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Cisapride



Cisapride
Systematic (IUPAC) name
4-amino-5-chloro-N- [1-[3-(4-fluorophenoxy)propyl]- 3-methoxy-4-piperidyl]-2-methoxy- benzamide
Identifiers
CAS number 81098-60-4
ATC code A03FA02
PubChem 2769
DrugBank APRD00454
Chemical data
Formula C23H29ClFN3O4 
Mol. mass 465.945 g/mol
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

Cisapride is a parasympathomimetic which acts as a serotonin 5-HT4 receptor agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It is sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the U.S.). It was discovered by Janssen Pharmaceutica in 1980.

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In many countries it has been either withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias, about which the FDA issued a warning letter to health care professionals and patients. [1]

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

Cisapride (Propulsid)was in fact voluntarily removed from the U.S. market as of July 14, 2000.

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Cisapride". A list of authors is available in Wikipedia.
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