Known brand names include Ritalin.
A stimulant tablet (Schedule II controlled substance) for ADHD in children 6 and older and adults, and for narcolepsy. It raises dopamine and norepinephrine activity in the brain, and it carries a boxed warning for abuse, misuse, and addiction.
Labeled use. In children 6 years and older and in adults.
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Stimulants (methylphenidate or amphetamines) are first-line drug therapy for ADHD in school-age children and adults. Immediate-release methylphenidate allows flexible short-acting dosing but needs 2 or 3 doses a day, so extended-release forms are often preferred for once-daily coverage and lower diversion risk. Nonstimulants such as atomoxetine or guanfacine are options when misuse risk, tics, intolerance, or cardiac concerns limit stimulant use. For narcolepsy, wake-promoting agents such as modafinil are common alternatives.
A CNS stimulant that inhibits presynaptic reuptake of dopamine and norepinephrine and increases their release into the synapse; how this treats ADHD and narcolepsy is unknown. It is a racemic mix in which the d-threo enantiomer is the more active form. Peak plasma level comes about 2 hours after a tablet, and it is metabolized mainly by de-esterification to ritalinic acid, which has little or no activity and is excreted in urine.
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The label does not describe a narrow therapeutic index or direct dosing by measured blood levels of the drug.
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Doses come from the FDA label. Study tool, not for clinical decisions.
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Not studied in renal impairment, but less than 1% of a dose is excreted unchanged in urine and the main metabolite, ritalinic acid, has little or no activity, so little effect is expected. No adjustment is given.
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Abuse, misuse, and addiction. Methylphenidate has a high potential for abuse and misuse that can progress to a substance use disorder, including addiction. Misuse can cause overdose and death, with higher risk at higher doses or when snorted or injected. Assess abuse risk before prescribing, teach patients and families about safe storage and disposal, and keep reassessing and monitoring for signs of misuse throughout treatment.
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No specific antidote. Overdose causes sympathomimetic toxicity: fast arrhythmias, high or low blood pressure, agitation, confusion, hallucinations, seizures, and life-threatening hyperthermia (above 104°F) with rhabdomyolysis. Give supportive care, consider multiple drug ingestion, and contact Poison Help or a toxicologist; dialysis does not help because of the large volume of distribution and rapid metabolism.
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Published studies and postmarketing reports have not found a drug-related risk of major birth defects, miscarriage, or other adverse outcomes. Stimulants can constrict blood vessels and may reduce blood flow to the placenta. A national pregnancy registry for ADHD medications collects outcome data.
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Methylphenidate is present in human milk, giving infant doses of 0.16% to 0.7% of the mother's weight-adjusted dose, with no reported effects on breastfed infants or milk production. Watch the infant for agitation, insomnia, poor feeding, and reduced weight gain.
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Established for ADHD at ages 6 to 17; not established under age 6, and long-term efficacy in children is not established. Start 5 mg twice daily before breakfast and lunch, increasing by 5 to 10 mg weekly; more than 60 mg per day is not recommended. Monitor height and weight, since stimulants can slow growth and treatment may need to be interrupted.