METHYLPHENIDATE

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Created Oct 2019 | Updated Oct 2020

METHYLPHENIDATE

  • [CONCERTA]
  • [RITALIN]
  • [METHYLIN]

DEA CODE 1724: Schedule 2

Ritalin, a trade name for the prescription drug methylphenidate, is a central nervous system stimulant. (Its effects are similar to, but more potent than, caffeine and less potent than amphetamine.) Ritalin often is prescribed to treat individuals (mostly children) who are diagnosed with ADD (attention deficit disorder) or ADHD (attention deficit hyperactivity disorder). Ritalin is abused for the stimulant effects it produces, including appetite suppression, wakefulness, euphoria, and increased focus and attentiveness.

NDIC PDF Methylphenidate

Highlights for Methylphenidate:

  • Methylphenidate oral tablet is available as a generic drug and as brand-name drugs. Brand names: Ritalin, Ritalin-SR, Concerta, Metadate ER, QuilliChew ER, Cotempla XR-ODT.
  • Methylphenidate tablet comes in these forms: oral immediate-release tablet, extended-release oral tablet, chewable oral tablet, extended-release chewable oral tablet, and extended-release orally disintegrating tablet. Methylphenidate also comes as an extended-release oral capsule, transdermal patch, oral suspension, and oral solution.
  • Methylphenidate oral tablet is used to treat narcolepsy and attention deficit hyperactivity disorder (ADHD).

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.

What does it look like?
Methylphenidate-based drugs are sold as powders, crystals, pellets and tablets. The powders and crystals tend to be white or off-white in colour, while the pellets and tablets can be different colours. Methylphenidate is a prescription only medicine that comes as yellow, grey and white tablets and as capsules which can be half green, half white or half blue, half white or half brown, half white or half lilac, half white, or half light grey, half purple, or half grey, half purple, or lilac.

Methylphenidate drug usage

47th most prescribed medicine in the United States for 2017

Ritalin is a short-acting formulation of methylphenidate that lasts about 3-4 hours.
Focalin is another form of methylphenidate that also lasts about 4 hours. Both of these medications begin to work about 30-45 minutes after taking them. For children who have trouble swallowing pills, this medication can be crushed and mixed with foods. There is also a liquid and a chewable tablet form of the short-acting methylphenidate. Other preparations of methylphenidate have been created to release the medication over greater period of time, extending the duration of the effect of the medication. This is of great benefit when trying to provide a response that lasts through a school day (typically 6-8 hours). Some of these compounds take effect as quickly as the short-acting forms of these medications. These compounds include:

  • Concerta is one of the longest-acting methylphenidate medications on the market, lasting 8 to 12 hours. Concerta can't be chewed or opened. It has to be swallowed whole in order for it to work the way it was designed. This can be a problem for some kids.
  • Ritalin-LA and Metadate CD are capsules that are filled with medication. These medications are very similar in that they both last about 6-8 hours. What's good about these is that for kids who can't swallow pills, you can open up the capsule and sprinkle it on food (i.e., yogurt, Nutella, applesauce, etc.).
  • Aptensio XR and Focalin XR are also capsules filled with medication that can be opened and mixed with food. They typically work longer than Ritalin LA or Metadate CD.
  • Quillivant XR is a long-acting formulation of methylphenidate in liquid form, which makes it a good alternative for kids who have trouble swallowing capsules and can't tolerate beads, either. The liquid formulation may also allow more precise dose adjustment or "titration."
  • Quillichew ER is a chewable long - acting formulation of methylphenidate that can last up to 8 hours.
  • Daytrana is a methylphenidate patch. It's another option for kids who can't swallow pills. You can wear the patch for up to 9 hours and often get another hour's worth of response after the patch is removed. However, the patch can often take 1-2 hours to start working.

What is the most important information I should know about methylphenidate or dexmethylphenidate?
Although some symptoms may improve within days of starting methylphenidate or dexmethylphenidate, it may take several weeks before you notice the full benefits of the medication.

Are there specific concerns about methylphenidate or dexmethylphenidate and pregnancy?
If you are planning on becoming pregnant, notify your healthcare provider so that he/she can best manage your medications. People living with ADHD who wish to become pregnant face important decisions, each with risks and benefits as they relate to how the illness, medications, and risks to the fetus may interact. This is a complex decision as untreated ADHD has risks to the fetus as well as the mother. Therefore, it is important to discuss this with your doctor and caregivers. Regarding breast-feeding, caution is advised since methylphenidate does pass into breast milk and there is limited information available about the safety of dexmethylphenidate while breastfeeding.

