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Look Up > Drugs > Methylphenidate
Methylphenidate
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Restrictions
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(meth il FEN i date)

U.S. Brand Names
Metadate ER®; Methylin™ ER; Ritalin®; Ritalin-SR®

Generic Available

Yes


Canadian Brand Names
PMS-Methylphenidate; Riphenidate

Synonyms
Methylphenidate Hydrochloride

Pharmacological Index

Stimulant


Use

Treatment of attention deficit disorder; symptomatic management of narcolepsy


Restrictions

C-II


Pregnancy Risk Factor

C


Contraindications

Known hypersensitivity or idiosyncrasy to sympathomimetic amines; patients with advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension (stage II or III), hyperthyroidism, glaucoma, agitated states; patients with a history of drug abuse; use during or within 14 days following MAO inhibitor therapy; stimulant medications are contraindicated for use in children with attention deficit/hyperactivity disorders and concomitant Tourette's syndrome or tics


Warnings/Precautions

Safety and efficacy in children <6 years of age not established. Use with caution in patients with bipolar disorder, diabetes mellitus, cardiovascular disease, seizure disorders, insomnia, porphyria, or mild hypertension (stage I). May exacerbate symptoms of behavior and thought disorder in psychotic patients. Potential for drug dependency exists - avoid abrupt discontinuation in patients who have received for prolonged periods. Stimulant use has been associated with growth suppression.


Adverse Reactions

Cardiovascular: Tachycardia, bradycardia, angina, hypertension, hypotension, palpitations, cardiac arrhythmias

Central nervous system: Nervousness, insomnia, headache, dyskinesia, toxic psychosis, Tourette's syndrome, NMS, dizziness, drowsiness

Dermatologic: Rash

Endocrine & metabolic: Growth retardation

Gastrointestinal: Nausea, vomiting, anorexia, nausea, abdominal pain, weight loss

Hematologic: Thrombocytopenia, anemia, leukopenia

Ocular: Blurred vision

Miscellaneous: Hypersensitivity reactions


Overdosage/Toxicology

Symptoms of overdose include vomiting, agitation, tremors, hyperpyrexia, muscle twitching, hallucinations, tachycardia, mydriasis, sweating, palpitations

There is no specific antidote for methylphenidate intoxication and the bulk of the treatment is supportive. Hyperactivity and agitation usually respond to reduced sensory input or benzodiazepines, however, with extreme agitation haloperidol (2-5 mg I.M. for adults) may be required. Hyperthermia is best treated with external cooling measures, or when severe or unresponsive, muscle paralysis with pancuronium may be needed. Hypertension is usually transient and generally does not require treatment unless severe. For diastolic blood pressures >110 mm Hg, a nitroprusside infusion should be initiated. Seizures usually respond to diazepam I.V. and/or phenytoin maintenance regimens.


Drug Interactions

Methylphenidate may antagonize the adrenergic blockade of guanethidine and guanadrel and inhibit the antihypertensive effect; use alternative antihypertensive

Methylphenidate may cause hypertensive effects when used in combination with MAOIs; it is best to avoid this combination

NMS has been reported in a patient receiving methylphenidate and venlafaxine


Mechanism of Action

Mild CNS stimulant; blocks the reuptake mechanism of dopaminergic neurons; appears to stimulate the cerebral cortex and subcortical structures similar to amphetamines


Pharmacodynamics/Kinetics

Immediate release tablet:

Peak cerebral stimulation effect: Within 2 hours

Duration: 3-6 hours

Sustained release tablet:

Peak effect: Within 4-7 hours

Duration: 8 hours

Absorption: Slow and incomplete from GI tract

Metabolism: In liver via hydroxylation to ritolinic acid

Half-life: 2-4 hours

Elimination: In urine as metabolites and unchanged drug with 45% to 50% excreted in feces via bile


Usual Dosage

Oral: (Discontinue periodically to re-evaluate or if no improvement occurs within 1 month)

Adults:

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

Depression: 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


Dietary Considerations

Food may increase oral absorption


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

Up to 10% of patients taking dextroamphetamines or amphetamine-like drugs may present with hypertension. The use of local anesthetic without vasoconstrictor is recommended in these patients.


