Pitolisant: Difference between revisions

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| bioavailability = Not formally established; oral once-daily adequate

| pregnancy = Limited data; pitolisant may reduce hormonal contraceptive efficacy

| legal = Rx — '''not a controlled substance''' (unique among wake-promoting agents)

| legal = Rx, '''not a controlled substance''' (unique among wake-promoting agents)

| intro = '''Pitolisant''' (brand name Wakix) is a selective histamine H3 receptor inverse agonist FDA-approved in August 2019 for excessive daytime sleepiness and cataplexy in narcolepsy. Notable for being '''not a controlled substance''' — unique among approved wake-promoting medicines, all of which have abuse potential and DEA scheduling (modafinil IV, methylphenidate II, amphetamine II, solriamfetol IV, sodium oxybate III).

| intro = '''Pitolisant''' (brand name Wakix) is a selective histamine H3 receptor inverse agonist FDA-approved in August 2019 for excessive daytime sleepiness and cataplexy in narcolepsy. Notable for being '''not a controlled substance''', unique among approved wake-promoting medicines, all of which have abuse potential and DEA scheduling (modafinil IV, methylphenidate II, amphetamine II, solriamfetol IV, sodium oxybate III).

Mechanism: H3 autoreceptors on histamine neurons in the tuberomammillary nucleus normally inhibit histamine release. Pitolisant blocks (or inverse-agonizes) these autoreceptors, disinhibiting histamine release and promoting wakefulness. Downstream effects on acetylcholine, norepinephrine, and dopamine pathways may also contribute. Slow titration required.

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[[Category:~~Stimulants~~]]

[[Category:Psychostimulants]]

[[Category:Eugeroics ~~(Wakefulness-Promoting Agents)~~]]

[[Category:Eugeroics]]

[[Category:Psychostimulants]]

[[Category:Histamine H3 Antagonists / Inverse Agonists]]

~~[[Category:Wake-Promoting Agents]]~~

[[Category:Histamine Modulators]]

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