Wakix: Uses, Dosage & Side Effects

A first-in-class histamine H3 receptor antagonist/inverse agonist for the treatment of narcolepsy with or without cataplexy in adults and children aged 6 years and older

Rx ATC: N07XX11 H3 Receptor Antagonist
Active Ingredient
Pitolisant
Available Forms
Film-coated tablet
Strengths
4.5 mg, 18 mg
Manufacturer
Bioprojet Pharma

Wakix (pitolisant) is a prescription medication and the first-in-class histamine H3 receptor antagonist/inverse agonist approved for the treatment of narcolepsy with or without cataplexy. Wakix works by enhancing histamine signaling in the brain to promote wakefulness and reduce episodes of sudden muscle weakness (cataplexy). It is approved for use in adults, adolescents, and children aged 6 years and older. Unlike traditional stimulant medications used for narcolepsy, pitolisant is not classified as a controlled substance in the European Union and has a distinct mechanism of action that modulates the brain's wake-promoting histamine system, as well as other neurotransmitters including acetylcholine, norepinephrine, and dopamine.

Quick Facts: Wakix

Active Ingredient
Pitolisant
Drug Class
H3 Antagonist
ATC Code
N07XX11
Common Uses
Narcolepsy
Available Forms
Oral Tablet
Prescription Status
Rx Only

Key Takeaways

  • Wakix (pitolisant) is the first-in-class histamine H3 receptor antagonist/inverse agonist specifically developed for the treatment of narcolepsy, addressing both excessive daytime sleepiness and cataplexy through enhanced histaminergic neurotransmission.
  • The dose is gradually titrated over 3 weeks, starting at 9 mg daily for adults (4.5 mg for children) up to a maximum of 36 mg daily (18 mg for children under 40 kg), taken once daily in the morning with breakfast.
  • Wakix has significant drug interactions — notably, it may reduce the effectiveness of hormonal contraceptives, and its metabolism is affected by CYP2D6 and CYP3A4 inhibitors and inducers. Dose adjustments may be required.
  • Unlike many other narcolepsy treatments, Wakix is not classified as a controlled substance in the EU and has a lower abuse potential than traditional stimulants, making it a valuable option for long-term management.
  • Common side effects include insomnia, headache, nausea, and anxiety. Patients should be monitored for psychiatric symptoms, including depression and suicidal ideation, and cardiac effects (QT prolongation) should be evaluated periodically.

What Is Wakix and What Is It Used For?

Quick Answer: Wakix (pitolisant) is a prescription medication used to treat narcolepsy with or without cataplexy in adults and children aged 6 years and older. It is the first and only histamine H3 receptor antagonist/inverse agonist approved for this indication. Wakix works by boosting histamine release in the brain, which promotes wakefulness and reduces cataplexy episodes.

Wakix contains the active substance pitolisant (as pitolisant hydrochloride), a novel pharmacological agent that belongs to a unique class of medications — histamine H3 receptor antagonists/inverse agonists. This drug was specifically developed for the treatment of narcolepsy, a chronic neurological disorder that affects the brain's ability to regulate the sleep-wake cycle. Narcolepsy is estimated to affect approximately 25–50 per 100,000 people worldwide, though the condition is frequently underdiagnosed and the true prevalence may be higher.

Narcolepsy is characterized by two cardinal features: excessive daytime sleepiness (EDS), which manifests as an overwhelming and irresistible need to sleep during the day, often leading to sudden sleep attacks in inappropriate situations; and cataplexy, which involves sudden, transient episodes of partial or complete muscle weakness triggered by strong emotions such as laughter, surprise, anger, or excitement. Not all patients with narcolepsy experience cataplexy — those who do are classified as having narcolepsy type 1 (NT1, previously called narcolepsy with cataplexy), while those without cataplexy are classified as having narcolepsy type 2 (NT2). Both forms can be treated with Wakix.

