ADHD Medication and Treatment Reviews

Methylphenidate: ADHD Medication Overview

Brand Names: Concerta, Ritalin, Jornay PM, Aptensio XR, Metadate CD, Methylin, Quillivant XR
Methylphenidate is a stimulant ADHD medication available in many formulations used to treat symptoms of ADHD and ADD in children and adults.

What is Methylphenidate?

Methylphenidate (Brand Names: Concerta, Ritalin, Daytrana, Aptensio XR, Metadate CD, Methylin, Quillivant XR, Jornay PM, Adhansia XR, Azstarys, Cotempla) is a central nervous system stimulant ADHD medication primarily used to treat symptoms of attention deficit hyperactivity disorder in children ages 6-12, adolescents, and adults up to age 65. Methylphenidate may improve ADHD symptoms including poor focus, impulsivity and hyperactive behavior. Methylphenidate is the generic or general name of the medication that is then sold under a number of brand names such as Ritalin and Daytrana.

Methylphenidate is not the same as Adderall XR, which is an amphetamine.

Methylphenidate has not been studied in children under the age of 6 by the FDA.  It has been extensively studied, however, in the Preschool ADHD Treatment Study (PATS 2016) and was shown to be both effective and safe in the treatment of pre-school children.

The American Academy of Pediatrics recommends ADHD treatment with behavioral therapy before medication for children under the age of 6. For children ages 6 to 11, the AAP says “The primary care clinician should prescribe US Food and Drug Administration–approved medications for ADHD and/or evidence-based parent- and/or teacher-administered behavior therapy as treatment for ADHD, preferably both.” Similarly, the National Institute of Mental Health finds the most successful treatment plans use a combination of ADHD medication and behavioral therapy.

Methylphenidate can also be used to treat narcolepsy.

Is Methylphenidate Effective at Treating ADHD Symptoms?

Methylphenidate is considered the most effective first-line treatment for ADHD symptoms in children. In 2018, researchers from the UK systematically compared 133 double-blind, randomized, controlled trials designed to contrast the effectiveness and tolerability of the following medications for ADHD in children, adolescents, and adults: amphetamines (including lisdexamfetamine), atomoxetine, bupropion, clonidine, guanfacine, methylphenidate, and modafinil. In studying drug effectiveness (change in severity of ADHD core symptoms based on teachers’ and clinicians’ ratings) and tolerability (proportion of participants who left the study due to side effects) in roughly 11,000 children, the researchers found that all medications were superior to placebo. However, according to teachers’ ratings, only methylphenidate and modafinil were superior to placebo.1

How Do You Use Methylphenidate to Treat ADHD?

Before starting or refilling a methylphenidate prescription, read the medication guide included with your pills, as it may be updated with new information.

This guide should not replace a conversation with your doctor, who has a holistic view of your or your child’s medical history, other diagnoses, and other prescriptions. If you have questions, ask your doctor or pharmacist before you begin taking the medication.

Not everyone gets benefit from or tolerates methylphenidate.  About 30% of people who try a methylphenidate formulation will need to try the other stimulant molecule, amphetamine.  About 15% of people do not get benefits or do not tolerate either of the two stimulant medications, methylphenidate and amphetamines.

Methylphenidate Dosage

The optimal dosage varies patient by patient. It is not determined by age, weight, or height, but rather by how a person absorbs and then metabolizes the medication, and the condition treated. Your doctor may adjust your daily dosage until you or your child experiences the best response — that is, the lowest dosage at which you experience the greatest improvement in symptoms without side effects.

