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Summary of the Medical Uses of Methylphenidate
by Seth
Dec 2002
Methylphenidate is a prescription drug often used for attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), and narcolepsy. Although the FDA has not approved these uses, it is also used in mild to moderate depression, brain injury, HIV infection fatigue, post-stroke patients, and for anesthesia-related hiccups.

Prescription drugs that the are considered addictive or recreational are scheduled by how much control the government believes is necessary to reduce inappropriate uses pursuant to U.S. Code of Federal Regulations, Title 20 Part 1308.1 (1987). Methylphenidate has been put into Schedule II, the most restrictive medical category. Due to its schedule, prescriptions for methylphenidate may not be called in or faxed to a pharmacy except in an emergency situation.

Use of methylphenidate for ADD and ADHD is common but controversial. Many people feel that it is over prescribed. A new non-stimulant treatment for ADD and ADHD that will be named Straterra (a nor-epinephrine reuptake inhibitor) could dramatically decrease the use of stimulants. Dr. Mary Ann Block, author of "No More Ritalin: Treating ADHD Without Drugs" is one of the foremost critics of the use of Ritalin. She maintains that methylphenidate dose not correct the underlying causes of ADHD. These may include: hypoglycemia, allergies and sensitivities, environmental factors and hyperthyrodism. The Feingold Association of the United States (http://www.feingold.org) is an organization that works on drug-free approaches to ADD and ADHD.

Chemically, methylphenidate hydrochloride is methyl-alpha-phenyl-2-piperidineacetate hydrochloride. It is a white, odorless, fine crystalline powder with a chemical formula C14H20ClNO2. . It is slightly acidic. A 5% aqueous solution is neutral to litmus.. It is freely soluble in water and methanol, soluble in alcohol, and slightly soluble in chloroform and acetone. Its molecular weight is 269.77. pKa equals 8.9. LD50 in mice (the dose that is lethal to 50% of the mice studied) is 190 mg/kg.

Methylphenidate is marketed under many names. Different companies have produced methylphenidate with a variety of delivery systems. These different systems are used to prevent children from having to take doses at school, to keep a steady level of the drug, or to cause the level to rise sharply at specific times. Novartis markets methylphenidate as Ritalin. Mallinckrodt markets it as Methylin, Alza calls it Concerta, and Medeva uses Metadate as their name.

The FDA has approved methylphenidate as part of a total treatment program in children with a behavioral syndrome characterized by moderate to severe distractibility, short attention span, hyperactivity, emotion lability, and impulsivity greater than that expected for a child that age. Stimulants are not for childen or adults who exhibit symptoms secondary to environmental factors or primary psyciatric disorders, including psychosis. When symptoms are associated with acute stress reactions, methylphenidate is usually not indicated.

The mode of action in people is not completely understood, but methylphenidate activates the brain stem arousal system and cortex to produce its stimulant effect. Mehtylphenidate is very similar to other amphetamines structurally. It appears to increase extracellular dopamine. This action is likely achieved through inhibition of dopamine transporter protein. Some research also shows that methylphendate inhibits serotonin transporter protein. This action may partially explain its antidepressant effects. Methylphenidate also increases norepinephrine (noradrenaline). Methylphenidate also affects regional cerebral blood flow in the cerebellar vermis.

Dosage should be individualized according to the needs of the patients.

Adult Dosages: #
Immediate release tablets should be given 2 or 3 times daily, preferabley 30-45 minutes before meals. Average dosage is 20 to 30 mg daily. Some patients may require 40-60 mg daily. In others 10 to 15 mg will be adequate. Patients who are unable to sleep should take their last dose before 6 pm. Women appear to absorb methylphenidate better than men, and may need slightly lower dosages.

Time released preparations vary. Sustained-release tablets such as Ritalin SR have a duration of approximately 8 hours and may be used in place of regular tablets. These tablets must be swallowed whole, never crushed or chewed. Crushing or chewing causes the time release mechanism to fail, delivering all of the medication at once.

Concerta should be given once daily in the morning, without regard to meals. Doses start at 18 mg in the morning and may range up to 54 mg. Each tablet releases the drug over 12 hours.

Metadate CD is given once daily in the morning. Capsules should not be opened. 30% of the dose is immediate release with the remainder releasing slowly. Fatty foods may delay absorption.

Children's Dosages: #
(children over 6 years old)
A typical starting dose is 5 mg twice daily (before breakfast and lunch) with gradual increase if necessary. The total dose should not exceed 60 mg. If improvement is not observed after dosage adjustment over 1 month, discontinuation is recommended.

It is not uncommon for patients on methylphenidate to get worse. Remember, it is a stimulant.

It is recommended that methylphenidate should be discontinued periodically to assess the condition. Improvement may be sustained when the drug is either temporarily or permanently discontinued. Drug treatment should not be indefinite and usually may be discontinued after puberty.