The pathophysiology of narcolepsy type 1 is well established: it results from the loss of hypothalamic neurons that produce the neuropeptide hypocretin (also called orexin). These hypocretin-producing neurons play a critical role in stabilizing the sleep-wake cycle, and their destruction (thought to be autoimmune-mediated) leads to the fragmented sleep patterns and inappropriate intrusions of REM sleep that characterize narcolepsy. Histamine-producing neurons in the tuberomammillary nucleus of the hypothalamus are one of the key downstream effectors of the hypocretin system, and they serve as a major wake-promoting center in the brain.

Pitolisant works by targeting histamine H3 receptors, which are presynaptic autoreceptors located on histaminergic neurons. Under normal conditions, these H3 receptors act as a negative feedback mechanism: when histamine levels rise, activation of H3 receptors inhibits further histamine synthesis and release. Pitolisant acts as an antagonist and inverse agonist at these receptors, meaning it both blocks the inhibitory feedback signal and actively promotes increased histamine production and release. The net result is a significant enhancement of histaminergic neurotransmission in the brain, which promotes sustained wakefulness.

Beyond its primary effect on the histamine system, pitolisant also modulates the release of several other neurotransmitters implicated in arousal and wakefulness, including acetylcholine, norepinephrine, and dopamine. This broader neurochemical profile likely contributes to its dual efficacy against both excessive daytime sleepiness and cataplexy. The anti-cataplectic effect is thought to be related to the enhancement of noradrenergic and histaminergic tone, which helps stabilize the REM sleep atonia switch that malfunctions during cataplexy episodes.

Clinical trials have demonstrated the efficacy of Wakix in both narcolepsy type 1 and type 2. The pivotal HARMONY I trial, a randomized, double-blind, placebo-controlled study, showed that pitolisant significantly reduced the Epworth Sleepiness Scale (ESS) score compared to placebo, indicating meaningful improvement in excessive daytime sleepiness. The HARMONY CTP trial specifically evaluated the anti-cataplectic effect and demonstrated a significant reduction in the weekly rate of cataplexy attacks compared to placebo. Additional studies, including HARMONY III (an open-label long-term safety study), have confirmed the sustained efficacy and tolerability of pitolisant over treatment periods exceeding 12 months.

Wakix was first approved by the European Medicines Agency (EMA) in March 2016, making it the first medicine in this pharmacological class to receive regulatory authorization. It was subsequently approved by the U.S. Food and Drug Administration (FDA) in August 2019. Wakix is now available in numerous countries across Europe, North America, and beyond. It is marketed by Bioprojet Pharma.

Understanding Narcolepsy

Narcolepsy is a lifelong neurological condition, not a behavioral or psychiatric disorder. Patients with narcolepsy do not simply feel tired — they experience an overwhelming biological drive to sleep that cannot be resisted, even in stimulating situations. Other symptoms may include sleep paralysis (temporary inability to move when falling asleep or waking up), hypnagogic hallucinations (vivid sensory experiences at sleep onset), and fragmented nighttime sleep. Early diagnosis and appropriate treatment, including medications like Wakix, can significantly improve quality of life and functional capacity.

What Should You Know Before Taking Wakix?

Quick Answer: Before taking Wakix, inform your doctor about any liver or kidney problems, heart conditions, history of psychiatric illness (particularly depression or suicidal thoughts), epilepsy, stomach ulcers, or weight changes. Wakix is contraindicated in severe hepatic impairment and during breastfeeding. It may reduce the efficacy of hormonal contraceptives, so alternative birth control is required.

Before starting treatment with Wakix, it is essential that your healthcare provider has a complete understanding of your medical history, current medications, and any conditions that could affect how the drug works or increase the risk of adverse effects. The following sections outline the key contraindications, warnings, and precautions associated with pitolisant.

