Prucalopride
- Atc Codes:A03AE04
- CAS Codes:179474-85-2
- PHARMGKB ID:179474-85-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Resolor; Belgium: Resolor; Estonia: Resolor; Germany: Resolor; Greece: Resolor; Ireland: Resolor; Latvia: Resolor; Lithuania: Resolor; Luxembourg: Resolor; Malta: Resolor; Netherlands: Resolor; Poland: Resolor; Portugal: Resolor; Romania: Resolor; Slovakia: Resolor; Slovenia: Resolor; Sweden: Resolor; UK: Resolor.
Drug combinations
Chemistry
Prucalopride Succinate: C~22~H~32~ClN~3~O~7~. Mw: 485.96. 4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide; butanedioic acid. CAS-179474-85-2.
Pharmacologic Category
Gastrointestinal Drugs; Prokinetic Agents; Selective Serotonin (5-HT~4~) Receptor Agonist. (ATC-Code: A03AE04).
Mechanism of action
Prucalopride is a selective, high-affinity serotonin (5-HT~4~) receptor agonist; this may explain its enterokinetic effects. Affinity for other receptors was detected in vitro only at concentrations exceeding its 5-HT~4~-receptor affinity by at least 150-fold. Prucalopride in vivo at doses above 5 mg/kg induced hyperprolactinemia in rats caused by an antagonistic action at the D~2~ receptor. In dogs, prucalopride alters colonic motility patterns via serotonin 5-HT~4~ receptor stimulation: it stimulates proximal colonic motility, enhances gastroduodenal motility and accelerates delayed gastric emptying. Furthermore, giant migrating contractions are induced by prucalopride. These are equivalent to the colonic mass movements in humans, and provide the main propulsive force to defecation. In dogs, the effects observed in the gastrointestinal tract are sensitive to blockade with selective 5-HT~4~ receptor antagonists, illustrating that the observed effects are exerted via selective action on 5-HT~4~ receptors.
Therapeutic use
Indicated for symptomatic treatment of chronic constipation in women in whom laxatives fail to provide adequate relief.
Pregnancy and lactiation implications
Cases of spontaneous abortion have been observed during clinical studies, although in the presence of other risk factors; the relationship to prucalopride is unknown. Not recommended during pregnancy or lactation.
Unlabeled use
Contraindications
Hypersensitivity to the active substance or to any of the excipients. Renal impairment requiring dialysis. Intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the intestinal tract, such as Crohn’s disease, and ulcerative colitis and toxic megacolon/megarectum.
Warnings and precautions
Caution in patients with severe and clinically unstable concomitant disease (e.g. liver, cardiovascular or lung disease, neurological or psychiatric disorders, cancer or AIDS and other endocrine disorders). In particular, should be used with caution in patients with history of arrhythmias or ischemic cardiovascular disease. In case of severe diarrhea, the efficacy of oral contraceptives may be reduced and the use of an additional contraceptive method is recommended to prevent possible failure of oral contraception. The tablets contain lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption must not take this medicinal product.