Patient Information

Take exactly as directed; do not change dosage or discontinue without consulting prescriber. Response may take some time. Do not crush or chew sustained release tablets. Avoid alcohol, caffeine, or other stimulants. Maintain adequate fluid intake (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience decreased appetite or weight loss (small frequent meals may help maintain adequate nutrition); restlessness, impaired judgment, or dizziness, especially during early therapy (use caution when driving or engaging in tasks requiring alertness until response to drug is known); Report unresolved rapid heartbeat; excessive agitation, nervousness, insomnia, tremors, or dizziness; blackened stool; skin rash or irritation; or altered gait or movement. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Do not crush or allow patient to chew sustained release dosage form; to effectively avoid insomnia, dosing should be completed by noon


Dosage Forms

Tablet:

As hydrochloride, sustained release: 20 mg

Extended release: 10 mg, 20 mg


References

Berkovitch M, Pope E, Phillips J, et al, "Pemoline-Associated Fulminant Liver Failure: Testing the Evidence for Causation," Clin Pharmacol Ther, 1995, 57(6):696-8.

Bond WS, "Recognition and Treatment of Attention Deficit Disorder," Clin Pharm, 1987, 6(8):617-24.

Emptage RE and Semla TP, "Depression in the Medically Ill Elderly: A Focus on Methylphenidate," Ann Pharmacother, 1996, 30(2):151-7.

Friberg TR, Gragoudas ES, and Regan CD, "Talc Emboli and Macular Ischemia in Intravenous Drug Abuse," Arch Ophthalmol, 1979, 97(6):1089-91.

Greenhill LL, "Pharmacologic Treatment of Attention Deficit Hyperactivity Disorder," Psychiatr Clin North Am, 1992, 15(1):1-27.

Gurian B and Rosowsky E, "Low-Dose Methylphenidate in the Very Old," J Geriatr Psychiatry Neurol, 1990, 3(3):152-4.

Katon W and Raskind M, "Treatment of Depression in the Medically Ill Elderly With Methylphenidate," Am J Psychiatry, 1980, 137:963-5.

Kelly DP and Aylward GP, "Attention Deficits in School-Aged Children and Adolescents," Pediatr Clin North Am, 1992, 39(3):487-512.

Lazarus LW, Moberg PJ, Langsley PR, et al, "Methylphenidate and Nortriptyline in the Treatment of Poststroke Depression: A Retrospective Comparison," Arch Phys Med Rehabil, 1994, 75(4):403-6.

Parran TV Jr and Jasinski DR, "Intravenous Methylphenidate Abuse: Prototype for Prescription Drug Abuse," Arch Intern Med, 1991, 151(4):781-3.

Pleak RR, "Adverse Effects of Chewing Methylphenidate," Am J Psychiatry, 1995, 152(5):811.

Shaywitz SE and Shaywitz BA, "Diagnosis and Management of Attention Deficit Disorder: A Pediatric Perspective," Pediatr Clin North Am, 1984, 31(2):429-57.

Stecyk O, Loludice TA, Demeter S, et al, "Multiple Organ Failure Resulting From Intravenous Abuse of Methylphenidate Hydrochloride," Ann Emerg Med, 1985, 14(6):597-9.

Wallace AE, Kofoed LL and West AN, "Double-Blind, Placebo-Controlled Trial of Methylphenidate in Older, Depressed, Medically Ill Patients," Am J Psychiatry, 1995, 152(6):929-31.

Warden C and Winger J, "Choreoathetoid Reaction Associated With a Methylphenidate Ingestion in a Toddler," Clin Toxicol, 1995, 33(5):522.

Wilens TE and Biederman J, "The Stimulants," Psychiatr Clin North Am, 1992, 15(1):191-222.


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