Pitolisant: Difference between revisions

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 {{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
-| routes             =
+| onset           = Wake-promoting effect over weeks of titration
-| onset              =
+| duration        = Daily morning dosing
-| duration           =
+| halflife        = ~20 hours
-| halflife           =
+| bioavailability = Not formally established; oral once-daily adequate
-| bioavailability    =
+| pregnancy       = Limited data; pitolisant may reduce hormonal contraceptive efficacy
-| pregnancy          =
+| legal           = Rx, '''not a controlled substance''' (unique among wake-promoting agents)
-| legal              =
+| 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              =
-| pharmacokinetics   =
+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   =
+| pharmacodynamics= High-affinity inverse agonist at human H3 receptor. Minimal binding at H1, H2, H4, monoamine transporters, or other monoamine receptors.
-| indications        =
+| 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.
-| dosing             =
+| interactions     = <pharmaInteractions/>
-| effects            =
-| contraindications  =
-| interactions       =
-| pregnancy_details  =
-| monitoring         =
-| counseling         =
-| anecdotes          =
-| seealso            =
-| references         =
 }}
 [[Category:Psychostimulants]]
+[[Category:Eugeroics]]
+[[Category:Psychostimulants]]
+[[Category:Histamine H3 Antagonists / Inverse Agonists]]
+[[Category:Histamine Modulators]]

MDElliottMD (talk | contribs)