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Dexmethylphenidate

Pronunciation

Pronunciation

(dex meth il FEN i date)

Index Terms

  • Dexmethylphenidate HCl
  • Dexmethylphenidate Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule Extended Release 24 Hour, Oral, as hydrochloride:

Focalin XR: 5 mg [contains fd&c blue #2 (indigotine)]

Focalin XR: 10 mg

Focalin XR: 15 mg [contains fd&c blue #2 (indigotine)]

Focalin XR: 20 mg

Focalin XR: 25 mg [contains fd&c blue #2 (indigotine)]

Focalin XR: 30 mg

Focalin XR: 35 mg, 40 mg [contains fd&c blue #2 (indigotine)]

Generic: 5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg

Tablet, Oral, as hydrochloride:

Focalin: 2.5 mg, 5 mg, 10 mg

Generic: 2.5 mg, 5 mg, 10 mg

Brand Names: U.S.

  • Focalin
  • Focalin XR

Pharmacologic Category

  • Central Nervous System Stimulant

Pharmacology

Dexmethylphenidate is the more active, d-threo-enantiomer, of racemic methylphenidate. It is a CNS stimulant; blocks the reuptake of norepinephrine and dopamine, and increases their release into the extraneuronal space.

Absorption

Immediate release: Rapid; Extended release: Bimodal (with 2 peak concentrations ~4 hours apart)

Distribution

Vd: 2.65 ± 1.11 L/kg

Metabolism

Via de-esterification to inactive metabolite, d-α-phenyl-piperidine acetate (d-ritalinic acid)

Excretion

Urine (90%, primarily as inactive metabolite)

Onset of Action

Rapid, within 1 to 2 hours of an effective dose

Time to Peak

Fasting:

Immediate release: 1 to 1.5 hours; after a high-fat meal: 2.9 hours

Extended release: First peak: 1.5 hours (range: 1 to 4 hours); Second peak: 6.5 hours (range: 4.5 to 7 hours)

Duration of Action

Immediate release: 3 to 5 hours; extended release: 9 to 12 hours (Dopheide 2009)

Half-Life Elimination

Immediate release: Children: 2 to 3 hours; Adults: 2 to 4.5 hours (Note: A few subjects displayed a half-life between 5 to 7 hours)

Protein Binding

Unknown; Racemic methylphenidate: 12% to 15%

Special Populations: Children

Children showed somewhat lower AUCs after administration of dexmethylphenidate immediate release.

Special Populations: Gender

In adults, the AUC of dexmethylphenidate immediate release was 25% to 35% higher in women compared with men. After administration of dexmethylphenidate ER, the first peak (Cmax) was 45% higher in women. Parameters for dexmethylphenidate immediate release were similar for boys and girls.

Use: Labeled Indications

Attention-deficit/hyperactivity disorder: Treatment of attention-deficit/hyperactivity disorder (ADHD) in patients ≥6 years

Contraindications

Marked anxiety, tension, and agitation; hypersensitivity to methylphenidate or any component of the formulation; glaucoma; motor tics; family history or diagnosis of Tourette syndrome; concurrent use with or within 14 days following discontinuation with monoamine oxidase inhibitor (MAOI) therapy.

Dosing: Adult

ADHD: Patients not currently taking methylphenidate or who are on other stimulants: Oral:

Immediate release: Initial: 2.5 mg twice daily; dosage may be adjusted in increments of 2.5 to 5 mg at weekly intervals (maximum dose: 20 mg/day)

Extended release: Initial: 10 mg once daily; dosage may be adjusted in increments of 10 mg at weekly intervals (maximum dose: 40 mg/day)

Conversion to dexmethylphenidate from methylphenidate: Immediate release and extended release: Initial: One-half the total daily dose of racemic methylphenidate

Conversion from dexmethylphenidate immediate release to dexmethylphenidate extended release: Patients currently using dexmethylphenidate immediate-release may be switched to the same daily dose of dexmethylphenidate extended-release.

Dose reductions and discontinuation: Reduce dose or discontinue in patients with paradoxical aggravation of symptoms. Discontinue if no improvement is seen after one month of treatment.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

ADHD: Children ≥6 years and Adolescents: Patients not currently taking methylphenidate or who are on other stimulants: Oral:

Immediate release: Initial: 2.5 mg twice daily; dosage may be adjusted in increments of 2.5 to 5 mg at weekly intervals (maximum dose: 20 mg/day)

Extended release: Initial: 5 mg once daily; dosage may be adjusted in increments of 5 mg at weekly intervals (maximum dose: 30 mg/day)

Conversion to dexmethylphenidate from methylphenidate: Immediate release and extended release: Initial: Refer to adult dosing.

