METHYLPHENIDATE (D,L)

brands

Class

• Neuroscience-based Nomenclature: dopamine, norepinephrine multimodal (DN-MM)
• Stimulant

METHYLPHENIDATE (D,L) commonly prescribed for

(Bold for FDA approved)

How METHYLPHENIDATE (D,L) works

• Increases norepinephrine and especially dopamine actions by blocking their reuptake

• Enhancement of dopamine and norepinephrine actions in certain brain regions (e.g., dorsolateral prefrontal cortex) may improve attention, concentration, executive function, and wakefulness

• Enhancement of dopamine actions in other brain regions (e.g., basal ganglia) may improve hyperactivity

• Enhancement of dopamine and norepinephrine in yet other brain regions (e.g., medial prefrontal cortex, hypothalamus) may improve depression, fatigue, and sleepiness

How long until METHYLPHENIDATE (D,L) works

• Some immediate effects can be seen with first dosing

• Can take several weeks to attain maximum therapeutic benefit, especially as dose is being titrated

Notable Side Effects

• Insomnia, headache, exacerbation of tics, nervousness, irritability, overstimulation, tremor, dizziness

• Anorexia, nausea, abdominal pain, weight loss, dry mouth

• Peripheral vasculopathy, including Raynaud’s syndrome

• Can temporarily slow normal growth in children (controversial)

• Blurred vision

• Transdermal: application site reactions, including contact sensitization (erythema, edema, papules, vesicles) and chemical leukoderma

Life Threatening Side Effects

• Rare priapism

• Psychotic episodes, especially with parenteral abuse

• Seizures

• Palpitations, tachycardia, hypertension

• Rare neuroleptic malignant syndrome

• Rare activation of hypomania, mania, or suicidal ideation (controversial)

• Cardiovascular adverse effects, sudden death in patients with preexisting cardiac structural abnormalities

weight gain

unusual

sedation

unusual

What to do about METHYLPHENIDATE (D,L) side effects

• Wait

• Adjust dose

• Switch to another formulation of d,lmethylphenidate

• Switch to another agent

• For insomnia, avoid dosing in afternoon/ evening

usual dosage range

• ADHD (oral): varies by formulation; see How to Dose section

• ADHD (transdermal): 10–30 mg/9 hours

• Narcolepsy: 20–60 mg/day in 2–3 divided doses

Dosage Forms

• Ritalin, generic methylphenidate (immediate-release tablet) 5 mg, 10 mg, 20 mg

• Generic methylphenidate (immediaterelease chewable tablet) 2.5 mg, 5 mg, 10 mg

• Methylin (oral solution) 5 mg/5 mL, 10 mg/5 mL

• Ritalin LA (sustained-release capsule) 10 mg, 20 mg, 30 mg, 40 mg

• Methylin ER (sustained-release tablet) 10 mg, 20 mg

• Metadate CD (sustained-release capsule) 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg

• Concerta (sustained-release tablet) 18 mg, 27 mg, 36 mg, 54 mg

• Relexxii (extended-release tablet) 18 mg, 27 mg, 36 mg, 45 mg, 54 mg, 63 mg, 72 mg

• QuilliChew ER (sustained-release chewable tablet) 20 mg scored, 30 mg, 40 mg

• Quillivant XR (extended-release oral suspension) 5 mg/mL

• Aptensio XR (extended-release capsule, multi-layer release) 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg

• Cotempla-XR-ODT (extended-release orally disintegrating tablet) 8.6 mg, 17.3 mg, 25.9 mg

• Jornay PM (extended-release capsule) 20 mg, 40 mg, 60 mg, 80 mg, 100 mg

• Daytrana (transdermal patch) 27 mg/12.5 cm2 (10 mg/9 hours; 1.1 mg/hour), 41.3 mg/18.75 cm2 (15 mg/9 hours; 1.6 mg/hours), 55 mg/25 cm2 (20 mg/9 hours; 2.2 mg/hour), 82.5 mg/37.5 cm2 (30 mg/9 hours; 3.3 mg/hour)

long term use

• Often used long-term for ADHD when ongoing monitoring documents continued efficacy

• Dependence and/or abuse may develop

• Tolerance to therapeutic effects may develop in some patients, in which case a dose increase should be considered

• Long-term stimulant use may be associated with growth suppression in children (controversial)

• Periodic monitoring of weight, blood pressure, heart rate, complete blood count, platelet counts, and liver function may be prudent

habit forming

• High abuse potential, Schedule II drug

• Patients may develop tolerance, psychological dependence

Renal Impairment

• No dose adjustment necessary

Hepatic Impairment

• No dose adjustment necessary

Cardiac Impairment

• Use with caution, particularly in patients with recent myocardial infarction or other conditions that could be negatively affected by increased blood pressure

• Do not use in patients with structural cardiac abnormalities, cardiomyopathy, serious heart arrhythmias, or coronary artery disease

Elderly

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy not established in children under age 6

• Use in young children should be reserved for the expert

• Methylphenidate has acute effects on growth hormone; long-term effects are unknown but weight and height should be monitored during long-term treatment

• Usual dosing has been associated with sudden death in children with structural cardiac abnormalities

• Current recommendations from the American Heart Association are that it is reasonable but not mandatory to obtain an ECG prior to prescribing a stimulant to a child; the American Academy of Pediatrics does not recommend an ECG prior to starting a stimulant for most children

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Infants whose mothers took methylphenidate during pregnancy may experience withdrawal symptoms

• Racemic methylphenidate has been shown to have teratogenic effects in rabbits when given in doses of 200 mg/kg/day throughout organogenesis

• In animal studies, d-methylphenidate caused delayed skeletal ossification and decreased postweaning weight gain in rats; no major malformations occurred in rat or rabbit studies

• Use in women of childbearing potential requires weighing potential benefits to the mother against potential risks to the fetus

• For ADHD patients, methylphenidate should generally be discontinued before anticipated pregnancies

Breast Feeding

• Unknown if methylphenidate is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or formula feed

• If infant shows signs of irritability, drug may need to be discontinued