pitolisant hydrochloride at a glance
Medicine class
Histamine H3-receptor antagonist and inverse agonist
Licensed uses
Narcolepsy with or without cataplexy; selected adults with persistent sleepiness associated with obstructive sleep apnoea
How it is taken
Film-coated tablets taken by mouth in the morning on waking
Contraception
May make hormonal contraception less effective
What is pitolisant hydrochloride used for?
UK-licensed uses for the selected product are:
Treating narcolepsy with or without cataplexy in adults, adolescents and children aged 6 years and over.
Improving wakefulness and reducing excessive daytime sleepiness in adults with obstructive sleep apnoea when primary therapy has not worked satisfactorily or cannot be tolerated. It does not treat the underlying airway obstruction.
How does pitolisant hydrochloride work?
Pitolisant blocks and inversely activates histamine H3 receptors, increasing the activity of histamine-producing neurons involved in wakefulness. It also influences acetylcholine, noradrenaline and dopamine signalling without increasing dopamine release in the brain’s main reward pathway.
pitolisant hydrochloride preparations and strengths
Tablet
Route: Oral
Strengths: 4.5 mg, 18 mg
How to take pitolisant hydrochloride
Take the tablets by mouth in the morning on waking, following the specialist’s instructions. Food does not materially affect absorption.
Do not change the prescribed amount yourself.
Persistent sleepiness can remain despite treatment; avoid driving or hazardous activities if you are not fully alert.
pitolisant hydrochloride side effects
Common or expected effects
- Difficulty sleeping
- Headache
- Feeling sick or vomiting
- Anxiety or irritability
- Dizziness, vertigo or tremor
- Depression or other sleep disturbance
- Tiredness
- Indigestion
Get urgent medical advice
- Suicidal thoughts or severe psychiatric symptoms
- Seizure or loss of consciousness
- Symptoms of a significant heart-rhythm problem, such as fainting, chest pain or breathlessness
- Severe hallucinations or marked behavioural change
pitolisant hydrochloride in pregnancy
Human pregnancy information is limited, and animal studies found reproductive harm. Pitolisant should generally be avoided during pregnancy unless a specialist judges that the expected benefit outweighs the fetal risk. Contact the prescriber promptly when planning pregnancy or if pregnancy occurs, without stopping treatment independently.
pitolisant hydrochloride while breastfeeding
Breastfeeding is contraindicated during pitolisant treatment because animal evidence shows that pitolisant or its metabolites enter milk. Discuss alternative feeding or treatment options with the specialist.
pitolisant hydrochloride interactions
Check prescribed, over-the-counter and herbal products with a pharmacist or prescriber. Important interactions include:
Hormonal contraceptives
Pitolisant may reduce contraceptive effectiveness, so an additional reliable non-hormonal method is required during treatment and for 21 days after stopping.
Sedating H1 antihistamines, including promethazine, chlorphenamine and diphenhydramine
These may oppose pitolisant’s histamine-mediated effect and reduce its effectiveness.
Imipramine, clomipramine and mirtazapine
Their H1-antihistamine activity may reduce pitolisant’s effectiveness; an alternative may be needed.
Common questions about pitolisant hydrochloride
Answers are fully visible for fast scanning and source review.
What type of treatment is pitolisant hydrochloride?
It is a wake-promoting histamine H3-receptor antagonist and inverse agonist, rather than a conventional amphetamine-like stimulant.
What is pitolisant hydrochloride licensed to treat in the UK?
It is licensed for narcolepsy with or without cataplexy and for selected adults with persistent excessive daytime sleepiness associated with obstructive sleep apnoea.
Can children take pitolisant hydrochloride?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.