Conversion from dexmethylphenidate immediate release to dexmethylphenidate extended release: Refer to adult dosing.

Dose reductions and discontinuation: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, considering extensive metabolism to inactive compounds, renal insufficiency expected to have minimal effect on kinetics of dexmethylphenidate.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Administration

Extended release: Should be administered once daily in the morning; do not crush, chew, or divide. Capsules may be opened and contents sprinkled over a spoonful of applesauce; consume immediately; do not store for future use.

Immediate release: Should be administered twice daily at least 4 hours apart; may be taken with or without food.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture.

Drug Interactions

Acebrophylline: May enhance the stimulatory effect of CNS Stimulants. Avoid combination

Antacids: May increase the absorption of Dexmethylphenidate. Specifically, antacids may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy

Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy

Fosphenytoin: Dexmethylphenidate may increase the serum concentration of Fosphenytoin. Monitor therapy

H2-Antagonists: May increase the absorption of Dexmethylphenidate. Specifically, H2-antagonists may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination

Ioflupane I 123: Dexmethylphenidate may diminish the diagnostic effect of Ioflupane I 123. Monitor therapy

MAO Inhibitors: May enhance the hypertensive effect of Dexmethylphenidate. Exceptions: Tedizolid. Avoid combination

PHENobarbital: Dexmethylphenidate may increase the serum concentration of PHENobarbital. Monitor therapy

Phenytoin: Dexmethylphenidate may increase the serum concentration of Phenytoin. Monitor therapy

Primidone: Dexmethylphenidate may increase serum concentrations of the active metabolite(s) of Primidone. Specifically, phenobarbital concentrations could become elevated. Dexmethylphenidate may increase the serum concentration of Primidone. Monitor therapy

Proton Pump Inhibitors: May increase the absorption of Dexmethylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy

Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy

Tricyclic Antidepressants: Dexmethylphenidate may enhance the adverse/toxic effect of Tricyclic Antidepressants. Dexmethylphenidate may increase the serum concentration of Tricyclic Antidepressants. Monitor therapy

Vitamin K Antagonists (eg, warfarin): Dexmethylphenidate may increase the serum concentration of Vitamin K Antagonists. Monitor therapy

Adverse Reactions

Actual frequency may be dependent upon dose and/or formulation.

>10%:

Central nervous system: Headache (25% to 39%), insomnia (children 5% to 17%), restlessness (adults 12%), anxiety (5% to 11%)

Gastrointestinal: Appetite decreased (children 30%), xerostomia (adults 7% to 20%), abdominal pain (children 15%)

1% to 10%:

Central nervous system: Dizziness (adults 6%), fever (children 5%), irritability (children ≤5%), depression (children ≤3%), mood swings (children ≤3%)

Dermatologic: Pruritus (children ≤3%)

Gastrointestinal: Nausea (children 9%), dyspepsia (5% to 9%), vomiting (children 2% to 9%), anorexia (children 5% to 7%), pharyngolaryngeal pain (adults 4% to 7%)

Respiratory: Nasal congestion (children ≤5%)

Postmarketing and/or case reports (Limited to important or life-threatening): Accommodation difficulties, anaphylaxis, hypersensitivity reactions

Also refer to Methylphenidate for adverse effects seen with other methylphenidate products.

ALERT: U.S. Boxed Warning

Drug dependence:

Give dexmethylphenidate cautiously to patients with a history of drug dependence or alcoholism. Long-term abusive use can lead to marked tolerance and psychological dependence with varying degrees of abnormal behavior. Frank psychotic episodes can occur, especially with parenteral abuse. Careful supervision is required during drug withdrawal from abusive use because severe depression may occur. Withdrawal following long-term therapeutic use may unmask symptoms of the underlying disorder that may require follow-up.

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular events: CNS stimulant use has been associated with serious cardiovascular events including sudden death in patients with preexisting structural cardiac abnormalities or other serious heart problems (sudden death in children and adolescents; sudden death, stroke, and MI in adults). These products should be avoided in patients with known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, coronary artery disease (adults), or other serious cardiac problems that could increase the risk of sudden death that these conditions alone carry. Patients should be carefully evaluated for cardiac disease prior to initiation of therapy. Patients who develop exertional chest pain, unexplained syncope, or other symptoms suggestive of cardiac disease should be evaluated promptly.

• Hypersensitivity reactions: Hypersensitivity reactions including angioedema and anaphylactic reactions have been observed in patients treated with methylphenidate.

• Peripheral vasculopathy: Stimulants are associated with peripheral vasculopathy, including Raynaud’s phenomenon; signs/symptoms are usually mild and intermittent, and generally improve with dose reduction or discontinuation. Digital ulceration and/or soft tissue breakdown have been observed rarely; monitor for digital changes during therapy and seek further evaluation (eg, rheumatology) if necessary.

