Prucalopride (Brand Name Resolor)

Prucalopride Basic Facts:

• Brand name Resolor - developed by Movetis.
• New drug for treatment of constipation.
• Acts as a selective, high affinity 5-HT4 receptor agonist.
• Targets the impaired motility associated with chronic constipation - leading to a normalisation of bowel movements.
• Indicated for symptomatic treatment of chronic constipation in women in whom laxatives fail to provide adequate relief.
• Median time to the first spontaneous bowel movement is 2 1/2 hours.

Actions:

• First in class dihydrobenzofurancarboxamide.
• Selective, high affinity serotonin (5-HT4) receptor agonist.
• Prucalopride alters colonic motility patterns via serotonin 5-HT4 receptor stimulation.
• The 5-HT4 receptor stimulation induces colonic mass movements.
• Prucalopride has >150-fold higher affinity for 5-HT4 receptors than for other receptors - differentiating it from tegaserod & cisapride.

Pharmacokinetics:

• Prucalopride is rapidly absorbed & extensively distributed.
• Elimination is mainly unchanged in the urine.
• The renal excretion of unchanged prucalopride involves both passive filtration & also active secretion.
• Plasma clearance averages 317 ml/min.
• Terminal half-life is 24–30 hours.
• Steady-state drug concentrations are reached within 3–4 days.

Dosing:

• 2 mg once daily.
• Exceeding the daily dose of 2 mg is not expected to increase efficacy.

Drug Interactions:

• Low interaction potential.
• Therapeutic concentrations of prucalopride do not affect the CYP-mediated metabolism of drugs.

Side Effects:

• Most common are headache & gastrointestinal symptoms.
• GI symptoms - Abdominal pain, diarrhoea, nausea - about 20% patients.
• These effects occur mostly at the start of therapy and tend to disappear within a few days.
• Prucalopride has no significant effect on QT interval.

Tags: 5-HT4 receptor antagonist - Constipation - Prucalopride - Resolor - Serotonin
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