methylphenidate (oral)

General

methylphenidate (oral)

Pronunciation:
meth-ill-fen-i-date


Descriptive text is not available for this image

Trade Name(s)

  • Adhansia XR
  • Aptensio XR
  • Biphentin Canadian Tradename
  • Concerta
  • Cotempla XR-ODT
  • Foquest Canadian Tradename
  • Jornay PM
  • Metadate CD
  • Methylin
  • Methylin ER
  • Quillichew ER
  • Quillivant XR
  • Ritalin
  • Ritalin LA
  • Ritalin SR Canadian Tradename

methylphenidate (transdermal)

Trade Name(s)

  • Daytrana

Ther. Class.
central nervous system stimulants

Controlled Substance Schedule: II

Indications

  •  Oral, orally distintegrating tablets, and transdermal: Attention-deficit/hyperactivity disorder (ADHD) (adjunct).
  •  Oral only: Narcolepsy.

Action

Produces CNS and respiratory stimulation with weak sympathomimetic activity.

Therapeutic Effect(s):

  • Increased attention span in ADHD.
  • Increased motor activity, mental alertness, and diminished fatigue in narcolepsy.

Pharmacokinetics

Absorption: Slow and incomplete after oral administration; absorption of sustained or extended-release tablet (SR) is delayed and provides continuous release; well absorbed from skin.  Aptensio XR, Metadate CD, Concerta, Ritalin LA– provides initial rapid release followed by a second continuous release (biphasic release).

Distribution: Unknown.

Metabolism and Excretion: Mostly metabolized (80%) by the liver.

Half-life: 2–4 hr.

TIME/ACTION PROFILE (CNS stimulation)

ROUTEONSETPEAKDURATION
POunknown1–3 hr4–6 hr
PO-ERunknown4–7 hr3–12 hr†
Transdermalunknownunknown12 hr
†Depends on formulation.

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity;
  • Hyperexcitable states;
  • Hyperthyroidism;
  • Patients with psychotic personalities or suicidal or homicidal tendencies;
  • Personal or family history of Tourette's syndrome;
  • Glaucoma;
  • Motor tics;
  • Concurrent use or use within 14 days of MAO inhibitors or MAO inhibitor-like drugs (linezolid or methylene blue);
  • Fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase insufficiency;
  • Surgery.

Use Cautiously in:

  • History of cardiovascular disease (sudden death has occurred in children with structural cardiac abnormalities or other serious heart problems);
  • Hypertension;
  • Diabetes mellitus;
  • History of contact sensitization with transdermal product (may be at ↑ risk for systemic sensitization reactions with oral products);
  • History or family history of vitiligo (may be at ↑ risk for loss of skin pigmentation with transdermal product);
  • Continual use (may result in psychological or physical dependence);
  • Seizure disorders (may lower seizure threshold);
  • Concerta product should be used cautiously in patients with esophageal motility disorders or severe GI narrowing (may ↑ the risk of obstruction);
  • OB:   Use during pregnancy only if potential maternal benefit outweighs potential fetal risk; may lead to premature delivery and low birth weight infants;
  • Lactation: Use while breastfeeding only if potential maternal benefit outweighs potential risk to infant;
  • Pedi:  Growth suppression may occur in children with long-term use; children <6 yr (↑ risk of adverse reactions, particularly weight loss in children 4–<6 yr);
  • Geri:  Safety and effectiveness of many of the products have not been evaluated in older adults.

