A-Z Drug Facts > Methylphenidate Hydrochloride

Methylphenidate Hydrochloride

Pronouncation: (meth-il-FEN-i-date hye-droe-KLOR-ide)
Class: CNS stimulant

Trade Names:
Concerta
- Tablets, extended-release 18 mg
- Tablets, extended-release 27 mg
- Tablets, extended-release 36 mg
- Tablets, extended-release 54 mg

Trade Names:
Daytrana
- Patch, transdermal 10 mg
- Patch, transdermal 15 mg
- Patch, transdermal 20 mg
- Patch, transdermal 30 mg

Trade Names:
Metadate CD
- Capsules, extended-release 10 mg
- Capsules, extended-release 20 mg
- Capsules, extended-release 30 mg

Trade Names:
Metadate ER
- Tablets, extended-release 10 mg
- Tablets, extended-release 20 mg

Trade Names:
Methylin
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg
- Tablets, chewable 2.5 mg
- Tablets, chewable 5 mg
- Tablets, chewable 10 mg
- Oral solution 5 mg per 5 mL
- Oral solution 10 mg per 5 mL

Trade Names:
Methylin ER
- Tablets, extended-release 10 mg
- Tablets, extended-release 20 mg

Trade Names:
Ritalin
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg

Trade Names:
Ritalin LA
- Capsules, extended-release 10 mg
- Capsules, extended-release 20 mg
- Capsules, extended-release 30 mg
- Capsules, extended-release 40 mg

Trade Names:
Ritalin-SR
- Tablets, sustained-release 20 mg

PMS-Methylphenidate (Canada)
ratio-Methylphenidate (Canada)

Pharmacology

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Exact mechanism of action unknown, but presumably activates brain stem cell arousal system and cortex to produce its stimulant effect. Methylphenidate is thought to block reuptake of norepinephrine and dopamine into the presynaptic neuron and increase release of these monoamines into extraneuronal space.

Pharmacokinetics

Absorption

Readily absorbed. Absolute bioavailability is approximately 30% in children. T _max is about 1.9 h for immediate-release (IR) tablets, and 4.7 h for extended-release (ER) and sustained-release (SR) tablets. T _max for Concerta is between 6 and 10 h. T _max for chewable tablets and oral solution is approximately 1 to 2 h. Presence of food delays T _max of all dose forms by 1 to 2 h.

Daytrana : Mean peak plasma level is 39 ng/mL (range, 0 to 114 ng/mL), which varies inversely by patient age (eg, 25 ng/mL in patients 12 yr of age; 53 ng/mL in patients 6 yr of age). Mean peak concentrations of d-methylphenidate are 1.9-fold higher than observed with a once-daily oral formulation over a period of 7.5 to 10.5 h. When applied to inflamed skin, both rate and extent of drug absorption are increased.

Distribution

Protein binding is low (10% to 33%); Vd is about 6 L/kg.

Metabolism

Metabolized by de-esterification to d-ritalinic acid (inactive).

Daytrana : Because the first-pass effect is decreased with transdermal administration, a lower dose on a mg/kg basis may produce higher exposure of d-methylphenidate compared with oral administration.

Elimination

Approximately 90% recovered in urine (approximately 80% as ritalinic acid). The t _½ of methylphenidate from IR tablets is about 2.9 h; about 3.4 h from ER and SR tablets and capsules; 6.8 h from Metadate CD .

Daytrana : Mean elimination t _½ in children 6 to 12 yr of age is approximately 3 to 4 h.

Special Populations

Renal Function Impairment

No experience with transdermal use in these conditions.

Hepatic Function Impairment

No experience with transdermal use in these conditions.

Indications and Usage

Treatment of attention-deficit disorder (ADD)/attention deficit hyperactivity disorder (ADHD); narcolepsy (except Concerta , Daytrana , Metadate CD , Ritalin LA ).

Unlabeled Uses

Depression in medically ill elderly patients; alleviation of neurobehavioral symptoms after traumatic brain injury; improvement in pain control, sedation, or both in patients receiving opiates.

Contraindications

Marked anxiety, agitation, and tension; glaucoma; motor tics; family history or diagnosis of Tourette syndrome; concurrent treatment with MAOIs and within a minimum of 14 days following discontinuation of an MAOI; hypersensitivity to methylphenidate or other components of the products.