Methylphenidate is available in several formulations:

  • Short-Acting Tablet: (Brand Name: Ritalin) Taken two to three times daily, 30 to 45 minutes before a meal. Available in 5mg, 10mg, and 20mg dosages. Tablets should be swallowed whole with water or other liquids. Tablets should never by crushed or chewed. Dosage higher than 60mg per day have not been formally studied by the FDA and so higher doses are not FDA-approved.  Uncommonly individual patients may require higher doses after careful evaluation by the patient’s clinician.
  • Sustained-Release Tablet: (Brand Name: Ritalin SR) Taken once daily in the morning with or without food. Available in 20mg dosage, effective for 8 hours. Tablets should be swallowed whole with water or other liquids. Tablets should never by crushed or chewed.
  • Extended-Release Capsule: (Brand Name: Metadate CD, Aptensio XR, Ritalin LA) Taken orally, with or without food, once daily. The first dose is typically taken first thing in the morning; it should be taken at the same time each day for the best results. Tablets should be swallowed whole with water or other liquids. If your child is unable to swallow the capsule, it can be opened and sprinkled over a spoonful of applesauce. Taken this way, the mixture should be swallowed whole without chewing, followed by a drink of water or other liquid. Capsules should never by crushed or chewed. Capsules are available in 10mg, 20mg, 30mg, 40mg, 50mg, and 60mg dosages. The time-release formulation is designed to maintain a steady level of medication in the body  for 8 to 10 hours.
  • Once-Daily Oral Capsule: (Brand Name: Azstarys) Azstarys is a once-daily central nervous system (CNS) stimulant. Formerly referred to as KP415, Azstarys comprises extended-release serdexmethylphenidate (SDX), and KemPharm’s prodrug of d-methylphenidate (d-MPH), co-formulated with immediate-release d-MPH. As a prodrug, SDX is specifically designed to be chemically inactive until after absorption via the lower gastrointestinal tract, where SDX is converted to d-MPH that by design is gradually released throughout the day. The result is a treatment that provides symptom control both rapidly with the d-MPH and for an extended duration with SDX. Azstarys can be taken with or without food. Patients may swallow capsules whole or open and sprinkle onto applesauce or add to water. Available in 26.1 mg/5.2 mg, 39.2 mg/7.8 mg, and 52.3 mg/10.4 mg.
  • Delayed-Release/Extended-Release Capsule: (Brand Name: Jornay PM)  Jornay capsules are filled with microbeads, each of which has a delayed release and extended release layer. This technology keeps the medication from activating for the first 10 to 12 hours — meaning that, when taken in the evening before bedtime, the effects are felt when a child wakes up.  The medication is then released into the body in steady amounts throughout the day.
  • Chewable Tablet: (Brand Name: Methylin) Taken two to three times daily, 30 to 45 minutes before a meal. Chew each tablet well, and swallow with at least a full glass of water or another liquid. Tablets not taken with enough liquid can swell and become a choking risk. Available in 2.5 mg, 5 mg, and 10mg dosages. Dosage does not typically exceed 60 mg per day.
  • Extended-Release Chewable Tablet: (Brand Name: Quillichew ER) Taken once daily in the morning with or without food. Chew each tablet well, and swallow with a full glass of water or another liquid. Available in 20mg, 30mg, and 40mg tablets. 20mg and 30mg tablets are scored and can be cut in half if necessary to achieve the optimal dose.
  • Oral Solution: (Brand Name: Methylin) Taken two to three times daily, 30 to 45 minutes before a meal. The liquid should be measured with the included device and swallowed entirely with water or another liquid. Dosage does not typically exceed 60 mg per day.
  • Extended-Release Suspension: (Brand Name: Quillivant XR) Taken once daily in the morning with or without food. Shake the bottle well for at least 10 seconds, and then measure with the included device. The time-release formulation is designed to maintain a steady level of medication in your body throughout the day. Dosage does not typically exceed 60 mg per day.
  • Extended-Release Osmotic Tablet: (Brand name: Concerta) Taken orally, with or without food, once daily — usually first thing in the morning. It should be taken at the same time each day for best results. Tablets should be swallowed whole with water or other liquids. If your child is unable to swallow the pill, your doctor may recommend another medication. Tablets should never be cut, crushed, or chewed because this would destroy the time release mechanism. The tablet is designed to release the medication without dissolving. The empty capsule passes through the digestive tract and out of the body without being digested. Capsules are available in 18mg, 27mg, 36mg, and 54mg dosages. The time-release formulation is designed to maintain a steady level of medication in your body throughout the day. Dosage should not exceed 54mg daily for children and adolescents, and 72mg daily for adults.  Most generics are of poor quality.  Ask your pharmacist to dispense the “branded generic” formulation.
  • Single isomer extended release capsule: (Brand name: Focalin XR.  Generic name: dexmethylphenidate ER).  Although all other methylphenidate formulations contain both the right and left-handed mirror image molecules of methylphenidate, only the right-handed version has benefits for ADHD.  The left-handed version increases side effects.  This formulation is just the beneficial right-handed version of the methylphenidate molecule and there is strong evidence that it has more efficacy and a lower level of side effects than other formulations.  It is also more expensive and, therefore, commonly does not have as good insurance coverage.  Capsules are available in 5mg increments from 5 mg up to 40 mg per capsule.
  • Transdermal Patch: (Brand Name: Daytrana) Apply the patch to the hip two hours before you need the medication to take effect. There are four dosage strengths available, designated as 10 mg, 15 mg, 20 mg, and 30 mg.  These nominal dosages strengths are just estimates since the efficiency of skin absorption varies greatly from person to person.   Each dosage is approved by the FDA for a wear time of just  9 hours a day:      This 9- hour wear time is merely how long the FDA studied in its Stage 3 trial.  In clinical practice your doctor may suggest that you keep the patch on for longer periods of time.  The patch was originally designed for up to 18 hours of wear time. This formulation may cause skin irritation (red, mildly painful areas of skin) where the patch was applied so the spot where the patch is applied should be changed each day.

