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Methylphenidate

Medical and Pharmacy Editor:

Brand Name: Ritalin, Ritalin SR, Ritalin LA, Aptensio XR, Concerta, Daytrana, Metadate, Metadate CD, Metadate ER, Methylin, Quillivant XR, QuilliChew ER

Generic Name: Methylphenidate

Drug Class: Opioid Analgesics

What Is Methylphenidate and How Does It Work?

Methylphenidate is used to treat attention deficit hyperactivity disorder - ADHD. It works by changing the amounts of certain natural substances in the brain. Methylphenidate belongs to a class of drugs known as stimulants. It can help increase your ability to pay attention, stay focused on an activity, and control behavior problems. It may also help you to organize your tasks and improve listening skills.

Methylphenidate is available under the following different brand names: Ritalin, Ritalin SR, Ritalin LA, Aptensio XR, Concerta, Daytrana, Metadate, Metadate CD, Metadate ER, Methylin, Quillivant XR, and QuilliChew ER.

Dosages of Methylphenidate

Dosage Forms and Strengths

Tablet: Schedule II

Ritalin

  • 5 mg
  • 10 mg
  • 20 mg

Capsule, extended-release: Schedule II

  • 10 mg (Aptensio XR, Ritalin LA, Metadate CD)
  • 15 mg (Aptensio XR)
  • 20 mg (Aptensio XR, Ritalin LA, Metadate CD)
  • 30 mg (Aptensio XR, Ritalin LA, Metadate CD)
  • 40 mg (Aptensio XR, Ritalin LA, Metadate CD)
  • 50 mg (Aptensio XR, Metadate CD)
  • 60 mg (Aptensio XR, Ritalin LA, Metadate CD)

Tablet, extended-release: Schedule II

  • 10 mg (Methylin, generics)
  • 18 mg (Concerta)
  • 20 mg (Methylin, Ritalin SR, generics)
  • 27 mg (Concerta)
  • 36 mg (Concerta)
  • 54 mg (Concerta)

Extended-release tablet, chewable (scored): Schedule II

QuilliChew ER

  • 20 mg
  • 30 mg
  • 40 mg

Tablet, chewable: Schedule II

  • Methylin
  • 2.5 mg
  • 5 mg
  • 10 mg

Transdermal patch: Schedule II

  • Daytrana
  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg

Oral solution: Schedule II

  • Methylin
  • 5 mg/5 mL
  • 10 mg/5 mL

Dosage Considerations – Should be Given as Follows:

  • Chronic abuse can lead to a marked tolerance and psychological dependence, with varying degrees of abnormal behavior.
  • Frank psychotic episodes can occur, especially with parenteral abuse.
  • Withdrawal from abusive use may result in depression.
  • Give cautiously to patients with a history of drug dependence or alcoholism.
  • Potential for drug dependency; withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up.

Attention Deficit Hyperactivity Disorder

Adult

Metadate CD: Initial, 20 mg orally every morning before breakfast; may increase in 10- to 20-mg increments, not to exceed 60 mg/day

Ritalin LA: Initial, 20 mg orally every morning; may adjust dose in weekly 10-mg increments, not to exceed 60 mg/day (patients requiring a lower initial dose may begin with 10 mg)

Concerta: Initial, 18-36 mg orally once/day; may increase by 18-mg increments at weekly intervals; maintenance dose is 18-72 mg/day

Metadate ER, Methylin ER, and Ritalin SR: Duration of action is approximately 8 hours; may use in place of methylphenidate IR tablets when 8-hour dosage of methylphenidate ER and SR tablets corresponds to the titrated 8-hour dosage of methylphenidate IR; not to exceed 60 mg/day

Methylin, Ritalin (immediate-release tablets, chewable tablets, and oral solution): 20-30 mg/day orally divided every 8-12 hours, 30-45 minutes before meals; may gradually increase dose at weekly intervals; some patients may require 40-60 mg/day; in others, 10-15 mg/day may be adequate

Aptensio XR: 10 mg orally once/day in the morning; may increase weekly by 10-mg increments; not to exceed 60 mg/day

QuilliChew ER (chewable extended-release tablets): 20 mg orally every morning initially; may be titrated up or down weekly in increments of 10 mg, 15 mg or 20 mg, not to exceed 60 mg/day

Pediatric:

