PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
indomethacin

2D structure

Overview

Generic Names: IMN; Indometacine; Indometacyna; Indomethacine; Indomethacinum; Indomethancin; Indomethazine; Indomethine; Indometicina; indomethacin
Trade Names: Amuno; Apo-Indomethacin; Argun; Arthrexin; Artracin; Artrinovo; Artrivia; Bonidin; Bonidon; Bonidon Gel; Catlep; Chibro-Amuno; Chrono-Indicid; Chrono-Indocid; Confortid; Dolcidium; Dolcidium Pl; Dolovin; Durametacin; Elmetacin; Flexin Continus; Hicin; Idomethine; Imbrilon; Inacid; Indacin; Indaflex; Indameth; Indmethacine; Indo-Lemmon; Indo-Phlogont; Indo-Rectolmin; Indo-Spray; Indo-Tablinen; Indocid; Indocid Pda; Indocid Sr; Indocin; Indocin I.V; Indocin I.V.; Indocin Sr; Indolar Sr; Indomecol; Indomed; Indomee; Indomethegan; Indomo; Indomod; Indoptic; Indoptol; Indorektal; Indoxen; Inflazon; Infrocin; Inteban Sp; Lausit; Liometacen; Metacen; Metartril; Methazine; Metindol; Miametan; Mikametan; Mobilan; Novo-Methacin; Novomethacin; Nu-Indo; Reumacide; Rhemacin La; Rheumacin La; Sadoreum; Tannex; Vonum
PharmGKB Accession Id: PA449982

Description

A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes. PubChem (source: Drug Bank)

Indication

For moderate to severe rheumatoid arthritis including acute flares of chronic disease, ankylosing spondylitis, osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis. (source: Drug Bank)

ATC Therapeutic Categories

  • C01EB:Other cardiac preparations
  • M01AB:Acetic acid derivatives and related substances

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Antiinflammatory effects of Indomethacin are believed to be due to inhibition of cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. (source: Drug Bank)

Pharmacology

Indomethacin, a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Take with food or antacids to reduce irritation. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. (source: Drug Bank)

Protein Binding

97% (source: Drug Bank)

Absorption

Bioavailability is approximately 100% following oral administration and 80â¿¿90% following rectal administration. (source: Drug Bank)

Toxicity

The following symptoms may be observed following overdosage: nausea, vomiting, intense headache, dizziness, mental confusion, disorientation, or lethargy. There have been reports of paresthesias, numbness, and convulsions. The oral LD<sub>50</sub> of indomethacin in mice and rats (based on 14 day mortality response) was 50 and 12 mg/kg, respectively. (source: Drug Bank)

Isomeric SMILES Code:

Cc1c(c2cc(ccc2n1C(=O)c3ccc(cc3)Cl)OC)CC(=O)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs3842787 at chr9:124173328 in PTGS1
    Risk-associated allele: not specified. Phenotype: In vitro inhibition studies with indomethacin demonstrated that the P17L variant was significantly more sensitive to indomethacin-mediated inhibition of PTGS1 activity relative to wild-type. Study type: FA
    Variant Name:
    PTGS1: P17L; (C>T)
    Related Drugs:
    indomethacin
    Evidence:
    PMID:17301694
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC1
  • CO
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
PTGS1
  •   
  •   
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
SLC22A11
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A6
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A8
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SLC22A9
  •   
  •   
  •   
  • FA
  •   
Publications

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

Drug Targets

Gene Description
PTGS1 Uncurated Annotation (source: Drug Bank)
PTGS2 Uncurated Annotation (source: Drug Bank)

PharmGKB Curated Pathways

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

Drug Interactions

Drug Description
acebutolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
acenocoumarol Uncurated Annotation The NSAID increases the anticoagulant effect (source: Drug Bank)
alendronate Uncurated Annotation Increased risk of gastric toxicity (source: Drug Bank)
anisindione Uncurated Annotation The NSAID increases the anticoagulant effect (source: Drug Bank)
atenolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
betaxolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
bevantolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
bisoprolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
bumetanide Uncurated Annotation The NSAID decreases the diuretic and antihypertensive effects of the loop diuretic (source: Drug Bank)
carteolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
carvedilol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
cyclosporine Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
dicumarol Uncurated Annotation The NSAID increases the anticoagulant effect (source: Drug Bank)
diflunisal Uncurated Annotation Diflunisal increases the effect and toxicity of indomethacin (source: Drug Bank)
esmolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
ethacrynic acid Uncurated Annotation The NSAID decreases the diuretic and antihypertensive effects of the loop diuretic (source: Drug Bank)
furosemide Uncurated Annotation The NSAID decreases the diuretic and antihypertensive effects of the loop diuretic (source: Drug Bank)
labetalol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
lithium Uncurated Annotation The NSAID increases serum levels of lithium (source: Drug Bank)
losartan Uncurated Annotation Indomethacin decreases the effect of losartan (source: Drug Bank)
methotrexate Uncurated Annotation The NSAID increases the effect and toxicity of methotrexate (source: Drug Bank)
metoprolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
nadolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
oxprenolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
penbutolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
pindolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
practolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
probenecid Uncurated Annotation Probenecid increases the effect/toxicity of indomethacin (source: Drug Bank)
propranolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
sotalol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
timolol Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
torasemide Uncurated Annotation The NSAID decreases the diuretic and antihypertensive effects of the loop diuretic (source: Drug Bank)
triamterene Uncurated Annotation Risk of acute renal impairment with this combination (source: Drug Bank)
warfarin Uncurated Annotation The NSAID increases the anticoagulant effect (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Leukemia
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Leukemia, Myeloid
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Leukemia, Myeloid, Acute
  • CO
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Neoplasms
  • CO
  •   
  •   
  • FA
  •   
Publications

Non-Curated Information

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

Additional Datasets

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

  1. Physicochemical determinants of human renal clearance

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00328
ChEBI ID:
5918
KEGG Compound ID:
C01926
KEGG Drug ID:
D00141
PubChem Compound ID:
3715
PubChem Substance ID:
148696
IUPHAR Ligand ID:
1909

Common Searches

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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.
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