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.
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
Drugs in this class
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- Cisapride (withdrawn in many countries: QT prolongation)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Why was cisapride withdrawn in many countries?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).
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 (DailyMed (U.S. National Library of Medicine), 2024); Prucalopride: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.