Pitolisant

Pitolisant is a prescription medication used for the treatment of excessive daytime sleepiness (EDS) or cataplexy in adults with narcolepsy. 

• Pitolisant is available under the following different brand names: Wakix.

Common side effects of Pitolisant include:

• Insomnia,
• Nausea, and
• Anxiety

Serious side effects of Pitolisant include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• Mood changes,
• Fast or irregular heartbeat,
• Severe dizziness,
• Fainting, and
• Severe dizziness

Rare side effects of Pitolisant include:

• None 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 4.45 mg
• 17.8 mg

Narcolepsy

Adult dosage

• Week 1: Initiate with 8.9 mg (two 4.45-mg tablets) orally once a day.
• Week 2: Increase to 17.8 mg (one 17.8-mg tablet) orally once a day.
• Week 3: May increase to a maximum dosage of 35.6 mg (two 17.8-mg tablets) once a day.

Adjust dose based on tolerability.

• May take up to 8 weeks to achieve a clinical response.

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Pitolisant has no noted severe interactions with any other drugs.
• Pitolisant has no noted serious interactions with any other drugs.
• Pitolisant has no noted moderate interactions with any other drugs.
• Pitolisant has no noted minor interactions with any other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Severe hepatic impairment
• Hypersensitivity to pitolisant or any component of the formulation

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Pitolisant?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Pitolisant?”

Cautions

• QT prolongation
  • Use prolonged QT intervals.
  • Avoid with history of cardiac arrhythmias, as well as other circumstances that may increase the risk of torsade de pointes or sudden death, including symptomatic bradycardia, hypokalemia, or hypomagnesemia, and the presence of congenital QT prolongation.
  • Patients with hepatic or renal impairment have a greater risk of QT prolongation due to higher pitolisant concentrations.
  • Monitor patients with hepatic or renal impairment for increased QT interval.
• Drug interaction overview
• Pitolisant is a CYP2D6 and CYP3A4 substrate; weak CYP3A4 inducer.
• Strong CYP2D6 inhibitors
  • Coadministration with strong CYP2D6 inhibitors increases pitolisant exposure by 2.2-fold.
• Strong CYP3A4 inducers
  • Concomitant use with strong CYP3A4 inducers decreases exposure of pitolisant by 50%.
• Sensitive CYP3A4 substrates
  • Concomitant use with sensitive CYP3A4 may reduce the efficacy of these sensitive CYP3A4 substrates.
  • Effectiveness of hormonal contraceptives (. g, ethinyl estradiol) may be reduced when used with pitolisant, and reduction in efficacy may last for 21 days after discontinuation of therapy.
• Drugs that prolong QT interval
  • Avoid coadministration with drugs known to prolong QT interval, owing to increased risk of serious cardiac arrhythmias.
  • Histamine-1 (H1) antagonists
    • Avoid centrally acting H1 antagonists.
    • Pitolisant increases histamine levels in the brain; therefore, H1 antagonists that cross the blood-brain barrier may reduce pitolisant effectiveness.

Pregnancy and Lactation

• Available case reports from clinical trials and postmarketing reports with use in pregnant women have not determined a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• Pregnancy exposure registry
  • monitors pregnancy outcomes in women exposed to pitolisant during pregnancy.
  • Encourage patients to enroll in the registry if they become pregnant.
  • To enroll or obtain information from the registry, contact 1-800-833-7460
• Contraception
  • Pitolisant may reduce the effectiveness of hormonal contraception owing to it being a weak CYP3A4 inducer.
  • Advise patients using hormonal contraception to use an alternative nonhormonal contraceptive method during treatment and for at least 21 days after discontinuing treatment.
• Lactation
  • The transfer of this drug into breastmilk is low based on data from a lactation study; the mean infant dose was 0.009 mg/day, and the relative infant dose was below 1% of the maternal weight-adjusted dose; there are no data on the effects of the drug on the breastfed infant, or effect of this drug on milk production.
• Pitolisant is present in the milk of lactating rats.
• When a drug is present in animal milk, it is likely that the drug will be present in human milk.
• Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need and any potential adverse effects on the breastfed child or from the underlying maternal condition.