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Metoclopramide | CAS No: 364-62-5 | GMP-certified suppliers
A medication that provides symptomatic relief for diabetic gastroparesis and gastroesophageal reflux disease, and prevents nausea and vomiting related to chemotherapy, surgery, and diagnostic procedures.
Therapeutic categories
Primary indications
- Metoclopramide in the oral tablet form is used for symptomatic treatment of both acute and recurrent diabetic gastroparesis, in addition to the treatment of gastroesophageal reflux disease (GERD) in patients who have failed to respond to traditional therapy
- A nasal spray formulation is also indicated to treat adults with acute, recurrent diabetic gastroparesis
- In the intravenous injection form, it is indicated for the above conditions as well as for the prevention of vomiting that may follow emetogenic chemotherapy or nausea and vomiting after surgery
Product Snapshot
- Metoclopramide is available in multiple formulation types including oral tablets, nasal spray, and intravenous injection
- It is primarily indicated for the treatment of diabetic gastroparesis, gastroesophageal reflux disease (GERD), prevention of chemotherapy-induced nausea and vomiting, and facilitation of gastric emptying for radiological procedures
- The product is approved for use in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, metoclopramide acts as a dopamine D2 receptor antagonist and serotonin 5-HT3 receptor antagonist within the chemoreceptor trigger zone (CTZ) in the area postrema, mediating its antiemetic effects. It also displays agonism at serotonin 5-HT4 receptors and inhibitory effects on presynaptic and postsynaptic D2 receptors, resulting in enhanced acetylcholine release. This leads to increased lower esophageal sphincter (LES) tone and accelerated gastric emptying without stimulating gastric acid or pancreatic secretions. The net effect is promotion of gastrointestinal motility and facilitation of gastric emptying.
Key absorption, distribution, metabolism, and elimination (ADME) parameters include administration via oral, intravenous, or nasal routes. Metoclopramide is metabolized hepatically, involving cytochrome P450 enzymes including CYP1A2, CYP2D6, and CYP3A4 isoforms, and excreted mainly by the kidneys. It is known to cross the blood-brain barrier, which is relevant to its central nervous system effects.
Safety considerations are critical for metoclopramide due to its antidopaminergic activity in the central nervous system, which can induce adverse reactions such as tardive dyskinesia, dystonia, and akathisia. Regulatory guidelines recommend limiting treatment duration to a maximum of 12 weeks to mitigate these risks. Use in populations susceptible to extrapyramidal symptoms should be carefully monitored.
Metoclopramide is marketed under various brand names globally and remains an essential agent within gastrointestinal and antiemetic therapeutic categories. When sourcing the active pharmaceutical ingredient (API), it is important to obtain material compliant with pharmacopeial standards and GMP guidelines. Attention should be paid to impurity profiles, potential polymorphic forms, and stability to ensure consistent formulation performance and regulatory acceptance.
