Description

Simple

A medication used to manage Attention Deficit Hyperactivity Disorder (ADHD) to improve the ability to pay attention and control impulses.

Clinical

A stimulant used in the management of Attention Deficit Hyperactivity Disorder (ADHD).

Overview

Methylphenidate is a central nervous system stimulant used most commonly in the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) and for narcolepsy. Also known as the marketed products Ritalin, Concerta, or Biphentin, methylphenidate is used with other treatment modalities (psychological, educational, cognitive behaviour therapy, etc) to improve the following group of developmentally inappropriate symptoms associated with ADHD: moderate-to-severe distractibility, short attention span, hyperactivity, emotional lability, and impulsivity. Long-acting formulations of psychostimulants such as methylphenidate, [DB01576], and [DB01255] are considered the most effective and widely used treatment for ADHD, and are considered first-line options for children, adolescents, and adults as recommended by CADDRA (Canadian ADHD Resource Alliance). [12] CADDRA recommends the use of methylphenidate due to long term studies, of over twenty years in duration, which show methylphenidate is safe and effective.

While its exact mechanism is unclear, methylphenidate (MPH) has been shown to act as a norepinephrine and dopamine reuptake inhibitor (NDRI), thereby increasing the presence of these neurotransmitters in the extraneuronal space and prolonging their action.[Read more

Pharmacology

Indication

Methylphenidate is indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in patients 6 years of age and older and for the treatment of narcolepsy.

Pharmacodynamic

Methylphenidate is a racemic mixture comprised of the d- and l-isomers. The d-isomer is more pharmacologically active than the l-isomer. Radioligand binding studies demonstrate that binding of methylphenidate in the brain is localized to dopamine-rich areas, in particular in the prefrontal cortex wh... Read more

Mechanism of action

While its exact mechanism is unclear, methylphenidate (MPH) has been shown to act as a norepinephrine and dopamine reuptake inhibitor (NDRI), thereby increasing the presence of these neurotransmitters in the extraneuronal space and prolonging their action.[ Read more

Absorption

Concerta®: Methylphenidate is readily absorbed. Following oral administration of Concerta, plasma methylhphenidate concentrations reach an initial maximum at about 1 hour followed by gradual ascending concentrations over the next 5-9 hours. Mean times to reach peak plasma concentrations across all d... Read more

Protein binding

Concerta: In humans, 15 ± 5% of methylphenidate in the blood is bound to plasma proteins. [15]

Biphentin: In blood, methylphenidate and its metabolites are distributed between plasma (57%) and
erythrocyte... Read more

Volume of distribution

Concerta: Plasma methylphenidate concentrations in adults decline bi-exponentiallyfollowing oral administration.[15]Biphentin: The apparent distribution volume of methylphenidate in children is approximately... Read more

Clearance

The apparent mean systemic clearance after an oral dose is 10.2 and 10.5 L/h/kg in children and adults, respectively for a 0.3 mg/kg dose, and 0.565 L/h/kg after an intravenous dose of the racemate in healthy adult volunteers.[ Read more

Half life

Concerta: The half-life of methylphenidate in adults following oral administration of Concerta® was approximately 3.5 h.[15]

Biphentin: Methylphenidate is eliminated from plasma with a mean half-life of 2.... Read more

Route of elimination

After oral administration of an immediate release formulation of methylphenidate, 78%-97% of the dose is excreted in the urine and 1%-3% in the feces in the form of metabolites within 48-96 hours. Only small quantities ( Read more