Time to initial effect and duration of action:
Methylphenidate is a CNS stimulant approved for the treatment of narcolepsy and attention deficit hyperactivity disorder (ADHD). Methylphenidate inhibits the reuptake of dopamine and norepinephrine, increased dopaminergic and noradrenergic activity in the prefrontal cortex may explain its efficacy in ADHD. There are many formulations available, these can be grouped into short-acting, intermediate-acting, and long-acting methylphenidate. When deciding which formulation is the most suitable for a given patient, it is important to consider two parameters: time to initial effect and duration of action.

Methylphenidate
Duration:

A psychostimulant commonly used in the treatment of ADHD, narcolepsy and obesity, particularly in the EU instead of Adderall. Methylphenidate is also a 5HT1A receptor agonist. Sometimes prescribed off-label to help the withdrawals from cocaine and other stimulants.

RouteOnsetDurationAfter Effects
Tripsit Factsheets
Insufflated:minutes2-4 hours1-24 hours
Insufflated-IR:5-10 minuteshours1-24 hours
Insufflated-XR:5-10 minuteshours1-24 hours
Oral-XR:30-120 minutes8-12 hours1-24 hours
Oral-IR:30-120 minutes3-6 hours1-24 hours
Methylphenidate Duration
Marquis:
Moderate orange yellow
Effects:
Increased alertness, Euphoria, Increased motivation, Reduced appetite, Flushing of the face, Increased body temperature, Tachycardia (Increased heart rate) Paranoia, Insomnia.

When did the U.S. Food and Drug Administration approve Ritalin in the United States?
Methylphenidate was first approved by the U.S. Food and Drug Administration in 1955 for treating what was then referred to as hyperactivity.

Is there a generic version of Ritalin available?
Yes, the generic name for Ritalin is methylphenidate and is for purchase in the United States. Some users have argued that the generic version may be weaker than the brand name version.

Are there any major differences between Ritalin and Adderall?
There are a lot of similarities between the two medications. Both drugs are stimulants used to treat ADHD, and both are habit-forming and classified as Schedule II controlled substances. Therefore, if you have a history of substance use problems, you should talk to your doctor about this before taking either medication. As far as differences, Ritalin comes in three formats: instant release (lasting 3-4 hours), sustained release (lasting 6-8 hours), and long-acting (lasting 8 hours). Adderall comes in two formats: instant release (lasting 4-6 hours) and extended release (lasting 12 hours).

Can children take Ritalin?
Children over the age of 6 may be prescribed Ritalin for ADHD. They should take the medication in the exact amount prescribed by their doctor. It's also important to tell your child's doctor about other medication complications or past substance use history.


Methylphenidate is a CNS stimulant approved for the treatment of narcolepsy and attention deficit hyperactivity disorder. The drug is believed to bind the dopamine transporter in the presynaptic cell membrane, thereby blocking the reuptake of dopamine and causing an increase in extracellular dopamine levels.

Interactions:
Persons taking methylphenidate should be aware of the possible adverse interactions with the following drugs: amphetamines, appetite suppressants, caffeine , chlophedianol, cocaine, asthma medication, cold, sinus and hay fever medications, nabilone, pemoline, monoamine oxidase inhibitors, and pimozide. Methylphenidate is also affected by epilepsy, Tourette's syndrome, glaucoma, high blood pressure, psychosis, severe anxiety , and tics .

Parental concerns:
The use of methyphenidate has been subject to controversy over the last several years. Parents concerned about whether the drug is being properly prescribed for their children should seek out the opinion of the most suitable physician for the type of problems their child is having. If a parent is uncomfortable with a physician's response, they should not hesitate to get a second opinion.

In June 2005, the US Food and Drug Administration issued a series of public health advisories warning that Ritalin and drugs like it may cause visual hallucinations, suicidal thoughts and psychotic behavior, as well as aggression or violent behavior.

One writer put it this way: "Parents are never told: 'Oh, by the way, once in a while a child dies simply by taking their prescribed medication.' Or 'By the way, children on stimulant medications have twice the future rate of drug abuse.' Or 'By the way, one third of all children on these medications develop symptoms of obsessive-compulsive behavior within the first year.'"

Breastfeeding:

Summary of Use During Lactation:
In dosages prescribed for medical indications, limited evidence indicates that methylphenidate levels in milk are very low and not detectable in infant serum.

The effects of methylphenidate in milk on the neurological development of the infant have not been well studied.

If methylphenidate is required by the mother, it is not a reason to discontinue breastfeeding.

It is possible that large dosages of methylphenidate might interfere with milk production, especially in women whose lactation is not well established.