Contraindications

Wakix should not be taken in the following circumstances:

  • Hypersensitivity: Do not take Wakix if you are allergic to pitolisant or to any of the other ingredients in the tablets. Signs of an allergic reaction may include rash, itching, swelling of the face or throat, difficulty breathing, or severe dizziness.
  • Severe hepatic (liver) impairment: Pitolisant is extensively metabolized in the liver. In patients with severe liver disease, the drug may accumulate to dangerously high levels because the liver cannot break it down efficiently. Wakix is contraindicated in this population.
  • Breastfeeding: Animal studies have shown that pitolisant is excreted in breast milk. Patients taking Wakix must stop breastfeeding, as the potential effects on the nursing infant have not been established.

Warnings and Precautions

Speak with your doctor before taking Wakix if any of the following conditions apply to you:

  • History of anxiety, depression, or suicidal thoughts: Some patients taking Wakix have reported psychiatric symptoms, including suicidal ideation. If you have a history of mental health conditions, you should be closely monitored during treatment. Tell your doctor immediately if you notice changes in mood, increased anxiety, or thoughts of self-harm.
  • Liver or kidney problems: Even mild to moderate hepatic or renal impairment may require dose adjustments. Your doctor will evaluate your liver and kidney function before prescribing Wakix and may start you on a lower dose.
  • Gastrointestinal conditions: If you have a history of gastric or duodenal ulcers, or if you are taking medications that can irritate the stomach lining (such as non-steroidal anti-inflammatory drugs), be aware that gastrointestinal side effects have been reported with Wakix.
  • Weight changes: Both weight gain and weight loss have been observed in patients taking pitolisant. If you have obesity or an eating disorder such as anorexia, your weight should be monitored during treatment.
  • Heart conditions: Pitolisant may affect the heart's electrical activity (QT interval). If you have a history of cardiac arrhythmias, heart failure, or are taking other QT-prolonging medications, your doctor will need to monitor your cardiac function regularly, including periodic electrocardiograms (ECGs).
  • Severe epilepsy: Caution is advised in patients with severe epilepsy, as the neurochemical changes induced by pitolisant could theoretically lower the seizure threshold.
Important: Psychiatric Monitoring

Some individuals with psychiatric conditions have experienced suicidal thoughts while taking Wakix. Tell your doctor immediately if you develop feelings of depression, unusual changes in behavior, or thoughts of self-harm. You may wish to ask a family member or close friend to help you watch for signs of depression or other behavioral changes.

Pregnancy and Breastfeeding

Pregnancy: Wakix should not be used during pregnancy unless specifically prescribed by your doctor after a careful benefit-risk assessment. There is insufficient data on the use of pitolisant in pregnant women to determine whether it poses risks to the developing fetus. If you are a woman of childbearing potential, you must use effective contraception during treatment with Wakix and for at least 21 days after stopping treatment.

Hormonal contraceptives: Wakix can reduce the effectiveness of hormonal contraceptives, including combined oral contraceptive pills, progestogen-only pills, implants, and hormonal intrauterine devices. Therefore, an alternative non-hormonal method of contraception (such as a copper IUD or barrier methods) must be used during treatment and for at least 21 days after discontinuation.

Breastfeeding: In animal studies, pitolisant was detected in breast milk. Because the potential effects on the nursing infant are unknown and could be harmful, breastfeeding must be stopped if Wakix treatment is required. Discuss alternative feeding options with your healthcare provider.

Children and Adolescents

Wakix is approved for use in children and adolescents aged 6 years and older with narcolepsy. It should not be given to children under 6 years of age, as safety and efficacy in this age group have not been established. For pediatric patients, the dose is adjusted based on body weight, and children weighing less than 40 kg should not exceed a maximum dose of 18 mg per day.

Driving and Operating Machinery

While Wakix is designed to improve wakefulness, narcolepsy itself can impair the ability to drive or operate heavy machinery safely. You should exercise caution when performing activities requiring alertness until you understand how Wakix affects you personally. Speak to your doctor if you are unsure whether your condition may negatively impact your ability to drive.

How Does Wakix Interact with Other Drugs?