Toxicity

Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and d... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Decreased appetite US
  • children
  • Kind: experimental
    • Percent: 25.5
  • Kind: placebo
    • Percent: 4.7
  • Clinical Trial
    Decreased appetite US
    • adolescent
  • Kind: experimental
    • Percent: 25.5
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Decreased appetite US
    • adult
  • Kind: experimental
    • Percent: 25.3
  • Kind: placebo
    • Percent: 6.6
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 22.2
  • Kind: placebo
    • Percent: 15.6
  • Clinical Trial
    Headache US
    • children
  • Kind: experimental
    • Percent: 15.3
  • Kind: placebo
    • Percent: 11.8
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: 14
  • Kind: placebo
    • Percent: 3.8
  • Clinical Trial
    Insomnia US
    • children
  • Kind: experimental
    • Percent: 13.3
  • Kind: placebo
    • Percent: 4.7
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 12.8
  • Kind: placebo
    • Percent: 3.3
  • Clinical Trial
    Headache US
    • adolescent
  • Kind: experimental
    • Percent: 12.4
  • Kind: placebo
    • Percent: 12.5
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 12.3
  • Kind: placebo
    • Percent: 6.1
  • Clinical Trial
    Nausea US
    • children
  • Kind: experimental
    • Percent: 12.2
  • Kind: placebo
    • Percent: 2.4
  • Clinical Trial
    Irritability US
    • adolescent
  • Kind: experimental
    • Percent: 11
  • Kind: placebo
    • Percent: 6.9
  • Clinical Trial
    Vomiting US
    • children
  • Kind: experimental
    • Percent: 10.2
  • Kind: placebo
    • Percent: 4.7
  • Clinical Trial
    Nausea US
    • adolescent
  • Kind: experimental
    • Percent: 9.7
  • Kind: placebo
    • Percent: 2.8
  • Clinical Trial
    Weight decreased US
    • children
  • Kind: experimental
    • Percent: 9.2
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Anxiety US
    • adult
  • Kind: experimental
    • Percent: 8.2
  • Kind: placebo
    • Percent: 2.4
  • Clinical Trial
    Tic US
    • children
  • Kind: experimental
    • Percent: 7.1
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Irritability US
    • children
  • Kind: experimental
    • Percent: 7.1
  • Kind: placebo
    • Percent: 4.7
  • Clinical Trial
    Abdominal Pain US
    • children
  • Kind: experimental
    • Percent: 7.1
  • Kind: placebo
    • Percent: 5.9
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 6.7
  • Kind: placebo
    • Percent: 5.2
  • Clinical Trial
    Weight decreased US
    • adult
  • Kind: experimental
    • Percent: 6.5
  • Kind: placebo
    • Percent: 3.3
  • Clinical Trial
    Insomnia US
    • adolescent
  • Kind: experimental
    • Percent: 6.2
  • Kind: placebo
    • Percent: 2.8
  • Clinical Trial
    Upper Abdominal Pain US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 6.2
  • Kind: placebo
    • Percent: 3.8
  • Clinical Trial
    Affect lability US
    • children
  • Kind: experimental
    • Percent: 6.1
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Irritability US
    • adult
  • Kind: experimental
    • Percent: 5.8
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Dizziness US
    • adolescent
  • Kind: experimental
    • Percent: 5.5
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Weight decreased US
    • adolescent
  • Kind: experimental
    • Percent: 5.5
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Anorexia US
    • children
  • Kind: experimental
    • Percent: 5.1
  • Kind: placebo
    • Percent: 1.2
  • Clinical Trial
    Hyperhidrosis US
    • adult
  • Kind: experimental
    • Percent: 5.1
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Anorexia US
    • adolescent
  • Kind: experimental
    • Percent: 4.8
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Abdominal Pain US
    • adolescent
  • Kind: experimental
    • Percent: 4.8
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Tachycardia US
    • adult
  • Kind: experimental
    • Percent: 4.8
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Initial Insomnia US
    • adult
  • Kind: experimental
    • Percent: 4.3
  • Kind: placebo
    • Percent: 2.8
  • Clinical Trial
    Depressed mood US
    • adult
  • Kind: experimental
    • Percent: 3.9
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Vomiting US
    • adolescent
  • Kind: experimental
    • Percent: 3.4
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial
    Restlessness US
    • adult
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Nervousness US
    • adult
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 0.5
  • Clinical Trial
    Palpitations US
    • adult
  • Kind: experimental
    • Percent: 3.1
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Insomnia US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 2.8
  • Kind: placebo
    • Percent: 0.3
  • Clinical Trial
    Nasopharyngitis US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 2.8
  • Kind: placebo
    • Percent: 2.2
  • Clinical Trial
    Vomiting US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 2.8
  • Kind: placebo
    • Percent: 1.6
  • Clinical Trial
    Tremor US
    • adult
  • Kind: experimental
    • Percent: 2.7
  • Kind: placebo
    • Percent: 0.5
  • Clinical Trial
    Agitation US
    • adult
  • Kind: experimental
    • Percent: 2.2
  • Kind: placebo
    • Percent: 0.5
  • Clinical Trial
    Upper Respiratory Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 2.2
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 2.2
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Pyrexia US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 2.2
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Muscle Tightness US
    • adult
  • Kind: experimental
    • Percent: 1.9
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Cough US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 1.9
  • Kind: placebo
    • Percent: 0.9
  • Clinical Trial
    Dizziness US
    • adolescent
    • children
  • Kind: experimental
    • Percent: 1.9
  • Kind: placebo
    • Percent: 0
  • Clinical Trial
    Oropharyngeal pain US
    • adult
  • Kind: experimental
    • Percent: 1.7
  • Kind: placebo
    • Percent: 1.4
  • Clinical Trial