Dosage and Administration

IR Tablets, Chewable Tablets, and Oral Solution
Adults

PO 10 to 60 mg/day in 2 to 3 divided doses.

Children older than 6 yr of age

PO 5 mg before breakfast and lunch initially; increase by increments of 5 to 10 mg/wk (max, 60 mg/day).

ER and SR Tablets
Adults and children older than 6 yr of age

PO May be used in place of IR tablets when the 8-h dosage of ER or SR tablets corresponds to the titrated 8-h dose of IR methylphenidate. Administer at 8-h intervals.

Concerta
Adults and children older than 6 yr of age Patients new to methylphenidate

PO 18 mg once daily in morning initially; increase in 18 mg increments/wk (max, 54 mg once daily in children 6 to 12 yr of age; 72 mg once daily in children 13 to 17 yr of age, not to exceed 2 mg/kg/day).

Patients currently receiving methylphenidate

PO Start with 18 mg once daily every morning in patients receiving methylphenidate 5 mg twice daily or 3 times daily; start with 36 mg every morning in patients receiving methylphenidate 10 mg twice daily or 3 times daily; start with 54 mg every morning in patients receiving methylphenidate 15 mg twice daily or 3 times daily. The initial conversion should not exceed 54 mg/day. After conversion, adjust dosages to a max of 72 mg/day once daily in the morning.

Metadate CD
Adults and children older than 6 yr of age

PO 20 mg once daily every morning before breakfast initially; increase in 10 to 20 mg increments/wk (max, 60 mg once daily in the morning).

Ritalin LA
Adults and children older than 6 yr of age Patients new to methylphenidate

PO 10 or 20 mg once daily in morning before breakfast initially; increase in 10 mg increments/wk (max, 60 mg once daily in the morning).

Patients currently receiving methylphenidate

PO Start with 10 mg once daily every morning in patients receiving methylphenidate 5 mg twice daily; start with 20 mg once daily every morning in patients receiving methylphenidate 10 mg twice daily or 20 mg SR; start with 30 mg every morning in patients receiving methylphenidate 15 mg twice daily; start with 40 mg every morning in patients receiving methylphenidate 20 mg twice daily or 40 mg SR; start with 60 mg every morning in patients receiving 30 mg twice daily or 60 mg SR.

Transdermal System
Adults and Children 6 yr of age and older

Transdermal Dosage should be titrated to effect. The patch size may be increased weekly if the response is not maximized. The recommended dosing schedule, is: Week 1: Patch size 12.5 cm ² , which delivers 10 mg per 9 h (1.1 mg/h); Week 2: Patch size 18.75 cm ² , which delivers 15 mg per 9 h (1.6 mg/h); Week 3: Patch size 25 cm ² , which delivers 20 mg per 9 h (2.2 mg/h); Week 4: Patch size 37.5 cm ² , which delivers 30 mg per 9 h (3.3 mg/h).

General Advice

• Tablets
• Administer IR tablets, chewable tablets, and oral solution 30 to 45 min before meals. Administer with food if GI upset occurs.
• Administer chewable tablets with at least 240 mL (8 oz) of water or other fluid to prevent choking.
• Measure and administer prescribed dose of oral solution using dosing syringe, dosing spoon, or dosing cup.
• Administer ER and SR tablets without regard to meals. Administer with food if GI upset occurs.
• Swallow ER and SR tablets whole with the aid of liquids (eg, water, juice). Do not crush, chew, or split ER or SR tablets.
• Administer ER capsules once daily in the morning before breakfast.
• For patients having difficulty swallowing ER capsules, capsules may be carefully opened and beads sprinkled over a spoonful of cool or cold applesauce. The mixture should be consumed immediately without chewing. Fluids (eg, water) should follow intake of applesauce mixture. Do not prepare the drug and applesauce mixture ahead of time and store for future use.

• Transdermal Patch
• Apply patch to hip area 2 h before an effect is needed. Remove patch 9 h after application.
• Apply transdermal patch to a clean, dry area of hip that is not oily, damaged, or irritated.
• Avoid applying transdermal patch to the waistline because clothing may cause patch to rub off.
• If possible, do not apply transdermal patch to same hip on consecutive days.
• Apply transdermal patch immediately after opening pouch and removing protective lining.
• Press transdermal patch firmly in place with the palm of the hand for approximately 30 sec.
• After proper application, bathing, swimming, or showering should not affect transdermal patch adherence.
• If transdermal patch falls off, a new patch may be applied at a different site, but total recommended wear time for the day should remain at 9 h.

