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  • Updated 06.17.2021
  • Released 07.06.1999
  • Expires For CME 06.17.2024




Methylphenidate, a mild CNS stimulant, is the most commonly used drug for management of attention deficit hyperactivity disorder (ADHD) in children and adults. Methylphenidate may influence several neurotransmitters, especially the release and reuptake of dopamine in the striatum. It enhances cognition by increasing extracellular catecholamine levels. The drug improves cognitive deficits and reduces hyperactivity. Tests are available to identify responders versus nonresponders to methylphenidate.

Key points

• The mode of action of methylphenidate is not completely understood, but it presumably activates the brain stem arousal system and cortex to produce its stimulant effect.

• Methylphenidate treatment has been shown to improve the working memory, inhibitory control, and mental flexibility of boys with attention deficit hyperactivity disorder.

• Effect of methylphenidate on attention deficit hyperactivity disorder patients with comorbid conditions has been studied as well.

• Clinical trials as well as use in practice has shown that most patients with attention deficit hyperactivity disorder respond to methylphenidate.

• Nonresponders to methylphenidate can be identified by tests to personalize the therapy for those who are responders.

Historical note and terminology

Methylphenidate was approved by the United States Food and Drug Administration in 1956. It is the most widely used psychostimulant for attention deficit hyperactivity disorder and accounts for 69% of the market for these drugs.

In 2000, the Food and Drug Administration approved an extended release preparation of methylphenidate hydrochloride for once daily dosing. A refined formulation of methylphenidate, dexmethylphenidate hydrochloride, is available. Some controversy has been generated, mostly by public groups, expressing concern at the excessive use of psychostimulants in attention deficit hyperactivity disorders and even raising the possibility of overdiagnosis of this disorder. No scientific evidence has emerged to support this concern.

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