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

Effect Regions Age Groups Incidences Evidence Type
Decreased appetite US
  • Kind: experimental
    • Percent: 39%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 36%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Decreased apetite US
  • Kind: experimental
    • Percent: 34%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 27%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Decreased apetite US
  • Kind: experimental
    • Percent: 27%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 20%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Abdominal Pain Upper US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Irritability US
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Weight decreased US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Weight decreased US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Increased heart rate US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Feling jittery US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Feelling jittery US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Decreased weight US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Increased blood pressure US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Affect lability US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Restlessness US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Decreased weight US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Erectile Dysfunction US
  • Kind: experimental
    • Percent: 2.6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Pyrexia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Tic US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Energy increased US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Upper Abdominal Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Recommended Actions:
      • Avoid use concurrently and within 14 days of stopping a MAOI.
    • Time Period: Use within 14 days following MAO inhibitor discontinuation
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Route:
      • Oral
    • Hypersensitivity:
      • true
      • Amphetamines
    • Regions: US
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • 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: 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

    Food Interactions

    Avoid antacids. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Antacids like sodium bicarbonate alkalinize the urine; therefore, they may reduce lisdexamfetamine elimination.

    Limit foods and supplements high in vitamin C. Urinary excretion of lisdexamfetamine is elevated when the urine is more acidic. Vitamin C acidifies the urine and, therefore, may increase lisdexamfetamine elimination.

    Take with or without food.