Definition
A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed)
Description
In many countries (including Canada) cisapride has been either withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias. The FDA issued a warning letter regarding this risk to health care professionals and patients.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Extensively metabolized via cytochrome P450 3A4 enzyme. Half Life: 6-12 hours
- Uses/Sources: For the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease.
- Symptoms: Diarrhea, upset stomach, stomach discomfort, vision changes, constipation.
- Treatment: In instances of overdose, patients should be evaluated for possible QT prolongation and ventricular arrhythmias, including torsades de pointes. Treatment should include gastric lavage and/or activated charcoal, close observation and general supportive measures. (L1712)
- Route of Exposure: Cisapride is rapidly absorbed after oral administration, with an absolute bioavailability of 35-40%.
Mechanism of Action
| Target Name | Mechanism of Action | References |
|---|---|---|
|
5-hydroxytryptamine receptor 2C 5-hydroxytryptamine receptor 2B D(2) dopamine receptor D(1A) dopamine receptor Beta-1 adrenergic receptor Serotonin Receptors Ubiquitin-conjugating enzyme E2 N |
8632342 12540230 17145705 16451077 |
|
|
Potassium voltage-gated channel subfamily H member 2 5-hydroxytryptamine receptor 2A 5-hydroxytryptamine receptor 4 5-hydroxytryptamine receptor 3A |
Cisapride acts through the stimulation of the serotonin 5-HT4 receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric (especially antral) contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. |
1600046 18448342 19260734 15911273 10027842 10510456 12190308 8632342 11752352 10556228 19110341 15967876 8423526 9374794 12388285 8093733 12873512 10328995 12593651 11034583 11131599 11218067 15272206 12729675 12209010 11005845 9697104 12747773 1969947 17408310 15745831 |
Cisapride Interacts with Diseases
| Disease | Inference Score | References/Inference Genes |
| Torsades de pointes | 8.66 |
|
| Cardiomyopathy, Dilated, 1E | 6.64 |
|
| Long Qt Syndrome 3 | 6.64 |
|
| Long QT syndrome type 3 | 6.64 |
|
| Sick Sinus Syndrome 1, Autosomal Recessive | 6.64 |
|
| Paroxysmal ventricular fibrillation | 6.29 |
|
| PROGRESSIVE FAMILIAL HEART BLOCK, TYPE IA | 6.29 |
|
| Atrial fibrillation | 6.2 |
|
| Short QT Syndrome 1 | 6.01 |
|
| CHOLESTASIS, BENIGN RECURRENT INTRAHEPATIC, 2 | 5.92 |
|
| Long QT Syndrome | 5.85 |
|
| Adrenal Hyperplasia, Congenital | 5.36 |
|
| Long Qt Syndrome 2 | 5.32 |
|
| Sudden Infant Death | 5.32 |
|
| Brugada syndrome | 5.26 |
|
| Cholestasis, progressive familial intrahepatic 1 | 5.23 |
|
| Coumarin Resistance | 5.22 |
|
| Afibrinogenemia | 5.12 |
|
| Peptic Ulcer Hemorrhage | 4.94 |
|
| Cardiac arrhythmia | 4.81 |
|