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# 5-HT4 receptor agonist prokinetics

Drugs that stimulate serotonin 5-HT4 receptors in the gut wall to release acetylcholine and push stool along; used in chronic constipation.

Updated Nov 1, 2026

## What they are

Prokinetic agents for chronic idiopathic constipation when laxatives fail. Older drugs of this type (cisapride, tegaserod) were limited by heart and vascular problems; prucalopride is highly selective for 5-HT4.

## Mechanism of action

5-HT4 receptors on enteric neurons increase acetylcholine release when stimulated. More acetylcholine strengthens contractions and triggers high-amplitude propagating contractions in the colon, so transit speeds up and stools become more frequent.

Target: Serotonin 5-HT4 receptors on enteric neurons

## Key points

- 5-HT4 agonism releases acetylcholine and stimulates colonic peristalsis.
- Prucalopride: watch mood; suicidal thoughts and depression have been reported.
- Contraindicated in bowel obstruction, perforation and severe inflammatory bowel disease.
- Older non-selective agents caused QT prolongation (cisapride).

## Drugs in this class

- [**Prucalopride** A selective 5-HT4 agonist that stimulates colonic peristalsis. Used for chronic idiopathic constipation in adults. Serotonin 5-HT4 receptor on enteric neurons](https://durgical.com/en/pharmacology/prucalopride/)

## Others in the class

- Tegaserod (restricted use)
- Cisapride (withdrawn in many countries: QT prolongation)

## Test yourself

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

## What does 5-HT4 stimulation release from enteric neurons?

Acetylcholine.

## Why was cisapride withdrawn in many countries?

QT prolongation and arrhythmias.

## Which bowel conditions contraindicate 5-HT4 prokinetics?

Bowel obstruction or perforation (also severe inflammatory bowel disease).

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

Sources: [DailyMed - PRUCALOPRIDE tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e1e9e36c-ce5a-4323-9d20-395bb5e80e64) (DailyMed (U.S. National Library of Medicine), 2024); [Prucalopride: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619011.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A06AX) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/classes/5-ht4-receptor-agonist-prokinetics/