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Chemistry – An oral GI prokinetic agent, cisapride is a substituted piperidinyl benzamide and is structurally, but not pharmacologically, related to procainamide. It is available commercially as a monohydrate, but potency is expressed in terms of the anhydrate.
Storage/Stability/Compatibility – Unless otherwise instructed by the manufacturer, store cisapride tablets in tight, light-resistant containers at room temperature.
Pharmacology – Cisapride increases lower esophageal peristalsis and sphincter pressure and accelerates gastric emptying. The proposed mechanism of action is that it enhances the release of acetylcholine at the myenteric plexus, but does not induce nicotinic or muscarinic receptor stimulation. Acetylcholinesterase activity is not inhibited. Cisapride blocks dopaminergic receptors to a lesser extent than does metoclopramide and does not increase gastric acid secretion.
Uses/Indications – Cisapride is a new agent. Proposed uses for it in small animals include esophageal reflux and treatment of primary gastric stasis disorders.
Pharmacokinetics – Human data: After oral administration, cisapride is rapidly absorbed with an absolute bioavailability of 35-40%. The drug is highly bound to plasma proteins and apparently extensively distributed throughout the body. Cisapride is extensively metabolized and its elimination half life is about 8-10 hours.
Contraindications/Precautions/Reproductive Safety – Cisapride is contraindicated in patients in whom increased gastrointestinal motility could be harmful (e.g., perforation, obstruction, GI hemorrhage) or those who are hypersensitive to the drug.
Cisapride at high dosages (> 40 mg/kg/day) caused fertility impairment in female rats. At doses 12 to 100 times the maximum recommended, cisapride was embryotoxic and fetotoxic in rabbits and rats. Its use during pregnancy should occur only when the benefits outweigh the risks. Cisapride is excreted in maternal milk in low levels; use with caution in nursing mothers.
Adverse Effects/Warnings – Usage in small animal medicine has been limited to this point and an adverse effect profile has not been determined. As expected in humans, the primary adverse effects are gastrointestinal related with diarrhea and abdominal pain most commonly reported.
Dosage may need to be decreased in patients with severe hepatic impairment.
Overdosage/Acute Toxicity – In one reported human overdose of 540 mg, the patient developed GI distress and urinary frequency. LD50 doses in various lab animals range from 160 – 4000 mg/kg. Significant overdoses should be handled using standard gut emptying protocols when appropriate; supportive therapy should be initiated when required.
Drug Interactions – Because cisapride can decrease GI transit times, absorption of other drugs given orally may be affected. Oral drugs with a narrow therapeutic index may need serum levels monitored more closely when adding or discontinuing cisapride. Use of anticholinergic agents may diminish the effects of cisapride. Cimetidine(not ranitidine) may increase cisapride serum levels and cisapride may accelerate cimetidine and ranitidineabsorption thereby enhancing their effects. Cisapride may enhance anticoagulants’ effects; additional monitoring and anticoagulant dosage adjustments may be required. Cisapride may enhance the sedative effects of alcohol or benzodiazepines. Elevated concentrations of cisapride with resultant ventricular arrhythmias may result if coadministered with ketoconazole, itraconazole, IV miconazole or troleandomycin. At present, the manufacturer states that cisapride should not be used with these drugs.
As a promotility agent:
a) Preliminary study: Author states that 0.1 mg/kg was superior to other doses used. No mention of dosage route or frequency was noted. (Roussel 1992)
Monitoring Parameters – Efficacy and adverse effects profile.
Client Information – Because cisapride is a “new” drug, inform client to watch carefully for and report any adverse effects noted.
Dosage Forms/Preparations/FDA Approval Status/Withholding Times –
Veterinary-Approved Products: None
Cisapride Oral Tablets 10 mg & 20 mg; Propulsid® (Janssen); Prepulsid® in Canada, New Zealand, etc. (Rx)
Cisapride Suspension: 1 mg/ml in 450 ml bottles; Propulsid®(Janssen) (Rx)