Adverse Reactions/Side Effects

CV: SUDDEN DEATH, hypertension, palpitations, tachycardia, hypotension, peripheral vasculopathy

Derm: contact sensitization (erythema, edema, papules, vesicles) (transdermal), erythema, loss of skin pigmentation (transdermal), rash

EENT: blurred vision, teeth grinding

GI: anorexia, constipation, cramps, diarrhea, dry mouth, metallic taste, nausea, vomiting

GU: priapism

Metabolic: growth suppression (especially with prolonged use), weight loss (especially with prolonged use)

MS: RHABDOMYOLYSIS

Neuro: akathisia, dyskinesia, tics, hyperactivity, insomnia, restlessness, tremor, behavioral disturbances, dizziness, hallucinations, headache, irritability, mania, thought disorder

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), fever, physical dependence, psychological dependence, tolerance

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • Concurrent use with  MAO inhibitors  or  MAO-inhibitor-like drugs, such as  linezolid  or  methylene blue  may result in serious, potentially fatal reactions; wait at least 14 days following discontinuation of MAO inhibitor before initiation of amphetamine mixtures.
  • Drugs that affect serotonergic neurotransmitter systems, including  MAO inhibitors,  tricyclic antidepressants,  SSRIs,  SNRIs,  fentanyl,  buspirone,  tramadol,  lithium, and  triptans  ↑ risk of serotonin syndrome.
  • ↑ sympathomimetic effects with other  adrenergics, including  vasoconstrictors,  decongestants, and  halogenated anesthetics.
  • Metabolism of  warfarin,  phenytoin,  phenobarbital,  primidone,  SSRIs, and  tricyclic   antidepressants  may be ↓ and effects ↑.
  • Avoid concurrent use with  pimozide  (may mask cause of tics).
  • May ↓ the effectiveness of  antihypertensives.
  •  Alcohol  may ↑ rate of release of drug from some methylphenidate formulations (Metadate CD, Ritalin LA)
  • Concurrent use with  risperidone  may ↑ risk of extrapyramidal symptoms.

Drug-Natural Products:

  • Use with caffeine-containing herbs ( guarana , tea, coffee) ↑ stimulant effect.
  •  St. John's wort  may ↑ risk of serotonin syndrome.

Drug-Food:

Excessive use of caffeine-containing foods or beverages (coffee, cola, tea) may cause ↑ CNS stimulation.

Route/Dosage

Attention-Deficit/Hyperactivity Disorder

PO (Adults <65 yr): Immediate-release tablets– 5–20 mg 2–3 times daily. When maintenance dose is determined, may change to extended-release formulation.  Methylphenidate SR– may be used in place of the immediate-release tablets when the 8-hr dose corresponds to the titrated 8-hr dosage of the immediate-release tablets;  Concerta (patients who have not taken methylphenidate previously)– 18–36 mg once daily in the morning initially, may be titrated as needed up to 72 mg/day.  Concerta (patients are currently taking other forms of methylphenidate)– 18 mg once daily in the morning if previous dose was 5 mg 2–3 times daily; 36 mg once daily in the morning if previous dose was 10 mg 2–3 times daily; 54 mg once daily in the morning if previous dose was 15 mg 2–3 times daily; 72 mg once daily in the morning if previous dose was 20 mg 2–3 times daily.  Aptensio XR– 10 mg once daily; may ↑ dose in 10-mg increments at weekly intervals (maximum dose = 60 mg/day).  Quillivant XR and Quillichew ER– 20 mg once daily; may ↑ dose in 10–20-mg increments at weekly intervals (maximum dose = 60 mg/day).  Adhansia XR– 25 mg once daily; may ↑ dose in 10–15-mg increments at weekly intervals (maximum dose = 100 mg/day).  Jornay PM– 20 mg once daily in the evening; may ↑ dose in 20-mg increments at weekly intervals (maximum dose = 100 mg/day).