  • Children under 6 years: Safety and efficacy not established
  • Children 6 years and older:
    • Methylin, Ritalin (immediate-release tablets, chewable tablets, and oral solution): 5 mg orally twice daily 30-45 minutes before breakfast and lunch initially; may increase by 5-10 mg/day at weekly intervals; not to exceed 60 mg/day divided two to three times daily
    • Metadate ER, Methylin ER, and Ritalin SR: May be given in place of immediate-release products once the daily dose is titrated and the titrated 8-hour dosage corresponds to SR or ER tablet size; not to exceed 60 mg/day
    • Metadate CD, Ritalin LA: Initial, 20 mg orally every morning; may increase by 10 mg (Ritalin LA) or 10-20 mg (Metadate CD) once/week to not to exceed 60 mg/day
    • Quillivant XR (6-12 years): 20 mg orally every morning initially; may titrate at weekly intervals by weekly 10- to 20-mg increments; not to exceed 60 mg/day
    • Aptensio XR: 10 mg orally once/day in the morning; may increase weekly by 10-mg increments; not to exceed 60 mg/day
    • QuilliChew ER (chewable extended-release tablets): 20 mg orally every morning initially; may be titrated up or down weekly in increments of 10 mg, 15 mg or 20 mg, not to exceed 60 mg/day
    • Immediate-release weight-based dosing
      • Initial: 0.3 mg/kg/dose orally before breakfast and lunch; may increase by 0.1 mg/kg/dose once/week
      • Maintenance: 0.3-1 mg/kg orally before breakfast and lunch; not to exceed 2 mg/kg/day orally divided every 12 hours

Concerta (methylphenidate-naïve)

  • Trilayer core tablets; extended-release core with immediate release
  • Initial: 18 mg orally once/day; dosage may be increased by 18 mg/day at weekly intervals
  • Do not exceed 54 mg/day in children (6-12 years) and 72 mg/day in adolescents (13-17 years)

Concerta (patients taking methylphenidate)

  • 18 mg orally every morning (if switching from methylphenidate 5 mg orally every 8-12 hours)
  • 36 mg orally every morning (if switching from methylphenidate 10 mg every 8-12 hours)
  • 54 mg orally every morning (if switching from methylphenidate 15 mg orally every 8-12 hours)
  • 72 mg orally every morning (if switching from methylphenidate 20 mg orally every 8-12 hours)

Transdermal patch (Daytrana)

  • Indicated for children aged 6-12 years and adolescents aged 13-17 years
  • Recommended starting dose for patients new to or converting from another formulation of methylphenidate is 10 mg
  • Apply patch on hip 2 hours before desired onset; remove after 9 hours; alternate application site
  • Dose titration, final dosage, and wear time should be individualized according to the needs and response of the patient
  • Titrate to effect for best results, following are manufacturer's recommendations:
    • Week 1: 10 mg (12.5 cm2 patch); releases 1.1 mg/hour
    • Week 2: 15 mg (18.75 cm2 patch); releases 1.6 mg/hour
    • Week 3: 20 mg (25 cm2 patch); releases 2.2 mg/hour
    • Week 4: 30 mg (37.5 cm2 patch); releases 3.3 mg/hour

Narcolepsy

Adult:

  • Methylin, Ritalin (immediate-release tablets, chewable tablets, and oral solution): 20-30 mg/day orally divided every 8-12 hours, 30-45 minutes before meals; some patients may require 40-60 mg/day; in others, 10-15 mg/day may be adequate
  • Metadate ER, Methylin ER, and Ritalin SR: Duration of action is approximately 8 hours; may use in place of methylphenidate IR tablets when 8-hour dosage of methylphenidate ER and SR tablets corresponds to the titrated 8-hour dosage of methylphenidate IR

Pediatric:

Children under 6 years

  • Safety and efficacy not established

Children 6 years and older:

  • Methylin, Ritalin (immediate-release tablets, chewable tablets, and oral solution): 5 mg orally every 12 hours; may increase by 5-10 mg/day weekly; not to exceed 60 mg/day
  • Metadate ER, Methylin ER, and Ritalin SR: May be given in place of immediate-release products once the daily dose is titrated and the titrated 8-hour dosage corresponds to SR or ER tablet size; not to exceed 60 mg/day

What Are Side Effects Associated with Using Methylphenidate?

Common side effects of methylphenidate include:

Postmarketing side effects of methylphenidate reported include:

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What Other Drugs Interact with Methylphenidate?

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

Severe Interactions of methylphenidate include:

  • iobenguane I 123
  • isocarboxazid
  • linezolid
  • phenelzine
  • procarbazine
  • rasagiline
  • safinamide
  • selegiline
  • selegiline transdermal
  • tranylcypromine

Methylphenidate has serious interactions with at least 30 different drugs.

Methylphenidate has moderate interactions with at least 196 different drugs.

Methylphenidate has mild interactions with at least 54 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

What Are Warnings and Precautions for Methylphenidate?

Warnings

  • Chronic abuse can lead to a marked tolerance and psychological dependence, with varying degrees of abnormal behavior.
  • Frank psychotic episodes can occur, especially with parenteral abuse.
  • Withdrawal from abusive use may result in depression.
  • Give cautiously to patients with a history of drug dependence or alcoholism.
  • Potential for drug dependency; withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up.
  • This medication contains methylphenidate. Do not take Ritalin, Ritalin SR, Ritalin LA, Aptensio XR, Concerta, Daytrana, Metadate, Metadate CD, Metadate ER, Methylin, Quillivant XR, or QuilliChew ER if you are allergic to methylphenidate or any ingredients contained in this drug.

