PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
cimetidine

2D structure

Overview

Generic Names: Cimetidine A/AB; Cimetidine Hcl
Trade Names: Acibilin; Acinil; Cimal; Cimetag; Cimetum; Dyspamet; Edalene; Eureceptor; Gastromet; Peptol; Tagamet; Tagamet HB; Tagamet HB 200; Tametin; Tratul; Ulcedin; Ulcedine; Ulcerfen; Ulcimet; Ulcofalk; Ulcomedina; Ulcomet; Ulhys
PharmGKB Accession Id: PA449001

Description

A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy. PubChem (source: Drug Bank)

Indication

For the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion. (source: Drug Bank)

ATC Therapeutic Category

  • A02BA:H2-receptor antagonists

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Cimetidine binds to an H<sub>2</sub>-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity. (source: Drug Bank)

Pharmacology

Cimetidine is a histamine H<sub>2</sub>-receptor antagonist. It reduces basal and nocturnal gastric acid secretion and a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli including food, caffeine, insulin, betazole, or pentagastrin. It is used to treat gastrointestinal disorders such as gastric or duodenal ulcer, gastroesophageal reflux disease, and pathological hypersecretory conditions. Cimetidine inhibits many of the isoenzymes of the hepatic CYP450 enzyme system. Other actions of Cimetidine include an increase in gastric bacterial flora such as nitrate-reducing organisms. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Best effect when taken with food.
Limit caffeine intake. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

15-20% (source: Drug Bank)

Absorption

Rapid 60-70% (source: Drug Bank)

Toxicity

Symptoms of overdose include nausea, vomiting, diarrhea, increased saliva production, difficulty breathing, and a fast heartbeat. (source: Drug Bank)

Isomeric SMILES Code:

Cc1c(nc[nH]1)CSCCNC(=NC#N)NC (source: Drug Bank)

Non-Curated Annotations (Non-Curated Annotation)

  1. rs11568493 at chr11:62520183 in SLC22A8
    Reduced estrone sulfate and cimetidine uptake in transfected cells
    Variant Name:
    SLC22A8: I260R
    Related Drugs:
    cimetidine, conjugated estrogens
    Evidence:
    PMID:19940846
  2. rs11568496 at chr11:62523015 in SLC22A8
    Reduced estrone sulfate and cimetidine uptake in transfected cells
    Variant Name:
    SLC22A8: Q239X
    Related Drugs:
    cimetidine, conjugated estrogens
    Evidence:
    PMID:19940846
  3. rs45566039 at chr11:62523883 in SLC22A8
    Reduced estrone sulfate and cimetidine uptake in transfected cells
    Variant Name:
    SLC22A8: R149S
    Related Drugs:
    cimetidine, conjugated estrogens
    Evidence:
    PMID:19940846
Variant names are different names that have been used in the literature and other resources to refer to the same variant. Non-curated variant information is accumulated solely by computational methods and has not been verified by the scientific staff at PharmGKB.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A2
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A6
  • CO
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A8
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
SLCO1B1
  • CO
  •   
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SLCO1B3
  • CO
  •   
  • PK
  •   
  • GN
Publications

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

Drug Targets

Gene Description
HRH2 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
galantamine
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
tacrine
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
  •   
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
warfarin
  •   
  •   
  •   
  •   
  •   
Publications

