Generic
Prucalopride
33 brands available in the market
At a glance
Prucalopride is a selective 5-HT4 receptor agonist with prokinetic effect, used for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief.
Description
Prucalopride is a selective stimulator of 5-HT4 receptors found throughout the GI tract primarily in smooth muscle cells, enterochromaffin cells, and myenteric plexus. Its activation produces acetylcholine release, the major excitatory neurotransmitter in the GI tract. Prucalopride stimulates motility by causing contraction of the muscle layer of the colon and relaxation of the circular muscle layer, leading to propulsion of luminal content.
Indications
- Chronic constipation in adults (where laxatives fail to provide adequate relief)
Therapeutic class
Osmotic purgatives
Pharmacological class
5-HT4 Receptor Agonist (Prokinetic)
Pharmacology
Prucalopride activates 5-HT4 receptors, causing acetylcholine release which is the major excitatory neurotransmitter in the GI tract. It stimulates contraction of the colon muscle layer and relaxation of the circular muscle layer, leading to propulsion of luminal content. It does not interact with hERG channels or 5-HT1 receptors, significantly reducing cardiovascular risk.
Mechanism of action
Increases GI motility by activating 5-HT4 receptors.
Dosage
Adult Dose (Oral):
- 2 mg once daily with or without food, at any time of the day
- Elderly: 1 mg once daily initially; may increase to 2 mg/day if needed
- Severe renal impairment (GFR <30 mL/min/1.73 m²): 1 mg once daily
- Severe hepatic impairment (Child-Pugh class C): 1 mg once daily initially; may increase to 2 mg/day if needed
Administration
- May be taken with or without food; take at a fixed time
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Headache (17.8%)
- Abdominal pain
- Nausea
- Diarrhea
Precautions & warnings
- May affect driving ability (dizziness, tiredness); especially on the first day
- Severe diarrhea may reduce efficacy of oral contraceptives; use additional contraceptive method
- Tablets contain lactose; patients with galactose intolerance should not take
- Inform doctor if no improvement after 4 weeks
Contraindications
- Intestinal obstruction or perforation
- Obstructive ileus
- Active severe inflammatory bowel conditions (Crohn's disease, toxic megacolon/megarectum, ulcerative colitis)
- Renal impairment requiring dialysis
- Pregnancy and lactation
Drug interactions
- Contraceptives (estrogens, progestins): Decreased serum concentration
- Levosulpiride: Enhanced adverse effect
- P-glycoprotein/ABCB1 inhibitors: Increased serum concentration
- Atropine-like substances: Reduced effect
Food interactions
It is not known whether it is safe to consume alcohol with Prucalopride.
Use in pregnancy
Use in Pregnancy: Information regarding use during pregnancy is not available; women of childbearing potential should use effective contraception.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; not recommended.
Pediatric use
Do not use in children and adolescents younger than 18 years.
Geriatric use
Elderly patients: 1 mg/day initially; may increase to 2 mg/day if needed.
Renal / hepatic impairment
Renal Impairment: Severe renal impairment (GFR <30 mL/min/1.73 m²): 1 mg/day; dialysis patients: contraindicated; consult your doctor.
Hepatic Impairment: Severe hepatic impairment (Child-Pugh C): 1 mg/day initially; may increase to 2 mg; mild-moderate: no dose adjustment needed; consult your doctor.
Overdose effects
Overdose: Headache, nausea, diarrhea (exaggeration of effects); no specific treatment; symptomatic and supportive care; electrolyte correction for fluid loss from diarrhea/vomiting.
Storage conditions
Store at room temperature, below 30°C; do not remove desiccant; dispense in original bottle.
Chemical structure
Prucalopride