Description
Generic Name
Methylphenidate (available as methylphenidate hydrochloride and, in the patch, as methylphenidate base)
Active Ingredient
Methylphenidate hydrochloride
Chemical Name
Methylphenidate hydrochloride is chemically described as methyl α-phenyl-2-piperidineacetate hydrochloride.
Methylphenidate hydrochloride is a white, fine crystalline powder. Its solutions are slightly acidic. It is freely soluble in water and in methanol, soluble in alcohol, and slightly soluble in chloroform and acetone. It has a molecular weight of about 269.77.
Medication Classification
Methylphenidate is a central nervous system (CNS) stimulant. It works by blocking the reuptake of the brain chemicals norepinephrine and dopamine, which increases their activity in the brain. This action is thought to improve attention and reduce impulsive, hyperactive behavior.
Methylphenidate is a Schedule II (CII) controlled substance under U.S. federal law.
Indications
Methylphenidate is indicated for:
- Attention-deficit hyperactivity disorder (ADHD): As part of a total treatment program in children 6 years of age and older, adolescents, and, for some products, adults.
- Narcolepsy: For certain immediate-release formulations, to help manage excessive daytime sleepiness.
Dosage Forms and Available Strengths
- Dosage Forms:
-
- Immediate-release oral tablets
- Extended-release oral tablets
- Extended-release oral capsules
- Chewable tablets
- Oral solution
- Transdermal patch (applied to the skin)
- Routes of Administration: Oral and transdermal
- Common Strengths (vary by product and manufacturer):
-
- Immediate-release tablets: 5 mg, 10 mg, and 20 mg
- Extended-release tablets: 10 mg, 18 mg, 20 mg, 27 mg, 36 mg, and 54 mg
- Extended-release capsules: 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, and 60 mg
- Chewable tablets: 2.5 mg, 5 mg, and 10 mg
- Oral solution: 5 mg per 5 mL and 10 mg per 5 mL
- Transdermal patch: 10 mg, 15 mg, 20 mg, and 30 mg (delivered over 9 hours)
Inactive Ingredients
Inactive ingredients vary by dosage form and manufacturer. Tablets may contain lactose, corn starch, magnesium stearate, talc, and colorants. Extended-release products use controlled-release systems and may contain cellulose polymers, polyethylene oxide, and other release-controlling agents. Chewable tablets may contain mannitol, artificial sweeteners, and flavoring, and some contain phenylalanine. The oral solution may contain glycerin, sucralose, and flavoring. The transdermal patch contains an adhesive layer and backing film. Refer to the specific product packaging or your pharmacist for exact ingredient details, especially if you have allergies, intolerances, or phenylketonuria (PKU).
Dosage & Administration
Important: Take or use methylphenidate exactly as prescribed by your healthcare provider. Your provider will start with a low dose and adjust it slowly based on how well it works and how you tolerate it. Use the lowest effective dose. Do not change your dose or stop taking it without medical guidance.
How to Take or Use Methylphenidate
- Immediate-release tablets: Swallow the tablet with water. These are usually taken two or three times daily, often 30 to 45 minutes before meals.
- Extended-release tablets: Swallow the tablet whole with water. Do not crush, chew, or divide it. Some extended-release tablets have an outer shell that may pass in the stool; this is normal and does not mean the medicine did not work.
- Extended-release capsules: Swallow the capsule whole. If you have trouble swallowing, some products may be opened and the beads sprinkled onto a small amount of soft food, such as applesauce, and taken right away. Do not chew or crush the beads. Follow the specific product instructions.
- Chewable tablets: Chew the tablet fully and drink at least 8 ounces of water or other liquid with each dose to avoid choking or throat blockage.
- Oral solution: Measure each dose carefully using the calibrated device provided. Do not use a household spoon, as it may give the wrong amount.
- Transdermal patch: Apply the patch to clean, dry skin on the hip, as directed. Rotate application sites. Apply it about 2 hours before an effect is needed, and remove it after the time set by your provider (usually 9 hours). Avoid direct heat on the patch, such as heating pads, which can increase how much medicine enters the body.
