Side Effects of pitolisant: A Synthesis of Findings from 14 Studies

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This page's analysis is based on PubMed data provided by the U.S. National Library of Medicine (NLM).

Original Abstract of the Article

Main Research Findings

Pitolisant is a medication used to treat sleep disorders such as narcolepsy and hypersomnia. 1 、 5 、 10 It acts as a histamine H3 receptor antagonist, promoting the activity of histaminergic neurons in the brain to maintain wakefulness. 7 This is expected to improve excessive sleepiness due to narcolepsy and daytime sleepiness due to obstructive sleep apnea (OSA). 13 、 9 It has also been reported that pitolisant is effective in suppressing cataplexy, a symptom of narcolepsy. 5 、 1 Furthermore, pitolisant has been suggested to be effective in treating other sleep disorders such as Prader-Willi syndrome. 2 、 14

Reason for Side Effects

Pitolisant works by blocking histamine H3 receptors, which can alter the balance of the histaminergic system. 12 This change may cause side effects. 12

Common Side Effects

Headache

Headache is a common side effect of pitolisant. 5 Changes in the balance of the histaminergic system may cause headaches. 12

Insomnia

Pitolisant is a wakefulness-promoting medication, so it can cause insomnia. 5 Adjusting the timing and dosage may reduce insomnia. 5

Nausea

Pitolisant may cause digestive side effects such as nausea. 5 Changes in the balance of the histaminergic system may cause digestive symptoms. 12

Side Effect Countermeasures

Headache

If you are concerned about headaches, it is important to consult your doctor and discuss appropriate management options. 5 Various solutions can be considered, such as taking headache medication or reviewing lifestyle habits. 5

Insomnia

If you are concerned about insomnia, it is important to consult your doctor and have the timing and dosage adjusted. 5 Reviewing your sleep habits is also effective. 5

Nausea

If you are concerned about nausea, it is important to consult your doctor and discuss appropriate management options. 5 Taking anti-nausea medication or dietary therapy may be considered. 5

Comparison Between Studies

Commonalities of Studies

Multiple studies have shown that pitolisant is effective in treating sleep disorders such as narcolepsy and hypersomnia. 13 、 5 、 1 It has also been suggested that pitolisant has a higher effect on suppressing cataplexy compared to other stimulants such as modafinil. 5 、 1

Differences Between Studies

There are variations in research findings regarding the efficacy and side effects of pitolisant. 6 For example, in some studies, pitolisant has been reported to exhibit anticonvulsant effects. 6 However, in other studies, anticonvulsant effects have not been confirmed. 6 Thus, research findings on the efficacy and side effects of pitolisant may vary depending on research methods and subjects. 6

Points to Note Regarding Application in Real Life

Pitolisant is a medication that may be effective in treating sleep disorders, but it is also important to consider the risks of side effects. 5 When taking pitolisant, be sure to follow your doctor's instructions and consult your doctor immediately if you experience any side effects. 5 Also, be aware that pitolisant may affect driving and operating machinery. 5

Current Limitations of Research

Research on pitolisant is still insufficient, and long-term effects and safety have not been fully elucidated. 5 Also, there has not been enough research on the use of pitolisant in children or pregnant women. 11 Further research is needed to confirm the safety and efficacy of pitolisant. 5

Future Research Directions

Clinical trials are needed to evaluate the long-term effects and safety of pitolisant. 5 Research is also needed to investigate the safety and efficacy of pitolisant in children and pregnant women. 11 Furthermore, research on combination therapy with pitolisant and other sleep disorder treatments is also expected. 5

Conclusion

Pitolisant may be an effective medication for treating sleep disorders such as narcolepsy and hypersomnia. 13 、 5 、 1 However, it is important to consider the risk of side effects. 5 When taking pitolisant, be sure to follow your doctor's instructions and consult your doctor immediately if you experience any side effects. 5

Literature analysis of 14 papers

Positive Content

Neutral Content

Negative Content

Article Type

Randomized Controlled Trial0

Meta-Analysis0

Systematic Review0

Review8

Journal Article13

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

Author: SarfrazNoeen, OkuampaDavid, HansenHannah, AlvarezMark, CornettElyse M, KakazuJuyeon, KayeAdam M, KayeAlan D

Cataplexy treatment

EDS treatment

Pitolisant, a novel histamine-3 receptor (H3R) antagonist, has shown promising results in treating excessive daytime sleepiness (EDS) and cataplexy in adults with narcolepsy. Studies have indicated that Pitolisant is non-inferior to Modafinil in treating EDS but superior in reducing cataplexy.

