Pronunciation:

(meth il FEN i date)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Use - Unlabeled/Investigational:

Restrictions:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

Cardiovascular: Angina, cardiac arrhythmia, cerebral arteritis, cerebral occlusion, hyper-/hypotension, palpitation, pulse increase/decrease, tachycardia

Central nervous system: Depression, dizziness, drowsiness, fever, headache, insomnia, nervousness, neuroleptic malignant syndrome (NMS), Tourette's syndrome, toxic psychosis

Dermatologic: Erythema multiforme, exfoliative dermatitis, hair loss, rash, urticaria

Endocrine & metabolic: Growth retardation

Gastrointestinal: Abdominal pain, anorexia, diarrhea, nausea, vomiting, weight loss

Hematologic: Anemia, leukopenia, thrombocytopenic purpura

Hepatic: Liver function tests abnormal, hepatic coma, transaminases increased

Neuromuscular & skeletal: Arthralgia, dyskinesia

Ocular: Blurred vision

Renal: Necrotizing vasculitis

Respiratory: Cough increased, pharyngitis, sinusitis, upper respiratory tract infection

Miscellaneous: Accidental injury, hypersensitivity reactions

Overdosage/Toxicology:

Drug Interactions:

Antihypertensive agents: Effectiveness of antihypertensive agent may be decreased; use with caution

Carbamazepine: Carbamazepine may decrease the serum concentration of methylphenidate.

Clonidine: Severe toxic reactions have been reported in combined use with methylphenidate.

CYP2D6 inhibitors: May increase the levels/effects of methylphenidate. Example inhibitors include chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, and ropinirole.

Linezolid: Due to MAO inhibition (see note on MAO inhibitors), concurrent use with methylphenidate should generally be avoided.

MAO inhibitors: Severe hypertensive episodes have occurred with amphetamine when used in patients receiving nonselective MAO inhibitors; methylphenidate may be less likely to interact, or reactions may be less severe; use with caution only when warranted; wait 14 days following discontinuation of MAO inhibitor.

Phenobarbital: Serum levels may be increased by methylphenidate (in some patients); monitor

Phenytoin: Serum levels may be increased by methylphenidate (in some patients); monitor

Selegiline: When selegiline is used at low dosages (<10 mg/day), an interaction with methylphenidate is less likely than with nonselective MAO inhibitors (see MAO inhibitor information), but theoretically possible; monitor

Sibutramine: Potential for reactions noted with amphetamines (severe hypertension and tachycardia) appears to be low; use with caution

Tricyclic antidepressants: Methylphenidate may increase serum concentrations of some tricyclic agents; clinical reports of toxicity are limited; dosage reduction of tricyclic antidepressants may be required; monitor

Venlafaxine: NMS has been reported in a patient receiving methylphenidate and venlafaxine.

Warfarin: Methylphenidate may decrease metabolism of coumarin anticoagulants; effect has not been confirmed in all studies; monitor INR

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may cause CNS depression).

Food: Food may increase oral absorption; Concerta® formulation is not affected. Food delays early peak and high-fat meals increase Cmax and AUC of Metadate® CD formulation.

Herb/Nutraceutical: Avoid ephedra (may cause hypertension or arrhythmias) and yohimbe (also has CNS stimulatory activity).

Stability:

Immediate release tablet: Do not store above 30°C (86°F); protect from light

Extended release capsule: Store in dose pack provided at 25°C (77°F)

Sustained release tablet: Do not store above 30°C (86°F); protect from moisture

Osmotic controlled release tablet (Concerta®): Store at 25°C (77°F); protect from humidity

Mechanism of Action:

Pharmacodynamics/Kinetics:

Onset of action: Peak effect:

Immediate release tablet: Cerebral stimulation: ~2 hours

Extended release capsule (Metadate® CD): Biphasic; initial peak similar to immediate release product, followed by second rising portion (corresponding to extended release portion)