Effects on Lactation and Breastmilk:
Methylphenidate reduces serum prolactin, but no studies have been located as of the revision date on the effect of methylphenidate on milk production.

The maternal prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Pediatric:
Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of methylphenidate in children 6 years of age and older (6 to 12 years of age for Ritalin LA).

Safety and efficacy have not been established in children younger than 6 years of age.

Geriatric:
Appropriate studies on the relationship of age to the effects of methylphenidate have not been performed in the geriatric population.

Other Interactions:

  • Ethanol

Other Medical Problems:
Make sure you tell your doctor if you have any other medical problems, especially:

  • Agitation
  • Glaucoma
  • Tics or Tourette syndrome, history of - Should not be used in patients with these conditions
  • Alcohol abuse, history of
  • Drug abuse or dependence, history of - Use with caution. Dependence may be more likely to develop
  • Allergy to aspirin - Use with caution. Adhansia XR contains a yellow dye called tartrazine, which may cause severe allergic reactions in patients with this condition
  • Asthma
  • Bipolar disorder (manic-depressive illness), history of
  • Depression, history of
  • Hypertension (high blood pressure)
  • Priapism (painful and prolonged erection of the penis)
  • Psychosis (mental illness), history of
  • Raynaud's phenomenon (blood vessel disease)
  • Seizures, history of
  • Tachycardia (rapid heart rate) - Use with caution. May make these conditions worse
  • Coronary artery disease
  • Heart attack, recent
  • Heart disease (eg, cardiomyopathy)
  • Heart failure
  • Heart rhythm problems (eg, ventricular arrhythmia), history of
  • Hyperthyroidism (overactive thyroid)
  • Stroke, history of - Use with caution. May make side effects become worse
  • Phenylketonuria - The chewable tablet contains aspartame, which can make this condition worse

Ritalin and Alcohol:
Understanding the two drugs involved in this combination is key to understanding the effects of mixing methylphenidate and alcohol. Methylphenidate, the main ingredient in Ritalin, is a psychostimulant drug regularly prescribed to combat the effects of attention deficit hyperactivity disorder. Alcohol is a central nervous system depressant that slows response times and produces a mild sense of euphoria when used in moderation. Both are metabolized through chemical processes in the liver, and excessive use of either may cause damage to that vital organ. The combination of methylphenidate and alcohol increases methylphenidate levels in the blood by up to 40 percent. This drastically increases the normal effects of the drug, resulting in a greater sensitivity to the euphoric effects of alcohol and the stimulation of methylphenidate.

What is the most important information I should know about methylphenidate?
Methylphenidate may be habit-forming. Tell your doctor if you have had problems with drug or alcohol abuse. Stimulants have caused stroke, heart attack, and sudden death in people with high blood pressure, heart disease, or a heart defect. Do not use methylphenidate if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine. Methylphenidate may cause new or worsening psychosis (unusual thoughts or behavior), especially if you have a history of depression, mental illness, or bipolar disorder. You may have blood circulation problems that can cause numbness, pain, or discoloration in your fingers or toes. Call your doctor right away if you have: signs of heart problems - chest pain, feeling light-headed or short of breath; signs of psychosis - paranoia, aggression, new behavior problems, seeing or hearing things that are not real; signs of circulation problems - unexplained wounds on your fingers or toes.

Concerns about abuse and dependence
A boxed warning for methylphenidate preparations states that it has a high potential for abuse and that prolonged administration may lead to dependence. Available data suggest that children with ADHD who are treated with stimulants are not more likely than those who did not receive stimulants to develop substance abuse later in life. A related problem is diversion - that is, patients selling their prescription stimulants to be used as cognitive enhancers or drugs of abuse.

Review question:
We reviewed the evidence of the effects of methylphenidate on the behaviour of children and adolescents with ADHD. Findings suggest that methylphenidate might improve some of the core symptoms of ADHD - reducing hyperactivity and impulsivity, and helping children to concentrate. Methylphenidate might also help to improve the general behaviour and quality of life of children with ADHD. However, we cannot be confident that the results accurately reflect the size of the benefit of methylphenidate.

Prescribed for:
    What Conditions does it Treat?
  • Attention deficit disorder with hyperactivity
  • Recurring sleep episodes during the day

Uses:
This medication is used to treat attention deficit hyperactivity disorder - ADHD. It works by changing the amounts of certain natural substances in the brain. Methylphenidate belongs to a class of drugs known as stimulants.

It can help increase your ability to pay attention, stay focused on an activity, and control behavior problems. It may also help you to organize your tasks and improve listening skills.

This medication is also used to treat a certain sleep disorder (narcolepsy).

