Cisapride

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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.

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In many countries it has been either withdrawn or had its indications limited because of reports of the side-effect long QT syndrome which predisposes to arrhythmias.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

[edit] Veterinary Uses

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

[edit] 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

v • d • e Drugs for functional gastrointestinal disorders (A03) Drugs for functional bowel disorders antimuscarinics: Mebeverine - Dicycloverine - Propantheline papaverine and derivatives: Papaverine - Drotaverine - Moxaverine acting on serotonin receptors: 5-HT3 antagonists (Alosetron, Cilansetron) - 5HT4 agonists (Mosapride, Tegaserod) other: Diisopromine - Isometheptene - Phloroglucinol - Proglumide - Tridihexethyl Belladonna and derivatives (antimuscarinics) Atropine - Hyoscyamine - Butylscopolamine - Methylscopolamine - Scopolamine - Tincture of Belladonna Propulsives primarily dopamine antagonists (Metoclopramide/Bromopride, Domperidone, Alizapride) - serotonin agonists (Cisapride) - Clebopride