Description

Simple

A medication used to treat mental health disorders, such as ADHD and eating disorders.

Clinical

A central nervous system (CNS) stimulant used to treat attention deficit hyperactivity disorder (ADHD) and moderate to severe eating disorders.

Overview

Also known as _Vyvanse_, lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine [4]. It is paired with the essential amino acid _L-lysine_. Lisdexamfetamine dimesylate increases attention span and decreases restlessness in children and adults who are overactive/hyperactive, cannot concentrate for long periods, or are easily distracted or impulsive [2].

As a central nervous system stimulant, lisdexamfetamine is utilized as an adjunct therapy in the treatment of attention deficit hyperactivity disorder (ADHD). As a prodrug, lisdexamfetamine was specifically engineered as an abuse-resistant product [10]. The mechanism by which this occurs is through delayed release after ingestion (unlike some other psychostimulant drugs, which may be abused). After oral administration and absorption, enzyme hydrolysis after contact with red blood cells metabolize lisdexamfetamine into L- lysine, a naturally occurring essential amino acid and active _d-amphetamine_, wh... Read more

Pharmacology

Indication

For the treatment of Attention-deficit/hyperactivity disorder (ADHD) and for moderate to severe binge eating disorder in adults [FDA label], [ Read more

Pharmacodynamic

Lisdexamfetamine dimesylate is a prodrug of _d-amphetamine_. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulating properties [FDA label]. This agent works primarily by inducing the release of the neurotransmitters dopamine and norepinephrine from their storage areas in pres... Read more

Mechanism of action

Lisdexamfetamine is a prodrug of dextroamphetamine. The active form of this drug blocks the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. The parent drug, lisdexamfetamine, does not bind to the sites for... Read more

Absorption

After oral administration, lisdexamfetamine is rapidly absorbed from the gastrointestinal tract [FDA label], [8].

**Chewable tablet form:** After a single dose of 60 mg a chewable tablet in healthy subjects u... Read more

Protein binding

Information currently not available.

Volume of distribution

There is no accumulation of d-amphetamine (as measured by AUC) at steady state in healthy adults and no accumulation of lisdexamfetamine dimesylate after once-daily dosing for seven consecutive days [FDA label], [8 Read more

Clearance

In a study of 47 subjects aged 55 years of age or older, amphetamine clearance was approximately 0.7L/hr/kg for subjects 55-74 years of age and 0.55L/hr/kg for subjects ≥75 years of age. This is slightly reduced compared to younger adults (approximately 1L/hr/kg for subjects 18-45 years of age) [ Read more

Half life

The mean plasma elimination half-life of dextroamphetamine was about 12 hours after oral administration of lisdexamfetamine dimesylate [FDA label].

The plasma elimination half-life of lisdexamfetamine alone averaged less than one hour in studies of lisdexamfetamine dimesylate administered in vol... Read more

Route of elimination

After the oral administration of a 70mg dose of radiolabeled lisdexamfetamine dimesylate to six healthy subjects, about 96% of the oral dose radioactivity was recovered in the urine and only 0.3% recovered in the feces [FDA label], [ Read more

Toxicity

**Acute toxicity**: Symptoms of acute overdosage with amphetamines include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, panic states, hyperpyrexia, and rhabdomyolysis. Fatigue and depression generally follow the symptoms central nervous system st... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: History of drug abuse
      • Drugbank Id: DBCOND0107489
  • Regions: US
  • Patient Conditions:
      • Name: Agitational state
      • Drugbank Id: DBCOND0104163
  • Regions: US
  • Patient Conditions:
      • Name: Glaucoma
      • Drugbank Id: DBCOND0010013
  • Regions: US
  • Patient Conditions:
      • Name: Allergy to amphetamines
      • Drugbank Id: DBCOND0116305
  • Regions: US
  • Patient Conditions:
      • Name: Hyperthyroidism
      • Drugbank Id: DBCOND0009048
  • Regions: US
  • Patient Conditions:
      • Name: Symptomatic cardiovascular disease
      • Drugbank Id: DBCOND0107487
      • Modification Of:
        • Base:
          • Name: Cardiovascular Disease
          • Drugbank Id: DBCOND0028376
        • Severity:
          • Includes:
            • symptomatic
  • Regions: US
  • Patient Conditions:
      • Name: Advanced arteriosclerosis
      • Drugbank Id: DBCOND0107486
  • Regions: US
  • Patient Conditions:
      • Name: Moderate to Severe Hypertension
      • Drugbank Id: DBCOND0042937
  • Regions: US
  • Patient Conditions:
      • Name: Increased risk of hypertensive crisis
      • Drugbank Id: DBCOND0108309
  • With Therapies:
      • Name: Within 14 days of stopping MAOIs therapy (including linezolid or intravenous methylene blue)
      • Drugbank Id: DBCOND0108308
      • Name: Concurrent use of monoamine oxidase inhibitors (MAOIs)
      • Drugbank Id: DBCOND0108307
  • Hypersensitivity:
    • amphetamines
  • Regions: US