Quick Answer: Wakix has several important drug interactions. It may reduce the effectiveness of hormonal contraceptives and can interact with certain antidepressants, sedating antihistamines, CYP enzyme inducers and inhibitors, and QT-prolonging medications. Always inform your doctor of all medications, supplements, and herbal remedies you are taking before starting Wakix.

Pitolisant is primarily metabolized in the liver by the cytochrome P450 enzyme system, particularly CYP2D6 and CYP3A4. It also has the potential to induce certain CYP enzymes and affect P-glycoprotein and organic cation transporter (OCT1) substrates. These metabolic characteristics create the potential for significant drug-drug interactions that may necessitate dose adjustments or avoidance of certain combinations.

Major Interactions

Wakix: Major Drug Interactions Requiring Caution
Interacting Drug Effect Clinical Recommendation
Hormonal contraceptives Reduced contraceptive efficacy due to CYP3A4 induction Use alternative non-hormonal contraception during treatment and for 21 days after stopping
Tricyclic antidepressants (imipramine, clomipramine) Potential pharmacodynamic interaction; risk of reduced antihistaminic effect Use with caution; monitor for efficacy and side effects
Sedating antihistamines (diphenhydramine, promethazine, chlorphenamine, doxylamine) May antagonize the wake-promoting effect of Wakix Avoid concomitant use; choose non-sedating alternatives
CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, phenobarbital, St. John’s Wort) Decreased pitolisant plasma levels due to increased metabolism Dose adjustment may be needed; monitor efficacy
CYP2D6 inhibitors (paroxetine, fluoxetine, bupropion, duloxetine, terbinafine, cinacalcet) Increased pitolisant plasma levels due to inhibited metabolism Dose reduction may be required; monitor for adverse effects
QT-prolonging medications (pimozide, halofantrin, cisapride) Additive risk of cardiac QT prolongation Avoid combination; ECG monitoring if unavoidable

Minor Interactions and Other Considerations

Wakix: Additional Drug Interactions
Interacting Drug Effect Clinical Recommendation
CYP2D6 substrates (venlafaxin, duloxetine, mirtazapine) Pitolisant may alter levels of co-administered CYP2D6 substrates Monitor for changes in efficacy or side effects of the co-administered drug
CYP3A4 substrates (midazolam, triazolam) Pitolisant may induce CYP3A4, reducing levels of these drugs Consider dose adjustment of the affected drug
OCT1/OCT2 substrates (metformin) Pitolisant may inhibit organic cation transporters, increasing metformin exposure Monitor blood glucose and renal function
P-glycoprotein substrates (dabigatran, digoxin) Pitolisant may increase plasma levels of P-gp substrates Use with caution; monitor drug levels and clinical response
Modafinil / Sodium oxybate No significant pharmacokinetic interaction expected Can be co-administered; standard monitoring
Morphine / Paracetamol Pitolisant may alter metabolism via UGT pathway interaction Clinical significance uncertain; standard monitoring
Herbal Supplements Warning

St. John’s Wort (Hypericum perforatum) is a potent CYP3A4 inducer and may significantly reduce pitolisant blood levels, potentially rendering Wakix less effective. If you are taking St. John’s Wort for mild depression or anxiety, discuss alternative options with your healthcare provider before starting Wakix.

What Is the Correct Dosage of Wakix?

Quick Answer: Wakix is taken once daily in the morning with breakfast. Adults typically start at 9 mg daily and gradually increase over 3 weeks to a maximum of 36 mg daily. Children aged 6 and older start at 4.5 mg daily, with a maximum of 36 mg (or 18 mg if under 40 kg). Lower doses may be needed for patients with liver or kidney impairment or those taking CYP2D6 inhibitors.

Wakix should always be taken exactly as prescribed by your doctor. The dose is gradually increased (titrated) over a period of approximately three weeks to find the most effective dose with the fewest side effects. Do not change your dose without consulting your doctor.