Before using:
Tell your doctor or pharmacist your medical history, especially of:

  • High blood pressure
  • Blood circulation problems (such as Raynaud's disease)
  • Glaucoma
  • Heart problems (such as irregular heartbeat, heart failure, previous heart attack, problems with heart structure)
  • Family history of heart problems (such as sudden cardiac death, irregular heartbeat)
  • Mental/mood conditions (especially anxiety, tension, agitation)
  • Personal/family history of mental/mood disorders (such as bipolar disorder, depression, psychosis, suicidal thoughts)
  • Personal/family history of uncontrolled muscle movements (motor tics, Tourette's syndrome)
  • Overactive thyroid (hyperthyroidism)
  • Seizure disorder

Precautions:

  • This drug may make you dizzy
  • Alcohol or marijuana (cannabis) can make you more dizzy
  • Do not drive, use machinery, or do anything that needs alertness until you can do it safely
  • Limit alcoholic beverages.
  • Talk to your doctor if you are using marijuana (cannabis).

WARNINGS:

Misuse or abuse of methylphenidate can result in serious (possibly fatal) heart and blood pressure problems.

This medication can be habit-forming and should be used cautiously by people who have mental/mood disorders or a substance use disorder (such as overuse of or addiction to drugs/alcohol). Before using this medication, tell your doctor if you have a personal or family history of a substance use disorder. Do not increase your dose, use it more often, or use it for a longer time or in a different way than prescribed. Doing so may result in a decrease in the effect of this drug, drug dependence, or abnormal thoughts/behavior.

Your doctor may monitor you for a while after the medication is stopped, especially if you have taken this drug for a long time or in high doses.

User Reviews:

180 Total User Reviews
Methylphenidate HCl Oral:
Read Reviews
Condition: Attention Deficit Disorder with Hyperactivity (120 Reviews):
Effectiveness(3.64)

Ease of Use(4.05)

Satisfaction(3.38)

Methylphenidate Hydrochloride
Maximum Dosage:
Prescribers Digital Reference
Adults100 mg/day PO for Adhansia XR; 72 mg/day PO for Concerta; 60 mg/day PO for all other oral formulations.
Geriatric100 mg/day PO for Adhansia XR; 60 mg/day PO for all other oral formulations. While some dosage forms have not been specifically studied in the elderly, use of stimulants off-label has been described in geriatric adults.
Adolescents85 mg/day PO for Adhansia XR; 72 mg/day (Max: 2 mg/kg/day) PO for Concerta (FDA-approved labeling); 60 mg/day PO for all other oral formulations excluding Cotempla XR-ODT and Jornay PM (FDA-approved labeling); 51.8 mg/day PO for Cotempla XR-ODT and 100 mg/day PO for Jornay PM; however, doses up to 100 to 108 mg/day PO have been used in patients weighing more than 50 kg for some formulations. For the transdermal patch, 30 mg/9-hour patch per day is the maximum.
Children6 to 12 years: 85 mg/day PO for Adhansia XR; 54 mg/day PO for Concerta (FDA-approved labeling); 60 mg/day PO for all other oral formulations excluding Cotempla XR-ODT and Jornay PM (FDA-approved labeling); 51.8 mg/day PO for Cotempla XR-ODT and 100 mg/day PO for Jornay PM; however, doses up to 100 to 108 mg/day PO have been used in patients weighing more than 50 kg for some formulations. For the transdermal patch, 30 mg/9-hour patch per day is the maximum.
Children3 to 5 years: Safety and efficacy have not been established. Maximum doses have not been adequately studied; however, The Preschool ADHD Treatment Study (PATS) has suggested immediate-release doses up to 30 mg/day PO.
Children1 to 2 years: Safety and efficacy have not been established.
InfantsSafety and efficacy have not been established.
NeonatesSafety and efficacy have not been established.

Ritalin, Concerta (methylphenidate) (Rx)
Black Box Warnings:

Assess risk of abuse prior to prescribing, and monitor for signs of abuse and dependence while on therapy

Chronic abuse can lead to a marked tolerance and psychological dependence, with varying degrees of abnormal behavior

Frank psychotic episodes can occur, especially with parenteral abuse

Withdrawal from abusive use may result in depression

Give cautiously to patients with a history of drug dependence or alcoholism

Potential for drug dependency; withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up

