Drug/Small Molecule:

metoclopramide

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
	CYP1A2	PK	Publications
	CYP2D6	PK	Publications

Non-Curated Information

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

Metabolizing Enzymes

• CYP2D6

Drug Targets

• DRD2
• CHRM1

Curated Information

The following drugs are in curated knowledge about this drug.

	Drug	Relationship	Evidence
	tamoxifen	PK	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
	tardive dyskinesia	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.

1. 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.

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

Downloads

You must sign in before you can download data.

LinkOuts

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Non-Curated Publications

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