Methylphenidate

Clinical dataPronunciationTrade namesRitalin, Concerta, othersOther namesMPHAHFS/Drugs.comMonographMedlinePlusa682188License dataPregnancy
categoryDependence
liabilityPhysical: None
Psychological: ModerateAddiction
liabilityModerateRoutes of
administrationMedical: Oral, transdermal
Recreational: Oral, insufflation, sublingual, rectal, intravenousDrug classStimulant; Norepinephrine–dopamine reuptake inhibitor (NDRI)ATC codeLegal statusLegal statusPharmacokinetic dataBioavailabilityOral: ~45% (range: 20–70%)Protein binding~25% (±5%) binds to plasma proteinsMetabolismLiver (70%) mostly CES1-mediatedMetabolitesα-phenyl-2-piperidine acetic acid (ritalinic acid)Onset of action~15–45 minutes, depending on formulationElimination half-life4–5 hoursDuration of actionExcretionUrine (80%), primarily as metabolitesIdentifiersCAS NumberPubChemCIDIUPHAR/BPSDrugBankChemSpiderUNIIKEGGChEBIChEMBLCompTox Dashboard(EPA)ECHA InfoCard100.003.662Chemical and physical dataFormulaC₁₄H₁₉NO₂Molar mass233.311 g·mol3D model (JSmol)Melting point74 °C (165 °F) Boiling point136 °C (277 °F) (verify)

Methylphenidate, sold under the brand names Ritalin and Concerta, among others, is a central nervous system (CNS) stimulant used primarily in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It may be taken by mouth or applied to the skin, and different formulations have varying durations of effect. For ADHD, the effectiveness of methylphenidate is generally comparable to atomoxetine, but its effect is modestly lower than that of amphetamine. However, methylphenidate is generally preferred as a first-line treatment in children, while amphetamine-based medications are often preferred in adults.

Methylphenidate reduces core ADHD symptoms and is thought to do so primarily by increasing dopamine and norepinephrine activity in the brain. It may also improve aspects of executive functions, including working memory, sustained attention, and inhibitory control. In clinical use, the effects are generally described as lasting for several hours, although individual response varies substantially between formulations and patients.

At therapeutic doses, methylphenidate increases alertness and concentration and reduces hyperactivity and impulsive behavior in people with ADHD. Common side effects include loss of appetite, weight loss, trouble sleeping, and small increases in heart rate and blood pressure. Long-term treatment in children has been associated with slightly slower growth. Methylphenidate can be misused; dependence and withdrawal are mainly reported with high-dose or non-medical use and are uncommon at therapeutic doses.

Methylphenidate is believed to work by blocking the reuptake of dopamine and norepinephrine by neurons. It is a CNS stimulant of the phenethylamine and piperidine classes. It is available as a generic medication. In 2023, it was the 50th most commonly prescribed medication in the United States, with more than 13million prescriptions.