Ritalin (methylphenidate)
Side Effects:
Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
RxList
Call your doctor at once if you have:
  • signs of heart problems - chest pain, trouble breathing, feeling like you might pass out
  • signs of psychosis - hallucinations (seeing or hearing things that are not real), new behavior problems, aggression, hostility, paranoia
  • signs of circulation problems - numbness, pain, cold feeling, unexplained wounds, or skin color changes (pale, red, or blue appearance) in your fingers or toes
  • penis erection that is painful or lasts 4 hours or longer (rare)
Methylphenidate can affect growth in children. Tell your doctor if your child is not growing at a normal rate while using this medicine.
Common side effects may include:
  • excessive sweating
  • mood changes, feeling nervous or irritable, sleep problems (insomnia)
  • fast heart rate, pounding heartbeats or fluttering in your chest, increased blood pressure
  • loss of appetite, weight loss
  • dry mouth, nausea, stomach pain
  • headache
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Liver:
Methylphenidate has been linked to a low rate of serum aminotransferase elevations during therapy and to rare instances of acute, clinically apparent liver injury, generally after its intravenous abuse.

Methylphenidate Hepatotoxicity:
In prelicensure clinical trials, methylphenidate was not associated with serum aminotransferase elevations or instances of hepatic injury, but reports of enzyme elevations were received by the sponsor and appeared in publications after it was marketed. The elevations were transient, mild-to-moderate in severity and rarely associated with jaundice or symptoms. In addition, there have been several case reports of marked serum enzyme elevations with jaundice and clinically apparent acute liver injury attributed to methylphenidate given intravenously. These cases occurred largely after illicit intravenous use of methylphenidate and frequently in patients with underlying chronic hepatitis C. The onset was generally soon after initiation of therapy. The pattern of liver enzyme elevations was hepatocellular and the clinical phenotype typical of acute hepatic necrosis with rapid onset and rapid recovery. Immunoallergic features were uncommon. A single case associated with low levels of autoantibodies has been published. Some cases have been severe and at least one fatality after intravenous abuse has been reported. Recurrence upon rechallenge was been documented in one instance (Case 1).

C [H] Likelihood score: C[H] (probable cause of clinically apparent liver injury when given in high doses)


Important information:
Methylphenidate may be habit-forming, and this medicine is a drug of abuse. Tell your doctor if you have had problems with drug or alcohol abuse.

Stimulants have caused stroke, heart attack, and sudden death in people with high blood pressure, heart disease, or a heart defect.

Do not use methylphenidate if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine.

Methylphenidate may cause new or worsening psychosis (unusual thoughts or behavior), especially if you have a history of depression, mental illness, or bipolar disorder.

You may have blood circulation problems that can cause numbness, pain, or discoloration in your fingers or toes.

Call your doctor right away if you have:

  • signs of heart problems - chest pain, feeling light-headed or short of breath;
  • signs of psychosis - paranoia, aggression, new behavior problems, seeing or hearing things that are not real;
  • signs of circulation problems - unexplained wounds on your fingers or toes.
Avoid drinking alcohol, especially if you take extended-release Methylphenidate.

Alcohol may cause the medicine to be released into the bloodstream too fast.

Methylphenidate may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Interactions:

Drug Interactions (114) Alcohol/Food Interactions (4) Disease Interactions (16)


What other drugs will affect Methylphenidate?
Ask your doctor before using a stomach acid medicine (including Alka-Seltzer or sodium bicarbonate). Some of these medicines can change the way your body absorbs methylphenidate, and may increase side effects. Do not use methylphenidate if you are taking a MAO inhibitor, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine. Many drugs can interact with methylphenidate. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all your current medicines and any medicine you start or stop using.

A total of 114 drugs are known to interact with Methylphenidate.

  • 20 major drug interactions
  • 84 moderate drug interactions
  • 10 minor drug interactions

FDA PDF Concerta

Medsafe PDF Ritalin

EMC PDF Methylphenidate

Methylphenidate was first made in 1944 and was approved for medical use in the United States in 1955. It is estimated that in 2013, 2.4 billion doses of methylphenidate were taken worldwide. In 2017, it was the 47th-most commonly prescribed medication in the United States, with more than 16 million prescriptions. The most common adverse effects include appetite loss, dry mouth, anxiety/nervousness, nausea, and insomnia. Gastrointestinal adverse effects may include abdominal pain and weight loss. Methylphenidate is a stimulant with an addiction liability and dependence liability similar to amphetamine. Methylphenidate was synthesized by Ciba (now Novartis) chemist Leandro Panizzon. He named the drug after his wife, nicknamed Rita, who used Ritalin to compensate for low blood pressure. Methylphenidate has been the subject of controversy in relation to its use in the treatment of ADHD. The prescription of psychostimulant medication to children to reduce ADHD symptoms has been a major point of criticism.

  
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