Overdosage: #
Overdosage results primarily in overstimulation of the central nercous system and  excessive sypathomimetic effects. Symptoms and signs of overdose may include:  vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsion (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia (high fever), tachcardia, palpitations, cardiac arrhythmias, hypertension, mydriais, and dryness of mucous membranes.

Treatment of methylphenidate overdoses consists of supportive measures and symptomatic treatments. The patient should be protected against self-inury and against external stimuli that would aggravate overstimulation. Gastric contents may be evacuated by gastric lavage. In severe intoxication, use of a SHORT ACTING barbituate before lavage is indicated. Other measures to detoxify the gut include use of activated charcoal and cathartics. External cooling measures may be required. Peritoneal dialysis or extracorporeal hemodialysis has not had efficacy proven.  Benzodiazepines are commonly used in emergency rooms to alleviate symptoms.  In case of severe overdoses, standard measures to reduce hypertension and hypertensive crises are used.

Alternatives to using methylphenidate: #
There are a variety of amphetamines by prescription with similar side effects and uses.  There has been some "off-label" use of modafinil (a novel stimulant) as a replacement for ritalin, but this use is not approved by the FDA and there is little anecdotal and no scientific evidence that it is effective as a replacement for methylphenidate for patients.

Straterra, a nor-epinephrine uptake inhibitor may also be used. It works similarly to Effexor.

DMAE (dimethylaminoethanol)--once available by prescription, this nutritional supplement is supportive for attention and concentration. It is a biological precursor to acetylcholine. As such, it is also useful for Alzheimer's disease. Most recently, topical DMAE has gained acceptance as a cosmetic ingredient to increase muscle tone in the face. DMAE is typically extracted from salmon. It is inexpensive. Twinlabs makes one that is $8.95 retail for 100. Blue Bonnet is $9.95 per 100 put typically offers a money back guarantee.

Essential Fatty Acids are perhaps the most important supplements for a person with concentration issues. One with a balance of omega 3, 6, and 9 fatty acids is ideal. Consider Total EFA by Health From the Sun (as they state on the label that theirs is cold pressed and hexane free) or Ultra 369 from KAL.

GABA Gamma-Aminobutyric Acid acts as an inhibiting amino acid. It may reduce anxiety, nervousness, etc… It is most ideal for those patients who have hyperactivity in addition to attention deficit.

Magnesium is supportive for concentration. It is essential for over 300 enzymatic reactions in people. If given in the evening, magnesium may also help with sleep.

Lifestyle Factors: #
Some alternative medicine experts believe the conditions treated with methylphendate can often be treated with less habituating, stimulating means.  Avoidance of refined sugars, food additives and dyes may be helpful. For more info, see  www.feingold.org . Food allergies may also be at play and patients considering methylphenidate might consider food allergy testing. Great Smokies Diagnostic Labs has my favorite test  www.gsdl.com  It tests for IgG and IgE antibodies.

Keeping on a schedule, getting regular sleep, consistently timed meals,  and reducing chaotic stress can help reduce ADD/ADHD symptoms.

Biofeedback is helpful for many children and adults who would otherwise use methylphenidate.  Some physicians recommend learning relaxation and meditation techniques.

Side Effects: #

The information in this document regarding side effects and warnings comes from Drugs.com and the Ritalin professional packet insert. The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)--not necessarily inclusive:

Symptoms requiring medical attention:

  • More Common Symptoms
    Hypertension (increased blood pressure), tachycardia (fast heartbeat)--especially with doses greater than 0.5 mg per kg of body weight (mg/kg)

  • Less Common Symptoms
    Angina (chest pain), arthralgia (joint pain), dyskinesia (uncontrolled movements of the body), fever, skin rash or hives, thrombocytopenia (rarely, unusual bleeding or bruising; black tarry stools; blood in urine or stools; pinpoint red spots on skin)--usually asymptomatic.
    Note: Arthralgia, fever, skin rash or hives, and thrombocytopenia may be indicative of a hypersensitivity reaction to methylphenidate. Rarely, exfoliative dermatitis and erythema multiforme have occurred.


  • Rare Symptoms
    Blurred vision or other changes in vision, convulsions, muscle cramps, Tourette's syndrome (uncontrolled vocal outbursts and/or tics [uncontrolled repeated body movements]), With prolonged use or at high doses, Psychosis, toxic (changes in mood; confusion; delusions; depersonalization; hallucinations), weight loss --possibly more frequent in children.