PO (Children  ≥6 yr [Ritalin LA for children 6–12 yr]): Immediate-release tablets– 0.3 mg/kg/dose or 2.5–5 mg before breakfast and lunch; may ↑ dose by 0.1 mg/kg/dose or by 5–10 mg/day at weekly intervals (not to exceed 60 mg/day or 2 mg/kg/day). When maintenance dose is determined, may change to extended-release formulation.  Methylphenidate SR– may be used in place of the immediate-release tablets when the 8-hr dose corresponds to the titrated 8-hr dosage of the immediate-release tablets;  Ritalin LA (patients who have not taken methylphenidate previously)– 20 mg once daily; may ↑ by 10 mg/day at weekly intervals (max = 60 mg/day);  Ritalin LA (patients currently taking other forms of methylphenidate)– can be used in place of immediate-release twice daily regimen given once daily at same total dose, or in place of SR product at same dose;  Concerta (patients who have not taken methylphenidate previously)– 18 mg once daily in the morning initially, may be titrated as needed up to 54 mg/day (children 6–12 yr old) or up to 72 mg/day (children 13–17 yr old).  Concerta (patients are currently taking other forms of methylphenidate)– 18 mg once daily in the morning if previous dose was 5 mg 2–3 times daily; 36 mg once daily in the morning if previous dose was 10 mg 2–3 times daily; 54 mg once daily in the morning if previous dose was 15 mg 2–3 times daily; 72 mg once daily in the morning if previous dose was 20 mg 2–3 times daily.  Aptensio XR– 10 mg once daily; may ↑ dose in 10-mg increments at weekly intervals (maximum dose = 60 mg/day).  Metadate CD– 20 mg once daily; may ↑ dose in 20-mg increments at weekly intervals (maximum dose = 60 mg/day).  Quillivant XR and Quillichew ER– 20 mg once daily; may ↑ dose in 10–20-mg increments at weekly intervals (maximum dose = 60 mg/day).  Adhansia XR– 25 mg once daily; may ↑ dose in 10–15-mg increments at weekly intervals (maximum dose = 85 mg/day).  Jornay PM– 20 mg once daily in the evening; may ↑ dose in 20-mg increments at weekly intervals (maximum dose = 100 mg/day).  Cotempla XR-ODT– 17.3 mg once daily in the morning; may ↑ dose in 8.6–17.3-mg increments at weekly intervals (maximum dose = 51.8 mg/day).

Transdermal (Children ≥6 yr): Apply one 10-mg patch initially (should be applied 2 hr before desired effect and removed 9 hr after application); may be titrated based on response and tolerability; may ↑ to 15-mg patch after 1 wk, and then to 20-mg patch after another wk, and then to 30-mg patch after another wk.

Narcolepsy

PO (Adults):  Immediate-release tablets– 10 mg 2–3 times/day; maximum dose 60 mg/day.

Availability (generic available)

Immediate-release tablets (Ritalin): 5 mg, 10 mg, 20 mg

Cost:

Generic: 5 mg $73.08/100, 10 mg $104.19/100, 20 mg $149.81/100

Extended-release capsules (Adhansia XR): 25 mg, 35 mg, 45 mg, 55 mg, 70 mg, 85 mg, 100 mg Canadian Tradename

Extended-release capsules (Aptensio XR): 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg

Extended-release capsules (Jornay PM): 20 mg, 40 mg, 60 mg, 80 mg, 100 mg

Extended-release capsules (Metadate CD): 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg

Cost:

Generic: 10 mg $560.21/100, 20 mg $560.21/100, 30 mg $560.21/100, 40 mg $711.52/100, 50 mg $944.19/100, 60 mg $944.19/100

Extended-release capsules (Ritalin LA): 10 mg, 20 mg, 30 mg, 40 mg

Cost:

Generic: 10 mg $630.47/100, 20 mg $630.47/100, 30 mg $644.82/100, 40 mg $66.274/100

Extended-release tablets (Concerta): 18 mg, 27 mg, 36 mg, 54 mg

Cost:

Generic: 18 mg $622.18/100, 27 mg $637.78/100, 36 mg $657.86/100, 54 mg $715.83/100

Extended-release tablets (Metadate ER): 20 mg

Extended-release tablets (Methylin ER): 10 mg, 20 mg

Cost:

Generic: 10 mg $171.91/100, 20 mg $247.21/100

Sustained-release tablets (Ritalin SR): 20 mg Canadian Tradename

Cost: $266.65/100

Extended-release orally-disintegrating tablets (Cotempla XR-ODT): 8.6 mg, 17.3 mg, 25.9 mg

