Cisapride
- Atc Codes:A03FA02
- CAS Codes:81098-60-4
- PHARMGKB ID:81098-60-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Prepulsid; France: Prepulsid; Greece: Systilan; Luxembourg: Cyprid, Prepulsid; Netherlands: Prepulsid; Poland: Coordinax, Gasprid; Portugal: Prepulsid.
North America
USA: Propulsid.
Latin America
Argentina: Pulsar; Brazil: Prepulsid; Mexico: Aposada, Cepriser, Cisaprida, Enteropride, Expril, Kinestase, Maprilex, Mavisid, Nodrix, Presistin, Prixin, Profercol, Sapriken, Unamol.
Drug combinations
Chemistry
Cisapride: C~23~H~29~ClFN~3~O~4~. Mw: 465.95. (1) Benzamide, 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-, cis-; (2) cis-4-Amino-5-chloro-N-[1-[3-(p-fluorophenoxy)propyl]-3-methoxy-4-piperidyl]-o-anisamide. CAS-81098-60-4 (1983).
Pharmacologic Category
Gastrointestinal Drugs; Prokinetic Agents. (ATC-Code: A03FA02).
Mechanism of action
Enhances the release of acetylcholine at the myenteric plexus. It increases lower esophageal sphincter pressure, increases the amplitude of peristalsis, accelerates gastric emptying, improves antroduodenal coordination, increases colonic motility, and enhances cecal and ascending colonic emptying. Cisapride prolongs cardiac repolarization without slowing conduction by selectively blocking the rapid component of the delayed rectifying potassium current, which leads to a lengthening of the action potential (QT syndrome).
Therapeutic use
Nocturnal symptoms of gastroesophageal reflux disease. Gastroparesis. Refractory constipation. Nonulcer dyspepsia.
Pregnancy and lactiation implications
Embryotoxic and fetotoxic in rats and rabbits when given at high dosages. Should be used during pregnancy only when the potential benefits justify the possible risks to the fetus. Distributed into human milk (should be used with caution in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to cisapride or any component of the formulation. Gastrointestinal hemorrhage, mechanical obstruction, gastrointestinal perforation, or other situations when gastrointestinal motility stimulation is dangerous. Concomitant oral or I.V. administration of antibiotics such as erythromycin, clarithromycin, troleandomycin, antidepressants such as nefazodone, antifungals such as fluconazole, itraconazole, miconazole, oral ketoconazole, or protease inhibitors such as indinavir, ritonavir, amprenavir, atazanavir. Prolonged QT intervals (QTc >450 ms), history of QTc prolongation, or known family history of congenital long QT syndrome, clinically significant bradycardia, renal failure, history of ventricular arrhythmias, ischemic heart disease, congestive heart failure, uncorrected electrolyte disorders (hypokalemia, hypomagnesemia), respiratory failure, and concomitant medications known to prolong QT interval and increase the risk of arrhythmia. Cisapride should not be used in patients with uncorrected hypokalemia or hypomagnesemia or who might experience rapid reduction of plasma potassium. Should not be co-administered with grapefruit juice.
Warnings and precautions
Serious cardiac arrhythmias including ventricular tachycardia, ventricular fibrillation, torsade de pointes, and QT prolongation reported. Should not be used in patients with uncorrected hypokalemia or hypomagnesemia, such as those with severe dehydration, vomiting or malnutrition, or those taking potassium-wasting diuretics. Should also not be used in patients who might experience rapid reduction of plasma potassium, such as those administered potassium-wasting diuretics and/or insulin in acute settings.