Adults

Standard Adult Dosing Schedule

Week 1: 9 mg once daily (two 4.5 mg tablets)

Week 2: 18 mg once daily (one 18 mg tablet)

Week 3 and onwards: 36 mg once daily (two 18 mg tablets) — or as adjusted by your doctor

Your doctor may increase or decrease the dose at any time depending on how well Wakix works for you and how well you tolerate it. The maximum recommended dose is 36 mg per day.

Treatment is usually initiated at a dose of 9 mg once daily. This can be achieved by taking two 4.5 mg tablets. The dose is then increased to 18 mg (one 18 mg tablet) in the second week, and may be further increased to 36 mg (two 18 mg tablets) in the third week. Your doctor will tailor the dose based on your individual clinical response and tolerability. It may take several days before you notice any effect from Wakix, and the maximum benefit is typically observed after several weeks of consistent use.

Children and Adolescents (6 Years and Older)

Pediatric Dosing Schedule

Week 1: 4.5 mg once daily (one 4.5 mg tablet)

Week 2: 9 mg once daily (two 4.5 mg tablets)

Week 3 and onwards: Up to 18 mg or 36 mg once daily — as adjusted by the doctor

Important: Children weighing less than 40 kg must not exceed 18 mg per day.

For children and adolescents aged 6 years and older, treatment starts at a lower dose of 4.5 mg once daily and is gradually increased over three weeks. The maximum dose depends on the child’s body weight: children weighing 40 kg or more may receive up to 36 mg daily, while those weighing less than 40 kg should not exceed 18 mg daily.

Patients with Hepatic or Renal Impairment

Patients with mild hepatic impairment may use Wakix at standard doses. Those with moderate hepatic impairment require dose adjustments and should not exceed 18 mg per day. Wakix is contraindicated in patients with severe hepatic impairment. For patients with renal impairment, dose adjustments may also be necessary depending on the severity, and the maximum dose should be determined by the prescribing physician.

Missed Dose

If you forget to take your Wakix tablet in the morning, skip the missed dose and take your next dose at the usual time the following morning. Do not take a double dose to make up for a forgotten dose. Taking Wakix in the afternoon or evening may cause difficulty sleeping (insomnia), so it is important to take it only in the morning.

Overdose

Overdose Warning

If you take more Wakix than prescribed, contact your nearest emergency department or poison control center immediately. Symptoms of overdose may include headache, abdominal pain, nausea, irritability, and difficulty sleeping. Bring the medication packaging and any remaining tablets with you. There is no specific antidote for pitolisant overdose; treatment is supportive and symptomatic.

Stopping Treatment

Continue taking Wakix for as long as your doctor instructs. Do not stop taking Wakix suddenly without medical advice. While pitolisant does not cause physical dependence or withdrawal symptoms in the traditional sense, abrupt discontinuation may result in a return of narcolepsy symptoms, including increased daytime sleepiness and cataplexy episodes.

Wakix Dosage Summary by Patient Group
Patient Group Starting Dose Maximum Dose Special Notes
Adults 9 mg/day 36 mg/day Titrate over 3 weeks
Children ≥40 kg 4.5 mg/day 36 mg/day Age 6+ only; titrate over 3 weeks
Children <40 kg 4.5 mg/day 18 mg/day Age 6+ only; do not exceed 18 mg
Moderate hepatic impairment 4.5 mg/day 18 mg/day Slower titration recommended
Severe hepatic impairment Contraindicated Contraindicated Do not use Wakix
Renal impairment 4.5 mg/day As directed Dose adjustment per physician

What Are the Side Effects of Wakix?

Quick Answer: The most common side effects of Wakix include insomnia, headache, nausea, anxiety, and irritability (affecting up to 1 in 10 users). Less common side effects include mood changes, tremor, dizziness, weight changes, and sleep disturbances. Rare but serious side effects can include suicidal ideation, hallucinations, and cardiac rhythm abnormalities. Report any unusual symptoms to your doctor promptly.