    Contraindications

    • Dose Form:
      • Capsule, extended release
      • Capsule, film coated, extended release
    • Time Period: Contraindicated during treatment with monoamine oxidase inhibitors, and also within a minimum of 14 days following discontinuation of treatment with a monoamine oxidase inhibitor (hypertensive crises may result).
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Regions: Canada
    • Patient Conditions:
        • Name: Pheochromocytoma
        • Drugbank Id: DBCOND0002904
    • Regions: Canada
    • Patient Conditions:
        • Name: Moderate to Severe Hypertension
        • Drugbank Id: DBCOND0042937
    • Regions: Canada
    • Patient Conditions:
        • Name: Symptomatic cardiovascular disease
        • Drugbank Id: DBCOND0107487
        • Modification Of:
          • Base:
            • Name: Cardiovascular Disease
            • Drugbank Id: DBCOND0028376
          • Severity:
            • Includes:
              • symptomatic
    • Regions: Canada
    • Patient Conditions:
        • Name: Advanced arteriosclerosis
        • Drugbank Id: DBCOND0107486
    • Regions: Canada
    • Patient Conditions:
        • Name: Thyrotoxicosis
        • Drugbank Id: DBCOND0021770
    • Dose Form:
      • extended release
      • chewable tablets
      • oral solution
      • transdermal patch
    • Regions: US
    • Patient Conditions:
        • Name: Motor tics
        • Drugbank Id: DBCOND0107725
    • Dose Form:
      • extended release
      • chewable tablets
      • oral solution
      • transdermal patch
    • Regions: US
    • Patient Conditions:
        • Name: Family history of Tourette's syndrome
        • Drugbank Id: DBCOND0107726
    • Dose Form:
      • extended release
      • chewable tablets
      • oral solution
      • transdermal patch
    • Regions: US
    • Patient Conditions:
        • Name: Tourette's Syndrome
        • Drugbank Id: DBCOND0028246
    • Regions: US
    • Patient Conditions:
        • Name: Anxiety
        • Drugbank Id: DBCOND0018828
    • Hypersensitivity:
      • methylphenidate
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Tension
        • Drugbank Id: DBCOND0018825
    • Regions: US
    • Patient Conditions:
        • Name: Agitation
        • Drugbank Id: DBCOND0017779
    • Regions: US
    • Patient Conditions:
        • Name: Glaucoma
        • Drugbank Id: DBCOND0010013

    Food Interactions

    Avoid alcohol. Co-administration with alcohol may cause a "dose-dumping" effect with some extended-release formulations of methylphenidate. It may also potentiate the CNS effects of methylphenidate.

    Take with or without food. Patients may take methylphenidate with food to alleviate GI upset.