Prucalopride Succinate tablet is indicated for the symptomatic treatment of chronic constipation in adults in whom laxatives do not provide adequate relief.

Prucalopride is a selective agonist of the 5-HT4 receptor and has no significant interaction with hERG channels or 5-HT1 receptors, which results in a lower cardiovascular risk compared to other similar agents. 5-HT4 receptors are widely distributed throughout the gastrointestinal tract, mainly in smooth muscle cells, enterochromaffin cells, and the myenteric plexus. Activation of these receptors stimulates the release of acetylcholine, the main excitatory neurotransmitter in the gut. By enhancing acetylcholine release, Prucalopride increases gastrointestinal motility, causing contraction of the colonic muscle layer and relaxation of circular muscles, thereby promoting propulsion of intestinal contents.

Adults: 2 mg once daily with or without food, at any time of the day. Due to the specific mode of action of prucalopride (stimulation of propulsive motility), exceeding the daily dose of 2 mg is not expected to increase efficacy.

Older people: Start with 1 mg once daily; if needed the dose can be increased to 2 mg once daily.

Children: Prucalopride should not be used in children and adolescents younger than 18 years.

In vitro data indicate that Prucalopride has a low potential for drug interactions. Therapeutic concentrations are not expected to affect CYP-mediated metabolism of co-administered drugs. Although Prucalopride may act as a weak substrate of P-glycoprotein (P-gp), it does not inhibit P-gp at clinically relevant concentrations.

Ketoconazole (200 mg twice daily), a strong CYP3A4 and P-gp inhibitor, increases systemic exposure to Prucalopride by about 40%, which is not considered clinically significant. Similar effects may be expected with other strong P-gp inhibitors such as verapamil, cyclosporine A, and quinidine.

Studies in healthy subjects show no clinically relevant effect of Prucalopride on warfarin, digoxin, alcohol, paroxetine, or oral contraceptives.

Prucalopride is contraindicated in patients with hypersensitivity to the active substance or any excipients, and in patients with renal impairment requiring dialysis.

The most common adverse effects are headache (17.8%), abdominal pain, nausea, and diarrhoea. These usually occur at the start of therapy and subside within a few days. Most reactions are mild to moderate in severity.

Prucalopride is not recommended during pregnancy. Women of reproductive age should use effective contraception during treatment. Animal studies show no direct harmful effects on pregnancy or fetal development. It is not recommended during breastfeeding due to lack of human data.

• Renal excretion is the main route of elimination; dose reduction to 1 mg is recommended in severe renal impairment.
• Caution is required in severe hepatic impairment (Child-Pugh C).
• Severe diarrhoea may reduce effectiveness of oral contraceptives; additional contraception is advised.
• Tablets contain lactose and are not suitable for patients with lactose intolerance or related hereditary disorders.

Renal impairment: 1 mg once daily in severe cases (GFR <30 ml/min). No adjustment needed in mild to moderate cases.

Hepatic impairment: Start with 1 mg once daily in severe cases; may increase to 2 mg if tolerated. No adjustment needed in mild to moderate cases.

Overdose may cause exaggerated pharmacological effects such as headache, nausea, and diarrhoea. Treatment is supportive, including fluid and electrolyte replacement if needed.

Osmotic purgatives

Store at room temperature below 30°C. Do not remove desiccant. Dispense in original container.