The article is based on previously conducted studies and contains no new studies with human participants or animals performed by the authors.

Limitations

  • Stated: ADHD aetiology and pathophysiology are incompletely understood; few published molecular studies evaluate the mechanism of action of MPH and LDX in ADHD, and most are based on animal models.
  • Stated: available information may be biased because it only informs on data reported for one of the drugs; the inflammatory profile of LDX has not been evaluated in an ADHD context, and no evidence was found on LDX effects on circadian rhythm in ADHD.
  • Evident from the text: as a narrative review without a formal systematic protocol, many mechanistic claims derive from animal or non-ADHD models, and MPH effects on BDNF, c-FOS, apoptosis, and oxidative stress are reported as inconsistent or dependent on age, dose, and brain region.

Model-written summary. Check it against the paper before relying on it.

Integrity signals

Registry

Crossref · 10.1007/s40120-022-00392-2

Cites

218 of 218 references verified0 citation errors · 0 not checkable

Statistics

Nothing to recompute.

Figures

Fig. 1 ADHD aetiology, pathophysiological processes and symptoms scheme
Fig. 1 ADHD aetiology, pathophysiological processes and symptoms schemeCC BY-NC · PubMed Central
Fig. 2 Mechanism of LDX/MPH in the synapse: 1. Patient with ADHD without treatment. 2. Patient with ADHD treated with MPH 3. Patient with ADHD treated with LDX
Fig. 2 Mechanism of LDX/MPH in the synapse: 1. Patient with ADHD without treatment. 2. Patient with ADHD treated with MPH 3. Patient with ADHD treated with LDXCC BY-NC · PubMed Central
Fig. 3 Relationship between function and behavioural effects of monoamines. Direct targets of the stimulant drugs are indicated in each monoaminergic pathway
Fig. 3 Relationship between function and behavioural effects of monoamines. Direct targets of the stimulant drugs are indicated in each monoaminergic pathwayCC BY-NC · PubMed Central

Verification

Claims the paper makes

89 No full text of the sources · 57 Partly supported · 32 Own interpretation · 25 Supported · 10 Couldn’t confirm · 8 No basis given · 5 Supported so far · 5 Sources not found · 4 Not checked yet · 2 Own method · 1 Not supported · accuracy not yet measured

Show all 108 claims

  • Probably not a substantial claim. 51
  • It may state two separate claims as one. 98
130 of 130
  • The paper relies on this without support.

    There is no medical test that determines the presence of ADHD.

    “There is no medical test that determines the presence of the condition.”
  • The paper relies on this without support.

    Predisposing environmental factors increase the risk of developing ADHD based on a genetically or biologically determined vulnerability pattern.

    “predisposing environmental factors increase the risk of developing ADHD based on a genetically or biologically determined vulnerability pattern.”
  • The paper relies on this without support.

    Increased density of DAT-1 in patients with ADHD results in inadequate extracellular DA levels in these brain regions.

    “Increased density of DAT-1 in patients with ADHD has been reported, resulting in inadequate extracellular DA levels in these brain regions.”
  • The paper relies on this without support.

    Abnormalities in NET function contribute to ADHD development by decreasing the extracellular NE levels.

    “Abnormalities in NET function contribute to ADHD development by decreasing the extracellular NE levels.”
  • The paper relies on this without support.

    BDNF dysregulation is associated with ADHD.

    “BDNF dysregulation is associated with ADHD.”
  • The paper relies on this without support.

    Findings from animal models and in vitro studies on the molecular effects of MPH and LDX are applicable to human ADHD pathophysiology and treatment.

    “Despite the studies published on the effect of MPH and LDX on pathophysiological processes and their specific molecules involved in ADHD, there are few data published on the subject and some are based on investigations run in animal models.”
  • The paper relies on this without support.

    The pathophysiological processes (NT imbalance, neuroinflammation and defective immunoregulation, circadian system dysfunction, altered neural viability and neurodegeneration) are causally involved in ADHD.

    “MPH and LDX show an impact on the aforementioned causative processes related to ADHD development (NT imbalance, neuroinflammation and defective immunoregulation, circadian system dysfunction and altered neural viability and neurodegeneration) owing to both drugs’ activity in ADHD symptomatology control.”
  • The paper relies on this without support.

    The drug-induced molecular changes observed in the reviewed studies are responsible for the clinical efficacy of MPH and LDX in ADHD.

    “Both LDX and MPH have improve the neuronal signalling that leads to an increase of DA and NE levels in the prefrontal cortex, by acting on DAT and NET and improving attentional deficit and cognitive functions.”
8 of 8

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

Each contradiction between two passages listed here was confirmed by an independent check.

3 of 3

Citations

Cites

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Metadata

Authors
Quintero, J., Gutiérrez-Casares, J. R., & Álamo, C.
Affiliations
  • Universidad Complutense de Madrid (ES)
  • Hospital Perpetuo Socorro (ES)
  • Universidad de Alcalá (ES)
Corresponding author
Gutiérrez-Casares, José R.
Venue
Neurology and Therapy
Published
2022-08-11
Volume
11
Issue
4
Pages
1489-1517
ISSN
  • 2193-6536 (ISSN-L)
  • 2193-8253
OpenAlex
W4291015895
Cited by
70
References
222
Citations by year
2026: 18 · 2025: 31 · 2024: 15 · 2023: 6
FWCI
7.52
Type
journal article
Language
en
Open access
Locations
  • Neurology and Therapy (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • PubMed Central (submittedVersion, cc-by-nc)
Funders
Takeda
Topics
  • Health Sciences › Medicine › Psychiatry and Mental health › Attention Deficit Hyperactivity Disorder
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
attention deficit hyperactivity disorder, lisdexamfetamine, methylphenidate, stimulants, mechanism of action, ADHD pathophysiology, molecular pathways, ADHD comorbidity, animal model of ADHD

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