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Drug Profile

The information on this site is intended to supplement and enhance, not replace, the advice of a physician who is familiar with your medical history. Decisions about your health should always be made ONLY after detailed conversation with your doctor.

Limited Use [what does this mean?]
Generic drug name: methylphenidate [extended or sustained release] (meth ill FEN i date)
Brand name(s): APTENSIO XR, CONCERTA, COTEMPLA XR-ODT, DAYTRANA [TRANSDERMAL], METADATE CD, METADATE ER, METHYLIN ER, QUILLICHEW, QUILLIVANT XR, RITALIN LA, RITALIN SR
GENERIC: not available FAMILY: Central Nervous System Stimulators
Find the drug label by searching at DailyMed.

Limited Use [what does this mean?]
Generic drug name: methylphenidate [immediate release] (meth ill FEN i date)
Brand name(s): METADATE, METHYLIN, QUILLICHEW ER, RITALIN
GENERIC: not available FAMILY: Central Nervous System Stimulators
Find the drug label by searching at DailyMed.

Pregnancy and Breast-feeding Warnings [top]

Pregnancy Warning

Methylphenidate caused malformations in animal studies. It also caused DNA damage (a precursor to some tumors) as well as a rare liver tumor in mice. Because of the potential for serious adverse effects to the fetus, these drugs should not be used by pregnant women.

Breast-feeding Warning

No information is available from either human or animal studies. It is likely that this drug, like many drugs, is excreted in human milk, and, because of the potential for adverse effects in nursing infants, you should not take this drug while nursing.

Safety Warnings For This Drug [top]

FDA BLACK BOX WARNING

DRUG ABUSE AND DEPENDENCE

Methylphenidate should be given cautiously to emotionally unstable patients, such as those with a history of drug dependence or alcoholism, because such patients may increase dosage on their own initiative.

Chronically abusive use can lead to marked tolerance and psychic dependence with varying degrees of abnormal behavior. Frank psychotic episodes can occur, especially with parenteral abuse. Careful supervision is required during drug withdrawal, since severe depression as well as the effects of chronic overactivity can be unmasked. Long-term follow-up may be required because of the patient’s basic personality disturbances.

Drug treatment is not suitable for all children with attention deficit hyperactivity disorder (ADHD). Drug treatment is not intended for use in patients who exhibit symptoms of the disorder that result primarily from environmental factors (school, home), learning disabilities, and/or other psychiatric disorders, including psychosis.

The FDA has extensively strengthened the warnings section of the professional product labels of stimulant ADHD drugs that contain methylphenidate to warn not only of sudden death and serious cardiovascular problems but also of psychiatric problems, stunted growth, seizures and visual disturbances.

Facts About This Drug [top]

These drugs are listed as Limited Use (offers limited benefit or benefits only certain people or conditions).

Methylphenidate (APTENSIO XR, CONCERTA, COTEMPLA XR-ODT, DAYTRANA [transdermal], METADATE CD, METADATE ER, METHYLIN, METHYLIN ER, QUILLIVANT XR, RITALIN, RITALIN LA, RITALIN-SR) is approved by the Food and Drug Administration (FDA) for the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Methylphenidate increases the neurotransmitters dopamine and...

These drugs are listed as Limited Use (offers limited benefit or benefits only certain people or conditions).

Methylphenidate (APTENSIO XR, CONCERTA, COTEMPLA XR-ODT, DAYTRANA [transdermal], METADATE CD, METADATE ER, METHYLIN, METHYLIN ER, QUILLIVANT XR, RITALIN, RITALIN LA, RITALIN-SR) is approved by the Food and Drug Administration (FDA) for the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Methylphenidate increases the neurotransmitters dopamine and norepinephrine.[1] This drug is not a cure for either ADHD or narcolepsy.

The chemical structure of methylphenidate resembles that of amphetamine ("speed"-like drugs).[2] Federal law classifies methylphenidate as a Schedule II controlled substance that requires a new, handwritten prescription for each new and refill prescription.

Narcolepsy is uncontrolled sleepiness, especially during the day. It is a rare condition. There is a lack of well-documented evidence that the benefits of using most stimulants to treat narcolepsy outweigh the risks.[3]

Tics, a neurological condition that waxes and wanes, occur mostly in children ages 7 to 13. There are reports of methylphenidate both decreasing vocal tics and worsening tics.[4]

Adverse effects

Little information on the long-term safety and effectiveness of methylphenidate is available. The safety and efficacy of using methylphenidate for children under age 6 have not been established.

