Pitolisant: Difference between revisions
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MDElliottMD (talk | contribs) Recategorize: Stimulants -> Psychostimulants |
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| bioavailability = Not formally established; oral once-daily adequate | | bioavailability = Not formally established; oral once-daily adequate | ||
| pregnancy = Limited data; pitolisant may reduce hormonal contraceptive efficacy | | pregnancy = Limited data; pitolisant may reduce hormonal contraceptive efficacy | ||
| legal = Rx | | 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''' | | 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. | 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. | ||