Pitolisant

What is Pitolisant?

• Pitolisant (WAKIX) is a histamine-3 (H3) receptor antagonist/inverse agonist.

What are the uses of this medicine?

• This medicine is used for the treatment of excessive daytime sleepiness (EDS) or cataplexy in adult patients with narcolepsy.

How does this medicine work?

• The mechanism of action of pitolisant in excessive daytime sleepiness (EDS) or cataplexy in adult patients with narcolepsy is unclear.
• However, its efficacy could be mediated through its activity as an antagonist/inverse agonist at histamine-3 (H3) receptors.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known hypersensitivity to pitolisant or any component of the formulation. Anaphylaxis has been reported in patients treated with WAKIX.
• severe hepatic impairment.

What drug interactions can this medicine cause?

• 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.
• Concomitant administration of WAKIX with strong CYP2D6 inhibitors(eg: paroxetine, fluoxetine, bupropion) increases pitolisant exposure. Reduce the dose of WAKIX by half.
• Concomitant use of WAKIX with strong CYP3A4 inducers decreases exposure of pitolisant by 50%.(eg: rifampin, carbamazepine, phenytoin)
• 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)

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

Recommended Dosage The recommended dosage range is 17.8 mg to 35.6 mg daily. Titrate dosage as follows:

• Week 1: Initiate with 8.9 mg once daily
• Week 2: Increase dosage to 17.8 mg once daily
• Week 3: May increase to the maximum recommended dosage of 35.6 mg once daily

Hepatic impairment:

• 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

Renal impairment:

• 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
• End−stage renal disease (ESRD): Not recommended

Use in Patients Who Are Known CYP2D6 Poor Metabolizers (PMs)

• Maximum recommended dosage is 17.8 mg once daily

Administration

• WAKIX is administered orally once daily in the morning upon wakening.
• Dose may be adjusted based on tolerability.
• If a dose is missed, patients should take the next dose the following day in the morning upon wakening.
• It may take up to 8 weeks for some patients to achieve a clinical response.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 4.45 mg and 17.8 mg

This medicine is available in fallowing brand namesː

• WAKIX

What side effects can this medication cause?

The most common side effects of this medicine include:

• insomnia
• nausea
• anxiety

What special precautions should I follow?

• WAKIX prolongs the QT interval.
• Avoid use with drugs that also increase the QT interval and in patients with risk factors for prolonged QT interval.
• Monitor patients with hepatic or renal impairment for increased QTc

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• WAKIX use in pregnant women have not determined a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women who are exposed to WAKIX during pregnancy.
• Patients should be encouraged to enroll in the WAKIX pregnancy registry if they become pregnant.
• To enroll or obtain information from the registry, patients can call 1-800-833-7460.

Can this medicine be used in children?

• The safety and effectiveness of WAKIX in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• PITOLISANT HYDROCHLORIDE

Inactive Ingredients:

• SILICON DIOXIDE
• CROSPOVIDONE
• MAGNESIUM STEARATE
• MICROCRYSTALLINE CELLULOSE
• POLYETHYLENE GLYCOL, UNSPECIFIED
• POLYVINYL ALCOHOL, UNSPECIFIED
• TALC
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

• Packager: Harmony Biosciences, LLC

What should I know about storage and disposal of this medication?

• 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).

• Dailymed label info on Pitolisant
• FDA Pitolisant

Pitolisant Resources
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