Common adverse effects of methylphenidate are headache, stomachache and loss of appetite. Short-acting forms are more apt to cause dizziness, and long-acting forms are more likely to cause insomnia.[5] The shell of the extended-release tablets may be observed in the stool. This does not mean the methylphenidate was not absorbed.

A 2013 article published in Prescrire International, a respected and independent source of drug information, reported cases of dystonia (in which muscles contract involuntarily) and trismus (commonly known as lockjaw) with methylphenidate use.[6]

Suppression of growth

Suppression of growth (weight or height) has been reported with the long-term use of stimulants in children.[1] Prescrire International published an article in October 2011 examining the effects of methylphenidate on suppression of growth in children. According to the article, the data examined in the studies showed that growth was affected in children, and this effect occurred especially during the first year of treatment.[7]

Psychiatric problems

Methylphenidate may induce psychosis with mood changes and hallucinations, especially when used for a long time and in high doses.4 Symptoms may include seeing or hearing things, believing things that are not real or becoming suspicious. Other psychiatric problems — such as new or worsened behavior and problems with clear thinking, bipolar illness and aggressive behavior or hostility — have been reported in patients taking methylphenidate and other stimulant medications.[8]

Methylphenidate should not be used in patients with marked anxiety, tension or agitation because it can aggravate these symptoms. It also should never be used in patents who have glaucoma, tics (involuntary repetitive movements) or Tourette’s syndrome (a neurological disorder that occurs in childhood or adolescence and is characterized by tics and involuntary vocalizations).

In 2015, Health Canada, an agency similar to the FDA, updated the warning section of the labels of drugs used to treat ADHD on the risk of suicidal thoughts and behaviors. The advisory stated that Health Canada had received reports that included thoughts of suicide, suicide attempts and, in a very small number of cases, suicide.[9]

Heart-related problems

There also have been reports of several heart-related problems in individuals taking usual doses of ADHD medications, including sudden death in patients who have an underlying serious heart problem or defect, stroke and heart attack in adults, and increased blood pressure and heart rate.[8]

In 2015, Prescrire International published an article on reports of pulmonary hypertension (high blood pressure in the lung that can later weaken the heart) and heart valve disorders associated with methylphenidate use in both children and adults.[10]

Priapsim

Prolonged and painful erections, sometimes requiring surgery, have been reported in both pediatric and adult patients using methylphenidate. This typically occurs after some time on the drug, often after a dose increase or during a period when the drug is stopped (a drug holiday). Patients who develop abnormally long or frequent and painful erections should seek immediate medical attention.[11]

Studies show...

In 2004, Prescrire International examined the benefits of sustained-release methylphenidate tablets compared with short-acting forms for the drug. The article stated that the effects of sustained-release forms taken once daily were not significantly different from those of short-acting methylphenidate tablets taken three times a day. The sustained-release formulation cannot be cut, crushed or chewed.[12]

Nearly one-half of almost 13,000 poisoning exposures to methylphenidate involved children under age 6 who usually swallowed prescriptions belonging to others. One-third of the cases in children from ages 6 to 12 involved the child’s own medication.[2] About one-third of cases of those over age 12 involved their own prescription, and some poisonings were suicide attempts. Many incidents involved unintentionally administering an incorrect dose.[13]

In 2012, the Danish Medicines Agency published a report on new data on the safety of methylphenidate when used in the treatment of ADHD. Since the first report was published in 2010, the agency continues to receive reports of adverse reactions associated with the use of methylphenidate. According to the information in the 2012 report, the most common adverse effects were of the nervous system and psychiatric symptoms, and the majority of the new cases were reported in children.[14]

In 2020, Lancet published results of research showing that use of methylphenidate was associated with an increased risk of seizure during the first 30 days after starting the drug. The increased risk was not found beyond 30 days of continued treatment with the drug.[15]

Regulatory actions surrounding methylphenidate

2007: The FDA directed manufacturers of ADHD drugs to develop Medication Guides. When a prescription for any ADHD drug is filled, pharmacists must distribute an FDA-approved Medication Guide that both alerts patients to the possible cardiovascular and psychiatric risks associated with the medicines and describes precautions that can be taken to help patients use the medication more safely.[16]

2013: The FDA issued an advisory that methylphenidate therapy has been associated in postmarketing reports with peripheral vasculopathy (damage to blood vessels outside of the heart), including Raynaud’s phenomenon. These disorders typically affect fingers and toes.[17] Raynaud’s phenomenon is characterized by a pale to blue to red sequence of color changes in the fingers or toes, most commonly after exposure to cold. Fingers or toes also may feel numb or painful.