Language : English

Pitolisant in an Adolescent with Prader-Willi Syndrome.

Author: PenningtonStephanie, StutzmanDanielle, SannarElise

Prader-Willi symptom improvement

This case report explores the potential benefits of pitolisant in a 15-year-old female with Prader-Willi syndrome, obsessive-compulsive disorder, autism spectrum disorder, and mild intellectual disability. The drug appears to be well-tolerated with minimal side effects.

Language : English

Orgasmolepsy in Narcolepsy Type 1 Responsive to Pitolisant: A Case Report.

Author: PellitteriGaia, DolsoPierluigi, ValenteMariarosaria, GigliGian Luigi

Cataplexy control

This case report presents a patient with narcolepsy type 1 who experienced orgasmolepsy, a rare form of cataplexy, during sexual intercourse. Pitolisant successfully controlled the cataplexy, highlighting its potential for treating orgasmolepsy in narcoleptic patients.

Language : English

Living with Narcolepsy: Current Management Strategies, Future Prospects, and Overlooked Real-Life Concerns.

Author: BarkerEmily C, FlygareJulie, ParuthiShalini, SharkeyKatherine M

Improved daytime functioning

New treatment options

Lack of efficacy

Side effects

Stigma

Narcolepsy is a sleep disorder characterized by excessive daytime sleepiness, cataplexy, and other sleep disturbances. This article reviews the current and prospective pharmacological therapies for treating narcolepsy, including new treatment options like solriamfetol and pitolisant. It also discusses challenges specific to children and women with narcolepsy, as well as the impact of health-related stigma.

Language : English

Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy.

Author: RomigiAndrea, VitraniGiuseppe, Lo GiudiceTemistocle, CentonzeDiego, FrancoValentina

This review discusses the efficacy and safety of pitolisant, a first-in-class drug for the treatment of narcolepsy. Pitolisant has been shown to be effective in treating cataplexy, daytime sleepiness, and other narcolepsy symptoms compared to placebo. It has a safe profile with headache, insomnia, and nausea being the most common side effects. Further long-term studies are needed to clarify its role in therapy and its potential as a first-line treatment option.

Language : English

Anticonvulsant effects of isomeric nonimidazole histamine H3 receptor antagonists.

Author: SadekBassem, SaadAli, SchwedJohannes Stephan, WeizelLilia, WalterMiriam, StarkHolger

Anticonvulsant effect

Proconvulsant effect

This study investigated the anticonvulsant effects of a series of H3 receptor ligands in rat models of epilepsy. The R-enantiomer of (R)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propaneamide (2) showed moderate protection in MES and STR models, while the S-enantiomer (1) had no effect. Structurally bulkier analogs, (R)-enantiomer (3) and its (S)-enantiomer (4), displayed significant dose-dependent anticonvulsant activity in MES and PTZ models, respectively. Notably, (R)-enantiomer (3) exhibited greater protection in MES than the standard H3R inverse agonist/antagonist pitolisant and comparable protection to phenytoin. These findings suggest that H3 receptor ligands, particularly the R-enantiomers, may hold promise as novel antiepileptic drugs.

Language : English

Multiple Targeting Approaches on Histamine H3 Receptor Antagonists.

Author: KhanfarMohammad A, AffiniAnna, LutsenkoKiril, NikolicKatarina, ButiniStefania, StarkHolger

Treat various conditions

Side effects

This study discusses the clinical applications of novel multifunctional histamine H3 receptor antagonists, particularly pitolisant (Wakix®). The combination of pharmacological properties in one molecule for improved pharmacological effects and reduced side effects is a promising strategy based on the increasing understanding of complex neurotransmitter regulations. Polypharmacological approaches on histamine H3 receptor antagonists are described, including interactions with G-protein coupled receptors, transporters, enzymes, and NO-signaling mechanisms.

Language : English

H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice.

