Chemical: Drug
metoclopramide

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last updated 09/01/2016

1. FDA Label for metoclopramide and CYB5R1,CYB5R2,CYB5R3,CYB5R4,G6PD

Actionable PGx
Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Methemoglobinemia
    • Adverse reactions section, Overdosage section, Precautions section
    • source: U.S. Food and Drug Administration
  • Sulfhemoglobinemia
    • Adverse reactions section, Precautions section
    • source: U.S. Food and Drug Administration
  • tardive dyskinesia
    • Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • CYB5R1
    • other, Precautions section
    • source: U.S. Food and Drug Administration
  • CYB5R2
    • other, Precautions section
    • source: U.S. Food and Drug Administration
  • CYB5R3
    • other, Precautions section
    • source: U.S. Food and Drug Administration
  • CYB5R4
    • other, Precautions section
    • source: U.S. Food and Drug Administration

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for metoclopramide

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2D6 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *10 N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYB5R3 deficiency N/A N/A N/A
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

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
Brand Mixture Names

PharmGKB Accession Id

PA450475

Type(s):

Drug

Description

A dopamine D2 antagonist that is used as an antiemetic.

Source: Drug Bank

Indication

For the treatment of gastroesophageal reflux disease (GERD). It is also used in treating nausea and vomiting, and to increase gastric emptying.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

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 Interaction

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

Half-Life

5-6 hr

Source: Drug Bank

Toxicity

Oral, mouse LD 50: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Approximately 85% of the radioactivity of an orally administered dose appears in the urine within 72 hours.

Source: Drug Bank

Volume of Distribution

  • 4.4±0.65 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C14H22ClN3O2

Source: Drug Bank

Isomeric SMILES

CCN(CC)CCNC(=O)c1cc(c(cc1CO)N)Cl

Source: OpenEye

Canonical SMILES

CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC

Source: Drug Bank

Average Molecular Weight

299.796

Source: Drug Bank

Monoisotopic Molecular Weight

299.14005467

Source: Drug Bank

SMILES

CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC

Source: Drug Bank

InChI String

InChI=1S/C14H22ClN3O2/c1-4-18(5-2)7-6-17-14(19)10-8-11(15)12(16)9-13(10)20-3/h8-9H,4-7,16H2,1-3H3,(H,17,19)

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
CHRM1 (source: Drug Bank )
DRD2 (source: Drug Bank )
HTR4 (source: Drug Bank )

Drug Interactions

Interaction Description
atovaquone - metoclopramide The agent decreases the effect of atovaquone (source: Drug Bank )
cyclosporine - metoclopramide Metoclopramide increases serum levels of cyclosporine (source: Drug Bank )
cyclosporine - metoclopramide Metoclopramide increases serum levels of cyclosporine (source: Drug Bank )
metoclopramide - atovaquone The agent decreases the effect of atovaquone (source: Drug Bank )
metoclopramide - atovaquone The agent decreases the effect of atovaquone (source: Drug Bank )
metoclopramide - cyclosporine Metoclopramide increases serum levels of cyclosporine (source: Drug Bank )
metoclopramide - cyclosporine Metoclopramide increases serum levels of cyclosporine (source: Drug Bank )
metoclopramide - levodopa Levodopa decreases the effect of metoclopramide (source: Drug Bank )
metoclopramide - levodopa Levodopa decreases the effect of metoclopramide (source: Drug Bank )
metoclopramide - succinylcholine The agent increases the effect of succinylcholine (source: Drug Bank )
metoclopramide - succinylcholine The agent increases the effect of succinylcholine (source: Drug Bank )
metoclopramide - venlafaxine Possible serotoninergic syndrome with this combination (source: Drug Bank )
metoclopramide - venlafaxine Possible serotoninergic syndrome with this combination (source: Drug Bank )
paliperidone - metoclopramide Metoclopramide may increase the risk of extrapyramidal side effects of paliperidone. Concomitant therapy should be avoided. (source: Drug Bank )
zuclopenthixol - metoclopramide Additive dopamine D2 receptor antagonism may cause dopaminergic imbalance in the nigrostriatal (dopamine D1 receptors) and striatopallidal (dopamine D2 receptors). Increased risk of extrapyramidal reactions and neuroleptic malignant syndrome. Concomitant therapy should be avoided. (source: Drug Bank )

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to metoclopramide: 8

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetics and pharmacogenetics of aminergic transmitter pathways in functional gastrointestinal disorders. Pharmacogenomics. 2015. Martinucci Irene, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetic insights into migraine treatment in children. Pharmacogenomics. 2014. Gentile Giovanna, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The genetics of pro-arrhythmic adverse drug reactions. British journal of clinical pharmacology. 2014. Petropoulou Evmorfia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of ABCB1, 5-HT3B receptor and CYP2D6 genetic polymorphisms with ondansetron and metoclopramide antiemetic response in Indonesian cancer patients treated with highly emetogenic chemotherapy. Japanese journal of clinical oncology. 2011. Perwitasari Dyah A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Composite functional genetic and comedication CYP2D6 activity score in predicting tamoxifen drug exposure among breast cancer patients. Journal of clinical pharmacology. 2010. Borges Silvana, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Review article: metoclopramide and tardive dyskinesia. Alimentary pharmacology & therapeutics. 2010. Rao A S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Metoclopramide-induced methemoglobinemia in a patient with co-existing deficiency of glucose-6-phosphate dehydrogenase and NADH-cytochrome b5 reductase: failure of methylene blue treatment. Haematologica. 2001. Karadsheh N S, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0591-2228-05
DrugBank:
DB01233
ChEBI:
107736
KEGG Compound:
C07868
KEGG Drug:
D00726
PubChem Compound:
4168
PubChem Substance:
152911
46505631
IUPHAR Ligand:
241
Drugs Product Database (DPD):
2243563
BindingDB:
50000491
ChemSpider:
4024
Therapeutic Targets Database:
DAP000530
FDA Drug Label at DailyMed:
10a7bd47-d6fe-4e10-8d2a-30c81cee4c2d

Clinical Trials

These are trials that mention metoclopramide and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.