pitolisant

Pitolisant is a selective antagonist and inverse agonist of the histamine H3 receptor, used primarily for the treatment of excessive daytime sleepiness (EDS) and cataplexy in patients with narcolepsy, including adults and children aged six years or older. By blocking presynaptic H3 autoreceptors in the brain, pitolisant increases histaminergic neurotransmission, which promotes wakefulness and alertness. It also modulates other neurotransmitters such as acetylcholine, noradrenaline, and dopamine (primarily outside the striatal complex), contributing to its efficacy in narcolepsy. Pitolisant is considered a eugeroic agent—distinct from traditional stimulants due to its lower abuse potential—and was developed as the first non-imidazole-based H3R antagonist/inverse agonist to reach clinical use[1][2][3][5][6][8].

Brand names

Wakix

Other names

pitolisant