Symptoms needing for medical attention only if they continue or are bothersome

  • Common Symptoms
    Anorexia (loss of appetite)--usually transient; possibly more frequent in children, CNS stimulation (nervousness; trouble in sleeping)--possibly more frequent in children

  • Less Common Symptoms
    Dizziness, drowsiness, headache, nausea, stomach pain --possibly more frequent in children


  • Symptoms indicating possible withdrawal and the need for medical attention if they occur after medication is discontinued:
    Mental depression, severe, unusual behavior, unusual tiredness or weakness

    Drug Interactions: #
    The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)--not necessarily inclusive (major clinical significance):


    Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

    Anticholinergics or other medications with anticholinergic activity (concurrent use may intensify anticholinergic effects because of secondary anticholinergic effects of methylphenidate).

    arial'>Anticonvulsants, especially phenytoin, phenobarbital, and primidone or Anticoagulants, coumarin-or indanedione-derivative or Phenylbutazone (serum concentrations of these medications may be increased because of inhibition of metabolism by methylphenidate, possibly resulting in toxicity; dosage adjustments may be necessary)



    Antidepressants, tricyclic, especially desipramine and imipramine    (serum concentrations of these medications may be increased because of inhibition of metabolism by methylphenidate, possibly resulting in toxicity; also, concurrent use may antagonize the effects of methylphenidate)

    Antihypertensives or Diuretics used as antihypertensives    (hypotensive effects may be reduced when these medications are used concurrently with methylphenidate; the patient should be carefully monitored to confirm that the desired effect is being obtained)

    CNS stimulation–producing medications, other  (concurrent use with methylphenidate may result in additive CNS stimulation to excessive levels, causing nervousness, irritability, insomnia, or possibly seizures or cardiac arrhythmias; close observation is recommended)

    Monoamine oxidase (MAO) inhibitors, including furazolidone, procarbazine, and selegiline (concurrent use may potentiate the effects of methylphenidate, possibly resulting in a hypertensive crisis; methylphenidate should not be administered during or within 14 days following the administration of MAO inhibitors)

    Pimozide (methylphenidate may provoke tics; before therapy with pimozide is initiated, methylphenidate should be withdrawn to determine the cause of observed tics; pimozide is not indicated for the treatment of tics caused by other medications)


    Vasopressors (pressor effects may be potentiated when vasopressors are used concurrently with methylphenidate)

    Medical considerations/Contraindications The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)-- not necessarily inclusive (major clinical significance).

    Except under special circumstances, this medication should not be used when the following medical problems exist: Anxiety, tension, or agitation, severe or Depressive disorder amenable to treatment with conventional antidepressants. Glaucoma or Motor tics other than Tourette's disorder (may be exacerbated).
    Risk-benefit should be considered when the following medical problems exist.

    Emotional instability, including history of drug dependence or alcoholism (increased potential for addiction or abuse).

    Epilepsy or other seizure disorders (seizure threshold may be lowered)

    Gastrointestinal Obstructions, pathologic or iatrogenic    (increased chance of obstructions due to nondeformable controlled-release tablet design)

    Gilles de la Tourette's syndrome, family history or diagnosis of    (motor and vocal tics may be exacerbated; however, some patients, under close supervision, may benefit from cautious trials)

    Hypertension (may be exacerbated)


    Psychosis: (symptoms of behavior disturbance and thought disorder may be exacerbated in children with psychoses)

    Sensitivity to methylphenidate

    Patient monitoring
    The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; major clinical significance):
    Assessment of amount and frequency of medication use    (recommended at periodic intervals to detect signs of dependence or abuse during long-term therapy)


    Blood pressure determinations (recommended at periodic intervals during therapy, especially for patients with hypertension)


    Complete blood cell, differential, and platelet counts (recommended at periodic intervals for patients on prolonged therapy)


    Monitoring of growth, both height and weight gain, in children (recommended during long-term therapy, since data are inadequate to determine whether chronic administration of methylphenidate may be associated with growth inhibition)

    Reassessment of need for therapy for behavioral syndrome in children (interruption of therapy at periodic intervals is recommended to determine if a recurrence of behavioral symptoms is sufficient to continue therapy; tapering of dose may be necessary to prevent withdrawal symptoms)


    References #
    1. Prescribing Information, Ritalin hydrochloride. November 1999, Novartis Pharmaceuticals Corporation, East Hanover New Jersey
    2. Greenblatt E.N., Osterberg A.C. J. Pharmacol. Exp. Ther. Toxicity Data 131, 115 (1961)
    3. Merk Index, 11th Ed. Merck & Co., Rahway, NJ 1990
    4. Drug Facts & Comparisons, Wolters Kluwer Company, St Louis, Missouri, 2002
    5. http://www.acnp.org/sciweb/journal/Npp110602427/default.htm
    6. http://www.drugs.com/xq/cfm/pageid_0/htm_001417/tgid_15/type_pros/bn_Ritalin/micrpro_medex/qx/index.htm