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Methylphenidate

Brands and Forms

  • Ritalin
    • immediate-release tablets: 5mg, 10mg, 20mg
    • 2-4 hour duration of action
  • Ritalin SR
    • sustained-release tablets: 20mg
    • 4-6 hour duration of action
  • Ritalin LA
    • extended-release tablets: 10mg, 20mg, 30mg, 40mg
    • 8 hour duration of action
  • Methylin
    • immediate-release tablets: 5mg, 10mg, 20mg
    • immediate-release chewable tablets: 2.5mg, 5mg, 10mg
    • oral solution: 5mg/5ml, 10mg/5ml
    • 2-4 hour duration of action
  • Methylin ER
    • extended-release tablets: 10mg, 20mg
    • 4-6 hour duration of action
  • Metadate ER
    • extended-release tablets: 10mg, 20mg
    • 4-6 hour duration of action
  • Metadate CD
    • extended-release capsules: 10mg, 20mg, 30mg
    • 8 hour duration of action
  • Concerta
    • extended-release tablets: 18mg, 27mg, 36mg, 54mg
    • 12 hour duration of action
  • Daytrana
    • transdermal patch: 10mg, 15mg, 20mg, 30mg
    • 9 hour duration of action
  • Biphentin
    • controlled-release capsule: 10mg, 15mg, 20mg, 30mg, 40mg, 50mg, 60mg, 70mg, 80mg

Uses of Methylphenidate

Methylphenidate is commonly used to treat ADHD and Narcolepsy. It can also be used in cases of treatment-resistent Depression.

How Methylphenidate Works

Methylphenidate is a stimulant. It increases norepinephrine and dopamine actions in the central nervous system by blocking their reuptake and facilitating their release.

Cautions when Using Methylphenidate

In people with heart disease (especially cardiac structural abnormalities), cardiovascular disease, hypertension, hyperthyroidism, a seizure disorder, or glaucoma, advice from the appropriate medical specialist should be obtained before starting Methylphenidate.

Methylphenidate can worsen states of anxiety and agitation. It can worsen or induce psychosis in people with Psychotic Disorders, and can worsen or induce Manic or Mixed Episodes in people with Bipolar Disorder. Methylphenidate can also induce or exaccerbate tics in people with a Tic Disorder.

Methylphenidate can be abused and lead to dependence, and thus may not be appropriate for people with a history of drug abuse.

Methylphenidate should not be used during or within 14 days following the administration of an MAOI, because a hypertensive crisis may result.

Dosing of Methylphenidate

The optimal dose of Methylphenidate is one where the individual is experiencing clinical benefits without enduring signficant side-effects. In children 6 years and older, the dose should not exceed 2mg/kg/day. In adults, the usual upper limit is 90mg/day, but in some cases larger doses may be used so long as side-effects are closely monitored and are not found to be prominent.

To determine the right dose for an individual, one should start with an immediate-release form of Methylphenidate, such as Ritalin or Methylin. This should be started at 5mg once in the morning and once about four hours later, around noon. Within a few days, the individual will be able to report on whether they feel any effect from this dose.

If they are already experiencing significant side-effects at this dose, then it means that it is likely not the right medication for them.

If they report that they are feeling clinical benefits at this dose, and without too much in the way of side-effects, then this dose should be continued.

Most likely, this dose will be too small to give much of an effect, especially in adults. The next step is to increase the two daily doses each by 5mg every few days until the point is reached where the individual is experiencing benefits without signficant side-effects. This point will be the optimal dose. If, in this process, the individual begins to run into significant side-effects before they experience any benefits, then the medication will likely need to be stopped.

A third daily dose, given sometime in the afternoon about 4 hours after the second dose, can be used if the person requires the clinical benefits of the medication for more hours of the day.

Once the optimal dose is found, it may be more convenient to switch to a long-acting form of Methylphenidate, such as Concerta, Ritalin LA or Metadate CD. These forms need to be taken only once a day in the morning, and give a smoother, more even effect throughout the day.

