Drug reference

Pitolisant

Antihistamine · Unknown

Also known as Pitolisant hydrochloride, Wakix

AntihistamineUnknown

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid unless potential benefit outweighs risk—toxicity in animal studies.

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AnagrelideSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter

Mechanism

Pitolisant acts as an inverse agonist at presynaptic histamine H3 receptors. These G protein-coupled receptors are primarily found in the brain and normally function as autoreceptors or heteroreceptors, decreasing histamine release via Gi protein coupling and reduction in cAMP. By acting as an inverse agonist, pitolisant counteracts this inhibitory autoregulation, leading to increased neuronal histamine release.

Indications

narcolepsy

Dosing

Renal adjustment: Manufacturer advises use with caution; maximum daily dose should not exceed 18 mg.
Hepatic adjustment: Manufacturer advises caution in moderate impairment; avoid in severe impairment. Consider dose increase two weeks after initiation in moderate impairment; maximum daily dose of 18 mg.
Max dose: 18 mg

Contraindications

Severe hepatic impairment

Side effects

Common

weaknessoedemaon and off phenomenonoral paraesthesiapainparaesthesiaQT interval prolongationsexual dysfunctionskin reactionssweat changestinnitusurinary frequency increasedvisual acuity decreasedweight decreased (review treatment if significant)weight increased (review treatment if significant)yawning

Serious