Overview
| Generic Names: | Metaclopramide; Metaclopromide; Methochlopramide; Methoclopramide; Metochlopramide; Metoclopramida [INN-Spanish]; Metoclopramide Hcl; Metoclopramide Hydrochloride; Metoclopramidum [INN-Latin]; metoclopramide |
|---|---|
| IUPAC Name: | 4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxybenzamide |
| Trade Names: | Apo-Metoclop; Cerucal; Clopra; Clopra-Yellow; Clopromate; DEL; Duraclamid; Elieten; Emetid; Emitasol; Emperal; Eucil; Gastrese; Gastro-Timelets; Gastrobid; Gastromax; Gastronerton; Gastrosil; Gastrotablinen; Gastrotem; Imperan; Maxeran; Maxolon; Meclopran; Metamide; Metoclol; Metoclopramide Intensol; Metoclopramide Omega; Metocobil; Metramid; Moriperan; Mygdalon; Neu-Sensamide; Nu-Metoclopramide; Octamide; Parmid; Paspertin; Peraprin; Plasil; Pms-Metoclopramide; Pramidin; Pramiel; Pramin; Primperan; Reclomide; Reglan; Reliveran; Terperan |
| PharmGKB Accession Id: | PA450475 |
Description
A dopamine D2 antagonist that is used as an antiemetic. [PubChem]
Indication
For the treatment of gastroesophageal reflux disease (GERD)
ATC Therapeutic Category
- A03FA:Propulsives
Pharmacology and Interactions
Mechanism Of Action
Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals.
Pharmacology
Metoclopramide, although chemically related to procainamide, does not possess local anesthetic or antiarrhythmic properties. Metoclopramide is used to enhance GI motility, to treat diabetic gastroparesis, as an antinauseant, and to facilitate intubation of the small bowel during radiologic examination. Metoclopramide may be used to treat chemotherapy-induced emesis and as a radiosensitizing agents in the treatment of non-small cell lung carcinoma and glioblastomas in the future.
Food Interactions
Food reduces availability, take 30 minutes before meals. Avoid alcohol.
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic
Protein Binding
30%
Absorption
Rapidly and well absorbed (oral bioavailability 80±15.5%).
Half Life
5-6 hr
Toxicity
Oral, mouse LD50: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.
Chemical Properties
Chemical Formula:
C14H22ClN3O2
SMILES Code:
CCN(CC)CCNC(=O)c1cc(c(cc1CO)N)Cl
(Format: OpenEye Isomeric)
Molecular Weight ( average / monoisotopic )
299.796 / 299.1401
Curated Information
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP1A2 |
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Publications |
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CYP2D6 |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other genes is available.
Metabolizing Enzymes
Drug Targets
Curated Information
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
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tamoxifen |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| atovaquone | The agent decreases the effect of atovaquone |
| cyclosporine | Metoclopramide increases serum levels of cyclosporine |
| levodopa | Levodopa decreases the effect of metoclopramide |
| succinylcholine | The agent increases the effect of succinylcholine |
| venlafaxine | Possible serotoninergic syndrome with this combination |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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tardive dyskinesia |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
- Drug-Induced Long QT Intervals




- PD
Submitted by Dan Roden, MD involving ADRB1, ADRB2, KCNE1, KCNE2, KCNH2, KCNQ1, SCN5A, almokalant, amiodarone, amitriptyline, bretylium, bupivacaine, cisapride, disopyramide, dofetilide, encainide, fluconazole, haloperidol, hydroquinidine, isoflurane, itraconazole, ketoconazole, lithium, loratadine, metoclopramide, nortriptyline, procainamide, quinidine, sematilide, sotalol, sulfamethoxazole, thioridazine, trimethoprim, , Long QT Syndrome, Proarrhythmia and Torsades de Pointes
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
Downloads
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
