Pitolisant: Difference between revisions
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Expand Pitolisant with Stahl-sourced detail (with skepticism) |
MDElliottMD (talk | contribs) Tier 1 taxonomy consolidation: removed redundant Category:Wake-Promoting Agents (canonical already present) |
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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. | ||
| pharmacodynamics= High-affinity inverse agonist at human H3 receptor. Minimal binding at H1, H2, H4, monoamine transporters, or other monoamine receptors. | | pharmacodynamics= High-affinity inverse agonist at human H3 receptor. Minimal binding at H1, H2, H4, monoamine transporters, or other monoamine receptors. | ||
| effects = Headache, insomnia, anxiety, nausea, abdominal pain, decreased appetite, sleep disturbances. QT prolongation possible (caution with other QT-prolonging | | effects = Headache, insomnia, anxiety, nausea, abdominal pain, decreased appetite, sleep disturbances. QT prolongation possible (caution with other QT-prolonging medicines). Can reduce hormonal contraceptive efficacy. | ||
| interactions = <pharmaInteractions/> | | interactions = <pharmaInteractions/> | ||
}} | }} | ||
[[Category: | [[Category:Psychostimulants]] | ||
[[Category:Eugeroics | [[Category:Eugeroics]] | ||
[[Category:Psychostimulants]] | [[Category:Psychostimulants]] | ||
[[Category:Histamine H3 Antagonists / Inverse Agonists]] | [[Category:Histamine H3 Antagonists / Inverse Agonists]] | ||
[[Category:Histamine Modulators]] | [[Category:Histamine Modulators]] | ||