General Dosing Principles
- Dosing is individualized based on age, the condition being treated, and your response.
- Different formulations are not interchangeable on a milligram-for-milligram basis. Do not switch products or forms without your provider's guidance.
- Your provider will set the exact dose, strength, and schedule for your situation.
Food Considerations
Immediate-release oral forms are often taken before meals. Some extended-release products may be taken with or without food, though food can affect how certain forms release the medicine. Follow the instructions for your specific product. Avoid alcohol, which may change how some extended-release forms release the drug.
Missed Dose Instructions
- If you miss a dose, take it as soon as you remember, unless it is late in the day.
- Do not take methylphenidate late in the afternoon or evening, as it may cause trouble sleeping.
- If it is close to your next scheduled dose, skip the missed dose and continue your regular schedule.
- Do not take two doses at once to make up for a missed dose.
- For the transdermal patch, follow your provider's instructions if a patch is missed or falls off.
Storage
- Store oral forms at 20° to 25°C (68° to 77°F), with brief excursions permitted between 15° to 30°C (59° to 86°F).
- Keep in a tightly closed container, away from moisture, heat, and light.
- Store transdermal patches flat, in their sealed pouches, and do not refrigerate or freeze them.
- Keep out of the reach of children. Accidental use by a child can be dangerous.
Disposal
Because methylphenidate is a controlled substance, store and dispose of it carefully to prevent theft, misuse, or accidental exposure. Dispose of unused or expired medication through a drug take-back program when possible. If no take-back program is available, follow current FDA guidance for safe household disposal. Used transdermal patches still contain active drug; fold each used patch in half so the sticky sides meet, then discard it as directed on the product label to keep it away from children and pets.
Special Instructions
Children: Methylphenidate is used as part of a total treatment program for ADHD in children 6 years and older. It is not recommended for children under 6. Your provider may check your child's height and weight during treatment. Keep the medication out of the reach of children. If a child swallows more than prescribed, seek emergency care immediately.
Elderly Patients: Methylphenidate has not been widely studied in older adults. If used, a provider may start at a lower dose and monitor closely for effects on heart rate and blood pressure.
Patients with Heart Conditions: Use with caution. Tell your provider about any heart problems before starting, since stimulants can raise heart rate and blood pressure.
Caregivers: Give the medication exactly as prescribed. Watch for chest pain, fainting, unusual behavior, agitation, or signs of an allergic reaction, and seek care right away if these occur. Keep the medication secured and out of sight, as it is a target for misuse.
Tapering and Discontinuation
- Methylphenidate can usually be stopped without a gradual taper, but talk to your provider before stopping, especially after long-term or high-dose use.
- Stopping suddenly after prolonged use may unmask depression or cause withdrawal-like symptoms, such as extreme tiredness, sleep changes, or low mood.
- Your provider may monitor you after stopping to watch for these effects.
- Tell your provider if you notice unusual symptoms after reducing or stopping the medication.
Overdose Warning
An overdose of methylphenidate can be serious and may be fatal. Symptoms of overdose may include:
- Agitation, restlessness, or confusion
- Tremors or muscle twitching
- Seizures
- A fast, pounding, or irregular heartbeat
- High blood pressure
- High body temperature (hyperthermia)
- Flushing, sweating, or headache
- Hallucinations
- Loss of consciousness or coma
In case of a suspected overdose, call the Poison Control Center at 1-800-222-1222 or seek emergency medical care immediately. If an overdose involves the transdermal patch, remove the patch right away.
Side Effects
Serious Side Effects Requiring Immediate Medical Attention
Stop taking methylphenidate and seek emergency care or contact your healthcare provider right away if you experience any of the following:
- Cardiovascular events: Chest pain, shortness of breath, fainting, or a fast, pounding, or irregular heartbeat. Sudden death, stroke, and heart attack have been reported, mainly in people with existing heart problems.
- Psychiatric symptoms: New or worsening agitation, aggression, hostility, anxiety, or panic. New psychotic symptoms, such as hearing voices, believing things that are not true, or being suspicious, or new manic symptoms, may occur even in people with no prior history.
