Prucalo2 mg

Prucalopride succinate is indicated for the treatment of chronic idiopathic constipation in adults who have not had an adequate response to laxatives.

Contains prucalopride (as Prucalo 2 mg) as the active ingredient, available as oral film-coated tablets in 1 mg and 2 mg strengths.

Prucalopride is an oral medicine used to treat chronic constipation that has not responded well enough to laxatives. It works by stimulating a specific serotonin receptor in the gut that promotes normal colonic movement, helping stool pass more regularly. It is taken once daily and is intended for adults whose constipation is not explained by another underlying condition or medication.

Therapeutic Class: Gastrointestinal Prokinetic Agent

Prucalopride is well absorbed after oral administration and has a long elimination half-life supporting once-daily dosing; steady-state concentrations are generally reached within 3-4 days. It is eliminated mainly by the kidneys, so exposure increases in patients with reduced kidney function, requiring dose adjustment in severe renal impairment.

• Taken orally, once daily, with or without food
• Can be taken at any time of day
• Swallow the tablet whole with water
• Mild gastrointestinal side effects in the first week of treatment (such as headache, nausea, abdominal pain, or diarrhoea) typically resolve on their own; treatment should not be stopped prematurely for these effects without discussing with a doctor

At the recommended dosage, prucalopride has a low potential for clinically significant drug interactions, since it is not extensively metabolized by major liver enzymes. Because prucalopride increases gastrointestinal motility, it may theoretically affect the absorption of some concurrently administered oral medicines, and this should be assessed by a healthcare professional if relevant, particularly for drugs with a narrow therapeutic window.

Common side effects

• Headache
• Nausea
• Abdominal pain or cramping
• Diarrhoea
• Dizziness

These effects are most common in the first day of treatment and typically decrease within a few days with continued use.

Serious side effects (seek medical attention)

• Signs of a severe allergic reaction: rash, swelling, difficulty breathing
• Severe or persistent diarrhoea
• New or worsening mood changes, including suicidal thoughts
• Signs of bowel obstruction or perforation: severe abdominal pain, inability to pass stool or gas, vomiting

Pregnancy

Data on prucalopride use in human pregnancy are limited; it should be used during pregnancy only if the treating doctor determines the potential benefit outweighs the potential risk.

Breastfeeding

It is not established whether prucalopride passes into human milk in clinically significant amounts; the decision to use it during breastfeeding should weigh the benefits of breastfeeding and the mother's clinical need for treatment, in consultation with a healthcare professional.

• Use with caution in patients with severe cardiovascular disease, given limited clinical experience in this population.
• Dose reduction is required in patients with severe renal impairment (CrCl below 30 mL/min); use is generally not recommended in patients on dialysis.
• Prucalopride has not been well studied in patients with secondary causes of constipation (such as endocrine, metabolic, or neurologic disorders) or medication-related constipation (such as from opioid use); some experts recommend avoiding use in these situations.
• Screen for a history of depression or suicidal ideation before starting treatment, and monitor for mood changes throughout treatment, given reports of psychiatric symptoms with serotonergic gut medicines.
• May cause dizziness or fatigue; advise caution with driving or operating machinery if these effects occur.

Overdose may cause more pronounced gastrointestinal effects, such as significant diarrhoea, abdominal pain, or headache. Suspected overdose should be evaluated by a healthcare professional; treatment is generally supportive, with attention to fluid and electrolyte status if significant diarrhoea occurs.

Store at room temperature, protected from moisture, as directed on the specific product's packaging.

• Elderly (65 years and older): No dose adjustment required based on age alone; efficacy is comparable to the overall adult population.
• Renal impairment: No adjustment needed for mild-to-moderate impairment; reduce to 1 mg once daily for severe impairment (CrCl below 30 mL/min); avoid use in dialysis-dependent end-stage renal disease.
• Hepatic impairment: No dose adjustment is generally required, including in moderate to severe impairment, based on available pharmacokinetic data, though clinical experience in severe impairment is limited.

Prucalopride can be continued long-term if it provides clinical benefit, unlike the shorter durations studied in clinical trials. If constipation does not improve after about 4 weeks of appropriate treatment, the diagnosis and ongoing need for prucalopride should be reassessed by the prescribing doctor.

Drug Class: Selective serotonin 5-HT4 receptor agonist

Prucalopride selectively stimulates serotonin 5-HT4 receptors in the colon, which enhances neurotransmission in the enteric nervous system. This promotes high-amplitude propagated contractions - the strong, coordinated colonic contractions responsible for moving stool along - increasing the frequency of bowel movements and reducing colonic transit time.

Safety and efficacy of prucalopride have not been established in pediatric patients, and it is not recommended for use in children.