Pitolisant belongs to the class of medications called wakefulness-promoting agents. It is used to reduce excessive sleepiness during the day and sudden weak or paralyzed muscles, symptoms of narcolepsy. Narcolepsy is a condition that causes daytime excessive sleepiness. 

Pitolisant works by increasing the natural chemicals (neurotransmitters) in the brain that balance sleep/wake states and encourage wakefulness. It may take up to 8 weeks to reach the maximum benefit from this medication.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

The recommended starting dose of pitolisant is 10 mg (two 5 mg tablets) by mouth, once daily in the morning. The dose may be increased to 20 mg every morning after 1 week. Depending on side effects and the effectiveness of the medication, your doctor may increase the dose to 40 mg once daily. The maximum dose is 40 mg daily.

Take pitolisant in the morning with food. Taking it later in the day may cause difficulty sleeping at night. Swallow the tablets whole with some fluids. Do not crush or chew the tablets.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

5 mg

Each white, round, biconvex, film-coated tablet, marked with "5" on one side and plain on the other side, contains 5 mg of pitolisant hydrochloride. Nonmedicinal ingredients: colloidal anhydrous silica, crospovidone, microcrystalline cellulose, magnesium stearate, polyethylene glycol, polyvinyl alcohol, purified water, talc, and titanium dioxide.

20 mg

Each white, round, biconvex, film-coated tablet, marked with "20" on one side and plain on the other side, contains 20 mg of pitolisant hydrochloride. Nonmedicinal ingredients: colloidal anhydrous silica, crospovidone, microcrystalline cellulose, magnesium stearate, polyethylene glycol, polyvinyl alcohol, purified water, talc, and titanium dioxide.

Do not take this medication if you:

• are allergic to pitolisant or any ingredients of the medication
• are breastfeeding
• have severely decreased liver function

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• acid reflux/heartburn
• anxiety
• back pain
• cold symptoms (e.g., runny or stuffy nose, sore throat, cough, sinus congestion, body aches, headache, sneezing, or fever)
• decreased appetite
• diarrhea
• dizziness
• dry mouth
• fatigue
• headache
• increased heart rate
• joint pain
• nausea
• stomach pain
• trouble sleeping

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

• changes in behaviour (i.e., aggression, irritability, or hostility)
• hallucinations (e.g., seeing or hearing things that aren’t there)
• signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
• symptoms of irregular heartbeat (e.g., chest pain, dizziness, rapid, pounding heartbeat, shortness of breath)

Stop taking the medication and seek immediate medical attention if any of the following occur:

• signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• seizures
• thoughts of suicide or self-harm

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Abnormal heart rhythm: Pitolisant may cause a heart rhythm problem called QT prolongation. If you have a history of QT prolongation, a medical condition associated with QT prolongation, or are taking certain medications (e.g., amiodarone, sotalol), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If you develop symptoms of dizziness, fainting, chest pain or discomfort, or a fast or pounding heartbeat, contact your doctor immediately.

Birth control: Pitolisant may decrease the effectiveness of birth control pills, which should not be used as the only method of contraception. Women who could become pregnant who are taking pitolisant and who are using hormonal birth control should use an additional non-hormonal method of birth control such as condoms during treatment and for 21 days after stopping the medication.

Drowsiness/reduced alertness: Pitolisant may affect the mental or physical abilities needed to drive or operate machinery. Avoid any hazardous activities, such as driving, until you know how this medication affects you.

Kidney function: Kidney disease may cause this medication to build up in the body, causing side effects. If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

Mental health: People with a history of mental health problems like anxiety and depression may experience increased symptoms when taking this medication. If you feel agitated, restless, anxious, aggressive, emotional, not feeling like yourself, or like you want to hurt yourself, contact your doctor as soon as possible.

If you experience symptoms of depression such as poor concentration, changes in weight, changes in sleep, decreased interest in activities, or notice them in a family member who is taking this medication, contact your doctor as soon as possible.

Seizures: If you have a history of epilepsy or medical conditions that increase the risk of seizures, you may experience an increase in the frequency of seizures. Talk to your doctor about how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Pregnancy: This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if pitolisant passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children.

Seniors: People over the age of 75 years may be more likely to experience side effects from pitolisant.

There may be an interaction between pitolisant and any of the following:

• abiraterone
• antiarrhythmic medications (e.g., amiodarone, disopyramide, dronedarone, procainamide, quinidine, sotalol)
• antihistamines (e.g., bilastine, cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine, rupatadine)
• apalutamide
• bupropion
• chlorpromazine
• cinacalcet
• oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone) – high doses
• cyclosporine
• darifenacin
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
• enzalutamide
• grapefruit juice
• haloperidol
• hormonal birth control
• lumacaftor and ivacaftor
• methadone
• midazolam
• mirabegron
• mirtazapine
• quinine
• rifampin
• St. John's wort
• seizure medications (e.g., carbamazepine, phenytoin, phenobarbital, primidone)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
• serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., desvenlafaxine, duloxetine, venlafaxine)
• terbinafine
• thioridazine
• tipranavir
• tricyclic antidepressants (e.g., clomipramine, desipramine, imipramine)
• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over the counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.