Methylphenidate

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Concerta, Equasym, Medikinet, Ritalin; Belgium: Concerta, Ritaline; Bulgaria: Concerta; Cyprus: Concerta; Czech Republic: Concerta, Ritalin; Denmark: Concerta, Equasym, Medikinet, Motiron, Ritalin; Estonia: Concerta; Finland: Concerta; France: Concerta, Ritaline; Germany: Concerta, Equasym, Medikid, Medikinet, Methylpheni, Methylphenidat, Ritalin; Greece: Concerta, Equasym, Ritalin; Hungary: Ritalin; Ireland: Concerta, Equasym, Ritalin; Italy: Ritalin; Latvia: Concerta, Ritalin; Lithuania: Concerta; Luxembourg: Concerta, Rilatine; Malta: Concerta, Equasym, Ritalin; Netherlands: Concerta, Equasym, Medikinet, Methylfenidaat, Ritalin; Poland: Concerta, Medikinet; Portugal: Concerta, Ritalina, Rubifen-Rubió; Romania: Concerta; Slovakia: Concerta; Slovenia: Concerta; Spain: Concerta, Medikinet, Omozín, Rubifén; Sweden: Concerta; UK: Ritalin.

North America

Canada: Biphentin, Concerta, Methylphenidate, Ritalin; USA: Concerta, Daytrana, Metadate, Methylin, Methylphenidate, Ritalin.

Latin America

Argentina: Concerta, Methylin, Ritalina, Rubifén; Brazil: Concerta, Ritalina; Mexico: Concerta, Metadate, Ritalín, Tradea.

Asia

Japan: Concerta, Ritalin.

Drug combinations

Chemistry

Methylphenidate: C~14~H~19~NO~2~. Mw: 233.31. (1) 2-Piperidineacetic acid, α-phenyl-, methyl ester; (2) α-Phenyl-2-piperidineacetic acid methyl ester. CAS-113-45-1 (2003).

Methylphenidate Hydrochloride: C~14~H~19~NO~2~ HCl. Mw: 269.77. 2-Piperidineacetic acid, α-phenyl-, methyl ester, hydrochloride, (R*,R*)-(±)-. CAS-298-59-9.

Pharmacologic Category

Anorexigenic Agents and Respiratory and Cerebral Stimulants, Miscellaneous. (ATC-Code: N06BA04).

Mechanism of action

Blocks reuptake of norepinephrine and dopamine into presynaptic neurons. Appears to stimulate cerebral cortex and subcortical structures similar to amphetamines.

Therapeutic use

Treatment of attention-deficit hyperactivity disorder. Symptomatic management of narcolepsy.

Pregnancy and lactiation implications

Animal studies have shown teratogenic effects to fetus. There are no adequate, well-controlled studies in pregnant women. Do not use in women of childbearing age unless potential benefit outweighs possible risk. Enters breast milk (use caution).

Unlabeled use

Depression (especially elderly or medically ill).

Contraindications

Hypersensitivity to methylphenidate, any component of the formulation, or idiosyncratic reactions to sympathomimetic amines. Marked anxiety, tension, and agitation. Glaucoma. Use during or within 14 days following MAOI therapy. Family history or diagnosis of Tourette’s syndrome or tics. Severe hypertension, heart failure, arrhythmia, hyperthyroidism, recent MI or angina. Concomitant use of halogenated anesthetics.

Warnings and precautions

Cardiovascular events, including sudden death in pre-existing structural cardiac abnormalities or other serious heart problems, might occur. Difficulty in accommodation and blurred vision reported with use of stimulants. Potential for drug dependency exists. Use with caution in hypertension and other cardiovascular conditions which might be exacerbated by increases in blood pressure or heart rate. Some products contraindicated in severe hypertension, hyperthyroidism or angina. Use with caution in pre-existing psychosis or bipolar disorder (may induce mixed/manic episode), and in history of seizure disorder. Use of stimulants associated with suppression of growth in children. Transdermal system may cause allergic contact sensitization. Some preparations might contain sucrose or lactose (avoid administration in hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption).

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