Chewable tablets (Methylin) (grape flavor): 2.5 mg, 5 mg, 10 mg

Cost: 2.5 mg $351.16/100, 5 mg $501.16/100, 10 mg $715.09/100

Extended-release chewable tablets (Quillichew ER): 20 mg, 30 mg, 40 mg

Oral solution (Methylin) (grape flavor): 5 mg/5 mL, 10 mg/5 mL

Cost:

Generic: 5 mg/5 mL $451.61/500 mL, 10 mg/5 mL $643.82/500 mL

Extended-release oral suspension (Quillivant XR) (banana flavor): 25 mg/5 mL

Transdermal patch: 10 mg/9 hr, 15 mg/9 hr, 20 mg/9 hr, 30 mg/9 hr

Cost: All strengths $249.35/30

Assessment

  • Monitor BP, pulse, and respiration before administering and periodically during therapy. Obtain a history (including assessment of family history of sudden death or ventricular arrhythmia), physical exam to assess for cardiac disease, and further evaluation (ECG and echocardiogram), if indicated. If exertional chest pain, unexplained syncope, or other cardiac symptoms occur, evaluate promptly.

    • Monitor closely for behavior change.
    • Assess risk of abuse prior to prescribing. After prescribing, keep accurate prescription records, educate patient and family about risk of abuse, monitor for signs of abuse and overdose, and evaluate need for use periodically during therapy.
    • Screen patients with bipolar disorder for risk of manic episode (comorbid or history of depressive symptoms or a family history of suicide, bipolar disorder, depression) prior to starting therapy.
    • Monitor for signs and symptoms of peripheral vasculopathy (numbness and burning in fingers, digital changes). May require reduction in dose or discontinuation.
    • Pedi:  Monitor growth, both height and weight, in children on long-term therapy. May need to interrupt therapy in patients who are not growing or gaining height or weight as expected.
    • May produce a false sense of euphoria and well-being. Provide frequent rest periods and observe patient for rebound depression after the effects of the medication have worn off.
  • ADHD: Assess children for attention span, impulse control, and interactions with others. Therapy may be interrupted at intervals to determine whether symptoms are sufficient to continue therapy.
  • Narcolepsy: Observe and document frequency of episodes.
  • Transdermal 

    Assess skin for signs of contact sensitization (erythema with edema, papules, or vesicles that does not improve within 48 hr or spreads beyond patch site) during therapy. May lead to systemic sensitization to other forms of methylphenidate (flare-up of previous dermatitis or prior positive patch-test sites, generalized skin eruptions, headache, fever, malaise, arthralgia, diarrhea, vomiting). If contact sensitization develops and oral methylphenidate is instituted, monitor closely.

    • Monitor for signs of skin depigmentation. May cause persistent loss of skin pigmentation at and around the application site and at other sites distant from application site. Discontinue transdermal if depigmentation occurs

Lab Test Considerations:

Monitor CBC, differential, and platelet count periodically in patients receiving prolonged therapy.

Implementation

  • Do not confuse Metadate ER/CD (methylphenidate), or methylphenidate with methadone. Do not confuse Metadate CD with Metadate ER.
  • PO 

    Administer immediate and sustained-release tablets on an empty stomach (30–45 min before a meal). Sustained-release tablets should be swallowed whole; do not break, crush, or chew.  Quillichew ER  chewable tablets may be broken in half.  Aptensio XL, Metadate CD  and  Ritalin LA  capsules may be opened and sprinkled on cool applesauce; entire mixture should be ingested immediately and followed by a drink of water. Do not store for future use.  Concerta  may be administered without regard to food, but must be taken with water, milk, or juice.

    • Shake extended-release oral suspension for 10 sec before administering. May be given with or without food.
  • Transdermal 

    Apply patch to a clean, dry site on the hip which is not oily, damaged, or irritated; do not apply to waistline where tight clothing may rub it. Press firmly in place with palm of hand for 30 sec to make sure of good contact with skin, especially around edges. Alternate site daily. Apply patch 2 hr before desired effect and remove 9 hr after applied; effects last several more hrs. Do not apply or reapply with dressings, tape, or other adhesives. Do not cut patches.