Author: DudekMagdalena, KuderKamil, KołaczkowskiMarcin, OlczykAdrian, ŻmudzkaElżbieta, RakAleksandra, BednarskiMarek, PytkaKarolina, SapaJacek, Kieć-KononowiczKatarzyna

Pitolisant for olanzapine side effects

Olanzapine side effects

Pitolisant, a histamine H3 receptor antagonist, was found to reduce sedation and depression-like symptoms induced by olanzapine, an atypical antipsychotic drug.

Language : English

Emerging drugs for common conditions of sleepiness: obstructive sleep apnea and narcolepsy.

Author: SullivanShannon S, GuilleminaultChristian

Daytime dysfunction

Poor sleep

Sleepiness

This article discusses the high prevalence and symptomatic burden of obstructive sleep apnea (OSA) and narcolepsy, as well as the challenges of current therapies for these sleep disorders.

Language : English

10.

Effects of pitolisant, a histamine H3 inverse agonist, in drug-resistant idiopathic and symptomatic hypersomnia: a chart review.

Author: Leu-SemenescuSmaranda, NitturNandy, GolmardJean-Louis, ArnulfIsabelle

Pitolisant for hypersomnia

Pitolisant is a wake-enhancing drug that increases histamine release in the brain. This study assessed its benefits and risks in patients with hypersomnia (excessive sleepiness) that did not respond to other stimulants.

Language : English

11.

Real-world treatment of pediatric narcolepsy with pitolisant: A retrospective, multicenter study.

Author: TrillerAnnika, PizzaFabio, LecendreuxMichel, LieberichLea, RezaeiRana, Pech de LaclauseAnna, VandiStefano, PlazziGiuseppe, KallweitUlf

Narcolepsy treatment

This study evaluated the effects and tolerability of pitolisant, an inverse histamine 3 receptor agonist, in children and adolescents with narcolepsy. Pitolisant is approved for the treatment of adult narcolepsy but its use in children is limited. The study found that pitolisant was well-tolerated and showed beneficial effects in a real-world setting.

Language : English

12.

Histamine receptors, agonists, and antagonists in health and disease.

Author: PanulaPertti

Treat narcolepsy

Insomnia side effects

Schizophrenia treatment risk

Histamine is a neurotransmitter that plays a role in a variety of functions, including alertness, wakefulness, and immune responses. Four types of histamine receptors are known, each with its own specific functions and potential therapeutic applications. H3 receptor antagonists are currently used to treat narcolepsy and hypersomnia, while H1 receptor antagonists are sometimes used to treat insomnia, but with caution due to potential side effects. H2 receptor antagonists have shown promise in treating schizophrenia, but are not widely used. H4 receptor ligands are being investigated for potential use in treating neuroimmunological and neurodegenerative disorders, but clinical trials are not yet underway.

Language : English

13.

Profile of Solriamfetol in the Management of Excessive Daytime Sleepiness Associated with Narcolepsy or Obstructive Sleep Apnea: Focus on Patient Selection and Perspectives.

Author: AbadVivien C

Improves wakefulness

Reduces sleepiness

Solriamfetol is a wake-promoting drug for treating excessive sleepiness (ES) associated with obstructive sleep apnea (OSA) or narcolepsy. It is a selective dopamine and norepinephrine reuptake inhibitor, demonstrating efficacy in reducing sleepiness and improving wakefulness. Solriamfetol is well tolerated and can be used as initial, replacement, or add-on therapy.

Language : English

14.

Sleep Disorders in Adults with Prader-Willi Syndrome: Review of the Literature and Clinical Recommendations Based on the Experience of the French Reference Centre.

Author: DodetPauline, SanapoFederica, Leu-SemenescuSmaranda, CoupayeMuriel, BellichaAlice, ArnulfIsabelle, PoitouChristine, RedolfiStefania

Improved quality of life

Wake-enhancing drugs

Cardiovascular side effects

Psychological side effects

Sleep disorders

Prader-Willi syndrome (PWS) is a rare genetic disorder associated with sleep alterations, including sleep-disordered breathing and central disorders of hypersomnolence. Wake-enhancing drugs like modafinil and pitolisant may be considered for patients with PWS and excessive daytime sleepiness, but their use should be carefully evaluated due to potential side effects.

Language : English

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