Dosing and uses of Focalin, Focalin XR (dexmethylphenidate)
Adult dosage forms and strengths
tablet
- 2.5mg
- 5mg
- 10mg
capsule, extended-release
- 5mg
- 10mg
- 15mg
- 20mg
- 25mg
- 30mg
- 35mg
- 40mg
Attention Deficit Hyperactivity Disorder
Focalin
- Initial: 2.5 PO twice daily; may increase in 2.5- to 5-mg increments qWeek if warranted
- Not to exceed 20 mg/day
Focalin Xr
- Not taking Focalin or methylphenidate: 10 mg PO qDay initially; may increase in 10-mg increments qWeek if warranted; not to exceed 20 mg/day
- Switch from Focalin: Administer the same total daily dose as Focalin but administer qDay
- Switch from methylphenidate: Initiate with half total daily dose of methylphenidate and administer qDay; not to exceed 40 mg/day
Dosing Modifications
Hepatic impairment: Safety and efficacy not established
Renal impairment: Not studied; expected to have minimal effects on kinetics of dexmethylphenidate considering its extensive metabolism to inactive compounds
Administration
Administer capsules once daily and tablets at least 4 hours apart
Pediatric dosage forms and strengths
tablet
- 2.5mg
- 5mg
- 10mg
capsule, extended-release
- 5mg
- 10mg
- 15mg
- 20mg
- 25mg
- 30mg
- 35mg
- 40mg
Attention Deficit Hyperactivity Disorder
<6 years
- Safety and efficacy not established
≥6 years (Focalin)
- Initial: 2.5 PO twice daily; may increase in 2.5- to 5-mg increments qWeek if warranted
- Not to exceed 20 mg/day
≥6 years (Focalin XR)
- Not taking Focalin or methylphenidate: 5 mg PO qDay initially; may increase in 5-mg increments qWeek if warranted; not to exceed 30 mg/day
- Switch from Focalin: Administer the same total daily dose as Focalin but administer qDay
- Switch from methylphenidate: Initiate with half total daily dose of methylphenidate and administer qDay; not to exceed 30 mg/day
Focalin, Focalin XR (dexmethylphenidate) adverse (side) effects
>10%
Abdominal pain (15%)
Headache (25-39%)
Insomnia (5-17%)
Restlessness (12%)
Anxiety (5-11%)
1-10%
Anorexia (5-7%)
Fever (5%)
Dizziness (6%)
Mood swings (<3%)
Nausea (9%)
Pruritus (<3%)
Pharyngolaryngeal pain (4-7%)
Irritability (5%)
Depression (<3%)
Dyspepsia (5-9%)
Postmarketing Reports
Anaphylaxis
Hypersensitivity reactions
Rhabdomyolysis
Warnings
Black box 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
Withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up
Contraindications
Hypersensitivity to methylphenidate; reactions may include angioedema and anaphylaxis
Notable tension and agitation, glaucoma, Tourette syndrome, motor tics, anxiety
MAOIs: Risk of severe hypertensive reaction; do not use within 14 days of taking MAOI
Cautions
Should be used as part of a comprehensive treatment program of attention deficit disorder
Caution in patients with history of drug dependence or alcoholism, HTN, preexisting structural cardiac abnormalities
Discontinue if no improvement after 1 month
Reevaluate need for treatment q6Week
Associated with peripheral vasculopathy, including Raynaud phenomenon
Difficulties with visual accommodation and blurring of vision have been reported with stimulant treatment
Do not use for depression, fatigue
Sudden deaths, stroke, and myocardial infarction reported in adults taking stimulants at usual doses
Patients who develop symptoms such as exertional chest pain, unexplained 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, and has been reported
Monitor growth of children ages 7 to 10 years during treatment 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
Use with caution in patients with hypertension and other vascular conditions, including heart failure, ventricular arrhythmia; recent myocardial infarction; CNS stimulants may increase heart rate and blood pressure
Hypersensitivity reactions, including anaphylactic reactions and angioedema reported in patients treated with methylphenidate
Use caution in patients with preexisting psychosis; stimulants may exacerbate symptoms of behavior and though disorder; use with caution in patients with bipolar disorder; stimulants may induce mixed/manic episodes; new onset of psychosis or mania may occur in children or adolescents with stimulant use; patients presenting with depressive symptoms should be screened for bipolar disorder, including family history of suicide, bipolar disorder, and depression; consider discontinuation of therapy if symptoms of psychosis develop
Appetite suppression may occur in children; stimulant use is associated with weight loss and slowing growth rate; monitor growth rate and weight during treatment; consider interrupting therapy in patients who are not increasing in height or gaining weight as expected
Abrupt discontinuation following high doses or prolonged periods may result in symptoms of wighdrawal including severe depression
Pregnancy and lactation
Pregnancy category: C
Lactation: Excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Focalin, Focalin XR (dexmethylphenidate)
Mechanism of action
The more pharmacologically active CNS stimulant of the d-threo-enantiomers; blocks reuptake of norepinephrine and dopamine, causing an increase of their release into the extraneuronal space
Absorption
Bioavailability: 22-25%
Onset of action: 12hr (extended release)
Peak plasma time: 1-1.5 hr (Focalin XR: 2nd peak at 6.5 hr)
Distribution
Protein bound: 12-25%
Vd: 1.54-3.76 L/kg
Metabolism
Metabolized by deesterification
Metabolites: Inactive
Elimination
Half-life: 2-4.5 hr (adults); 2-3 hr (children)
Excretion: Urine (90%)
