Repositioning Candidate Details
| Candidate ID: | R0459 |
| Source ID: | DB01233 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Metoclopramide |
| Synonyms: | 2-methoxy-4-amino-5-chloro-N,N-(dimethylaminoethyl)benzamide; 2-methoxy-5-chloroprocainamide; 4-amino-5-chloro-2-methoxy-N-(β-diethylaminoethyl)benzamide; 4-amino-5-chloro-N-(2-(diethylamino)ethyl)-o-anisamide; Metoclopramide |
| Molecular Formula: | C14H22ClN3O2 |
| SMILES: | CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC |
| Structure: |
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| DrugBank Description: | Diabetic gastroparesis is a condition that causes frequent nausea and vomiting, which has a negative impact on quality of life and poses a significant burden on the healthcare system. Metoclopramide is a dopamine antagonist used to treat nausea and vomiting that may be associated with diabetic gastroparesis in addition to gastroesophageal reflux disease (GERD). It can also be used to prevent nausea or vomiting associated with chemotherapy or certain surgical or diagnostic procedures. One unique property of this drug is that it does not increase gastric acid secretion. It is available in the oral tablet form or in solution, and can also be administered through the intravenous route. Metoclopramide was initially approved by the FDA in 1980. |
| CAS Number: | 364-62-5 |
| Molecular Weight: | 299.796 |
| DrugBank Indication: | 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. Intravenous metoclopramide facilitates intubation of the small bowel and stimulates gastric emptying and barium flow in patients who require radiological examination of the stomach or small intestine. In some cases, the delay of gastrointestinal emptying interferes with the radiographic visualization of the gastrointestinal tract, and metoclopramide is used to facilitate emptying in these cases, allowing for adequate diagnostic visualization. Some off-label uses of metoclopramide include the management of radiation-induced nausea and vomiting, gastric bezoars, intractable hiccups, and migraine pain. |
| DrugBank Pharmacology: | 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. |
| DrugBank MoA: | 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. |
| Targets: | Dopamine D2 receptor antagonist; Muscarinic acetylcholine receptor M1 agonist; 5-hydroxytryptamine receptor 4 agonist; 5-hydroxytryptamine receptor 3A antagonist |
| Inclusion Criteria: | Indication associated |
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