During treatment, your doctor may periodically ask you to stop taking your methylphenidate so that he or she can monitor ADHD symptoms; check vital statistics including blood, heart, and blood pressure; or evaluate height and weight. If any problems are found, your doctor may recommend modifying treatment or switching to another molecule such as amphetamine.

Very rarely some patients report developing a tolerance to methylphenidate after long-term use. If you notice that your dosage is no longer controlling your symptoms, talk to your doctor to plan a course of action.

Methylphenidate Side Effects

As with all medications, follow your methylphenidate prescription instructions exactly. If patients experience upset stomach as a side effect, this medication can be taken with food. Taking methylphenidate late in the day can disrupt sleep.

The most common side effects of methylphenidate are as follows:Decreased of appetite with possible weight loss, jitteriness, irritability, difficulty falling asleep, stomach discomfort, heart racing, and constipation.

The transdermal patch form of methylphenidate can cause skin irritation, and permanent skin discoloration where the patch is applied.

At one time there was a concern that methylphenidate caused a slowing of growth for which the child then compensated in a later time.  This is now considered doubtful and consequently no international professional guidelines now recommend the use of “drug holidays” to allow for this compensatory growth.

Other serious but rare side effects include priapism and eyesight changes or blurred vision.

If side effects are bothersome, or do not go away, talk to your doctor. Most people taking this medication do not experience any of these side effects.

Report to your doctor any heart-related problems or a family history of heart and blood pressure problems prior to starting methylphenidate. Patients with structural cardiac abnormalities and other serious heart problems have experienced sudden death, stroke, heart attack, and increased blood pressure while taking methylphenidate. Stimulants can increase blood pressure and heart rate. Physicians should monitor these vital signs closely during treatment. Call your doctor immediately if you or your child experiences warning signs such as severe chest pain, excessive shortness of breath without cause, or fainting while taking methylphenidate.

Also disclose to your physician all mental health issues including any family history of suicide, bipolar illness, tics, or depression. Methylphenidate may create new or exacerbate existing behavior problems, bipolar illness, or Tourette’s syndrome. The FDA recommends evaluating patients for bipolar disorder, tics, and Tourette’s syndrome prior to stimulant administration. It can cause psychotic or manic symptoms in children and teenagers. Call your doctor immediately if you or your child experiences new or worsening mental health symptoms including hallucinations or sudden suspicions.