Storage/Stability

Store IR, ER, and SR tablets at or below 86°F. Protect from light and moisture. Store ER capsules and transdermal patch at controlled room temperature (59° to 86°F). Protect from moisture. Do not store patches unwrapped. Store chewable tablets and oral solution at controlled room temperature (68° to 77°F). Protect chewable tablets from moisture.

Drug Interactions

Antacids/Acid suppressant ( Ritalin LA only)

Coadministration could alter the release of methylphenidate.

Anticonvulsants (eg, phenobarbital, phenytoin, primidone), coumarin anticoagulants, SSRIs (eg, fluoxetine), tricyclic antidepressants (eg, imipramine)

Plasma levels of these agents may be increased by methylphenidate, increasing the risk of adverse reactions.

Antihypertensive agents (eg, guanethidine)

The antihypertensive effects of guanethidine may be decreased.

Clonidine

Risk of serious adverse reactions may be increased.

MAOIs (eg, phenelzine)

Because of the risk of hypertensive crisis, methylphenidate is contraindicated in patients receiving MAOIs and for a minimum of 14 days after discontinuation of an MAOI.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Angina; cardiac arrhythmias; cerebral arteritis and/or occlusion; changes in pulse and BP; palpitations; tachycardia; thrombocytopenia (postmarketing).

CNS

Nervousness and insomnia (common; 5%); dizziness (2%); drowsiness; dyskinesias; headache; toxic psychosis; transient depressed mood; neuroleptic malignant syndrome (very rare).

Transdermal

Insomnia (13%); tic (7%); affect lability (6%).

Dermatologic

Scalp hair loss.

EENT

Rhinitis (3%); blurred vision, difficulties with visual accommodation (postmarketing).

Transdermal

Nasal congestion (6%).

GI

Anorexia (9%); abdominal pain (7%); vomiting (4%); diarrhea (2%); nausea; weight loss during prolonged therapy.

Transdermal

Nausea, vomiting (12%).

Genitourinary

Dysmenorrhea (2%).

Hematologic

Anemia; leukopenia

Hepatic

Abnormal liver function.

Metabolic-Nutritional

Transdermal

Decreased appetite (26%); weight loss (9%); anorexia (5%).

Respiratory

Upper respiratory tract infection (8%); cough, pharyngitis (4%); sinusitis (3%).

Miscellaneous

Accidental injury (6%); fever (3%); Tourette syndrome (rare); hypersensitivity reactions (eg, arthralgia, erythema multiforme, exfoliative dermatitis, itching, joint pain, purpura, rash, thrombocytopenia, urticaria).

Transdermal

Nasopharyngitis (5%).

Precautions

Warnings Tolerance/psychological dependence may result from chronic abusive use. Psychotic episodes have been reported, especially with parenteral abuse. Monitor during drug withdrawal for severe depression and effects of chronic overactivity. Long-term follow-up is needed. Use with caution in emotionally unstable patients, or patients with a history of drug dependence or alcoholism because these patients may increase doses at own initiative.

Monitor Monitor CBC, differential, and platelet counts periodically during prolonged therapy. Monitor BP in all patients taking methylphenidate. Monitor growth and weight during long-term therapy.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 6 yr of age.

Depression/Fatigue

Do not use to treat depression or fatigue.

Dose reduction/Discontinuation

Reduce dose, or discontinue therapy if necessary, if paradoxical aggravation of symptoms or other adverse reactions occur. If improvement in ADD, ADHD, or narcolepsy symptoms is not observed after appropriate dosage adjustment over a 1-mo period, discontinue the drug. Use of transdermal patch may lead to contact sensitization; discontinue if sensitization occurs.

GI obstruction

Because the Concerta tablet is nondeformable and does not change shape in the GI tract, do not administer to patients with preexisting, severe GI narrowing.

Growth suppression

Has been reported with long-term use of stimulants in children. Consider interrupting treatment in patient who is not growing or gaining weight as expected.