Like all medications, Wakix can cause side effects, although not everyone experiences them. Most side effects are mild to moderate in severity and tend to occur during the initial dose titration phase, often improving as the body adjusts to the medication. However, some side effects can be serious and warrant immediate medical attention.

The side effects listed below are organized by frequency, as determined in clinical trials and post-marketing surveillance:

Common

May affect up to 1 in 10 users

  • Insomnia (difficulty sleeping)
  • Anxiety
  • Irritability
  • Depressed mood
  • Sleep disturbances
  • Headache
  • Dizziness (vertigo)
  • Poor balance
  • Tremor
  • Nausea
  • Vomiting
  • Indigestion (dyspepsia)
  • Fatigue (exhaustion)

Uncommon

May affect up to 1 in 100 users

  • Excessive sweating
  • Decreased or increased appetite
  • Edema (swelling)
  • Nervousness, restlessness
  • Visual or auditory hallucinations
  • Mood swings, emotional instability
  • Abnormal dreams, nightmares
  • Difficulty falling or staying asleep
  • Excessive sleepiness (somnolence)
  • Apathy (lack of emotion)
  • Panic reactions
  • Suicidal thoughts
  • Changed or increased sexual interest
  • Involuntary muscle twitching or movement
  • Attention disturbance
  • Migraine
  • Muscle weakness
  • Tingling or prickling sensations (paresthesia)
  • Feeling unsteady
  • Reduced visual acuity, eyelid twitching
  • Tinnitus (ringing in the ears)
  • Abnormal heartbeat, slow or fast heart rate
  • Increased or decreased blood pressure
  • Hot flushes
  • Yawning
  • Dry mouth
  • Diarrhea, abdominal pain, constipation
  • Heartburn, gastritis
  • Itching, facial redness (rosacea-like)
  • Joint pain, back pain, muscle stiffness
  • Abnormal urination
  • Irregular uterine bleeding
  • Weight gain or weight loss
  • Abnormal ECG or liver function tests
  • Chest pain, general malaise

Rare

May affect up to 1 in 1,000 users

  • Decreased or increased appetite
  • Abnormal behavior, confusion
  • Depressed mood, irritability
  • Emotional and mental discomfort
  • Hypnagogic hallucinations (hallucinations while falling asleep)
  • Loss of consciousness
  • Tension headache, memory problems
  • Poor sleep quality
  • Abdominal discomfort, difficulty swallowing
  • Flatulence, gastrointestinal inflammation
  • Skin infection, abnormal photosensitivity
  • Neck pain, chest pain (musculoskeletal)
  • Spontaneous abortion (miscarriage)
  • Night sweats, feeling of heaviness
  • Elevated creatine phosphokinase levels
  • Altered ECG findings
When to Seek Immediate Medical Attention

Contact your doctor or seek emergency care immediately if you experience: thoughts of self-harm or suicide, severe allergic reactions (difficulty breathing, swelling of face/throat), chest pain or irregular heartbeat, loss of consciousness, or severe mood or behavioral changes. While these reactions are uncommon, they require urgent evaluation.

If you experience any side effects, including those not listed here, talk to your doctor or pharmacist. Reporting side effects helps regulatory authorities continue to monitor the benefit-risk balance of Wakix. In the EU, suspected adverse reactions can be reported to the national medicines agency. In the US, adverse events can be reported to the FDA MedWatch program.

How Should You Store Wakix?

Quick Answer: Store Wakix at room temperature with no special storage requirements. Keep it out of the sight and reach of children. Do not use after the expiration date printed on the packaging. Dispose of unused medication responsibly through a pharmacy take-back program — do not flush or throw it in household waste.

Proper storage of medication is important to maintain its safety and effectiveness throughout the treatment period. Wakix does not require any special storage conditions. Store the tablets at room temperature in their original packaging to protect them from moisture and light.

