Methyl Phenidate

Indications
Oral
Narcolepsy
Adult: 20-30 mg daily in divided doses. Effective dose may be 10-60 mg daily.
Oral
Hyperactivity disorders
Child: Conventional forms: ≥6 yr: Initially, 5 mg once or bid before breakfast or lunch. Increase, as necessary, by 5-10 mg at wkly intervals to a max of 60 mg daily in divided doses. Consider a later dose in the evening if the effect wears off. Discontinue periodically to re-evaluate or if there is no improvement within 1 mth. Modified-release forms: Dose depends on brand.
Transdermal
Hyperactivity disorders
Child: 6-12 yr: Apply once daily to the hip area 2 hr before an effect is needed and remove after a max of 9 hr. Start patient on the lowest patch strength, then titrate according to response. Increase at wkly intervals as needed. Max: 3.3 mg/hr at wk 4.
Contraindications
Marked anxiety, tension, agitation; glaucoma; Tourette's syndrome or tics. Known severe structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac disorders that could increase the risk of sudden death. Extended-release form: Severe hypertension, heart failure, arrhythmia, hyperthyroidism, recent MI or angina.
Warnings / Precautions
Pregnancy and lactation. History of alcohol or drug abuse. Hypertension and other CV disorders that might be exacerbated by increases in BP or heart rate. Pre-existing psychosis or bipolar disorder; monitor for symptoms of aggression or hostility. History of seizure disorder. Children <6 yr (growth suppression); monitor growth during therapy. May impair ability to drive or operate machinery. Transdermal: Avoid exposure of application site to any direct external heat source.
Adverse Reactions
Angina, arrhythmia, cerebral arteritis, cerebral occlusion, changes in BP, MI, necrotising vasculitis, palpitation, pulse changes, tachycardia; depression, dizziness, drowsiness, fever, headache, insomnia, nervousness, neuroleptic malignant syndrome (NMS), Tourette's syndrome, toxic psychosis; erythema multiforme, exfoliative dermatitis, hair loss, rash, urticaria; growth retardation; abdominal pain, anorexia, diarrhoea, nausea, vomiting, weight loss; anaemia, leukopenia, thrombocytopenic purpura, thrombocytopenia; abnormal LFTs, hepatic coma, increased transaminases; arthralgia, dyskinesia; blurred vision, visual accommodation disturbance; cough, pharyngitis, sinusitis, upper respiratory tract infection; accidental injury, hypersensitivity. Transdermal: Insomnia, decreased appetite; nausea; tic, emotional instability; vomiting, anorexia; nasal congestion, nasopharyngitis; weight loss.
Overdose Reactions
Symptoms: Vomiting, tremor, agitation, muscle twitching, hyperpyrexia, hallucinations, tachycardia, mydriasis, palpitations, sweating. Management: No specific antidote; symptomatic supportive. Transdermal: Remove patch and thoroughly cleanse area; absorption may continue in absence of patch.
Drug Interactions
May reduce effects of antihypertensive agents. Reduced serum level with carbamazepine. Increased serum levels or effects with CYP2D6 inhibitors e.g. chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, ropinirole. May increase serum levels of phenytoin, TCAs. Possible severe hypertension and tachycardia with sibutramine. CNS depression with alcohol.
Potentially Fatal: Severe toxic reactions with clonidine. Increased risk of hypertensive crisis with MAOIs.
See Below for More methylphenidate Drug Interactions
Food Interactions
Food may increase oral absorption of methylphenidate. Hypertension or arrhythmias may occur when used with ephedra and additive CNS stimulation may occur with yohimbe.
Mechanism of Actions
Methylphenidate is a central stimulant and indirect-acting sympathomimetic.
Onset: Immediate-release forms/Transdermal: Approx 2 hr. Sustained-release forms: 4-7 hr.
Duration: Immediate-release forms: 3-6 hr. Sustained-release forms: 8 hr. Extended-release forms: 8-12 hr.
Absorption: Oral: Readily absorbed from the GI tract. Food enhances rate of absorption. Peak plasma levels in about 2 hr. Transdermal: Absorption increased when applied to inflamed skin or exposed to heat; absorption continuous for 9 hr after application.
Distribution: Protein-binding: Low. Distributed into breast milk.
Metabolism: Undergoes extensive first-pass metabolism. Via de-esterification to minimally active metabolite. Major metabolite is ritanilic acid.
Excretion: Via urine (90% as metabolites and unchanged drug); via faeces (small amounts); about 2 hr (elimination half-life).
Administration
Methylphenidate (ritalin): Should be taken on an empty stomach. (Take 30-45 min before meals.)
Methylphenidate (concerta): May be taken with or without food. (Swallow whole, do not divide/chew/crush.)
Storage Conditions
Oral: Chewable tablet/Solution: Store at 20-25°C (68-77°F). Extended-release capsule: Store in dose pack provided at 25°C (77°F). Immediate-release/Sustained-release tablet: Do not store above 30°C (86°F). Osmotic-controlled release tablet: Store at 25°C (77°F). Protect from humidity. Transdermal: at 15-30°C (59-86°F). Store in protective pouch.
ATC Classification
N06BA04 - methylphenidate ; Belongs to the class of centrally-acting sympathomimetics. Used as CNS stimulant.
Storage
Oral: Chewable tablet/Solution: Store at 20-25°C (68-77°F). Extended-release capsule: Store in dose pack provided at 25°C (77°F). Immediate-release/Sustained-release tablet: Do not store above 30°C (86°F). Osmotic-controlled release tablet: Store at 25°C (77°F). Protect from humidity. Transdermal: at 15-30°C (59-86°F). Store in protective pouch.
Available As
  • Methyl Phenidate 10 mg
  • Methyl Phenidate 20 mg
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