Pitolisant

WAKIX

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Pronunciation: pi-TOL-i-sant

Pitolisant ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Pitolisant ballicule

Pitolisant WAKIX mascot mnemonic cartoon — Visual mnemonic: Pitolisant mascot
**“Wacky Pitstop”**

What it isHistamine H3 inverse agonist raising histamine release; narcolepsy.

Why this oneNon-scheduled and non-stimulant, which is unique among the wake-promoting agents.

What limits itQT prolongation. It reduces oral contraceptive efficacy; CYP2D6-dependent.

Pitolisant molecular structure (skeletal formula) — Molecular structure: Pitolisant

FDA-approved for

narcolepsy (2019)

Off-label

idiopathic hypersomnia

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Narcolepsy — EDS or cataplexy	Adults	8.9 mg QAM (Wk1)	17.8 mg QAM (Wk2)	35.6 mg QD
Narcolepsy — EDS or cataplexy	Peds ≥6 yr	4.45 mg QAM (Wk1)	8.9–17.8 mg QD	17.8 mg QD (<40 kg) / 35.6 mg QD (≥40 kg)

Titration Increase at weekly intervals (7 days for renal-impaired, 14 days for hepatic-impaired)

Renal eGFR <60: start 8.9 mg QD, max 17.8 mg QD (increase after 7 days); ESRD not recommended

Hepatic Moderate (Child-Pugh B): start 8.9 mg QD, max 17.8 mg QD after 14 days; severe impairment contraindicated

Instructions

Take once daily in the morning upon wakening

Available strengths

tab 4.45, 17.8 mg

Contraindications

Severe hepatic impairment

Cautions

QT-interval prolongation — avoid with QT-prolonging drugs and in patients with arrhythmia risk factors; monitor QTc in hepatic/renal impairment

Adverse reactions

Insomnia
Nausea
Anxiety (adults)
Headache, insomnia (peds ≥6 yr)

Pregnancy Pregnancy exposure registry; no established drug-associated risk; embryofetal toxicity in animals

Lactation Low transfer into breast milk (RID <1%); no data on breastfed infant

Cost

Pitolisant (WAKIX)

Strength		#/mo	generic $/mo	CostPlus
4.45 mg	tab	30 qd		not offered
17.8 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Pitolisant is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2026

NO BOXED WARNINGS

Principal riskQT prolongation; it reduces contraceptive efficacy

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityQT prolongation and CYP-mediated interactions; insomnia and anxiety are common.

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Memory aids: interaction avatars

CYP3A4 inducer (weak — unverified)

CYP3A4 substrate

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