- Priapism: A painful erection lasting more than 4 hours. This is a medical emergency that requires prompt treatment.
- Peripheral vasculopathy, including Raynaud's phenomenon: Fingers or toes that feel numb, cool, or painful, or that change color to pale, blue, or red. In rare cases, skin breakdown or sores can occur.
- Serious allergic reactions: Rash, hives, swelling of the face, lips, tongue, or throat, or trouble breathing or swallowing. The transdermal patch may also cause serious skin reactions or a lasting loss of skin color at or beyond the application site.
- Growth suppression in children: Slowed growth in height or weight during long-term treatment.
- Seizures: Especially in people with a history of seizures.
- Vision changes: Blurred vision or difficulty focusing.
Common Side Effects
The following side effects may occur and are not always cause for urgent concern. Talk to your healthcare provider if they persist or become bothersome:
- Decreased appetite
- Trouble sleeping (insomnia)
- Headache
- Stomachache or abdominal pain
- Nausea
- Increased heart rate
- Dry mouth
- Dizziness
- Nervousness or irritability
- Weight loss
For the transdermal patch, mild redness or itching at the application site may also occur.
This is not a complete list of possible side effects. Contact your healthcare provider for guidance about any symptoms that concern you.
To report suspected adverse reactions, contact the FDA at 1-800-FDA-1088
Warnings & Precautions
FDA Boxed Warning: Abuse and Dependence
- Methylphenidate is a CNS stimulant with a high potential for abuse and dependence.
- Assess the risk of abuse before prescribing, and monitor for signs of abuse and dependence throughout treatment.
- Misuse and abuse of CNS stimulants, including methylphenidate, can lead to overdose and death. This risk is higher with intravenous misuse and when the medication is combined with other substances.
- Keep the medication in a secure place to prevent misuse or theft.
Cardiovascular Risk
Stimulants can raise blood pressure and heart rate. Sudden death has been reported in people with structural heart problems or other serious heart conditions. Before starting methylphenidate, your provider should check for heart disease and review your medical and family history. Tell your provider right away if you develop chest pain, shortness of breath, or fainting during treatment.
Psychiatric Risk
Methylphenidate may cause new or worsening psychiatric symptoms, including psychosis, mania, aggression, or hostility. It may also worsen symptoms of bipolar disorder. Report any new or unusual changes in mood, thinking, or behavior to your provider.
Conditions to Disclose to Your Healthcare Provider
Before taking methylphenidate, tell your healthcare provider if you have or have had any of the following:
- Heart problems, heart defects, high blood pressure, or an irregular heartbeat
- A family history of sudden death or heart rhythm problems
- Mental health conditions, including depression, bipolar disorder, psychosis, or suicidal thoughts
- A history of tics or Tourette's syndrome
- Seizures or a seizure disorder
- Circulation problems in the fingers or toes
- Glaucoma
- Thyroid problems
- Liver or kidney problems
- A history of alcohol, prescription medicine, or street drug abuse or dependence
- Pregnancy or plans to become pregnant
- Breastfeeding or plans to breastfeed
Contraindications
Do not take methylphenidate if you:
- Have a known hypersensitivity to methylphenidate or any component of the formulation
- Are taking, or have taken within the past 14 days, a monoamine oxidase inhibitor (MAOI), because this can cause a dangerous rise in blood pressure
Drug Interactions
Tell your healthcare provider and pharmacist about all medications, supplements, and herbal products you take. Key interactions include:
- Monoamine oxidase inhibitors (MAOIs): Combined use, or use within 14 days of an MAOI, can cause a serious and possibly fatal rise in blood pressure. This combination is contraindicated.
- Antihypertensive medicines: Methylphenidate may reduce the effect of blood pressure medicines. Your provider may need to monitor your blood pressure and adjust treatment.
- Anticoagulants (blood thinners): Methylphenidate may increase the levels or effects of certain blood thinners, such as warfarin. Your provider may need to monitor and adjust your dose.
