Cisapride
From Wikipedia, the free encyclopedia
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Cisapride
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| 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. weight | 465.945 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ~100% |
| 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 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In many countries it has been either withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias, about which the FDA issued a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]
[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
