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Cisapride | CAS No: 81098-60-4 | GMP-certified suppliers
A medication that provides symptomatic relief of nocturnal heartburn in adults with gastroesophageal reflux disease, enhancing gastrointestinal motility and gastric emptying.
Therapeutic categories
Primary indications
- For the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease
Product Snapshot
- Cisapride is an oral small molecule available in multiple tablet and suspension formulations including delayed release and orally disintegrating forms
- It is primarily indicated for symptomatic treatment of nocturnal heartburn associated with gastroesophageal reflux disease in adults
- The product holds regulatory approval in Canada and the US, with variable status including approved, investigational, and withdrawn in certain contexts
Clinical Overview
Pharmacodynamically, cisapride functions as a serotonin 5-HT4 receptor agonist. Activation of these receptors in the enteric nervous system stimulates acetylcholine release within the myenteric plexus, enhancing gastrointestinal motility. This increased cholinergic activity results in augmented tone and amplitude of gastric contractions, particularly antral contractions, relaxation of the pyloric sphincter and duodenal bulb, and accelerated peristalsis in the duodenum and jejunum. These effects collectively promote accelerated gastric emptying and intestinal transit. Cisapride also increases lower esophageal sphincter resting pressure, contributing to its therapeutic role in GERD. Notably, it does not affect muscarinic or nicotinic receptors nor inhibit acetylcholinesterase, and it lacks significant effects on colonic or gallbladder motility.
Metabolically, cisapride is a known substrate of multiple cytochrome P450 enzymes, including CYP3A4, CYP2C19, CYP2D6, CYP2C8, CYP2B6, and CYP2A6. This extensive metabolism contributes to potential drug-drug interactions. Its pharmacokinetic profile includes metabolism predominantly via hepatic pathways.
Cisapride’s safety profile has been significantly impacted by its association with QT interval prolongation and the risk of torsades de pointes and other serious arrhythmias. Due to these cardiac safety concerns, many regulatory authorities, including the FDA and Health Canada, have restricted its use or withdrawn the drug from the market. A warning regarding this risk has been widely disseminated to healthcare professionals and patients. These safety considerations limit its current clinical use and necessitate stringent cardiac monitoring if used.
Given the safety and regulatory status, sourcing cisapride as an active pharmaceutical ingredient requires rigorous quality control, including confirmation of identity, purity, absence of genotoxic impurities, and stability. Compliance with regulatory standards for QT-prolonging agents and comprehensive documentation to support controlled distribution and use are critical for API procurement.
Identification & chemistry
| Generic name | Cisapride |
|---|---|
| Molecule type | Small molecule |
| CAS | 81098-60-4 |
| UNII | UVL329170W |
| DrugBank ID | DB00604 |
Pharmacology
| Summary | Cisapride is a serotonin 5-HT4 receptor agonist that enhances acetylcholine release in the enteric nervous system, promoting motility in the upper gastrointestinal tract. It increases gastric contractility and relaxes sphincters to accelerate gastric emptying and intestinal transit. Cisapride primarily targets 5-HT4 receptors with additional activity at 5-HT3A, 5-HT2A receptors, and potassium channels, without significant effects on muscarinic or nicotinic receptors. |
|---|---|
| Mechanism of action | Cisapride acts through the stimulation of the serotonin 5-HT<sub>4</sub> receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric (especially antral) contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. |
| Pharmacodynamics | Cisapride is a parasympathomimetic which acts as a serotonin 5-HT<sub>4</sub> agonist; upon activation of the receptor signaling pathway, cisapride promotes the release of acetylcholine neurotransmitters in the enteric nervous system. Cisapride stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Cisapride increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Cisapride does not induce muscarinic or nicotinic receptor stimulation, nor does it inhibit acetylcholinesterase activity. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 4 | Humans | agonist |
| 5-hydroxytryptamine receptor 3A | Humans | agonist |
| 5-hydroxytryptamine receptor 2A | Humans | agonist |
ADME / PK
| Absorption | Cisapride is rapidly absorbed after oral administration, with an absolute bioavailability of 35-40%. |
|---|---|
| Half-life | 6-12 hours |
| Protein binding | 97.5% |
| Metabolism | Hepatic. Extensively metabolized via cytochrome P450 3A4 enzyme. |
Formulation & handling
- Cisapride is a small molecule API formulated exclusively for oral administration in multiple dosage forms including tablets, suspensions, and granules.
