[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Wake-promoting agents and narcolepsy drugs](https://durgical.com/en/pharmacology/classes/wake-promoting-agents-and-narcolepsy-drugs/) › Pitolisant

# Pitolisant

## Wake-promoting agents and narcolepsy drugs?

Wake-promoting agents and narcolepsy drugs

A histamine H3 receptor blocker for daytime sleepiness and cataplexy in narcolepsy. It can prolong the QT interval and weaken hormonal contraceptives.

Updated Nov 1, 2026

## Quick facts

**Group**
[Wake-promoting agents and narcolepsy drugs](https://durgical.com/en/pharmacology/classes/wake-promoting-agents-and-narcolepsy-drugs/)

**Target**
Histamine H3 receptor

**Used for**
Excessive daytime sleepiness

**Key effects**
Headache · Insomnia · Nausea and less appetite

**Monitor**
ECG and potassium · Daytime sleepiness

**ATC**
N07XX11

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

Pitolisant is a selective antagonist and inverse agonist of the histamine H3 receptor, which normally acts as a brake on histamine release in the brain. Blocking it lets histaminergic neurons release more histamine, a key wake-promoting signal. It has little affinity for H1, H2 or H4 receptors.

- Blocks the H3 autoreceptor on histamine neurons
- The brake is released and more histamine is set free
- Wakefulness rises; sleepiness and cataplexy decrease

## Indications

- Excessive daytime sleepiness in narcolepsy (adults and children from 6 years) [Narcolepsy →](https://durgical.com/en/conditions/narcolepsy/)
- Cataplexy in adults with narcolepsy

## Adverse effects

### Common

- Headache
- Insomnia
- Nausea and less appetite
- Anxiety and irritability

### Serious (rare, important)

- QT prolongation with fast or irregular heartbeat or fainting
- Hallucinations

## Contraindications

- Liver disease, which can rule it out
- Hypersensitivity to pitolisant

## Key interactions

**Hormonal contraceptives**
Less effective; another method is used during treatment and for 21 days after

**Other drugs that prolong the QT interval**
Added risk of arrhythmia

## What is monitored

- ECG and potassium and magnesium when there is QT risk
- Daytime sleepiness and cataplexy episodes

## Administration and safety

- Given by mouth, starting low and raising the dose step by step
- Liver and kidney disease are reviewed before starting

## Pregnancy and breastfeeding

It weakens hormonal contraceptives, so another method is used; pregnancy plans are discussed with the prescriber.

## Nursing care

- Ask about heart rhythm problems, low potassium or magnesium and liver disease
- Counsel on non-hormonal contraception during treatment and for 21 days after
- Teach to report palpitations, fainting or hallucinations

## Pharmacokinetics

**Metabolism**
In the liver; CYP2D6 genotype can change the dose needed

## Memory aid

Pitolisant: «Pull the H3 brake, histamine wakes» – watch the QT and the pill.

## Test yourself

Think of the answer, then tap the question to see it.

## What does the H3 receptor normally do?

It is an autoreceptor that brakes histamine release.

## Which ECG change is a concern with pitolisant?

QT prolongation.

## For how long after stopping pitolisant is another contraceptive method used?

For 21 days.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/pitolisant/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 3

- [Modafinil](https://durgical.com/en/pharmacology/modafinil/)
- [Solriamfetol](https://durgical.com/en/pharmacology/solriamfetol/)
- [Sodium oxybate](https://durgical.com/en/pharmacology/sodium-oxybate/)

## Related conditions 1

- [Narcolepsy](https://durgical.com/en/conditions/narcolepsy/)

[← Back to the class: Wake-promoting agents and narcolepsy drugs](https://durgical.com/en/pharmacology/classes/wake-promoting-agents-and-narcolepsy-drugs/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Pitolisant: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619055.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N07XX11) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/pitolisant/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/pitolisant/