Keep Wakix out of the sight and reach of children. Accidental ingestion by a child could cause serious adverse effects and requires immediate medical attention.

Do not use Wakix after the expiration date (EXP) printed on the carton and bottle. The expiration date refers to the last day of the stated month. Once a bottle is opened, the tablets remain stable for the remainder of the shelf life indicated on the packaging.

Do not dispose of medications by flushing them down the toilet or putting them in household waste. Take any unused or expired tablets to a pharmacy for safe disposal. These measures help protect the environment and prevent accidental exposure.

What Does Wakix Contain?

Quick Answer: Wakix is available in two strengths: 4.5 mg and 18 mg film-coated tablets. The active ingredient is pitolisant (as pitolisant hydrochloride). Inactive ingredients include microcrystalline cellulose, crospovidone, talc, magnesium stearate, colloidal anhydrous silica, polyvinyl alcohol, titanium dioxide (E 171), and macrogol 3350.

Understanding the composition of your medication is important, especially if you have known allergies or sensitivities to pharmaceutical excipients. Below is a detailed breakdown of the composition of Wakix.

Active Ingredient

The active substance is pitolisant (as pitolisant hydrochloride):

  • Wakix 4.5 mg tablet: Each tablet contains pitolisant hydrochloride equivalent to 4.45 mg of pitolisant.
  • Wakix 18 mg tablet: Each tablet contains pitolisant hydrochloride equivalent to 17.8 mg of pitolisant.

Inactive Ingredients (Excipients)

Wakix Composition: Active and Inactive Ingredients
Ingredient Role Notes
Pitolisant hydrochloride Active substance (H3 receptor antagonist) 4.5 mg or 18 mg per tablet
Microcrystalline cellulose Filler / binder Provides bulk and structure
Crospovidone (Type A) Disintegrant Promotes tablet dissolution
Talc Glidant Improves powder flow during manufacturing
Magnesium stearate Lubricant Prevents tablet sticking to equipment
Colloidal anhydrous silica Glidant / anti-caking agent Ensures uniform powder distribution
Polyvinyl alcohol Film-coating agent Part of the tablet coating
Titanium dioxide (E 171) Colorant / opacifier Gives the tablet its white appearance
Macrogol 3350 Plasticizer Improves film-coating flexibility

Appearance and Pack Sizes

Wakix 4.5 mg is a white, round, biconvex film-coated tablet with a diameter of 3.7 mm, marked with “5” on one side. Wakix 18 mg is a white, round, biconvex film-coated tablet with a diameter of 7.5 mm, marked with “20” on one side.

Wakix is supplied in bottles containing 30 or 90 tablets. The 4.5 mg strength is available in packs of 1 bottle (30 tablets). The 18 mg strength is available in packs of 1 bottle with 30 tablets, 1 bottle with 90 tablets, or a multipack of 90 tablets (3 bottles of 30). Not all pack sizes may be marketed in every country.

Marketing Authorization Holder and Manufacturer

Wakix is developed and marketed by Bioprojet Pharma (9 rue Rameau, 75002 Paris, France). The 18 mg tablets are manufactured by Inpharmasci (Prouvy, France), and the 4.5 mg tablets are manufactured by Patheon (Bourgoin-Jallieu, France). Wakix is approved throughout the European Union, the United States, and numerous other countries worldwide. For further information, contact the local representative of the marketing authorization holder or visit the European Medicines Agency (EMA) website.

Frequently Asked Questions About Wakix

Wakix (pitolisant) is a prescription medication used to treat narcolepsy in adults, adolescents, and children aged 6 years and older. It addresses both excessive daytime sleepiness (EDS) — the uncontrollable urge to sleep during the day — and cataplexy, which is sudden muscle weakness triggered by emotions such as laughter or surprise. Wakix works by enhancing the brain’s histamine signaling system to promote sustained wakefulness.