Discuss circulation problems with your doctor before taking methylphenidate, which has been known to cause numbness, coolness, or pain in fingers or toes, including Raynaud’s phenomenon. Report to your doctor any new blood-flow problems, pain, skin color changes, or sensitivities to temperature while taking methylphenidate.

Stimulants like methylphenidate have a high potential for abuse and addiction, especially among people who do not have ADHD. It is a “Schedule II Stimulant,” a designation that the Drug Enforcement Agency uses for drugs with a high potential for abuse.. All of the first line (i.e. most effective) stimulant medications for ADHD are also in Schedule II. People with a history of drug abuse should use caution when trying this medication. Taking the medication exactly as prescribed can reduce potential for abuse.

The above is not a complete list of potential side effects. If you notice any health changes not listed above, discuss them with your doctor or pharmacist.

What Precautions Are Associated with Methylphenidate?

Store methylphenidate in a secure place out of the reach of children, and at room temperature. Do not share your methylphenidate prescription with anyone, even another person with ADHD. Sharing prescription medication is illegal, and can cause harm.

You should not take methylphenidate if you have any of the following conditions: allergy or hypersensitivity to methylphenidate HCI or any of the ingredients in methylphenidate medications, anxiety/agitation, glaucoma, tics or history of Tourette’s syndrome, or if you are taking monoamine oxidase inhibitors (MAOIs).

Chewable tablets can contain phenylalanine, and can be harmful to people with phenylketonuria.

You should use caution while taking methylphenidate if you have a history of heart or circulation problems.

If you’re thinking of becoming pregnant, discuss the use of methylphenidate with your doctor. Animal studies indicate a potential risk of fetal harm but no harm has been found in human beings. Methylphenidate is passed through breastmilk but the effects of ADHD medications in breast milk have never been studied.  The American Association of Pediatrics recommends that mothers do not nurse while taking  methylphenidate “out of an abundance of caution.”

What Interactions Are Associated with Methylphenidate?

Before taking methylphenidate, discuss all other active prescription medications with your doctor. Methylphenidate can have a dangerous, possibly fatal, interaction with a group of rarely used antidepressants  called  the monoamine oxidase inhibitors (MAOIs).

Share a list of all vitamin or herbal supplements, and prescription and non-prescription medications you take with the pharmacist when you fill your prescription, and let all doctors and physicians know you are taking methylphenidate before having any surgery or laboratory tests. Methylphenidate can have a dangerous interaction with certain anesthetics. The above is not a complete list of all possible drug interactions.

More Information on Methylphenidate and Other ADHD Medications:

Free Download: The Ultimate Guide to ADHD Medication
A Parent’s Guide to ADHD Medications
Making the Switch: Trying a New ADHD Medication
ADDitude Directory: Find ADHD Specialists and Clinics Near You

Sources:

http://www.fda.gov/downloads/Drugs/DrugSafety/ucm088635.pdf
http://www.fda.gov/downloads/Drugs/DrugSafety/ucm088575.pdf
http://pi.actavis.com/data_stream.asp?product_group=1707&p=pi
Methylphenidate Chewable tabs: http://www.fda.gov/downloads/drugs/drugsafety/ucm088639.pdf
Methylphenidate Oral solution: http://www.fda.gov/downloads/drugs/drugsafety/ucm088640.pdf
Methylphenidate Extended release suspension: http://www.fda.gov/downloads/drugs/drugsafety/ucm322209.pdf
Methylphenidate Extended release chewable tablet: https://www.quillivantxr-quillichewer.com/
Methylphenidate Short-acting tablet: http://www.fda.gov/downloads/drugs/drugsafety/ucm089090.pdf
https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/ritalin_ritalin-sr.pdf

1Cortese S, Adamo N, Del Giovane C, et al. Comparative efficacy and tolerability of medications for attention-deficit hyperactivity disorder in children, adolescents, and adults: a systematic review and network meta-analysis. Lancet Psychiatry. 2018 Aug 7. doi: 10.1016/S2215-0366(18)30269-4