    • If difficulty in separating patch from release liner, tearing, or other damage occurs during removal from liner, discard patch and apply a new patch. Inspect release liner to ensure no adhesive containing medication has transferred to liner; if transfer has occurred, discard patch. Avoid touching adhesive during application; wash hands immediately after application.
    • If patch does not fully adhere or partially detaches, remove and replace with another patch. Wear patch for a total of 9 hr, regardless of number used. Exposure to water during bathing, swimming, or showering may affect patch adherence.
    • Patches may be removed earlier before decreasing dose if an unacceptable loss of appetite or insomnia occurs.
    • Store patches at room temperature in a safe place to prevent abuse and misuse; do not refrigerate or freeze.
    • To remove patch, peel off slowly. An oil-based product (petroleum jelly, olive oil, mineral oil) may be applied gently to facilitate removal. Upon removal, fold so that adhesive side of patch adheres to itself and flush down toilet or dispose of in an appropriate lidded container.

Patient/Family Teaching

  • Instruct patient to take medication as directed. If an oral dose is missed, take the remaining doses for that day at regularly spaced intervals; do not double doses. Take the last dose before 6 pm to minimize the risk of insomnia. Instruct patient not to alter dose without consulting health care professional. Abrupt cessation of high doses may cause extreme fatigue and mental depression. Instruct parent/caregiver to read the  Medication Guide  prior to use and with each Rx refill; new information may be available.

    • Advise patient to check weight 2–3 times weekly and report weight loss to health care professional.
    • Advise patient that methylphenidate is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
    • May cause dizziness or blurred vision. Caution patient to avoid driving or activities requiring alertness until response to medication is known.
    • Inform patient and/or parents that shell of  Concerta  tablet may appear in the stool. This is no cause for concern.
    • Advise patient to avoid using caffeine-containing beverages concurrently with this therapy.
    • Advise patient to notify health care professional if nervousness, insomnia, palpitations, vomiting, skin rash, fever, painful and prolonged erections, or circulation problems (fingers or toes feel numb, cool, painful; fingers or toes change color from pale, to blue, to red) occur.
    • Advise patient and/or parents to notify health care professional of behavioral changes.
    • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
    • Inform patient that health care professional may order periodic holidays from the drug to assess progress and to decrease dependence.
    • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breast feeding. May lead to premature delivery and low birth weight infants. Inform patients who become pregnant while taking methylphenidate of National Pregnancy Registry of ADHD Medications that monitors pregnancy outcomes in women exposed to ADHD medications during pregnancy. Enroll patient by calling 1-866-961-2388 or visit online at https://womensmentalhealth.org/adhd-medications/. Monitor breastfeeding infants for agitation, insomnia, anorexia, and reduced weight gain.
    • Emphasize the importance of routine follow-up exams to monitor progress.
  • Transdermal 

    Encourage parent or caregiver to use the administration chart included in package to monitor application and removal time and disposal method.

    • Caution patient to avoid exposing patch to direct external heat sources (hair dryers, heating pads, electric blankets, heated water beds, etc.). May increase rate and extent of absorption.
    • Inform parent/caregiver that skin redness, itching and small bumps on the skin are common. If swelling or blistering occurs, the patch should not be worn and health care professional notified. Caution parent/caregiver not to apply hydrocortisone or other solutions, creams, ointments, or emollients prior to application.
  • Advise patient referred for MRI test to discuss patch with referring health care professional and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
  • Home Care Issues: Pedi:  Advise parents to notify school nurse of medication regimen.

Evaluation/Desired Outcomes

  • Improved attention span and social interactions in ADHD.
  • Decreased frequency of narcoleptic symptoms.
methylphenidate (oral) is a sample topic from the Davis's Drug Guide.

To view other topics, please or .

Anesthesia Central is an all-in-one web and mobile solution for treating patients before, during, and after surgery. This collection of drugs, procedures, and test information is derived from Davis’s Drug, MGH Clinical Anesthesia Procedures, Pocket Guide to Diagnostic Tests, and PRIME Journals. .