- Other CNS stimulants: Combining methylphenidate with other stimulants may increase the risk of high blood pressure, fast heart rate, and other side effects.
- Serotonergic drugs: Combined use with certain antidepressants or other serotonergic medicines may, in rare cases, increase the risk of serotonin syndrome.
- Certain seizure medicines and some antidepressants: Methylphenidate may affect their levels; dose adjustments may be needed.
Monitoring Requirements
Your healthcare provider may monitor:
- Heart rate and blood pressure, before and during treatment
- Growth (height and weight) in children during long-term use
- New or worsening psychiatric symptoms, such as agitation, aggression, mood changes, or psychosis
- Signs of circulation problems in the fingers and toes
- Signs of abuse, misuse, or dependence throughout treatment
- Your overall response to treatment and any side effects
Abuse, Dependence, and Misuse Warnings
Methylphenidate is a Schedule II controlled substance.
- Methylphenidate may be a target for people who abuse prescription medicines or street drugs.
- Physical and psychological dependence can develop, particularly with higher doses or prolonged use.
- Tolerance may develop over time.
- Do not increase your dose on your own.
- Do not sell or give away methylphenidate. Doing so may harm others and is against the law.
- Misusing this medication, including crushing, snorting, or injecting it, can cause serious harm, overdose, and death.
Long-Term Use Considerations
- If long-term treatment is needed, your provider should regularly reassess whether it is still appropriate.
- Children on long-term treatment should have their growth monitored, and treatment may be adjusted if growth slows.
- Dependence may develop with continued use, so any decision to stop should be made with your provider.
- Your provider may periodically pause treatment to assess whether it is still needed.
Patient Counseling Information
Safe Medication Use
- Take or use methylphenidate exactly as prescribed. Do not take more than directed or use it more often than prescribed.
- Swallow extended-release tablets and capsules whole unless your product allows sprinkling; never crush or chew extended-release forms.
- Drink plenty of liquid with chewable tablets to avoid choking.
- Measure the oral solution with the device provided, not a household spoon.
- Apply and remove the transdermal patch exactly as directed, and avoid direct heat on the patch.
- Do not stop or change your dose without talking to your provider first.
- Do not share methylphenidate with anyone else. Sharing is dangerous and against the law.
- Keep it in a safe, secure place, away from children and others, to prevent accidental exposure, misuse, or theft.
- Read the FDA-approved Medication Guide provided with your prescription.
Risk Prevention
- Cardiovascular risk: Tell your provider about any heart problems or a family history of sudden death. Report chest pain, shortness of breath, or fainting right away.
- Mental health: Watch for new or worsening mood, thinking, or behavior changes, including aggression, agitation, or thoughts of self-harm, and report these promptly.
- Driving and machinery: Methylphenidate can affect your alertness or cause dizziness. Do not drive or operate machinery until you know how it affects you.
- Alcohol: Avoid alcohol, which can add to side effects and may affect how some extended-release forms release the drug.
- Pregnancy: Tell your provider if you are pregnant or plan to become pregnant, so treatment can be managed safely.
- Breastfeeding: Methylphenidate can pass into breast milk. Talk to your provider before breastfeeding while taking it.
- All medicines: Tell your healthcare provider about all prescription and over-the-counter medicines, vitamins, and herbal supplements you take. Do not start or stop other medicines without talking to your provider first, and never take an MAOI within 14 days of methylphenidate.
When to Contact a Healthcare Provider
Contact your healthcare provider or seek emergency care right away if you:
- Have chest pain, shortness of breath, or fainting
- Have a fast, pounding, or irregular heartbeat
- Develop new or worsening agitation, aggression, anxiety, or thoughts of harming yourself
- Notice new psychotic symptoms, such as hearing voices, seeing things, or believing things that are not true
- Have an erection that lasts more than 4 hours
- Notice fingers or toes that feel numb, cool, or painful, or that change color
- Have a seizure
- Have a severe allergic reaction or serious skin reaction, such as swelling of the face or throat, hives, blistering, or trouble breathing
- Notice slowed growth in a child during treatment
- Have any symptom that concerns you or does not go away