Overview
| Generic Names: | Metaclopramide; Metaclopromide; Methochlopramide; Methoclopramide; Metochlopramide; Metoclopramida [INN-Spanish]; Metoclopramide Hcl; Metoclopramide Hydrochloride; Metoclopramidum [INN-Latin]; metoclopramide |
|---|---|
| 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 (source: Drug Bank)
Indication
For the treatment of gastroesophageal reflux disease (GERD) (source: Drug Bank)
ATC Therapeutic Category
- A03FA:Propulsives
Pharmacology, Interactions, and Contraindications
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. (source: Drug Bank)
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. (source: Drug Bank)
Food Interactions
Food reduces availability, take 30 minutes before meals. Avoid alcohol. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
30% (source: Drug Bank)
Absorption
Rapidly and well absorbed (oral bioavailability 80±15.5%). (source: Drug Bank)
Toxicity
Oral, mouse LD<sub>50</sub>: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions. (source: Drug Bank)
Isomeric SMILES Code:
CCN(CC)CCNC(=O)c1cc(c(cc1CO)N)Cl (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
CYP1A2 |
|
Publications |
|
CYP2D6 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| CHRM1 |
|
(source: Drug Bank) |
| DRD2 |
|
(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
tamoxifen |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| atovaquone |
|
The agent decreases the effect of atovaquone (source: Drug Bank) |
| cyclosporine |
|
Metoclopramide increases serum levels of cyclosporine (source: Drug Bank) |
| levodopa |
|
Levodopa decreases the effect of metoclopramide (source: Drug Bank) |
| succinylcholine |
|
The agent increases the effect of succinylcholine (source: Drug Bank) |
| venlafaxine |
|
Possible serotoninergic syndrome with this combination (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
tardive dyskinesia |
|
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.
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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.