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pitolisant

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Also known as BF2.649, tiprolisant

Pitolisant, sold under the brand name Wakix among others, is a medication used for the treatment of excessive daytime sleepiness in adults with narcolepsy. It is an inverse agonist of the histamine H3 receptor. It represents the first commercially available medication in its class, so that the U.S. Food and Drug Administration (FDA) declares it a first-in-class medication. Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person's wakefulness. It was approved by the European Medicines Agency (EMA) in March 2016 for narcolepsy with or without cata

Key facts

Drug.Verifiedfields
changed
Drug.Watchedfields
changed
Drug.verifiedrevid
464208162
Drug.image
Pitolisant skeletal.svg
Drug.image_class
skin-invert-image
Drug.width
250
Drug.caption
Molecular structure of pitolisant
Drug.image2
Pitolisant 3D.png
Drug.image_class2
bg-transparent
Drug.tradename
Wakix, Ozawade
Drug.MedlinePlus
a619055
Drug.DailyMedID
Pitolisant
Drug.routes_of_administration
By mouth
Drug.caption2
3D representation of a pitolisant molecule
Drug.class
Histamine H3 receptor inverse agonist
Drug.ATC_prefix
N07
Drug.ATC_suffix
XX11
Drug.legal_CA
Rx-only

via Wikipedia infobox

Wikidata facts

Mass
295.170292
Show 4 more facts
chemical formula
C₁₇H₂₆ClNO
canonical SMILES
C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
Commons category
Pitolisant
defined daily dose
18
Sources (4)

via Wikidata · CC0

~6 min read

Article

8 sections
Contents
  • Medical uses
  • Side effects
  • Pharmacology
  • History
  • Society and culture
  • Legal status
  • References
  • External links

Pitolisant, sold under the brand name Wakix among others, is a medication used for the treatment of excessive daytime sleepiness in adults with narcolepsy. It is an inverse agonist of the histamine H3 receptor. It represents the first commercially available medication in its class, so that the U.S. Food and Drug Administration (FDA) declares it a first-in-class medication. Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person's wakefulness. It was approved by the European Medicines Agency (EMA) in March 2016 for narcolepsy with or without cataplexy, and for excessive daytime sleepiness by the FDA in August 2019. The most common side effects include difficulty sleeping, nausea, and feeling worried.

== Medical uses == Pitolisant is indicated in adults for the treatment of narcolepsy. Narcolepsy is a chronic sleep disorder that causes overwhelming daytime drowsiness. Pitolisant is also indicated to improve alertness and reduce excessive daytime sleepiness in adults with obstructive sleep apnea.

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