The FDA also issued a safety alert warning that methylphenidate products may be associated with rare cases of priapism (prolonged and sometimes painful erections). The drug product label and Medication Guide for these products were revised.[18]

2015: The FDA issued a safety warning that permanent, disfiguring loss of skin color is associated with methylphenidate transdermal system (DAYTRANA; known as the methylphenidate patch).[19]

Before You Use This Drug [top]

Do not use if you have or have had:

  • agitation, anxiety, or tension
  • mental depression
  • glaucoma
  • motor tics other than Tourette’s syndrome

Tell your doctor if you have or have had:

  • allergies, including to lactose or aspartame (NutraSweet)
  • anorexia, bulimia, or failure to thrive[5]
  • dependence on alcohol or drugs
  • epilepsy
  • gastrointestinal obstructions
  • growth retardation[5]
  • heart problems
  • high blood pressure
  • phenylketonuria (PKU)
  • pregnancy or are breast-feeding
  • psychosis
  • seizures
  • difficulty swallowing[5]
  • Tourette’s syndrome, including family history, or other motor tics

Tell your doctor about any other drugs you take, including aspirin, herbs, vitamins, and other nonprescription products.

When You Use This Drug [top]

  • Avoid using alcohol and recreational drugs.
  • Avoid or limit caffeine.[5]
  • Do not take more than the prescribed amount because of possible habituation.
  • Do not drive, ride a bicycle, operate hazardous equipment, or perform dangerous activities if you experience dizziness or euphoria or if your narcolepsy is not controlled.

For ADHD:

  • Reduce distractions, for example, sit toward the front of classrooms, or make lists of several small deadlines at work.[20]
  • Select schools that have structured rules and expectations, and that provide regular feedback.[20]
  • Recognize that your appetite may be greatest late in the day as methylphenidate wears off.
  • Seek education about ADHD and counseling for skills development, or join support groups.
  • Augment treatment with biofeedback, cognitive-behavioral therapy, educational skills training, parenting skills, and/or social skills.
  • Try parent counseling to increase self-confidence, and learn to discipline consistently and appropriately, reinforcing good behavior with immediate rewards, reducing disruptive behavior, and decreasing family stress.[20],[21]

For narcolepsy:

  • Avoid alcohol and drugs that cause drowsiness. These include amitriptyline, benzodiazepines, buspirone, chlorpromazine, diphenhydramine, hydrocodone, meprobamate, methyldopa, phenobarbital, and propranolol.[22]
  • Do not drive until sleepiness is controlled. Avoid other dangerous activities.
  • Try scheduling naps.
  • Tell any doctor, dentist, emergency help, or pharmacist you see that you take methylphenidate.

How to Use This Drug [top]

  • If you miss a dose, take it as soon as you remember, but skip it if it is almost time for the next dose or it is after 6 p.m. Then take any remaining doses for that day at regularly spaced intervals. Do not take double doses.
  • Do not share your medication with others.
  • Take the drug at the same time(s) each day.
  • The initial dose of methylphenidate is taken in the morning. For immediate-release forms, doses may be repeated once or twice more, at least four hours apart. The last dose usually is taken by late afternoon or at least by 6 p.m. to avoid insomnia. Taking with food may prevent abdominal pain and insomnia. However, avoid high-fat meals, which may delay absorption and cause erratic effects.
  • Chew chewable tablets with at least eight ounces of fluid. Fluid is necessary to prevent tablets from swelling in your throat and causing choking.
  • Swallow extended-release tablets (Concerta) whole with or without food. It is preferable to be consistent about taking with or without food. Do not chew, crush, or divide.
  • Swallow methylphenidate (METADATE CD) capsules whole with fluid, or empty entire capsule contents onto soft food, such as applesauce, jelly, or ketchup. Do not crush or chew. Swallow immediately. Follow with fluids. Do not store mixtures for future use.
  • Store at room temperature with lid on tightly. Do not store in the bathroom. Do not expose to heat, moisture, or strong light.
  • If you take more than prescribed, call the poison control center (800-222-1222) immediately.