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Lisdexamfetamine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Lisdexamfetamine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-benzylimidazole
The therapeutic efficacy of 1-benzylimidazole can be decreased when used in combination with Lisdexamfetamine.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Lisdexamfetamine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of serotonin syndrome can be increased when Lisdexamfetamine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,5-diiodothyropropionic acid
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 3,5-diiodothyropropionic acid.
3,5-Diiodotyrosine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 3,5-Diiodotyrosine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of serotonin syndrome can be increased when Lisdexamfetamine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of serotonin syndrome can be increased when Lisdexamfetamine is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 6-O-benzylguanine.
7-Deazaguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 7-Deazaguanine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypertensive activities of Lisdexamfetamine.
7,9-Dimethylguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 7,9-Dimethylguanine.
8-azaguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 8-azaguanine.
8-chlorotheophylline
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 8-chlorotheophylline.
9-Deazaguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 9-Deazaguanine.
9-Methylguanine
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with 9-Methylguanine.
Abaloparatide
The risk or severity of adverse effects can be increased when Lisdexamfetamine is combined with Abaloparatide.
Abatacept
The metabolism of Lisdexamfetamine can be increased when combined with Abatacept.
10 References
  1. 1 . Jasinski DR, Krishnan S: Human pharmacology of intravenous lisdexamfetamine dimesylate: abuse liability in adult stimulant abusers. J Psychopharmacol. 2009 Jun;23(4):410-8. doi: 10.1177/0269881108093841. Epub 2008 Jul 17.PubMed: 18635707
  2. 2 . Madaan V: Lisdexamfetamine dimesylate for childhood ADHD. Drugs Today (Barc). 2008 May;44(5):319-24. doi: 10.1358/dot.2008.44.5.1215724.PubMed: 18548134
  3. 3 . Krishnan S, Moncrief S: An evaluation of the cytochrome p450 inhibition potential of lisdexamfetamine in human liver microsomes. Drug Metab Dispos. 2007 Jan;35(1):180-4. Epub 2006 Oct 11.PubMed: 17035599
  4. 4 . Goodman DW: Lisdexamfetamine dimesylate (vyvanse), a prodrug stimulant for attention-deficit/hyperactivity disorder. P T. 2010 May;35(5):273-87.PubMed: 20514273
  5. 5 . Miller GM: The emerging role of trace amine-associated receptor 1 in the functional regulation of monoamine transporters and dopaminergic activity. J Neurochem. 2011 Jan;116(2):164-76. doi: 10.1111/j.1471-4159.2010.07109.x.PubMed: 21073468
  6. 6 . Liu JF, Li JX: TAAR1 in Addiction: Looking Beyond the Tip of the Iceberg. Front Pharmacol. 2018 Mar 27;9:279. doi: 10.3389/fphar.2018.00279. eCollection 2018.PubMed: 29636691
  7. 7 . Pei Y, Asif-Malik A, Canales JJ: Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, Neurochemistry, and Clinical Implications. Front Neurosci. 2016 Apr 5;10:148. doi: 10.3389/fnins.2016.00148. eCollection 2016.PubMed: 27092049
  8. 8 . Vyvanse, Canadian Monograph File
  9. 9 . EPAR: Lisdexamfetamine dimesylate File
  10. 10 . WHO Summary: Lisdexamfetamine File