Pitolisant - Revision history

MDElliottMD: Tier 1 taxonomy consolidation: removed redundant Category:Wake-Promoting Agents (canonical already present)

2026-05-21T17:01:58Z

Tier 1 taxonomy consolidation: removed redundant Category:Wake-Promoting Agents (canonical already present)

← Older revision		Revision as of 17:01, 21 May 2026
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	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]
	[[Category:Histamine H3 Antagonists / Inverse Agonists]]		[[Category:Histamine H3 Antagonists / Inverse Agonists]]
	~~[[Category:Wake-Promoting Agents]]~~
	[[Category:Histamine Modulators]]		[[Category:Histamine Modulators]]

MDElliottMD: Retag from Category:Eugeroics (Wakefulness-Promoting Agents) to Category:Eugeroics: verbose category name simplified per the standing category-naming convention.

2026-05-19T03:42:16Z

Retag from Category:Eugeroics (Wakefulness-Promoting Agents) to Category:Eugeroics: verbose category name simplified per the standing category-naming convention.

← Older revision		Revision as of 03:42, 19 May 2026
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	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]
	[[Category:Eugeroics ~~(Wakefulness-Promoting Agents)~~]]		[[Category:Eugeroics]]
	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]
	[[Category:Histamine H3 Antagonists / Inverse Agonists]]		[[Category:Histamine H3 Antagonists / Inverse Agonists]]
	[[Category:Wake-Promoting Agents]]		[[Category:Wake-Promoting Agents]]
	[[Category:Histamine Modulators]]		[[Category:Histamine Modulators]]

MDElliottMD: Em-dash sweep: replace em-dash with comma per project rule; PendellsCorner verbatim quotes preserved.

2026-05-19T03:16:10Z

Em-dash sweep: replace em-dash with comma per project rule; PendellsCorner verbatim quotes preserved.

← Older revision		Revision as of 03:16, 19 May 2026
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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 — '''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.		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.

MDElliottMD: Recategorize: Stimulants -> Psychostimulants

2026-05-17T10:51:01Z

Recategorize: Stimulants -> Psychostimulants

← Older revision		Revision as of 10:51, 17 May 2026
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	}}		}}

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

MDElliottMD: Recategorize: Stimulants & Wake-Promoting Agents -> Stimulants

2026-05-17T10:45:15Z

Recategorize: Stimulants & Wake-Promoting Agents -> Stimulants

← Older revision		Revision as of 10:45, 17 May 2026
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	}}		}}

	[[Category:Stimulants ~~& Wake-Promoting Agents~~]]		[[Category:Stimulants]]
	[[Category:Eugeroics (Wakefulness-Promoting Agents)]]		[[Category:Eugeroics (Wakefulness-Promoting Agents)]]
	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]

Maintenance script: Terminology sweep: drug/medication → medicine

2026-05-16T02:27:26Z

Terminology sweep: drug/medication → medicine

← Older revision		Revision as of 02:27, 16 May 2026
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	\| pregnancy = Limited data; pitolisant may reduce hormonal contraceptive efficacy		\| 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 ~~medications~~, 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.		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 ~~drugs~~). Can reduce hormonal contraceptive efficacy.		\| 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/>
	}}		}}

Maintenance script: Expand Pitolisant with Stahl-sourced detail (with skepticism)

2026-05-16T02:03:46Z

Expand Pitolisant with Stahl-sourced detail (with skepticism)

