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Pronunciation |
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(meth
il FEN i
date) |
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U.S. Brand
Names |
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Metadate ER®; Methylin™ ER;
Ritalin®; Ritalin-SR® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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PMS-Methylphenidate; Riphenidate |
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Synonyms |
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Methylphenidate Hydrochloride |
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Pharmacological Index |
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Stimulant |
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Use |
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Treatment of attention deficit disorder; symptomatic management of narcolepsy
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Restrictions |
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C-II |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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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 |
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Warnings/Precautions |
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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. |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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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.
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Drug
Interactions |
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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
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Mechanism of
Action |
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Mild CNS stimulant; blocks the reuptake mechanism of dopaminergic neurons;
appears to stimulate the cerebral cortex and subcortical structures similar to
amphetamines |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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 |
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Dietary
Considerations |
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Food may increase oral absorption |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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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. |
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Patient
Information |
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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. |
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Nursing
Implications |
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Do not crush or allow patient to chew sustained release dosage form; to
effectively avoid insomnia, dosing should be completed by
noon |
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Dosage Forms |
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Tablet:
As hydrochloride, sustained release: 20 mg
Extended release: 10 mg, 20 mg |
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References |
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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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