Pitolisant
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami Ardakani
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Overview
Pitolisant is a Histamine-3 (H3) Receptor Antagonist/Inverse Agonist that is FDA approved for the treatment of Excessive daytime sleepiness (EDS) or cataplexy in adult patients and in pediatric patients aged 6 years and older with narcolepsy.. Common adverse reactions include Insomnia, Nausea, Anxiety, Headache, Irritability, Dizziness, Depression, Tremor, Sleep disorders, Fatigue, Vomiting, Vertigo, Dyspepsia, and Heartburn..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Excessive Daytime Sleepiness (EDS) or Cataplexy in Narcolepsy: Initial Dose: 8.9 mg once daily in the morning upon awakening for 1 week. Week 2: Increase to 17.8 mg once daily. Week 3: May increase to the maximum recommended dose of 35.6 mg once daily, based on response and tolerability.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Pitolisant in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Pitolisant in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Excessive Daytime Sleepiness (EDS) or Cataplexy in Narcolepsy: Initial Dose: 8.9 mg once daily in the morning upon awakening for 1 week. Week 2: Increase to 17.8 mg once daily. Week 3: May increase to the maximum recommended dose of 35.6 mg once daily, based on response and tolerability.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Pitolisant in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Pitolisant in pediatric patients.
Contraindications
Severe hepatic impairment. Known hypersensitivity to Pitolisant or any component of the formulation.
Warnings
QT Interval Prolongation: Pitolisant may prolong the QT interval. Avoid use with other drugs known to prolong the QT interval and in patients with known QT prolongation or in combination with drugs that increase Pitolisant exposure. Monitor ECG in patients with cardiac disease. CYP2D6 Poor Metabolizers: Higher Pitolisant concentrations may occur in these patients. Dose reduction is recommended. Contraception: Pitolisant may reduce the effectiveness of hormonal contraceptives. Advise patients to use alternative non-hormonal contraceptive methods during treatment and for at least 21 days after discontinuation.
Adverse Reactions
Clinical Trials Experience
Insomnia Nausea Anxiety Headache Irritability Dizziness Depression Tremor Sleep disorders Fatigue Vomiting Vertigo Dyspepsia Heartburn
Postmarketing Experience
There is limited information regarding Pitolisant Postmarketing Experience in the drug label.
Drug Interactions
CYP2D6 Inhibitors: Concomitant use may increase Pitolisant exposure. Dose reduction may be necessary. CYP3A4 Inducers: Concomitant use may decrease Pitolisant exposure, potentially reducing efficacy. Dose adjustment may be necessary. QT-Prolonging Drugs: Avoid concomitant use due to the potential additive effect on QT prolongation. Hormonal Contraceptives: Pitolisant may reduce their effectiveness. Advise the use of alternative non-hormonal contraceptive methods.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Pitolisant in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Pitolisant in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Pitolisant during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Pitolisant in women who are nursing.
Pediatric Use
Pitolisant is approved for pediatric patients aged 6 years and older with narcolepsy. Safety and efficacy have not been established for children under 6 years of age.
Geriatic Use
No overall differences in safety or efficacy were observed between elderly and younger patients in clinical trials. However, caution should be exercised due to possible age-related decline in renal or hepatic function.
Gender
There is no FDA guidance on the use of Pitolisant with respect to specific gender populations.
Race
There is no FDA guidance on the use of Pitolisant with respect to specific racial populations.
Renal Impairment
No dose adjustment is required for patients with mild to moderate renal impairment.
Hepatic Impairment
Pitolisant is contraindicated in patients with severe hepatic impairment. Dosage reduction is recommended for patients with moderate hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Pitolisant in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Pitolisant in patients who are immunocompromised.
Administration and Monitoring
Administration
orally, once daily in the morning upon awakening. Tablets should be swallowed whole and can be taken with or without food. Doses should be titrated gradually to the recommended therapeutic level over a 3-week period
Monitoring
Monitor ECG in patients with known QT prolongation or cardiac disease. Assess for adverse effects such as insomnia, nervousness, and gastrointestinal symptoms, which may require dose adjustments.
IV Compatibility
There is limited information regarding the compatibility of Pitolisant and IV administrations.
Overdosage
Symptoms of overdose may include agitation, insomnia, irritability, and gastrointestinal discomfort. Treatment should consist of symptomatic and supportive care. There is no specific antidote for Pitolisant.
Pharmacology
There is limited information regarding Pitolisant Pharmacology in the drug label.
Mechanism of Action
Pitolisant is a histamine-3 (H3) receptor antagonist/inverse agonist. By enhancing histaminergic neurotransmission in the brain, it promotes wakefulness and reduces excessive daytime sleepiness (EDS) and cataplexy in narcolepsy.
Structure
There is limited information regarding Pitolisant Structure in the drug label.
Pharmacodynamics
Pitolisant increases the release of histamine, dopamine, and norepinephrine in the central nervous system, which contributes to its wake-promoting and alertness-enhancing effects.
Pharmacokinetics
Absorption: Pitolisant is rapidly absorbed, with peak plasma concentrations occurring approximately 3–5 hours after oral administration. Metabolism: Metabolized primarily by CYP2D6 and CYP3A4 enzymes. Elimination: Approximately 60% excreted in urine and 25% in feces. Half-life: The terminal half-life is approximately 10–12 hours.
Nonclinical Toxicology
There is limited information regarding Pitolisant Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Pitolisant Clinical Studies in the drug label.
How Supplied
Pitolisant is supplied as 4.45 mg and 17.8 mg film-coated tablets, which are round, biconvex, and debossed with identifying marks.
Storage
Store Pitolisant at 20°C to 25°C (68°F to 77°F), with permitted excursions between 15°C and 30°C (59°F to 86°F). Keep in a tightly closed container, away from moisture and heat.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Pitolisant Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol use during treatment may exacerbate central nervous system (CNS) effects, such as dizziness or drowsiness. Patients are advised to limit or avoid alcohol consumption while taking Pitolisant. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Wakix
Look-Alike Drug Names
There is limited information regarding Pitolisant Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.