← Older revision		Revision as of 02:03, 16 May 2026
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	{{MedTemplate		{{MedTemplate
	~~\| generic = Pitolisant~~		\| brand = Wakix
	\| brand = Wakix		\| classes = Histamine H3 receptor inverse agonist / antagonist, wake-promoting agent
	~~\| structure =~~		\| mechanism = Selective inverse agonist (or antagonist depending on assay) at presynaptic histamine H3 autoreceptors. H3 receptors normally inhibit histamine release; blocking them disinhibits histamine release from tuberomammillary nucleus, promoting wakefulness. Also enhances acetylcholine, norepinephrine, dopamine release (downstream of histamine signaling).
	\| classes = ~~Eugeroic~~		\| uses = Excessive daytime sleepiness or cataplexy in adults with narcolepsy (FDA-approved August 2019)
	\| mechanism = ~~Histamine H3 receptor~~ inverse agonist/antagonist		\| starting_dose = Week 1: 8.9 mg PO once daily in the morning. Week 2: 17.8 mg. Week 3+: 35.6 mg (max). Titrate as needed.
	\| uses =		\| preparations = 4.45 mg, 17.8 mg tablets
	\| starting_dose =		\| fda_max = 35.6 mg/d
	\| preparations =		\| routes = Oral
	\| fda_max =		\| onset = Wake-promoting effect over weeks of titration
	\| routes =		\| duration = Daily morning dosing
	\| onset =		\| halflife = ~20 hours
	\| duration =		\| bioavailability = Not formally established; oral once-daily adequate
	\| halflife =		\| pregnancy = Limited data; pitolisant may reduce hormonal contraceptive efficacy
	\| bioavailability =		\| legal = Rx — '''not a controlled substance''' (unique among wake-promoting agents)
	\| pregnancy =		\| 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 medications, all of which have abuse potential and DEA scheduling (modafinil IV, methylphenidate II, amphetamine II, solriamfetol IV, sodium oxybate III).
	\| legal =
	\| intro =		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.
	~~\| pharmacokinetics =~~		\| pharmacodynamics= High-affinity inverse agonist at human H3 receptor. Minimal binding at H1, H2, H4, monoamine transporters, or other monoamine receptors.
	\| pharmacodynamics =		\| effects = Headache, insomnia, anxiety, nausea, abdominal pain, decreased appetite, sleep disturbances. QT prolongation possible (caution with other QT-prolonging drugs). Can reduce hormonal contraceptive efficacy.
	~~\| indications =~~		\| interactions = <pharmaInteractions/>
	~~\| dosing~~ =
	\| effects =
	\| interactions = <pharmaInteractions/>
	~~\| pregnancy_details =~~
	~~\| monitoring =~~
	~~\| counseling =~~
	~~\| anecdotes =~~
	~~\| seealso =~~
	~~\| references =~~
	}}		}}


	[[Category:Stimulants & Wake-Promoting Agents]]		[[Category:Stimulants & Wake-Promoting Agents]]
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	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]
	[[Category:Histamine H3 Antagonists / Inverse Agonists]]		[[Category:Histamine H3 Antagonists / Inverse Agonists]]
			[[Category:Wake-Promoting Agents]]
			[[Category:Histamine Modulators]]

MDElliottMD: Comprehensive categorization: +Histamine H3 Antagonists / Inverse Agonists

2026-05-15T18:42:06Z

Comprehensive categorization: +Histamine H3 Antagonists / Inverse Agonists

← Older revision		Revision as of 18:42, 15 May 2026
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	[[Category:Eugeroics (Wakefulness-Promoting Agents)]]		[[Category:Eugeroics (Wakefulness-Promoting Agents)]]
	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]
			[[Category:Histamine H3 Antagonists / Inverse Agonists]]

MediaWiki default: Assign pharmacological categories from List_of_CNS-active_medicines

2026-05-14T15:06:56Z

Assign pharmacological categories from List_of_CNS-active_medicines

← Older revision		Revision as of 15:06, 14 May 2026
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	}}		}}


			[[Category:Stimulants & Wake-Promoting Agents]]
			[[Category:Eugeroics (Wakefulness-Promoting Agents)]]
	[[Category:Psychostimulants]]		[[Category:Psychostimulants]]

MDElliottMD: Pharmacopedia: add

2026-05-14T03:31:06Z

Pharmacopedia: add <pharmaInteractions/>

← Older revision		Revision as of 03:31, 14 May 2026
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	\| dosing =		\| dosing =
	\| effects =		\| effects =
	\| interactions =		\| interactions = <pharmaInteractions/>
	\| pregnancy_details =		\| pregnancy_details =
	\| monitoring =		\| monitoring =