Hypertension/CV disease

Use drug with caution.

Maintenance/Extended treatment

Periodically evaluate long-term usefulness with periods off medication to assess patient's functioning without pharmacotherapy.

Phenylketonuria

Chewable tablets contain phenylalanine: 0.42 mg in 2.5 mg tablet; 0.84 mg in 5 mg tablet; 1.68 mg in 10 mg tablet.

Psychosis

May exacerbate symptoms of behavior disturbance and thought disorders.

Seizures

May lower convulsive threshold and induce seizure activity in patients with history of seizures, prior EEG abnormalities in absence of seizures, and, very rarely, in the absence of history of seizures and no prior EEG abnormalities. Discontinue therapy if seizures occur.

Sudden death

Sudden death has occurred in association with CNS-stimulant treatment at usual doses in children with structural cardiac abnormalities.

Visual disturbances

Blurring of vision and difficulties with accommodation may occur.

Overdosage

Symptoms

Agitation, cardiac arrhythmias, confusion, convulsions, delirium, dry mucous membranes, euphoria, flushing, hallucinations, headache, hyperpyrexia, hyperreflexia, hypertension, muscle twitching, mydriasis, palpitations, sweating, tachycardia, tremors, vomiting.

Patient Information

• Advise patient or caregiver to read patient information leaflet provided with medication before starting therapy and with each refill.
• Advise patient or caregiver that this drug is part of a total treatment program for ADD or ADHD that should also include psychological, educational, and social interventions.
• Advise patient or caregiver to notify school or day care personnel about medication use and administration.
• Advise patient or caregiver that health care provider may periodically change the dose to obtain maximal benefit, and to take as prescribed and not to stop taking or change the dose unless advised by health care provider.
• Advise patient or caregiver that health care provider may periodically discontinue medication to assess behavior and determine need to continue therapy.
• Caution patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
• Advise patient or caregiver to notify health care provider if visual changes, appetite loss, nervousness, or difficulty sleeping occur and are bothersome, or if any unusual or unexplained symptoms or feelings are noted.

• IR Tablets
• Advise patient or caregiver that tablets should be taken 30 to 45 min before meals, but to take with food if stomach upset occurs.
• Advise patient or caregiver that last dose should be taken before 6 PM to avoid sleeplessness.

• ER Tablets
• Advise patient or caregiver that prescribed dose should be taken once daily in the morning with the aid of liquids.
• Caution patient or caregiver that tablets must be swallowed whole and not to crush, chew, or split the tablets.
• Advise patient or caregiver that the tablet shell passes through the intestine and is not absorbed and may appear in their stool. Inform patient that this is normal and not to be concerned.

• ER Capsules
• Advise patient or caregiver that prescribed dose should be taken once daily in the morning before breakfast with the aid of liquids.
• Caution patient or caregiver that capsules should be swallowed whole and not crushed, chewed, or the contents divided.
• If patient has difficulty swallowing capsules, advise patient or caregiver that capsules may be carefully opened and the beads sprinkled over a spoonful of applesauce. The mixture should be consumed immediately without chewing and then followed by fluids (eg, water). Caution patient or caregiver not to prepare drug and applesauce mixture ahead of time and store for future use.

• Chewable Tablet
• Advise patient or caregiver that chewable tablets should be taken 30 to 45 min before a meal with a full glass (8 oz) of water to help prevent choking.
• Instruct patient to immediately seek medical attention if experiencing any of the following after taking the chewable tablet: chest pain, vomiting, or difficulty swallowing or breathing.
• Advise patient with phenylketonuria that the chewable tablet contains phenylalanine.

• Oral Solution
• Advise patient or caregiver that oral solution should be taken 30 to 45 min before a meal.
• Advise patient or caregiver to measure and administer prescribed dose of oral solution using a dosing syringe, dosing spoon, or dosing cup.

• Transdermal Patch
• Advise patient to avoid exposing patch application site to direct external heat sources (eg, heating pads, electric blankets) while wearing the patch.
• Advise patient to cleanse the patch area after removal to remove any remaining adhesive.
• Encourage parent or caregiver to use administration chart included with each carton of transdermal patches to monitor application and removal times, and method of disposal.
• Advise patient that if appetite loss or insomnia occur, to try removing the patch at an earlier time before decreasing the patch size.

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