Stimulants: Methylphenidates

Methylphenidate

  • Methylphenidate was first synthesized in 1944 by the CIBA Pharmaceutical company. 
  • In the 1960s and 1970s, Methylphenidate was first marketed for “hyperkinetic syndrome” (now known as ADHD), narcolepsy, and depression.
  • Methylphenidate, like many other stimulants (e.g., cocaine) binds to, and inhibits, the dopamine transporter (DAT) on dopaminergic neurons and the norepinephrine transporter (NET) on norepinephrine neurons in the brain.
  • Inhibition of DAT and NET increases extracellular levels of dopamine and norepinephrine, respectively, in target areas of the brain. 
  • Methylphenidate is primarily used to treat Attention Deficit Hyperactivity Disorder, Narcolepsy, Depression, and Chronic Fatigue.
  • Methylphenidate comes in a number of formulations with different durations of action.
  • Brand names for methylphenidate-based medications include Focalin, Ritalin, Metadate, Concerta, Daytrana, and Methylin

Methylphenidate (Ritalin, Concerta)

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