Identification & chemistry
| Generic name | Metoclopramide |
|---|---|
| Molecule type | Small molecule |
| CAS | 364-62-5 |
| UNII | L4YEB44I46 |
| DrugBank ID | DB01233 |
Pharmacology
| Summary | Metoclopramide exerts therapeutic effects primarily through dopamine D2 receptor antagonism and serotonin 5-HT3 receptor inhibition in the chemoreceptor trigger zone, reducing nausea and vomiting. It also acts as a serotonin 5-HT4 receptor agonist and modulates muscarinic receptors to enhance acetylcholine release, which increases gastrointestinal motility and accelerates gastric emptying. These combined actions facilitate upper gastrointestinal transit while avoiding increased secretions, supporting its use in gastroparesis and gastroesophageal reflux disease. |
|---|---|
| Mechanism of action | Metoclopramide causes antiemetic effects by inhibiting dopamine D2 and serotonin 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) located in the area postrema of the brain. Administration of this drug leads to prokinetic effects via inhibitory actions on presynaptic and postsynaptic D2 receptors, agonism of serotonin 5-HT4 receptors, and antagonism of muscarinic receptor inhibition. This action enhances the release of acetylcholine, causing increased lower esophageal sphincter (LES) and gastric tone, accelerating gastric emptying and transit through the gut. Metoclopramide antagonizes the dopamine D2 receptors. Dopamine exerts relaxant effect on the gastrointestinal tract through binding to muscular D2 receptors. |
| Pharmacodynamics | Metoclopramide increases gastric emptying by decreasing lower esophageal sphincter (LES) pressure. It also exerts effects on the area postrema of the brain, preventing and relieving the symptoms of nausea and vomiting. In addition, this drug increases gastrointestinal motility without increasing biliary, gastric, or pancreatic secretions. Because of its antidopaminergic activity, metoclopramide can cause symptoms of tardive dyskinesia (TD), dystonia, and akathisia, and should therefore not be administered for longer than 12 weeks. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 4 | Humans | agonist |
| 5-hydroxytryptamine receptor 3A | Humans | antagonist |
| Muscarinic acetylcholine receptor M1 | Humans | agonist |
ADME / PK
| Absorption | Metoclopramide is rapidly absorbed in the gastrointestinal tract with an absorption rate of about 84%. The bioavailability of the oral preparation is reported to be about 40.7%, but can range from 30-100%. Nasal metoclopramide is 47% bioavailable. A 15mg dose reaches a C<sub>max</sub> of 41.0 ng/mL, with a T<sub>max</sub> of 1.25 h, and an AUC of 367 ng\*h/mL. |
|---|---|
| Half-life | The mean elimination half-life of metoclopramide in people with healthy renal function ranges from 5 to 6 hours but is prolonged in patients with renal impairment. Downward dose adjustment should be considered. |
| Protein binding | Metoclopramide is 30% bound to plasma proteins, mainly to alpha-1-acid glycoprotein. |
| Metabolism | Metoclopramide undergoes first-pass metabolism and its metabolism varies according to the individual. This drug is metabolized by cytochrome P450 enzymes in the liver. CYP2D6 and CYP3A4 both contribute to its metabolism, with CYP2D6 being more heavily involved. CYP1A2 is also a minor contributing enzyme. The process of N-4 sulphate conjugation is a primary metabolic pathway of metoclopramide. |
| Route of elimination | About 85% of an orally administered dose was measured in the urine within 72 hours during a pharmacokinetic study. An average of 18% to 22% of 10-20 mg dose was recovered as free drug within 3 days of administration. |
| Volume of distribution | The volume of distribution of metoclopramide is approximately 3.5 L/kg. This implies a high level of tissue distribution. Metoclopramide crosses the placental barrier and can cause extrapyramidal symptoms in the fetus. |
| Clearance | The renal clearance of metoclopramide is 0.16 L/h/kg with a total clearance of 0.7 L/h/kg. Clinical studies showed that the clearance of metoclopramide may be reduced by up to 50% in patients with renal impairment. After high intravenous doses, total metoclopramide clearance ranged from 0.31 to 0.69 L/kg/h. |
Formulation & handling
- Metoclopramide is a small molecule suitable for multiple routes including oral, parenteral (intramuscular, intravenous), nasal, and rectal administration. It is recommended to administer the oral form 30 minutes before meals due to decreased bioavailability with food. The API has moderate water solubility and requires handling compatible with solution and solid oral dosage forms.
