Drug/Small Molecule:
metoclopramide

2D structure

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
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
CHRM1 Uncurated Annotation (source: Drug Bank)
DRD2 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
atovaquone Uncurated Annotation The agent decreases the effect of atovaquone (source: Drug Bank)
cyclosporine Uncurated Annotation Metoclopramide increases serum levels of cyclosporine (source: Drug Bank)
levodopa Uncurated Annotation Levodopa decreases the effect of metoclopramide (source: Drug Bank)
succinylcholine Uncurated Annotation The agent increases the effect of succinylcholine (source: Drug Bank)
venlafaxine Uncurated Annotation Possible serotoninergic syndrome with this combination (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
tardive dyskinesia
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  • GN
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.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance
  2. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01233
KEGG Compound ID:
C07868
KEGG Drug ID:
D00726
PubChem Compound ID:
4168
PubChem Substance ID:
152911
IUPHAR Ligand ID:
241

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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