Prucalopride
5-HT4 receptor agonist prokinetics
5-HT4 receptor agonist prokinetics
A selective 5-HT4 agonist that stimulates colonic peristalsis. Used for chronic idiopathic constipation in adults.
Quick facts
- Group
- 5-HT4 receptor agonist prokinetics
- Target
- Serotonin 5-HT4 receptor on enteric neurons
- Used for
- Chronic idiopathic constipation
- Key effects
- Headache · Abdominal pain · Nausea
- Monitor
- Mood and suicidal thoughts · Renal function
- ATC
- A06AX05
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows serotonin in the human 5-HT4 receptor; prucalopride activates the same receptor.
Prucalopride is a selective serotonin 5-HT4 receptor agonist with little action on other serotonin receptors such as 5-HT2B or 5-HT3. On enteric neurons it increases acetylcholine release, strengthening contractions and triggering high-amplitude propagating contractions of the colon, so bowel motility increases.
- Prucalopride activates enteric 5-HT4 receptors
- Acetylcholine release increases
- Colonic peristalsis strengthens; stools become more frequent
Indications
- Chronic idiopathic constipation in adults
Adverse effects
Common
- Headache
- Abdominal pain, bloating, flatulence
- Nausea, vomiting, diarrhoea
- Dizziness, fatigue
Contraindications
- Hypersensitivity to prucalopride
- Intestinal perforation or obstruction, obstructive ileus
- Severe inflammatory conditions of the gut: Crohn's disease, ulcerative colitis, toxic megacolon or megarectum
Key interactions
- Other laxatives
- More diarrhoea and cramping
- Ketoconazole (strong CYP3A and P-glycoprotein inhibitor)
- Modestly higher prucalopride levels
What is monitored
- Mood and suicidal thoughts
- Bowel frequency and diarrhoea
- Renal function (dose depends on it)
Administration and safety
- Oral tablet, with or without food.
- A lower dose is used in severe renal impairment.
- Stopped at once if mood changes or suicidal thoughts appear.
Pregnancy and breastfeeding
Human data from case reports are insufficient to define a risk; animal studies showed no developmental harm.
Nursing care
- Ask about depression or suicidal thoughts before starting.
- Teach the patient and family to watch for mood changes and report them at once.
- Warn that headache and abdominal pain are common in the first days.
- Check that there is no bowel obstruction or active severe IBD.
Pharmacokinetics
- Absorption
- High oral bioavailability; food has no effect
- Elimination
- Mainly renal, largely unchanged; dose is lowered in severe renal impairment
- Half-life
- About one day
Test yourself
Think of the answer, then tap the question to see it.
Which receptor does prucalopride stimulate?
The serotonin 5-HT4 receptor on enteric neurons.
Which psychiatric warning applies?
Suicidal thoughts and behaviour, and new or worsening depression.
Why is the dose lowered in severe kidney disease?
It is excreted mainly unchanged by the kidneys.
Connections
← Back to the class: 5-HT4 receptor agonist prokinetics
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); RCSB PDB - 7XT8: Serotonin 4 (5-HT4) receptor-Gs-Nb35 complex (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.