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Prucalopride Succinate: Pharmacodynamics, Pharmacokinetic Properties and Adverse Effects

Nov 8，2024

Prucalopride Succinate is a serotonin-4 (5-HT4) receptor agonist indicated for the treatment of chronic idiopathic constipation (CIC) in adults.

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Pharmacodynamics

Prucalopride Succinate is a selective, high affinity serotonin (5-HT4) receptor agonist with enterokinetic activities. Prucalopride Succinate alters colonic motility patterns via serotonin 5-HT4 receptor stimulation: it stimulates colonic mass movements, which provide the main propulsive force for defecation.

Pharmacokinetic Properties

Prucalopride is rapidly absorbed (Cmax attained 2–3 hours after single 2 mg oral dose) and is extensively distributed. Metabolism is not the major route of elimination. In vitro, human liver metabolism is very slow and only minor amounts of metabolites are found. A large fraction of the active substance is excreted unchanged (about 60% of the administered dose in urine and at least 6% in feces). Renal excretion of unchanged prucalopride involves both passive filtration and active secretion. Plasma clearance averages 317 ml/min, terminal half-life is 24–30 hours, and steady-state is reached within 3–4 days.

Adverse Effects

The most frequently reported side effects of Prucalopride succinate are headache and gastrointestinal symptoms (abdominal pain, nausea or diarrhea). Such reactions occur predominantly at the start of therapy and usually disappear within a few days with continued treatment.

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