pitolisant hydrochloride: clinical use

Prescribing considerations

• Initiation should be by a clinician experienced in sleep disorders or obstructive sleep apnoea and cardiovascular risk.
• Regularly reassess continuing benefit and residual sleepiness, including fitness to drive or perform hazardous tasks.
• For obstructive sleep apnoea, continue or periodically retry primary airway treatment and reassess the underlying condition annually.
• Review renal and hepatic function, cardiovascular and QT risk, psychiatric history, epilepsy, weight and interacting medicines.
• Counsel people who could become pregnant about reduced hormonal-contraceptive effectiveness.

Contraindications and cautions

• Hypersensitivity to pitolisant or an excipient
• Severe hepatic impairment
• Breastfeeding

Monitoring

• Clinical response and continuing benefit
• Residual daytime sleepiness and driving risk
• Mood, suicidal thinking, hallucinations and behavioural change
• Weight and appetite where clinically relevant
• Cardiac status in people with cardiovascular disease, hypertension, QT risk, interacting treatment or increased pitolisant exposure
• Renal and hepatic function where impairment is present
• Adherence to primary obstructive sleep apnoea therapy

Clinical pharmacology

Pitolisant is an orally active H3-receptor antagonist and inverse agonist. It is metabolised mainly through CYP2D6 and CYP3A pathways, has substantial interindividual exposure variability and an elimination half-life of approximately 10–12 hours.

Formulation and product differences

• The selected product is a white, round, biconvex film-coated tablet marked “5” on one side.
• No special storage conditions are required.

Tablet

Route: Oral

Strengths: 4.5 mg, 18 mg