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Cisapride: Wikis

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Cisapride
Systematic (IUPAC) name
4-amino-5-chloro-N-((3S,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl)-2-methoxybenzamide
Identifiers
CAS number 81098-60-4
ATC code A03FA02
PubChem 2769
DrugBank APRD00454
ChemSpider 2667
Chemical data
Formula C23H29ClFN3O4 
Mol. mass 465.945 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 30-40%
Protein binding 97.5%
Metabolism hepatic, intestinal
Half life 10 hours
Excretion renal, biliary
Therapeutic considerations
Pregnancy cat. B1 (Australia)
Legal status Schedule 4 (Australia)
Routes tablets, suspension
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Cisapride is a parasympathomimetic and gastroprokinetic agent that acts as a serotonin 5-HT4 receptor agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It has been sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the U.S.). It was discovered by Janssen Pharmaceutica in 1980. In many countries it has been either withdrawn from the market or had its indications limited because of side effects.

Contents

Clinical uses

Cisapride increases muscle tone in the esophageal sphincter in people with gastroesophageal reflux disease. It also increases gastric emptying in people with diabetic gastroparesis. It has been used to treat bowel constipation.

In many countries it has been either withdrawn or had its indications limited because of reports of the side-effect long QT syndrome which predisposes to arrhythmias. The U.S. Food and Drug Administration (FDA) issued a warning letter to doctors,[1] and Cisapride (Propulsid) was voluntarily removed from the U.S. market on July 14, 2000.

Veterinary uses

Cisapride is still available in the United States for use in animals and is commonly prescribed by veterinarians to treat megacolon in cats.

See also

References

Sources

  • Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
  • Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
  • Medline Plus
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