| ndication | For the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. |
| Pharmacodynamics | 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. Cisapride stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Cisapride increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Cisapride does not induce muscarinic or nicotinic receptor stimulation, nor does it inhibit acetylcholinesterase activity. |
| Mechanism of action | 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. |
| Absorption | Cisapride is rapidly absorbed after oral administration, with an absolute bioavailability of 35-40%. |
| Volume of distribution | Not Available |
| Protein binding | 97.5% |
| Metabolism | Hepatic. Extensively metabolized via cytochrome P450 3A4 enzyme. |
| Route of elimination | Not Available |
| Half life | 6-12 hours |
| Clearance | Not Available |
| Toxicity | Not Available |