• Priapism: Prolonged and painful erections (priapism), sometimes requiring surgical intervention, have been reported (rarely) with methylphenidate and atomoxetine use in pediatric and adult patients. Priapism has been reported to develop after some time on the drug, often subsequent to an increase in dose but also during a period of drug withdrawal (drug holidays or discontinuation). Patients with certain hematological dyscrasias (eg, sickle cell disease), malignancies, perineal trauma, or concomitant use of alcohol, illicit drugs, or other medications associated with priapism may be at increased risk. Patients who develop abnormally sustained or frequent and painful erections should discontinue therapy and seek immediate medical attention. An emergent urological consultation should be obtained in severe cases. Priapism has been associated with different dosage forms and products; it is not known if rechallenge with a different formulation will risk recurrence. Avoidance of stimulants and atomoxetine may be preferred in patients with severe cases that were slow to resolve and/or required detumescence (Eiland 2014).

• Tourette syndrome/tics: Use with caution in patients with Tourette syndrome or other tic disorders. Stimulants may exacerbate tics (motor and phonic) and Tourette syndrome; however, evidence demonstrating increased tics is limited. Evaluate for tics and Tourette syndrome prior to therapy initiation (AACAP [Pliszka 2007]).

• Visual disturbance: Difficulty in accommodation and blurred vision has been reported with the use of stimulants.

Disease-related concerns:

• Abuse potential: [US Boxed Warning]: Use with caution in patients with a history of alcohol or drug dependence. Chronic abusive use can lead to marked tolerance and psychological dependence with varying degrees of abnormal behaviors. Frank psychotic episodes can occur, especially with parenteral abuse.

• Hypertension: CNS stimulants may increase heart rate (mean increase: 3 to 6 bpm) and blood pressure (mean increase: 2 to 4 mm Hg). Use with caution in patients with hypertension and other cardiovascular conditions (eg, heart failure, recent myocardial infarction, ventricular arrhythmia) that might be exacerbated by increases in blood pressure or heart rate.

• Psychiatric disorders: Use with caution in patients with preexisting psychosis; stimulants may exacerbate symptoms of behavior and thought disorder. Use with caution in patients with bipolar disorder; stimulants may induce mixed/manic episodes. New onset psychosis or mania may occur in children or adolescents with stimulant use. Patients presenting with depressive symptoms should be screened for bipolar disorder, including details regarding family history of suicide, bipolar disorder, and depression. Consider discontinuation if such symptoms (eg, delusional thinking, hallucinations, or mania) occur. May be associated with aggressive behavior or hostility (causal relationship not established); monitor for development or worsening of these behaviors.

• Seizure disorder: Limited information exists regarding amphetamine use in seizure disorder (Cortese 2013). Use with caution in patients with a history of seizure disorder; may lower seizure threshold leading to new onset or breakthrough seizure activity.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Pediatric: Appetite suppression may occur, particularly in children. Use of stimulants has been associated with weight loss and slowing of growth rate; monitor growth rate and weight during treatment. Treatment interruption may be necessary in patients who are not increasing in height or gaining weight as expected.

Other warnings/precautions:

• Discontinuation of therapy: Abrupt discontinuation following high doses or for prolonged periods may result in symptoms of withdrawal including severe depression.

Monitoring Parameters

Blood pressure and heart rate (especially in hypertensive patients), CBC with differential, platelet count; signs of peripheral vasculopathy (eg, digital changes); height and weight in children; signs of misuse, abuse, or addiction. Patients should be re-evaluated at appropriate intervals to assess continued need of the medication.

When used for the treatment of ADHD, thoroughly evaluate for cardiovascular risk. Monitor heart rate, blood pressure, and consider obtaining ECG prior to initiation (Vetter 2008).

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. Dexmethylphenidate is the more active d-threo-enantiomer of racemic methylphenidate; refer to Methylphenidate monograph for additional information

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue, anxiety, abdominal pain, headache, weight loss, lack of appetite, insomnia, or dry mouth. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), angina, shortness of breath, severe dizziness, passing out, joint pain, purple patches on skin or mouth, bradycardia, tachycardia, arrhythmia, severe headache, severe nausea, vomiting, blurred vision, vision changes, seizures, dark urine, jaundice, chills, pharyngitis, tremors, abnormal movements, sweating a lot, loss of strength and energy, burning or numbness feeling, change in color of hands or feet from pale to blue or red, temperature sensitivity, wounds on fingers or toes, priapism, urinary retention, change in amount of urine passed, muscle pain, signs of depression (suicidal ideation, anxiety, emotional instability, or illogical thinking), hallucinations, or behavioral changes (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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