Pitolisant
Sleep Wake Disorders
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
NO
Pharmaceutical Class
Histamine-3 Receptor Antagonist/Inverse Agonist
Controlled Drug Substance
NO
Pitolisant
Summary
Pitolisant is primarily used to treat excessive daytime sleepiness and cataplexy in adults with narcolepsy. It's also approved for treating excessive daytime sleepiness in children aged 6 years and older with narcolepsy.
Pitolisant works by altering the levels of certain natural substances in the brain that control sleep and wakefulness. It acts as an antagonist/inverse agonist at histamine-3 (H3) receptors, helping regulate the levels of histamine, a substance involved in wakefulness.
For adults, the recommended dosage range for Pitolisant is 17.8 mg to 35.6 mg taken once daily in the morning. For children aged 6 years and older, the starting dose is 4.45 mg, which can be increased weekly to a maximum of 17.8 mg for those weighing less than 40 kg and up to 35.6 mg for those weighing 40 kg or more.
Common side effects of Pitolisant include headache, insomnia, nausea, and anxiety. Serious adverse effects can include fast or irregular heartbeat, difficulty breathing, and hallucinations.
Pitolisant is contraindicated in patients with severe hepatic impairment and those with known hypersensitivity to the drug. It can prolong the QT interval, so it should be avoided in patients with known QT prolongation or those taking other QT-prolonging drugs. Caution is advised for patients with cardiac arrhythmias, bradycardia, or electrolyte imbalances.
Indications and Purpose
How does Pitolisant work?
Pitolisant acts as an antagonist/inverse agonist at histamine-3 (H3) receptors in the brain. This action helps regulate the levels of histamine, a natural substance involved in wakefulness, thereby reducing excessive daytime sleepiness and cataplexy in narcolepsy patients.
Is Pitolisant effective?
Pitolisant's effectiveness in treating excessive daytime sleepiness and cataplexy in narcolepsy patients has been demonstrated in clinical trials. In studies, it showed significant improvement in the Epworth Sleepiness Scale scores compared to placebo, indicating reduced sleepiness. It also reduced the frequency of cataplexy attacks in patients with narcolepsy.
What is Pitolisant?
Pitolisant is used to treat excessive daytime sleepiness and cataplexy in adults with narcolepsy. It works by altering the levels of certain natural substances in the brain that control sleep and wakefulness, acting as an antagonist/inverse agonist at histamine-3 (H3) receptors.
Directions for Use
For how long do I take Pitolisant?
Pitolisant is typically used as a long-term treatment for narcolepsy. It may take up to 8 weeks or longer to feel the full benefit, and it should be continued even if you feel well-rested. Always follow your doctor's guidance on the duration of use.
How do I take Pitolisant?
Pitolisant should be taken once daily in the morning, with or without food. There are no specific food restrictions, but it's important to take it at the same time each day. Always follow your doctor's instructions regarding dosage and administration.
How long does it take for Pitolisant to start working?
Pitolisant may take up to 8 weeks or longer for some patients to feel the full benefit. It's important to continue taking the medication as prescribed, even if you feel well-rested, and consult your doctor for any concerns about its effectiveness.
How should I store Pitolisant?
Store Pitolisant at room temperature, between 20°C to 25°C (68°F to 77°F), away from excess heat and moisture. Keep it in its original container, tightly closed, and out of reach of children. Do not store it in the bathroom to avoid moisture exposure.
What is the usual dose of Pitolisant?
For adults, the recommended dosage range for Pitolisant is 17.8 mg to 35.6 mg taken once daily in the morning. For children aged 6 years and older, the starting dose is 4.45 mg, which can be increased weekly to a maximum of 17.8 mg for those weighing less than 40 kg, and up to 35.6 mg for those weighing 40 kg or more.
Warnings and Precautions
Can I take Pitolisant with other prescription drugs?
Pitolisant interacts with strong CYP2D6 inhibitors, increasing its exposure, and strong CYP3A4 inducers, decreasing its effectiveness. It may also reduce the effectiveness of hormonal contraceptives. Avoid using it with drugs that prolong the QT interval to prevent cardiac risks.
Can Pitolisant be taken safely while breastfeeding?
Pitolisant is present in breast milk in low amounts, with less than 1% of the maternal dose reaching the infant. The effects on the breastfed infant are unknown. Consider the benefits of breastfeeding along with the mother's need for Pitolisant and any potential risks to the infant.
Can Pitolisant be taken safely while pregnant?
There is a pregnancy exposure registry for Pitolisant, but available data from clinical trials and postmarketing reports have not determined a drug-associated risk of major birth defects or miscarriage. Animal studies showed potential risks at high doses. Pregnant women should consult their doctor before using Pitolisant.
Is Pitolisant safe for the elderly?
Limited data is available for elderly patients using Pitolisant. While no significant differences in safety or effectiveness were observed in clinical trials, older adults may be more sensitive to the drug. It's recommended to start at the lower end of the dosing range, considering potential decreased organ function and other medications.
Who should avoid taking Pitolisant?
Pitolisant is contraindicated in patients with severe hepatic impairment and those with known hypersensitivity to the drug. It can prolong the QT interval, so it should be avoided in patients with known QT prolongation or those taking other QT-prolonging drugs. Caution is advised for patients with cardiac arrhythmias, bradycardia, or electrolyte imbalances.