Cisapride is a gastroprokinetic agent, a drug that increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT₄ receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases ace + some more technical info; mechanistically this promotes acetylcholine release from enteric cholinergic neurons, enhances coordinated peristaltic activity in the esophagus and stomach, increases lower esophageal sphincter tone and accelerates gastric emptying. Cisapride is absorbed orally and undergoes hepatic metabolism predominantly via cytochrome P450 3A4, and clinically relevant effects include QT interval prolongation through hERG channel interaction, which underlies its safety restrictions and drug interaction profile with strong CYP3A4 inhibitors.
Typical active pharmaceutical ingredient control for cisapride includes characterization and limits for process-related and degradation-related impurities; commonly identified related compounds include N-desmethyl cisapride (norcisapride), O-desmethyl and O-dealkylated products, N-oxide derivatives and positional isomers derived from synthetic intermediates. Typical quantitative limits used in specifications are individual identified related impurities controlled at or below 0.10 percent w/w and total impurities controlled at or below 0.50 percent w/w, with any genotoxic or mutagenic impurities held to trace levels consistent with applicable thresholds for toxicological concern, typically below 0.05 percent or as set by regulatory guidance. Residual solvents and elemental impurities are controlled per ICH Q3C and Q3D, respectively, and stability testing defines additional limits for oxidation, hydrolysis and photolytic degradation products.
Cisapride has been restricted or withdrawn in many countries including India because postmarketing data showed a risk of serious cardiac arrhythmias, including QT prolongation and torsades de pointes, particularly when used with CYP3A4 inhibitors or in patients with underlying risk factors. These safety concerns led regulators to remove or severely limit systemic human use to protect public health.
Yes, Cisapride is a prokinetic agent that increases upper gastrointestinal motility by agonism at serotonin 5-HT4 receptors and by enhancing cholinergic neurotransmission in the enteric nervous system.
A well known brand name for cisapride was Propulsid. It is also referred to in some sources as cisapride monohydrate or by chemical synonyms used in regulatory filings.
No, Cisapride and metoclopramide are both used to enhance gastrointestinal motility but they have different primary mechanisms and safety profiles. Cisapride is a 5-HT4 receptor agonist with notable cardiac risk, while metoclopramide acts mainly as a dopamine D2 receptor antagonist and has a higher risk of central nervous system and extrapyramidal adverse effects.
