pitolisant

Pitolisant is a wake-promoting medication that acts as a selective histamine H3 receptor inverse agonist/antagonist. By reducing H3 receptor activity in the brain, it increases the release of histamine and modulates other neurotransmitter systems involved in arousal, helping to promote wakefulness in people with disorders such as narcolepsy.

Indications and use: Pitolisant is approved for the treatment of excessive daytime sleepiness in adults with narcolepsy, with or without cataplexy, in several regulatory regions. It is considered an alternative to stimulant therapies for patients who do not tolerate or do not respond to other wake-promoting agents.

Administration and dosing: Pitolisant is taken by mouth, usually once daily. Dosing typically starts at a lower level and is titrated to a daily dose up to a regionally approved maximum, commonly 35 mg per day, depending on guidelines and individual response. The medication can be taken with or without food, and dose adjustments may be needed for hepatic impairment or drug interactions.

Safety and interactions: Pitolisant is metabolized in the liver and can interact with strong inhibitors or inducers of cytochrome P450 enzymes, particularly CYP2D6, as well as with other drugs that affect the QT interval. Caution is advised in hepatic impairment and when combining with QT-prolonging agents. Common adverse effects include nausea, headache, insomnia, anxiety, and palpitations. Data on use in pregnancy are limited, and the drug should be used during pregnancy only if the potential benefit justifies the potential risk.

Regulatory status and overview: Pitolisant is marketed under the brand Wakix in many regions and is positioned as a non-stimulant option for managing excessive daytime sleepiness in narcolepsy, offering an alternative to traditional stimulant therapies.