Regulatory status
| Lifecycle | The API is available in mature markets including the US and Canada, with several key patents having expired between 2017 and 2021, while one patent remains active until 2030, impacting generic entry and market competition. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Metoclopramide involves numerous packagers and generic manufacturers, indicating a well-established supply chain with strong B2B sourcing activity. Branded products are primarily present in the US and Canadian markets, with multiple formulations available. While some patents have expired as of 2018 and 2021, enabling generic competition, the presence of a valid patent until 2030 suggests ongoing brand exclusivity for specific formulations or uses, allowing continued branded product presence alongside generics. |
|---|
Safety
| Toxicity | The rat oral LD50 of metoclopramide is 750 mg/kg. Some symptoms of an overdose with metoclopramide include drowsiness, disorientation, and extrapyramidal reactions. Drugs that manage Parkinson's disease or anticholinergic drugs or antihistamines with anticholinergic properties should be employed to treat extrapyramidal symptoms. Normally, these symptoms subside within 24 hours. Unintentional overdose in infants receiving the oral solution of metoclopramide resulted in seizures, extrapyramidal symptoms, in addition to a lethargic state. In addition, methemoglobinemia has been found to occur in premature and full-term neonates after a metoclopramide overdose. Intravenous methylene blue may treat metoclopramide-associated methemoglobinemia. It is important to note that methylene blue administration may lead to hemolytic anemia in patients who suffer from G6PD deficiency, which can result in fatality. Dialysis has not been shown to be effective in sufficiently eliminating metoclopramide in an overdose situation due to low plasma distribution of this drug. |
|---|
- Metoclopramide exhibits moderate acute toxicity with a rat oral LD50 of 750 mg/kg
- Overdose may result in central nervous system effects including extrapyramidal symptoms and methemoglobinemia, particularly in neonates
- Treatment of methemoglobinemia with methylene blue requires caution in G6PD-deficient patients due to risk of hemolytic anemia
Metoclopramide is a type of Dopamine antagonists
Dopamine antagonists belong to the pharmaceutical API subcategory that plays a crucial role in the management of various medical conditions. These compounds act by blocking dopamine receptors, which are responsible for transmitting signals in the brain. By inhibiting dopamine activity, dopamine antagonists exhibit diverse therapeutic effects.
One significant application of dopamine antagonists is in the treatment of psychiatric disorders. They are commonly used to manage schizophrenia, a severe mental disorder characterized by hallucinations, delusions, and disorganized thinking. Dopamine antagonists help reduce the symptoms of schizophrenia by normalizing the excessive dopamine activity in the brain.
Additionally, these pharmaceutical APIs find application in managing other conditions such as bipolar disorder, nausea, vomiting, and certain movement disorders. Dopamine antagonists can effectively alleviate the symptoms associated with these conditions by modulating dopamine levels and restoring the balance in neural signaling.
Pharmaceutical companies utilize advanced synthesis and purification techniques to produce high-quality dopamine antagonists for use as active ingredients in various medications. These APIs undergo stringent quality control measures to ensure their safety, efficacy, and compliance with regulatory standards.
In conclusion, dopamine antagonists constitute an important subcategory of pharmaceutical APIs, offering valuable therapeutic benefits for psychiatric disorders, nausea, vomiting, and movement disorders. Their ability to selectively block dopamine receptors makes them indispensable in modern medicine, enabling improved patient outcomes and quality of life.
Metoclopramide (Dopamine antagonists), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Metoclopramide API manufacturers & distributors
Compare qualified Metoclopramide API suppliers worldwide. We currently have 14 companies offering Metoclopramide API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Amsa S.P.A. | Producer | Italy | Italy | CoA, GMP | 10 products |
| Anphar Labs. | Producer | India | India | CoA, WC | 5 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, WC | 250 products |
| Cosma | Producer | Italy | Italy | CoA, USDMF | 20 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Hari Ganesh Pharma Privat... | Distributor | India | India | CoA, FDA, GMP, USDMF | 35 products |
| ICROM | Producer | Italy | Italy | CEP, CoA, FDA, GMP, USDMF | 19 products |
| Ipca Labs. | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 69 products |
| Lundbeck Pharma | Producer | Italy | Italy | CoA, USDMF | 15 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, ISO9001, USDMF | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shandong Chenghui Shuangd... | Producer | China | China | CEP, CoA, ISO9001 | 98 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
When sending a request, specify which Metoclopramide 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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