Products
Prucalopride is commercially available in the form of film-coated tablets (Resolor). It was approved in many countries and in the EU in 2010.
Structure and properties
Prucalopride (C18H26ClN3O3, Mr = 367.87 g/mol) is a dihydrobenzofurancarboxamide. It has structural similarities to the prokinetic cisapride (prepulside, out of commerce).
Effects
Prucalopride (ATC A03AE04) has enterokinetic properties, meaning it promotes intestinal motility and emptying. The effects are due to selective and high-affinity agonism at serotonin(5-HT4)-receptors in the intestine. The structurally similar cisapride was withdrawn from the market due to cardiac adverse effects. Studies have demonstrated that prucalopride is not proarrhythmic and does not inhibit the HERG potassium channel at therapeutic doses.
Indications
Idiopathic chronic constipation in adults for which previous therapy with dietary measures and laxatives has not been sufficiently effective. In men, insufficient efficacy and safety data are available to date.
Dosage
According to the drug label. Tablets may be taken with or without food at any time during the day.
Contraindications
- Hypersensitivity
- Impairment of kidney function requiring dialysis
- Intestinal perforation
- Constipation due to structural or functional disease of the intestinal wall
- Obstructive ileus
- Severe inflammatory diseases of the intestinal tract, such as Crohn’s disease and ulcerative colitis and toxic megacolon/megarectum
Full precautions can be found in the drug label.
Interactions
The potential for drug-drug interactions is considered low because prucalopride does not interact with CYP450. Prucalopride is a weak substrate for P-glycoprotein, which does not appear to be clinically relevant. Full details of interactions can be found in the Drug Information Leaflet.
Adverse effects
The most common adverse effects include headache, nausea, diarrhea, and abdominal pain. Commonly occurring: Vomiting, dyspepsia, rectal bleeding, flatulence, abnormal bowel sounds, pollakiuria, fatigue, and dizziness. Occasional: anorexia, tremor, palpable heartbeats, fever, malaise.