- The compound exhibits low water solubility and moderate lipophilicity (LogP 2.49), which should be considered during formulation to optimize bioavailability.
- Avoid co-administration with grapefruit products and St. John's Wort, and administer at least 15 minutes before meals to mitigate food-drug interaction risks.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient patents expired in the United States as of July 15, 2014, allowing for generic versions in the US and Canadian markets. The API is currently in a mature market phase with established availability in both countries. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Cisapride is manufactured and packaged by a limited number of originator companies, primarily under Janssen-affiliated entities. Its branded products are present predominantly in the US and Canadian markets. The primary US patent expired in 2014, indicating that generic competition is currently established or likely to be present. |
|---|
Cisapride is a type of Prokinetics
Prokinetics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of gastrointestinal (GI) disorders. These medications are designed to enhance the motility of the GI tract, specifically the muscles involved in digestion and the movement of food.
Prokinetics work by stimulating the release of acetylcholine, a neurotransmitter that promotes muscle contractions. By increasing the muscular contractions, prokinetics accelerate the movement of food through the GI tract, facilitating efficient digestion and absorption of nutrients. This can be beneficial in conditions such as gastroesophageal reflux disease (GERD), gastroparesis, and functional dyspepsia.
One common prokinetic API is metoclopramide, which acts by blocking dopamine receptors in the brain and enhancing motility in the upper GI tract. Another widely used prokinetic is domperidone, which primarily works by blocking dopamine receptors in the gut. These medications are available in various formulations, including tablets, capsules, and suspensions.
Prokinetics can offer relief to patients suffering from GI disorders by alleviating symptoms like nausea, vomiting, bloating, and heartburn. However, it is important to note that these medications should be used under the guidance of healthcare professionals, as they may have potential side effects and drug interactions.
In conclusion, prokinetics are a valuable subcategory of pharmaceutical APIs used in the treatment of GI disorders. By enhancing GI motility, these medications promote proper digestion and provide relief from symptoms associated with impaired gut function. Consultation with a healthcare provider is essential to ensure safe and effective use of prokinetics.
Cisapride (Prokinetics), classified under Gastrointestinal Agents
Gastrointestinal Agents belong to the pharmaceutical API category that focuses on treating disorders and ailments related to the digestive system. These agents play a crucial role in addressing various gastrointestinal conditions, such as acid reflux, ulcers, irritable bowel syndrome (IBS), and inflammatory bowel disease (IBD).
One of the key types of gastrointestinal agents is proton pump inhibitors (PPIs), which work by reducing the production of stomach acid. PPIs help in treating conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. Another essential class of agents is antacids, which neutralize excessive stomach acid, providing relief from heartburn and indigestion.
Gastrointestinal agents also include antispasmodics that alleviate abdominal cramps and spasms associated with conditions like IBS. These drugs work by relaxing the smooth muscles of the digestive tract. Additionally, there are drugs categorized as laxatives that aid in relieving constipation by promoting bowel movements.
Moreover, certain gastrointestinal agents act as antiemetics, effectively reducing nausea and vomiting. These drugs are particularly useful for patients undergoing chemotherapy or experiencing motion sickness.
Pharmaceutical companies develop and manufacture a wide range of gastrointestinal agents in various forms, including tablets, capsules, suspensions, and injections. These agents are typically formulated using active pharmaceutical ingredients (APIs) and other excipients to ensure their efficacy and safety.
In conclusion, gastrointestinal agents form a vital category of pharmaceutical APIs, providing relief from digestive disorders and improving overall gastrointestinal health. The availability of diverse agents catering to different conditions ensures that patients can receive targeted treatment for their specific gastrointestinal needs.
Cisapride API manufacturers & distributors
Compare qualified Cisapride API suppliers worldwide. We currently have 1 companies offering Cisapride API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Janssen Pharma | Producer | Belgium | Unknown | CoA, USDMF | 63 products |
When sending a request, specify which Cisapride API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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