Ibolax

• Chronic Idiopathic Constipation (CIC):
  Indicated for the treatment of chronic idiopathic constipation in adults who have had inadequate response to laxatives.
• Off-label Uses:
• Opioid-induced constipation resistant to laxatives.
• Constipation-predominant irritable bowel syndrome (IBS-C), based on clinical judgment.

• Adults:
• Recommended dose: 2 mg orally once daily.
• If not tolerated, dose can be reduced to 1 mg once daily.
• Assess treatment effectiveness after 4 weeks. Treatment may be continued based on clinical response.
• Elderly Patients:
• Same dose as adults, but reduce to 1 mg daily in cases of severe renal impairment.
• Renal Impairment:
• Mild to moderate (creatinine clearance 30-80 mL/min): No dose adjustment required.
• Severe (creatinine clearance <30 mL/min): 1 mg once daily recommended.
• Hepatic Impairment:
• Mild to moderate: No dose adjustment necessary.
• Severe: Use with caution; limited data.
• Pediatric Patients:
• Safety and efficacy not established; use not recommended.
• Administration:
• Oral tablet; may be taken with or without food at the same time daily.

Prucalopride is a selective, high-affinity serotonin 5-HT4 receptor agonist. It stimulates 5-HT4 receptors on the enteric neurons in the gastrointestinal tract, enhancing peristaltic reflexes and colonic mass movements. This action accelerates colonic transit and facilitates bowel evacuation, thereby relieving symptoms of chronic constipation.

• Absorption: Rapid and almost complete absorption after oral administration; peak plasma concentration achieved in approximately 2 hours.
• Bioavailability: Approximately 90%.
• Distribution: Volume of distribution approximately 567 liters; plasma protein binding approximately 50%.
• Metabolism: Minor metabolism via CYP3A4, CYP2D6, and CYP2C19 enzymes; majority excreted unchanged.
• Elimination: Primarily renal (60-70% unchanged in urine).
• Half-life: Approximately 24 hours.
• Onset of action: Therapeutic effects typically observed within 24 to 72 hours of initiation.

• Pregnancy: Classified as FDA Pregnancy Category C. Animal studies have indicated adverse effects at high doses, but human data are insufficient. Use only if potential benefits justify the risk.
• Lactation: Unknown if excreted in human milk. Breastfeeding should be avoided or discontinued during treatment unless benefits outweigh risks.

• Primary class: Prokinetic agent
• Subclass: Selective serotonin (5-HT4) receptor agonist

• Hypersensitivity to prucalopride or any component of the formulation.
• Severe renal impairment without appropriate dose adjustment.
• Mechanical gastrointestinal obstruction, perforation, or severe inflammatory conditions (e.g., Crohn’s disease, ulcerative colitis).
• Severe ileus.

• Use caution in patients with known cardiac conduction disorders or arrhythmias.
• Monitor patients for serotonin syndrome when used concomitantly with other serotonergic drugs.
• Discontinue immediately if signs of bowel obstruction or severe abdominal pain occur.
• Use cautiously in patients with severe hepatic impairment due to limited safety data.
• Neuropsychiatric symptoms such as mood changes and hallucinations have been reported rarely.

• Common: Headache, abdominal pain, nausea, diarrhea, dizziness.
• Less common: Fatigue, flatulence, vomiting, mood alterations.
• Rare but serious: Cardiac arrhythmias, hypersensitivity reactions (rash, angioedema).
• Most side effects are mild to moderate and tend to resolve with continued therapy.

• CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase prucalopride plasma levels, but no significant clinical effect observed.
• Risk of serotonin syndrome when combined with other serotonergic agents (SSRIs, SNRIs, triptans).
• Caution with other drugs affecting gastrointestinal motility.
• No significant interaction with food or alcohol reported.

• Current constipation management guidelines recommend prucalopride as a second-line treatment after failure of traditional laxatives.
• Safety profile remains favorable with no new major warnings from regulatory agencies.
• Extended use beyond 12 weeks is considered acceptable under specialist supervision.
• Emphasis on cardiac monitoring in predisposed patients as per recent safety advisories.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in original packaging until use.
• No refrigeration needed.
• Keep out of reach of children.