Pitolisant hydrochloride

Pitolisant hydrochloride is a histamine H3 receptor antagonist/inverse agonist. It is used in the treatment of narcolepsy, a chronic neurological disorder that affects the brain's ability to control sleep-wake cycles. Pitolisant hydrochloride is marketed under the brand name Wakix.

Pharmacology

Pitolisant hydrochloride acts as an antagonist and inverse agonist at the H3 histamine receptor. This receptor is found in the central nervous system and plays a role in controlling the release of histamine and other neurotransmitters. By blocking this receptor, pitolisant hydrochloride increases the release of histamine, which promotes wakefulness.

Clinical Use

Pitolisant hydrochloride is used for the treatment of narcolepsy, a condition characterized by excessive daytime sleepiness and sudden attacks of sleep. It is also used to treat cataplexy, a sudden loss of muscle tone triggered by strong emotions, which often accompanies narcolepsy.

Side Effects

Common side effects of pitolisant hydrochloride include insomnia, headache, nausea, and anxiety. Serious side effects may include irregular heartbeat, hallucinations, and suicidal thoughts.

History

Pitolisant hydrochloride was developed by the French pharmaceutical company Bioprojet. It was approved for medical use in the European Union in March 2016, and in the United States in August 2019.

See Also

• Histamine H3 receptor
• Narcolepsy
• Bioprojet