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

Drug Interactions

Drug Description
acenocoumarol Uncurated Annotation The anti-H2 increases the anticoagulant effect (source: Drug Bank)
alfentanil Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
alprazolam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
aminophylline Uncurated Annotation Increases the effect of theophylline (source: Drug Bank)
amitriptyline Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
amoxapine Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
anisindione Uncurated Annotation The ANTI-H2 increases the anticoagulant effect (source: Drug Bank)
astemizole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atazanavir Uncurated Annotation This gastric pH modifier decreases the levels/effects of atazanavir (source: Drug Bank)
carbamazepine Uncurated Annotation Increases the effect of carbamazepine (source: Drug Bank)
carmustine Uncurated Annotation Increases myelosuppression caused by carmustine (source: Drug Bank)
chlordiazepoxide Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
clomipramine Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
clonazepam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
clorazepate Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
clozapine Uncurated Annotation Increases the effect of clozapine (source: Drug Bank)
codeine Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
desipramine Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
diazepam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
dicumarol Uncurated Annotation The anti-H2 increases the anticoagulant effect (source: Drug Bank)
dofetilide Uncurated Annotation Increases effect/toxicity of dofetilide (source: Drug Bank)
donepezil Uncurated Annotation Possible antagonism of action (source: Drug Bank)
doxepin Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
dyphylline Uncurated Annotation Increases the effect of theophylline (source: Drug Bank)
dyphylline Uncurated Annotation Increases the effect of theophylline (source: Drug Bank)
enoxacin Uncurated Annotation The agent decreases the absorption of enoxacin (source: Drug Bank)
epirubicin Uncurated Annotation Cimetidine can increase epirubicin levels (source: Drug Bank)
estazolam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
ethotoin Uncurated Annotation Increases the effect of hydantoin (source: Drug Bank)
fentanyl Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
flecainide Uncurated Annotation Increases serum levels of flecainide (source: Drug Bank)
fluorouracil Uncurated Annotation Increases the effect of and toxicity of fluorouacil (source: Drug Bank)
flurazepam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
fosphenytoin Uncurated Annotation Increases the effect of hydantoin (source: Drug Bank)
galantamine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
halazepam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
heroin Uncurated Annotation Cimetidine increases the effect of the narcotic (source: Drug Bank)
hydrocodone Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
hydromorphone Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
imipramine Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
itraconazole Uncurated Annotation The anti-H2 decreases the absorption of the imidazole (source: Drug Bank)
ketazolam Uncurated Annotation Cimetidine increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole Uncurated Annotation The anti-H2 decreases the absorption of the imidazole (source: Drug Bank)
labetalol Uncurated Annotation Cimetidine increases the effect of the beta-blocker (source: Drug Bank)
levorphanol Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
lidocaine Uncurated Annotation Increases the effect and toxicity of lidocaine (source: Drug Bank)
meperidine Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
mephenytoin Uncurated Annotation Increases the effect of hydantoin (source: Drug Bank)
metformin Uncurated Annotation Increases the effect of metformin (source: Drug Bank)
methadone Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
metoprolol Uncurated Annotation Increases the effect of the beta-blocker (source: Drug Bank)
midazolam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
moclobemide Uncurated Annotation Increases the effect of moclobemide (source: Drug Bank)
morphine Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
nalbuphine Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
nifedipine Uncurated Annotation Increases the effect of the calcium channel blocker (source: Drug Bank)
nimodipine Uncurated Annotation Increases the effect of the calcium channel blocker (source: Drug Bank)
nitrendipine Uncurated Annotation Increases the effect of the calcium channel blocker (source: Drug Bank)
nortriptyline Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
oxtriphylline Uncurated Annotation Increases the effect of theophylline (source: Drug Bank)
oxycodone Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
oxymorphone Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
pentazocine Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
phenytoin Uncurated Annotation Increases the effect of hydantoin (source: Drug Bank)
posaconazole Uncurated Annotation Significant decrease of posaconazole levels (source: Drug Bank)
pramipexole Uncurated Annotation Increases the effect and toxicity of pramipexole (source: Drug Bank)
prazepam Uncurated Annotation Cimetidine increases the effect of the benzodiazepine (source: Drug Bank)
procainamide Uncurated Annotation The histamine H2-receptor antagonist increases the effect of procainamide (source: Drug Bank)
propoxyphene Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
propranolol Uncurated Annotation Increases the effect of the beta-blocker (source: Drug Bank)
protriptyline Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
quazepam Uncurated Annotation Cimetidine increases the effect of the benzodiazepine (source: Drug Bank)
quinidine Uncurated Annotation Increases the effect of quinidine (source: Drug Bank)
quinidine Uncurated Annotation Increases the effect of quinidine (source: Drug Bank)
rivastigmine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
sildenafil Uncurated Annotation Increases the effect and toxicity of sildenafil (source: Drug Bank)
sufentanil Uncurated Annotation Increases the effect of the narcotic (source: Drug Bank)
tacrine Uncurated Annotation Increases the effect and toxicity of tacrine (source: Drug Bank)
terfenadine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
theophylline Uncurated Annotation Increases the effect of theophylline (source: Drug Bank)
timolol Uncurated Annotation Increases the effect of the beta-blocker (source: Drug Bank)
tolazoline Uncurated Annotation Anticipated loss of efficacy of tolazoline (source: Drug Bank)
triazolam Uncurated Annotation Increases the effect of the benzodiazepine (source: Drug Bank)
trimipramine Uncurated Annotation Increases the effect of tricyclic agent (source: Drug Bank)
warfarin Uncurated Annotation The anti-H2 increases the anticoagulant effect (source: Drug Bank)
zaleplon Uncurated Annotation Increases the effect and toxicity of zaleplon (source: Drug Bank)

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. mRNA expression levels of PXR splice variants in livers
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • FA
    Submitted by Erin G. Schuetz, PhD involving CYP3A4, NR1I2, , amiodarone, cimetidine, dopamine, erythromycin, ethanol, glucocorticoids, hmg coa reductase inhibitors, midazolam, nicotine, phenobarbital, phenytoin, propofol, thyroid preparations and vasopressin
  2. SLC22A2 Functional Protein Variants
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • FA
    Submitted by Kathleen M. Giacomini, PhD involving SLC22A2, , cimetidine, metformin, MPP+, phenformin, procainamide and quinidine
  3. SLC22A8 Functional Protein Variants
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • FA
    Submitted by Kathleen M. Giacomini, PhD involving SLC22A8, , cimetidine and estrone

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

Web Resource:
Wikipedia
DrugBank:
DB00501
ChEBI ID:
30731
KEGG Drug ID:
D00295
PubChem Compound ID:
2756
PubChem Substance ID:
180968
IUPHAR Ligand ID:
1231

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.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
Add New Alternate Name
Add New ATC Term
Add Cross Reference
Add a metabolite
Add a text annotation
Add a drug target
hint: enter a gene
    Add a drug interaction
    hint: enter a drug
    PharmGKB® is a registered trademark of HHS and is financially supported by NIH/NIGMS. It is managed at Stanford University (GM61374).
    ©2001-2010 PharmGKB.