Interactions with Other Drugs [top]

The following drugs, biologics (e.g., vaccines, therapeutic antibodies), or foods are listed in Evaluations of Drug Interactions 2003 as causing “highly clinically significant” or “clinically significant” interactions when used together with any of the drugs in this section. In some sections with multiple drugs, the interaction may have been reported for one but not all drugs in this section, but we include the interaction because the drugs in this section are similar to one another. We have also included potentially serious interactions listed in the drug’s FDA-approved professional package insert or in published medical journal articles. There may be other drugs, especially those in the families of drugs listed below, that also will react with this drug to cause severe adverse effects. Make sure to tell your doctor and pharmacist the drugs you are taking and tell them if you are taking any of these interacting drugs:

Use of methylphenidate with monoamine oxidase (MAO) inhibitors may cause a dangerous increase in blood pressure called hypertensive crisis. Do not take within two weeks of taking methylphenidate: deprenyl, ELDEPRYL, furazolidone, FUROXONE, isocarboxazid, MARPLAN, MATULANE, NARDIL, PARNATE, phenelzine, procarbazine, selegiline, tranylcypromine.

Methylphenidates may inhibit anticoagulants. Your doctor may do more tests and adjust doses of: COUMADIN, warfarin.

This drug may antagonize the effect of methylphenidate, and your dose may be adjusted: HALDOL, haloperidol.

Methylphenidate may cause tics. If tics are present, methylphenidate should be discontinued to determine if the medication is the cause before using it for tics: ORAP, pimozide.

Although generally classified as less apt to be clinically significant, methylphenidate can affect a number of other drugs that may result in the need for adjustments in doses.

Methylphenidate may increase anticonvulsants, and dose of anticonvulsant may be lowered: DILANTIN, LUMINAL, MYSOLINE, phenobarbital, phenytoin, primidone.

Use of other stimulants may add to the effects of methylphenidate. These include caffeine, ephedrine (in numerous over-the-counter medications, herbs, and club drugs), phenylpropanolamine (removed from market in 2000), pseudoephedrine (present in numerous cough and cold products), SUDAFED.

Methylphenidate may decrease the effectiveness of drugs used for high blood pressure, and doses may be adjusted: all blood pressure pills (see p. 45), ACE inhibitors (see p. 91), beta-blockers (see p. 87), calcium channel blockers (see p. 96), and reserpine.

Methylphenidate with certain antidepressants may require less antidepressant: desipramine, imipramine, NORPRAMIN, PERTOFRANE, SSRIs, TOFRANIL, tricyclics.

Many other drugs may interact with methylphenidate, such as AVANDAMET, GLUCOVANCE, METAGLIP, metformin, orlistat, and XENICAL. Check any concerns with your doctor or pharmacist.

Adverse Effects [top]

Call your doctor immediately if you experience:

  • unusual bleeding or bruising
  • blood pressure increase
  • chest pain
  • confusion
  • convulsions
  • muscle cramps
  • delusions
  • feelings of estrangement, being automated, or extremities changing size
  • hallucinations
  • fast or irregular heartbeat
  • fever
  • mood changes
  • uncontrolled movements of body
  • pinpoint red spots, hives, or rash on skin
  • black, bloody, or tarry stools
  • tics
  • bloody urine
  • blurred or changed vision
  • vocal outbursts that are uncontrolled
  • weight loss

Signs of overdose:

  • agitation
  • blood pressure increase
  • fast, pounding, or irregular heartbeat
  • extreme confusion
  • dry mouth
  • false sense of well-being
  • fever
  • hallucination
  • severe headache
  • muscle twitch
  • enlarged pupils
  • overactive reflexes
  • increased sweating
  • shaking or trembling
  • vomiting

If you suspect an overdose, call this number to contact your poison control center: (800) 222-1222.

Call your doctor if these symptoms continue:

  • appetite decrease
  • coughing increase
  • dizziness
  • drowsiness
  • hair pulling, nail biting, or skin picking
  • headache
  • nausea
  • nervousness
  • sleeping problems
  • stomach pain

Call your doctor immediately if these symptoms occur after you stop taking this drug:

  • depression
  • unusual behavior
  • unusual tiredness or weakness

Periodic Tests[top]

Ask your doctor which of these tests should be done periodically while you are taking this drug:

By your doctor:

  • blood pressure and pulse
  • complete blood count, differential and platelet counts
  • monitoring of growth, both height and weight gain, in children
  • reassessment of continued need for therapy, dose of medication, and signs of dependence or abuse
  • Test of Variables of Attention

By parent(s):

  • rating scales, such as Achenbach’s Child Behavior Checklist, Conner’s Parent Questionnaire

By teacher(s):

  • rating scales, such as Child Attention Problems, Conner’s Teacher Rating Scale

last reviewed May 31, 2021