pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy

Narcolepsy is a debilitating sleep disorder that presents with excessive daytime sleepiness (EDS) and cataplexy, which is a sudden paralysis of muscle tone triggered by strong emotions such as laughing. It is also associated with many other disorders, including psychiatric disorders, neurologic illn...

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Main Authors: Noeen Sarfraz, David Okuampa, Hannah Hansen, Mark Alvarez, Elyse M. Cornett, Juyeon Kakazu, Adam M. Kaye, Alan D. Kaye
Format: Article
Language:English
Published: Open Medical Publishing 2022-05-01
Series:Health Psychology Research
Online Access:https://doi.org/10.52965/001c.34222
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author Noeen Sarfraz
David Okuampa
Hannah Hansen
Mark Alvarez
Elyse M. Cornett
Juyeon Kakazu
Adam M. Kaye
Alan D. Kaye
author_facet Noeen Sarfraz
David Okuampa
Hannah Hansen
Mark Alvarez
Elyse M. Cornett
Juyeon Kakazu
Adam M. Kaye
Alan D. Kaye
author_sort Noeen Sarfraz
collection DOAJ
description Narcolepsy is a debilitating sleep disorder that presents with excessive daytime sleepiness (EDS) and cataplexy, which is a sudden paralysis of muscle tone triggered by strong emotions such as laughing. It is also associated with many other disorders, including psychiatric disorders, neurologic illnesses, and medication side effects. Common causes of delayed and incorrect diagnoses of these conditions include lack of physician familiarity with narcolepsy symptoms and comorbidities which mask narcolepsy signs and symptoms. Current pharmacologic therapies include Modafinil and Armodafinil for EDS and sodium oxybate for cataplexy. This review discusses the epidemiology, pathophysiology, risk factors, presentation, treatment of narcolepsy, and the role of a novel drug, Pitolisant, in the treatment of EDS in adults with narcolepsy. Pitolisant is a histamine-3 receptor (H3R), competitive antagonist, and inverse agonist, acting through the histamine system to regulate wakefulness. It is a novel drug approved in August 2019 by the FDA, is not classified as a controlled substance, and is approved for use in Europe and the United States to treat EDS and cataplexy in narcolepsy. Recent phase II and III trials have shown that Pitolisant helps reduce the ESS score and cataplexy. In summary, based on comparative studies, recent evidence has shown that Pitolisant is non-inferior to Modafinil in the treatment of EDS but superior to Modafinil in reducing cataplexy.
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issn 2420-8124
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spelling doaj-art-c35015e44ae2490da1739592b27f39ce2025-02-11T20:30:26ZengOpen Medical PublishingHealth Psychology Research2420-81242022-05-01102pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsyNoeen SarfrazDavid OkuampaHannah HansenMark AlvarezElyse M. CornettJuyeon KakazuAdam M. KayeAlan D. KayeNarcolepsy is a debilitating sleep disorder that presents with excessive daytime sleepiness (EDS) and cataplexy, which is a sudden paralysis of muscle tone triggered by strong emotions such as laughing. It is also associated with many other disorders, including psychiatric disorders, neurologic illnesses, and medication side effects. Common causes of delayed and incorrect diagnoses of these conditions include lack of physician familiarity with narcolepsy symptoms and comorbidities which mask narcolepsy signs and symptoms. Current pharmacologic therapies include Modafinil and Armodafinil for EDS and sodium oxybate for cataplexy. This review discusses the epidemiology, pathophysiology, risk factors, presentation, treatment of narcolepsy, and the role of a novel drug, Pitolisant, in the treatment of EDS in adults with narcolepsy. Pitolisant is a histamine-3 receptor (H3R), competitive antagonist, and inverse agonist, acting through the histamine system to regulate wakefulness. It is a novel drug approved in August 2019 by the FDA, is not classified as a controlled substance, and is approved for use in Europe and the United States to treat EDS and cataplexy in narcolepsy. Recent phase II and III trials have shown that Pitolisant helps reduce the ESS score and cataplexy. In summary, based on comparative studies, recent evidence has shown that Pitolisant is non-inferior to Modafinil in the treatment of EDS but superior to Modafinil in reducing cataplexy.https://doi.org/10.52965/001c.34222
spellingShingle Noeen Sarfraz
David Okuampa
Hannah Hansen
Mark Alvarez
Elyse M. Cornett
Juyeon Kakazu
Adam M. Kaye
Alan D. Kaye
pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
Health Psychology Research
title pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
title_full pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
title_fullStr pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
title_full_unstemmed pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
title_short pitolisant, a novel histamine-3 receptor competitive antagonist, and inverse agonist, in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
title_sort pitolisant a novel histamine 3 receptor competitive antagonist and inverse agonist in the treatment of excessive daytime sleepiness in adult patients with narcolepsy
url https://doi.org/10.52965/001c.34222
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