Wakix is the first-in-class histamine H3 receptor antagonist/inverse agonist approved for narcolepsy. Unlike traditional stimulants (such as methylphenidate or amphetamines) or sodium oxybate, Wakix promotes wakefulness through a unique mechanism — enhancing histamine release in the brain rather than directly stimulating dopaminergic pathways. In the European Union, Wakix is not classified as a controlled substance, which means it has a lower potential for abuse and dependence compared to many other narcolepsy treatments. It can also be used alongside modafinil and sodium oxybate.

Wakix may reduce the effectiveness of hormonal contraceptives, including birth control pills, patches, implants, and hormonal IUDs. This is because pitolisant can induce the CYP3A4 enzyme system, which accelerates the breakdown of hormonal contraceptives. Women of childbearing potential must use an alternative non-hormonal method of contraception (such as a copper IUD or barrier methods like condoms) during Wakix treatment and for at least 21 days after stopping the medication.

You may start to notice some improvement in wakefulness within the first few days of treatment, but the full therapeutic effect of Wakix typically develops over several weeks. The dose is gradually increased over a 3-week titration period to reach the optimal effective dose. Most patients experience the greatest benefit after reaching their stable maintenance dose. Your doctor will typically evaluate the effectiveness of treatment after 3–6 months.

Wakix is not considered to have significant abuse potential. In the European Union, it is not classified as a controlled substance. In the United States, it is classified as Schedule IV, indicating a low potential for abuse relative to Schedule II stimulants commonly used for narcolepsy. Clinical studies have not shown evidence of physical dependence or withdrawal symptoms upon discontinuation. However, stopping Wakix may result in a return of narcolepsy symptoms.

Yes, Wakix is approved for children and adolescents aged 6 years and older who have been diagnosed with narcolepsy. The dosing is adjusted based on the child’s body weight: children weighing 40 kg or more may receive up to the full adult dose of 36 mg daily, while children under 40 kg should not exceed 18 mg daily. The dose is titrated gradually, starting at 4.5 mg daily. Wakix is not recommended for children under 6 years of age.

References

  1. European Medicines Agency (EMA). Wakix (pitolisant) – Summary of Product Characteristics. Last updated 2025. Available at: EMA Wakix EPAR.
  2. U.S. Food and Drug Administration (FDA). Wakix (pitolisant) – Prescribing Information. Harmony Biosciences. Revised 2024.
  3. Dauvilliers Y, Bassetti C, Lammers GJ, et al. Pitolisant versus placebo or modafinil in patients with narcolepsy: a double-blind, randomised trial (HARMONY I). Lancet Neurol. 2013;12(11):1068–1075. doi:10.1016/S1474-4422(13)70225-4.
  4. Szakacs Z, Dauvilliers Y, Mikhaylov V, et al. Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial (HARMONY CTP). Lancet Neurol. 2017;16(3):200–207. doi:10.1016/S1474-4422(16)30333-7.
  5. Dauvilliers Y, Arnulf I, Szakacs Z, et al. Long-term use of pitolisant to treat patients with narcolepsy: HARMONY III Study. Sleep. 2019;42(11):zsz174. doi:10.1093/sleep/zsz174.
  6. American Academy of Sleep Medicine (AASM). Clinical Practice Guideline for the Treatment of Central Disorders of Hypersomnolence. J Clin Sleep Med. 2021;17(9):1881–1893.
  7. European Academy of Neurology (EAN)/European Sleep Research Society (ESRS). European guideline and expert statements on the management of narcolepsy in adults and children. Eur J Neurol. 2021;28(8):2815–2830.
  8. Schwartz JC. The histamine H3 receptor: from discovery to clinical trials with pitolisant. Br J Pharmacol. 2011;163(4):713–721. doi:10.1111/j.1476-5381.2011.01286.x.
  9. World Health Organization (WHO). Neurological Disorders: Public Health Challenges. 2023. Available at: WHO Neurology.
  10. British National Formulary (BNF). Pitolisant. National Institute for Health and Care Excellence (NICE). 2025.

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