Sustained release tablet: 4-7 hours

Osmotic release tablet (Concerta®): Initial: 1-2 hours

Duration: Immediate release tablet: 3-6 hours; Sustained release tablet: 8 hours

Absorption: Readily

Metabolism: Hepatic via de-esterification to active metabolite

Half-life elimination: 2-4 hours

Time to peak: Cmax: 6-8 hours

Excretion: Urine (90% as metabolites and unchanged drug)

Dosage:

Children 6 years and Adults: ADHD: Initial: 0.3 mg/kg/dose or 2.5-5 mg/dose given before breakfast and lunch; increase by 0.1 mg/kg/dose or by 5-10 mg/day at weekly intervals; usual dose: 0.5-1 mg/kg/day; maximum dose: 2 mg/kg/day or 90 mg/day

Extended release products:

Metadate™ ER, Methylin™ ER, Ritalin® SR: Duration of action is 8 hours. May be given in place of regular tablets, once the daily dose is titrated using the regular tablets and the titrated 8-hour dosage corresponds to sustained release tablet size.

Metadate® CD, Ritalin® LA: Initial: 20 mg once daily; may be adjusted in 10-20 mg increments at weekly intervals; maximum: 60 mg/day

Concerta®: Duration of action is 12 hours:

Initial dose:

Children not currently taking methylphenidate: 18 mg once daily in the morning

Children currently taking methylphenidate: Note: Dosing based on current regimen and clinical judgment; suggested dosing listed below:

Patients taking methylphenidate 5 mg 2-3 times/day or 20 mg/day sustained release formulation: 18 mg once every morning

Patients taking methylphenidate 10 mg 2-3 times/day or 40 mg/day sustained release formulation: 36 mg once every morning

Patients taking methylphenidate 15 mg 2-3 times/day or 60 mg/day sustained release formulation: 54 mg once every morning

Dose adjustment: May increase dose in increments of 18 mg; dose may be adjusted at weekly intervals. A dosage strength of 27 mg is available for situations in which a dosage between 18-36 mg is desired. Maximum dose should not exceed 2 mg/kg/day or 54 mg/day in children 6-12 years or 72 mg/day in children 13-17 years.

Adults:

Narcolepsy: 10 mg 2-3 times/day, up to 60 mg/day

Depression (unlabeled use): Initial: 2.5 mg every morning before 9 AM; dosage may be increased by 2.5-5 mg every 2-3 days as tolerated to a maximum of 20 mg/day; may be divided (ie, 7 AM and 12 noon), but should not be given after noon; do not use sustained release product

Administration:

Concerta®: Administer dose once daily in the morning. May be taken with or without food, but must be taken with water, milk, or juice.

Metadate® CD, Ritalin® LA: Capsules may be opened and the contents sprinkled onto a small amount (equal to 1 tablespoon) of applesauce. Swallow applesauce without chewing. Do not crush or chew capsule contents.

Monitoring Parameters:

Dietary Considerations:

Patient Education:

Additional Information:

Concerta® is an osmotic controlled release formulation (OROS®) of methylphenidate. The tablet has an immediate-release overcoat that provides an initial dose of methylphenidate within 1 hour. The overcoat covers a trilayer core. The trilayer core is composed of two layers containing the drug and excipients, and one layer of osmotic components. As water from the gastrointestinal tract enters the core, the osmotic components expand and methylphenidate is released.

Metadate® CD capsules contain a mixture of immediate release and extended release beads, designed to release 30% of the dose (6 mg) immediately and 70% (14 mg) over an extended period.

Ritalin® LA uses a combination of immediate release and enteric coated, delayed release beads.

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Dosage Forms:

Capsule, extended release, as hydrochloride:

Metadate® CD: 10 mg, 20 mg, 30 mg

Ritalin® LA: 10 mg, 20 mg, 30 mg, 40 mg

Tablet, as hydrochloride (Methylin™, Ritalin®): 5 mg, 10 mg, 20 mg

Tablet, extended release, as hydrochloride: 20 mg

Concerta®: 18 mg, 27 mg, 36 mg, 54 mg [osmotic controlled release]

Metadate™ ER, Methylin™ ER: 10 mg, 20 mg

Tablet, sustained release, as hydrochloride (Ritalin-SR®): 20 mg

International Brand Names: