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Histamine H3 receptor antagonists / inverse agonists for ADHD and ASD


Histamine H3 receptor antagonists / inverse agonists for ADHD and ASD

Histamine H3 receptor antagonists / inverse agonists increase the activity of histaminergic neurons in the brain and thereby promote arousal and cognition1

H3 antagonists / inverse agonists have great potential for the treatment of a variety of CNS disorders, including2

  • ADHD
  • Alzheimer’s disease
  • mild cognitive impairment
  • Schizophrenia

A number of H3 antagonists / inverse agonists have been investigated in animal studies. The results included an increase in dopamine levels due to reduced dopamine reuptake in the areas of the brain relevant to ADHD and an improvement in the social deficits typical of ASD.
This may be a key to the frequent comorbidity of ADHD and ASD.

A larger double-blind RCT study of 335 adults with ADHD found only slight improvements of an H3 antagonist (Bavisant) compared to 80 mg atomoxetine and 54 mg OROS-MPH. The mean change in ADHD RS-IV total score after 42 days of use was:3

  • -8.8 in the placebo group, 2.7 % TEA
  • -9.3 Bavisant 1 mg, 61.8 % TEA
  • -11.2 Bavisant 3 mg, 82.4 % TEA
  • -12.2 Bavisant 10 mg, 89 % TEA
  • -15.3 Atomoxetine 80 mg, 83.8 TEA
  • -15.7 OROS methylphenidate 54 mg, 82.4 % TEA
    TEA indicates the frequency of side effects.

Although the first HR3 antagonists are available as drugs (e.g. pitolisant (as Ozawade® for daytime sleepiness in obstructive sleep apnoea or as Wakix® for narcolepsy), no drug has yet been approved for the treatment of ADHD or ASD.

More on H3 agonists at H3 histamine receptor in the article Histamine.

Diese Seite wurde am 11.01.2024 zuletzt aktualisiert.