In general, the doses of the different forms of Methylphenidate should be equivalent in terms of total daily dose. For example, Ritalin or Methylin 10mg three times a day is equivalent to Ritalin SR, Methylin ER, or Metadate ER 15mg twice a day, which is equivalent to Ritalin LA or Metadate CD 30mg once a day.

The exception to this dose conversion rule is with Concerta. Concerta 18mg/day is equivalent to 12mg/day of the other forms of Methylphenidate. Therefore, 5mg of Ritalin or Methylin used two or three times a day can be converted to 18mg of Concerta daily.

After several weeks of use of Methylphenidate, a dose that had been effective may start to be less effective, and an adjustment upwards in the dose may be necessary.

Onset of action

Therapeutic effect in ADHD can be seen as soon as the first day of use. It can take several weeks to attain maximum therapeutic effect. If no significant effects are seen after a few days at a dose where the patient is already experiencing side-effects, then it likely will not work at all.

Kidney impairment

No dose adjustment necessary.

Liver impairment

No dose adjustment necessary.

Side-effects of Methylphenidate

Below is a list of most of the reported side-effects of Methylphenidate. Most of these side-effects occur in only a minority of individuals, and many also resolve with time while the medication is continued.

Cardiovascular: palpitations; tachycardia; elevation of blood pressure; arrhythmias; see also serious side-effects.

Central Nervous System: dizziness; headache; insomnia; dyskinesia; tremor; exacerbation of motor and phonic tics; see also serious side-effects.

Endocrine: evidence shows that Methylphenidate does not cause significant suppression of normal growth in children [ref].

Eyes, Ears, Nose and Throat: dry mouth; unpleasant taste; blurred vision; worsening of glaucoma.

Gastrointestinal: nausea; diarrhea; constipation; abdominal pain; loss of appetite; weight loss.

Genitourinary: urinary retention; dysmenorrhea.

Psychiatric: anxiety; irritability; restlessness; agitation; psychosis (more likely in people with Psychotic Disorders or Bipolar Disorder); mania and mixed states (more likely in people with Bipolar Disorder); substance abuse and dependence (more likely in people with a history of substance misuse).

Respiratory: upper respiratory tract infections; cough; pharyngitis; sinusitis.

Common side-effects of Methylphenidate

Insomnia, headache, nervousness, restlessness, loss of appetite, nausea, dry mouth, constipation, diarrhea, weight loss.

Rare but serious side-effects of Methylphenidate

  • heart attack and stroke, more likely in people with pre-existing cardiovascular disease
  • seizures, more likely in people with pre-existing seizure disorders.
  • rare reports of cardiomyopathy
  • sudden death has been reported in a few individuals with pre-existing cardiac structural abnormalities.

Methylphenidate overdose

Restlessness, panic states, agitation, psychosis, tremor, fever, rapid respiration, nausea, vomiting, diarrhea, abdominal cramps, hyperreflexia, rhabdomyolysis, arrhythmias, hypertension or hypotension, circulatory collapse, seizures. Can lead to coma and death.

Methylphenidate and pregnancy

Category C: some animal studies show adverse effects at very high doses, but no controlled human studies have been done; should only be used in pregnancy if clearly needed and if benefits outweigh potential risks.

Medical Monitoring for Methylphenidate

Blood pressure should be monitored regularly. Weight and height should be measured in children.

Drug Interactions with Methylphenidate

  • Use caution when combining Methylphenidate with other noradrenergic or dopaminergic medications, like Methylphenidate, Bupropion, Venlafaxine, Duloxetine, and most Tricyclic Antidepressants.
  • Methylphenidate should not be used during or within 14 days following the administration of an MAOI, because a hypertensive crisis may result.
  • Methylphenidate can increase blood levels of certain SSRIs, Tricyclic Antidepressants, anticonvulsants, and coumarin anticoagulants.
  • Serious adverse reactions may occur if combined with Clonidine.
  • Methylphenidate may decrease the antihypertensive effects of Guanethidine.