https://wikimd.org/index.php?action=history&feed=atom&title=PitolisantPitolisant - Revision history2026-05-13T22:13:05ZRevision history for this page on the wikiMediaWiki 1.44.2https://wikimd.org/index.php?title=Pitolisant&diff=4963478&oldid=prevPrab at 18:01, 6 June 20232023-06-06T18:01:27Z<p></p>
<p><b>New page</b></p><div>== '''What is Pitolisant?''' ==<br />
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* Pitolisant (WAKIX) is a '''histamine-3 (H3) receptor antagonist/inverse agonist'''.<br />
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[[File:Pitolisant-structure.png|thumb]]<br />
[[File:Pitolisant skeletal.svg|thumb]]<br />
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== '''What are the uses of this medicine?''' ==<br />
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* This medicine is used for the treatment of excessive daytime sleepiness (EDS) or [[cataplexy]] in adult patients with [[narcolepsy]].<br />
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== '''How does this medicine work?''' ==<br />
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* The mechanism of action of pitolisant in excessive daytime sleepiness (EDS) or [[cataplexy]] in adult patients with [[narcolepsy]] is unclear. <br />
* However, its efficacy could be mediated through its '''activity as an antagonist/inverse agonist at histamine-3 (H3) receptors'''.<br />
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== '''Who Should Not Use this medicine ?''' ==<br />
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This medicine cannot be used in patients with:<br />
* known [[hypersensitivity]] to pitolisant or any component of the formulation. [[Anaphylaxis]] has been reported in patients treated with WAKIX.<br />
* severe hepatic impairment. <br />
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== '''What drug interactions can this medicine cause?''' ==<br />
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* WAKIX may reduce effectiveness of sensitive CYP3A4 substrates(eg: [[midazolam]], hormonal contraceptives, [[cyclosporine]]). Use an alternative non-hormonal contraceptive method during treatment with WAKIX and for at least 21 days after discontinuation of treatment.<br />
* Concomitant administration of WAKIX with strong CYP2D6 inhibitors(eg: [[paroxetine]], [[fluoxetine]], [[bupropion]]) increases pitolisant exposure. Reduce the dose of WAKIX by half.<br />
* Concomitant use of WAKIX with strong CYP3A4 inducers decreases exposure of pitolisant by 50%.(eg: [[rifampin]], [[carbamazepine]], [[phenytoin]])<br />
* WAKIX increases the levels of histamine in the brain; therefore, H1 receptor antagonists that cross the blood-brain barrier may reduce the effectiveness of WAKIX.(eg: [[pheniramine maleate]], [[diphenhydramine]], [[promethazine]] (anti-histamines) [[imipramine]], [[clomipramine]], [[mirtazapine]] (tri or tetracyclic antidepressants)<br />
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== '''Is this medicine FDA approved?''' ==<br />
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* It was approved for use in the United States in 2019.<br />
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== '''How should this medicine be used?''' ==<br />
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'''Recommended Dosage'''<br />
The recommended dosage range is 17.8 mg to 35.6 mg daily. Titrate dosage as follows:<br />
* Week 1: Initiate with 8.9 mg once daily<br />
* Week 2: Increase dosage to 17.8 mg once daily<br />
* Week 3: May increase to the maximum recommended dosage of 35.6 mg once daily <br />
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'''Hepatic impairment:'''<br />
* Moderate hepatic impairment: Initial dosage is 8.9 mg once daily. Titrate to a maximum dosage of 17.8 mg once daily after 14 days<br />
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'''Renal impairment:'''<br />
* Moderate and severe impairment: Initial dosage is 8.9 mg once daily. Titrate to maximum dosage of 17.8 mg once daily after 7 days<br />
* End−stage renal disease (ESRD): Not recommended<br />
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'''Use in Patients Who Are Known CYP2D6 Poor Metabolizers (PMs)'''<br />
* Maximum recommended dosage is 17.8 mg once daily<br />
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'''Administration'''<br />
* WAKIX is administered orally once daily in the morning upon wakening.<br />
* Dose may be adjusted based on tolerability.<br />
* If a dose is missed, patients should take the next dose the following day in the morning upon wakening.<br />
* It may take up to 8 weeks for some patients to achieve a clinical response.<br />
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== '''What are the dosage forms and brand names of this medicine?''' ==<br />
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This medicine is available in fallowing doasage form:<br />
* '''As Tablets:''' 4.45 mg and 17.8 mg<br />
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This medicine is available in fallowing brand namesː<br />
*'''WAKIX'''<br />
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=='''What side effects can this medication cause?'''==<br />
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The most common side effects of this medicine include:<br />
* [[insomnia]]<br />
* nausea<br />
* [[anxiety]]<br />
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==''' What special precautions should I follow?''' ==<br />
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* WAKIX prolongs the QT interval. <br />
* Avoid use with drugs that also increase the QT interval and in patients with risk factors for prolonged QT interval. <br />
* Monitor patients with hepatic or renal impairment for increased QTc<br />
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== '''What to do in case of emergency/overdose?''' ==<br />
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* {{overdose}}<br />
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== '''Can this medicine be used in pregnancy?''' ==<br />
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* WAKIX use in pregnant women have not determined a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.<br />
* There is a pregnancy exposure registry that monitors pregnancy outcomes in women who are exposed to WAKIX during pregnancy. <br />
* Patients should be encouraged to enroll in the WAKIX pregnancy registry if they become pregnant. <br />
* To enroll or obtain information from the registry, patients can call 1-800-833-7460.<br />
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=='''Can this medicine be used in children?'''==<br />
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* The safety and effectiveness of WAKIX in pediatric patients have not been established.<br />
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== '''What are the active and inactive ingredients in this medicine?''' ==<br />
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'''Active Ingredient: '''<br />
* PITOLISANT HYDROCHLORIDE <br />
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Inactive Ingredients: <br />
* SILICON DIOXIDE<br />
* CROSPOVIDONE <br />
* MAGNESIUM STEARATE <br />
* MICROCRYSTALLINE CELLULOSE <br />
* POLYETHYLENE GLYCOL, UNSPECIFIED <br />
* POLYVINYL ALCOHOL, UNSPECIFIED <br />
* TALC <br />
* TITANIUM DIOXIDE <br />
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== '''Who manufactures and distributes this medicine?''' ==<br />
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* '''Packager:''' Harmony Biosciences, LLC<br />
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== '''What should I know about storage and disposal of this medication?''' ==<br />
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* Store at 20° C to 25° C (68° F to 77° F); excursions permitted between 15° C to 30° C (59° F to 86° F).<br />
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{{Histamine receptor modulators}}<br />
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[[Category:Chloroarenes]]<br />
[[Category:Ethers]]<br />
[[Category:H3 receptor antagonists]]<br />
[[Category:Piperidines]]<br />
[[Category:Stimulants]]<br />
[[Category:Orphan drugs]]<br />
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