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Droxidopa for ADHD


Droxidopa for ADHD

Droxidopa (L-threo-dihydroxyphenylserine, L-DOPS) is a prodrug of dopamine and norepinephrine. It can cross the blood-brain barrier and is converted to dopamine and norepinephrine in the brain.

USA: Northera (since 2014)
Japan: DOPS (since 1989)
Switzerland: no approval so far

Droxidopa is considered an orphan drug.

A combination of droxidopa and benserazide, a peripheral amino acid decarboxylase inhibitor, had a stimulatory effect on the PFC and inhibited dopaminergic neurons in rats. Further, in juvenile SHR/NCrl rats, which serve as an animal model of ADHD-C, showed:1

  • Hyperactivity reduced
  • Impulsivity reduced
  • Inattention reduced

In juvenile WKY/NCrl rats, which serve as an animal model of ADHD-I subtype, administration of droxidopa with benserazide induced:1

  • Impulsivity reduced
  • Inattention unchanged

Its use in the treatment of ADHD in humans has hardly been researched to date.
A small open-label trial of droxidopa (200 to 600 mg 3 times a day for 3 weeks) found improvement in ADHD symptoms without significant side effects. Nevertheless, 7 of the 20 participants terminated participation prematurely.2