Contents

Methylphenidate HCl

Indication

Treatment of attention-deficit hyperactivity disorder (ADHD). The efficacy of Concerta in the treatment of ADHD was established in controlled trials of children and adolescents aged 6-17 and adults aged 18-65 who met DSM-IV criteria for ADHD.Methylphenidate should be used as a part of a comprehensive treatment program where remedial measures alone prove insufficient. A comprehensive treatment program for the treatment of ADHD may include other measures (psychological, educational, social) for patients with this disorder. Diagnosis must be made according to DSM-IV criteria or the guidelines in ICD-10 and should be based on a complete history and evaluation of the patient.Methylphenidate is not indicated in all patients with ADHD and the decision to use the drug must be based on a very thorough assessment of the severity of the patient’s symptoms. Stimulants are not intended for use in the patient who exhibits symptoms secondary to environmental factors and/or other primary psychiatric disorders including psychosis. Appropriate educational placement is essential and psychosocial intervention is often helpful.Specific etiology of the syndrome is unknown and there is no single diagnostic test. Adequate diagnosis requires the use of medical and special psychological, educational, and social resources. Learning may or may not be impaired.

Dosage / Direction For Use

Administer orally once daily. As the effect has been shown to be present 12 hrs after dosing, Concerta should be taken in the morning.Concerta should be swallowed whole with the aid of liquid and must not be chewed, divided or crushed (see Cautions for Usage). Concerta may be administered with or without food (see Pharmacokinetics under Actions).Patients New to Methylphenidate: The recommended starting dose of Concerta for patients who are not currently taking methylphenidate, or stimulants other than methylphenidate, is 18 mg once daily for children and adolescents and 18 or 36 mg once daily for adults.Patients Currently Using Methylphenidate: The recommended dose of Concerta for patients who are currently taking methylphenidate twice daily or 3 times daily, at doses of 10-60 mg/day is as follows: On previous methylphenidate 5 mg twice daily or 3 times daily, the recommended starting dose for Concerta is 18 mg every morning. The recommended dose of Concerta for patients currently taking methylphenidate HCl 10 mg twice or 3 times daily is 36 mg. The recommended dose of Concerta for patients currently taking methylphenidate HCl 15 mg twice or 3 times daily is 54 mg. The recommended dose of Concerta for patients currently taking methylphenidate HCl 20 mg twice or 3 times daily is 72 mg.Clinical judgement should be used when selecting the dose for patients currently taking methylphenidate in other regimens.Dose Titration: Dosage should be individualized according to the needs and responses of the patient. Doses may be increased in 18 mg increments at weekly intervals. Daily dosages above 54 mg in children, 72 mg in adolescents and 108 mg in adults have not been studied and are not recommended. Maintenance/Extended Treatment: The long-term use of methylphenidate has not been systematically evaluated in controlled trials. The physician who elects to use methylphenidate for extended periods in patients with ADHD should periodically re-evaluate the long-term usefulness of the drug for the individual patient with trials off medication to assess the patient’s functioning without pharmacotherapy. Dose Reduction and Discontinuation: If paradoxical aggravation of symptoms or other adverse events occur, the dosage should be reduced, or if necessary, Concerta should be discontinued.

Overdosage

Symptoms: Signs and symptoms of methylphenidate overdosage, resulting principally from overstimulation of the central nervous system and from excessive sympathomimetic effects, may include the following: Vomiting, agitation, muscle twitching, convulsion, grand mal convulsion, confusional state, hallucinations (auditory and/or visual), hyperhidrosis, headache, pyrexia, tachycardia, palpitations, increased heart rate, sinus arrhythmia, hypertension, mydriasis and dry mouth.Treatment: Consists of appropriate supportive measures. The patient must be protected against self-injury and against external stimuli that would aggravate overstimulation already present. Gastric contents may be evacuated by gastric lavage as indicated. Before performing gastric lavage, control agitation and seizures if present and protect the airway. Other measures to detoxify the gut include administration of activated charcoal and a cathartic. Intensive care must be provided to maintain adequate circulation and respiratory exchange; external cooling procedures may be required for pyrexia.Efficacy of peritoneal dialysis or extracorporeal hemodialysis for Concerta overdosage has not been established.The prolonged release of methylphenidate from Concerta should be considered when treating patients with overdose.

Administration

May be taken with or without food: Swallow whole, do not divide/chew/crush.

Contraindication

Hypersensitivity. Marked anxiety; tension & agitation; glaucoma; family history or diagnosis of Tourette’s syndrome. Treatment w/ MAOIs or w/in a min of 14 days following discontinuation of a MAOI. Childn <6 yr.

Special Precaution

Onset or exacerbation of motor & verbal tics; growth suppression w/ long-term therapy; preexisting severe GI narrowing; dysphagia; depression & fatigue. May exacerbate symptoms of behavior disturbance & thought disorder in psychotic patients; patients whose underlying medical conditions may be compromised by increases in BP or heart rate; history of drug dependence/alcoholism & seizures. Pregnancy & lactation.

Adverse Reactions

Headache, stomachache, loss of appetite & insomnia. Aggravation reaction, asthenia, HTN, nausea, vomiting, dyspepsia, wt loss, twitching (tics), dizziness, emotional lability, somnolence, anxiety, depression, nervousness, hostility & rash.

Drug Interaction

MAOIs. Vasopressor agents; coumarin anticoagulants, anticonvulsants & antidepressants. Clonidine & other centrally-acting α-2 agents.

Storage

Store at temperatures not exceeding 25°C.

Description

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Action

Pharmacology: Pharmacodynamics: Methylphenidate HCl is a central nervous system stimulant. The mode of therapeutic action in ADHD is not known. Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Methylphenidate is a racemic mixture comprised of the d- and l-isomers. The d-isomers are more pharmacologically active than the l-isomer.Pharmacokinetics: Absorption: Methylphenidate is readily absorbed. Following oral administration of Concerta to adults, plasma methylphenidate concentrations increase rapidly reaching an initial maximum at about 1-2 hrs, then increase gradually over the next several hrs. Peak plasma concentrations are achieved at about 6-8 hrs after which a gradual decrease in plasma levels of methylphenidate begins. Concerta once daily minimizes the fluctuations between peak and trough concentrations associated with immediate-release methylphenidate 3 times daily. The relative bioavailability of Concerta once daily and methylphenidate 3 times daily in adults is comparable.