Contraindications

Effects of Drug Abuse

  • Chronic abuse can lead to a marked tolerance and psychological dependence, with varying degrees of abnormal behavior.
  • Frank psychotic episodes can occur, especially with parenteral abuse.
  • Withdrawal from abusive use may result in depression.
  • Give cautiously to patients with a history of drug dependence or alcoholism.
  • Potential for drug dependency; withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up.

Short-Term Effects

  • See "What Are Side Effects Associated with Using Methylphenidate?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Methylphenidate?"

Cautions

  • Use caution in hypertension.
  • Stimulants used to treat ADHD are associated with serious cardiovascular events including sudden death, stroke, and heart attack (myocardial infarction [MI]); avoid in patients with structural cardiac abnormalities or other serious heart problems.
  • Stimulants used to treat ADHD are associated with peripheral vasculopathy, including Raynaud's phenomenon; may improve with dose reduction or discontinuation.
  • Difficulties with accommodation and blurring of vision have been reported with stimulant treatment.
  • Sudden deaths, stroke, and myocardial infarction reported in patients with structural cardiac abnormalities or other serious heart problems taking stimulants at usual doses.
  • Patients who develop symptoms such as exertional chest pain, unexplained fainting (syncope), or other symptoms suggestive of cardiac disease during stimulant treatment should undergo a prompt cardiac evaluation.
  • Particular care should be taken in using stimulants to treat ADHD patients with comorbid bipolar disorder because of concern for possible induction of mixed/manic episode in such patients.
  • Aggressive behavior or hostility is often observed in children and adolescents with ADHD; monitor for the appearance of or worsening of aggressive behavior or hostility.
  • Monitor growth during treatment of children with stimulants; may need to interrupt therapy in patients not growing or gaining weight as expected.
  • Stimulants may lower convulsive threshold in patients with prior history of seizure, patients with prior EEG abnormalities in absence of seizures, and very rarely, patients without a history of seizures and no prior EEG evidence of seizures; discontinue therapy in the presence of seizures.
  • Use with caution in patients who use other sympathomimetic drugs.
  • Amphetamines may exacerbate motor and phonic tics and Tourette's syndrome; perform clinical evaluation for tics and Tourette's syndrome in children and their families prior to treating with stimulant medications.
  • Rare instances of prolonged and sometimes painful erections (priapism), sometimes requiring surgical intervention, reported with methylphenidate products; typically not reported during initiation, but often subsequent to an increase in dose; seek immediate medical attention for abnormally sustained or frequent and painful erections.
  • Carefully supervise during withdrawal.
  • Possibility of tolerance, psychologic dependence, and strange behavior.
  • Monitor blood pressure and pulse; consider benefits and risks in patients for whom increase in blood pressure or heart rate would be problem.
  • Central nervous system (CNS) stimulants may cause psychotic or manic symptoms in patients with no prior history, or exacerbation of symptoms in patients with pre-existing psychiatric illness; evaluate for bipolar disorder prior to initiating therapy.
  • Instances of abnormal liver function, ranging from transaminase elevation to severe hepatic injury reported.
  • Do not use Concerta with pre-existing severe gastrointestinal narrowing conditions, including esophageal motility disorders, cystic fibrosis, history of peritonitis, small bowel disease, or chronic intestinal pseudo-obstruction, or Meckel's diverticulum.
  • Transdermal patch:
    • Chemical leukoderma (permanent loss of skin pigmentation) may occur at and around application site; loss of pigmentation, in some cases, has been reported at other sites distant from the application site; patients or their caregivers should watch for new areas of lighter skin, especially under the drug patch, and immediately report these changes to their health care professional; discontinue therapy if it occurs
    • Acts faster on inflamed skin
    • Use of transdermal methylphenidate may lead to contact sensitization; discontinue treatment if contact sensitization is suspected; erythema is commonly seen with use of transdermal methylphenidate and is not by itself an indication of sensitization; suspect sensitization if erythema is accompanied by evidence of a more intense local reaction, like edema, papules, and vesicles and do not significantly improve within 48 hours or spreads beyond patch site
    • Avoid exposing application site to direct external heat sources; heat applied after patch application, increases both the rate and extent of absorption
    • Perform periodic complete blood count (CBC), differential, and platelet counts during prolonged therapy

    Pregnancy and Lactation

    • Use methylphenidate with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done.
    • It is unknown if methylphenidate passes into breast milk; avoid during breastfeeding; use caution.
    Reviewed on 1/26/2018

    References:
    Medscape. Methylphenidate.
    https://reference.medscape.com/drug/ritalin-sr-methylphenidate-342999
    RxList. Aptensio XR Side Effects Drug Center.
    https://www.rxlist.com/aptensio-xr-side-effects-drug-center.htm

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