Cisapride
Substituted piperidinyl benzamide
Also known as: Propulsid · cisapridum · R-51619
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Audited v13 dosing evidence
Structured calculator evidenceGastrointestinal stasis after obstruction has been excluded
- q8–12h
Governing clinical context (2)
- Exclude emergent diagnoses (obstruction, enterotoxemia)
- Prokinetic agent (after excluding the possibility of obstruction)
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Cisapride is a potent gastrointestinal prokinetic agent used primarily in veterinary medicine to manage conditions like feline megacolon, gastric stasis, and reflux esophagitis.
Clinical Pearl: Due to severe cardiac arrhythmias (QT prolongation) in humans, cisapride was voluntarily removed from the human market. It is now exclusively available for veterinary patients through compounding pharmacies. Despite the cardiac risks in humans, it is generally very well tolerated in dogs and cats.
It is highly effective at stimulating motility from the esophagus down to the colon, making it a cornerstone therapy for chronic constipation in felines.
Mechanism of action
Cisapride acts primarily as a serotonin 5-HT4 receptor agonist in the gastrointestinal tract.
- 5-HT4 activation → stimulates the release of acetylcholine at the myenteric plexus.
- This increases lower esophageal sphincter pressure, enhances esophageal peristalsis, and accelerates gastric emptying and colonic motility.
- Unlike metoclopramide, it has minimal dopamine receptor blockade (no extrapyramidal effects) and does not stimulate gastric acid secretion.
- Acetylcholinesterase activity is not inhibited.
Safety & warnings
Contraindications
- Gastrointestinal perforation
- Gastrointestinal obstruction
- Gastrointestinal hemorrhage
- Hypersensitivity to cisapride
Adverse effects
- Vomiting
- Diarrhea
- Abdominal discomfort
- Prolonged QT intervals or cardiac arrhythmias (very rare in veterinary patients)
Precautions
Use with caution in pregnant or nursing animals; high doses caused embryotoxicity and fetotoxicity in lab animals. Dosage may need to be decreased in patients with severe hepatic impairment. Avoid concurrent use with CYP3A4 inhibitors or QT-prolonging drugs due to the risk of severe cardiac arrhythmias.
Drug interactions
May diminish the prokinetic effects of cisapride.
Cisapride may enhance the sedative effects of benzodiazepines.
Cisapride may enhance anticoagulant effects; additional monitoring and dosage adjustments may be required.
Cisapride decreases GI transit times, potentially altering the absorption of other oral drugs. Serum levels may need closer monitoring.
Inhibit cisapride metabolism, leading to increased cisapride levels and an increased risk for cisapride cardiotoxicity.
May increase the risk of QT interval prolongation and fatal arrhythmias when used concurrently with cisapride.
Monitoring
- Efficacy (resolution of GI stasis, constipation, regurgitation)
- Adverse effects profile (GI upset, signs of arrhythmias)
Pharmacokinetics
Absorption
After oral administration, cisapride is rapidly absorbed with an absolute bioavailability of 35-40% (human data).
Distribution
Highly bound to plasma proteins and apparently extensively distributed throughout the body.
Metabolism
Extensively metabolized via cytochrome P450 (CYP3A4 in humans).
Elimination
Elimination half-life is about 8-10 hours (human data).
Overdose
LD50 doses in various lab animals range from 160 - 4000 mg/kg. The reported oral lethal dose in dogs is 640 mg/kg.
Clinical Signs: Most common adverse effects seen in dogs and cats are diarrhea, lethargy, ataxia, hypersalivation, muscle fasciculations, agitation, abnormal behavior, hyperthermia, and possibly seizures (dogs).
Treatment: Significant overdoses should be handled using standard gut emptying protocols when appropriate. Supportive therapy should be initiated when required. Activated charcoal is effective in binding unabsorbed cisapride.
Available products
Formulations
- Compounded oral suspension
- Compounded capsules
- Compounded tablets
Veterinary
- None commercially available (Must be compounded)
Human-labeled
- None (Removed from US market due to adverse cardiac effects)
Regulatory status
No regulatory data for: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Store cisapride tablets in tight, light-resistant containers at room temperature. Compounded oral suspensions (e.g., 1 mg/mL in Ora-Plus/Ora-Sweet) retain >90% potency for 60 days stored at both 5°C and 25°C. Compounded preparations should be protected from light.
Client information
- Administration: Give exactly as prescribed, ideally 15 to 30 minutes before a meal for maximum effectiveness.
- Sourcing: This medication is no longer commercially manufactured and must be specially made by a veterinary compounding pharmacy.
- Side Effects: Generally very safe for pets. Watch for mild stomach upset, vomiting, or diarrhea. Report any unusual lethargy or abnormal behavior to your veterinarian.
- Interactions: Inform your vet about all medications and supplements your pet is taking, as cisapride has many significant drug interactions that can be dangerous.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.
