Cisapride Cas 81098-60-4

Specification

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Cisapride is a gastrointestinal prokinetic agent that was widely used in the 1990s and early 2000s to treat conditions like gastroesophageal reflux disease (GERD), gastroparesis, and functional dyspepsia. However, due to serious safety concerns, its availability has been severely restricted or withdrawn in most countries.

What is Cisapride?

Mechanism of Action: It is a serotonin 5-HT4 receptor agonist. It works by stimulating the release of acetylcholine in the gut's enteric nervous system, which enhances motility (movement) throughout the entire gastrointestinal tract (esophagus, stomach, and intestines).

Original Uses: It was prescribed to accelerate gastric emptying, increase lower esophageal sphincter pressure (to prevent acid reflux), and improve bowel movements.

Historical Selling Points (Before Withdrawal/Restriction)

When Cisapride was on the market, its main advantages over other drugs (like metoclopramide or domperidone) were:

Full Gut Prokinetic: Unlike some agents that only work on the stomach, Cisapride promoted motility from the esophagus down to the colon.

Non-Dopaminergic: It did not block dopamine receptors. This meant it lacked the common neurological side effects associated with dopamine antagonists, such as:

No risk of tardive dyskinesia (involuntary movements).

No elevation of prolactin levels (avoiding issues like gynecomastia or galactorrhea).

Less sedation compared to some alternatives.

High Efficacy: It was considered very effective for severe GERD (especially nocturnal heartburn) and gastroparesis where other treatments failed.

Critical Safety Issues & Current Status (2026)

Cisapride is no longer freely available for general prescription in most of the world (including the US, EU, and China) due to life-threatening cardiac side effects.

The Problem: Cisapride blocks the hERG potassium channel in the heart. This can lead to QT interval prolongation, a dangerous electrical disturbance that can cause a fatal arrhythmia known as Torsades de Pointes.

Drug Interactions: The risk was significantly heightened when taken with common medications that inhibit the CYP3A4 enzyme (e.g., certain antibiotics like erythromycin, antifungals like ketoconazole, and even grapefruit juice), leading to toxic levels of Cisapride in the blood.

Current Availability (2026):

Restricted Access: In many regions, it is completely withdrawn. In some specific jurisdictions, it may be available only under a highly restricted "compassionate use" or investigational program for patients with severe, life-threatening motility disorders who have failed all other therapies.

Research Use: It is currently primarily sold as a chemical reagent for scientific research (e.g., studying 5-HT4 receptors or hERG channels) and is explicitly labeled "Not for human use."

Alternatives: Safer prokinetics like Mosapride or Prucalopride (which are more selective 5-HT4 agonists with less cardiac risk) are generally used instead.

Summary: While Cisapride was once a "wonder drug" for gut motility due to its potency and lack of neurological side effects, its potential to cause fatal heart arrhythmias led to its removal from the general market. Today, it is essentially a historical drug or a research chemical, not a standard treatment option.

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