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Cinitapride | CAS No: 66564-14-5 | GMP-certified suppliers
A medication that treats gastrointestinal motility disorders by improving gastric emptying and alleviating symptoms of GERD, non-ulcer dyspepsia, and delayed gastric emptying.
Therapeutic categories
Primary indications
- It is indicated to treat gastrointestinal disorders associated with motility disturbances like gastroesophageal reflux disease (GERD), non-ulcer dyspepsia and delayed gastric emptying
Product Snapshot
- Cinitapride is an oral small molecule formulation available in tablets, solutions, granules, chewable tablets, and suspensions
- It is primarily intended for the treatment of gastrointestinal motility disorders such as gastroesophageal reflux disease, non-ulcer dyspepsia, and delayed gastric emptying
- Cinitapride is currently in the investigational stage and has not received regulatory approval
Clinical Overview
Clinically, cinitapride is indicated for the management of gastrointestinal motility disorders, including gastroesophageal reflux disease (GERD), non-ulcer dyspepsia, and delayed gastric emptying. Its pharmacological activity facilitates gastrointestinal motility and accelerates gastric emptying, contributing to symptomatic relief in these conditions.
The mechanism of action is primarily mediated via modulation of serotonin receptors in the gastrointestinal tract. Stimulation of 5-HT4 receptors enhances acetylcholine release, promoting peristalsis and gastric emptying. Concurrent 5-HT2 antagonism may reduce visceral sensitivity and support ulcer healing. The agonist activity at 5-HT1 receptors could further influence motility regulation, although detailed pharmacodynamics data remain unspecified.
Key absorption, distribution, metabolism, and excretion (ADME) parameters for cinitapride are not comprehensively documented in this context. However, as a centrally active agent with serotonergic modulation, attention to systemic exposure and blood-brain barrier penetration may be pertinent.
Safety considerations include the theoretical risk of serotonin syndrome owing to serotonergic receptor interactions. Monitoring for adverse effects related to excessive serotonergic activity or hypersensitivity reactions should be integrated into clinical use protocols.
Cinitapride is currently marketed in select regions, including Spain and Mexico, and remains investigational in other territories. Notable brands are region-specific, with limited global availability.
For API sourcing and procurement, cinitapride's nitrophenyl ether structure necessitates stringent quality control measures to ensure purity, as residual nitroaromatic compounds may pose toxicity risks. Compliance with pharmacopeial standards and supplier qualification protocols is essential to maintain consistent API quality for formulation and regulatory purposes.
Identification & chemistry
| Generic name | Cinitapride |
|---|---|
| Molecule type | Small molecule |
| CAS | 66564-14-5 |
| UNII | R8I97I2L24 |
| DrugBank ID | DB08810 |
Pharmacology
| Summary | Cinitapride is a substituted benzamide that modulates gastrointestinal motility through mixed agonist and antagonist activity at 5-HT1A, 5-HT2A, and 5-HT4 receptors. Its pharmacological action targets serotonergic pathways involved in the regulation of gastric emptying and esophageal motility. This activity supports its use in managing motility-related gastrointestinal disorders such as GERD, non-ulcer dyspepsia, and delayed gastric emptying. |
|---|---|
| Mechanism of action | Cinitapride is a substituted benzamide with 5-HT receptor antagonist and agonist activity. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 1A | Humans | agonist |
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
| 5-hydroxytryptamine receptor 4 | Humans | agonist |
ADME / PK
| Absorption | The absorption of cinitapride (12mg) following oral administration was rapid, with peak levels being achieved 2 h after dosing; absorption following intramuscular administration (4mg) was even more rapid, with peak levels (50% more that oral levels) being achieved 1 h after dosing. |
|---|---|
| Half-life | 3-5 h during the first 8 h and a residual half-life greater than 15 h thereafter. |
Formulation & handling
- Cinitapride is a small molecule intended for oral administration, commonly formulated as tablets, granules, or solutions.
- Its low water solubility (1.41e-02 g/L) and moderate LogP (2.79) suggest consideration for solubility enhancement and suitable excipients in formulation.
- As a stable solid aromatic nitrophenyl ether compound, standard handling and storage conditions apply without special sensitivity.
Regulatory status
Safety
| Toxicity | The symptoms of overdose include drowsiness, confusion and extrapyramidal effects. |
|---|
- Overdose may result in central nervous system depression manifested by drowsiness and confusion
- Extrapyramidal symptoms have been reported following excessive exposure
- Use appropriate protective measures to minimize occupational exposure and prevent adverse neurological effects
Cinitapride 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.
Cinitapride (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.
Cinitapride API manufacturers & distributors
Compare qualified Cinitapride API suppliers worldwide. We currently have 4 companies offering Cinitapride 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 |
|---|---|---|---|---|---|
| Chromo Labs. | Producer | India | India | CoA, GMP, WC | 11 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Symed Labs | Producer | India | India | CoA, GMP, WC | 28 products |
When sending a request, specify which Cinitapride 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.).
Use the list above to find high-quality Cinitapride API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
