Chemical: Drug
diclofenac

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.



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

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

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.

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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 diclofenac

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2C8 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2C8 *3 N/A N/A N/A
No VIP available No VIP available VA CYP2C8 *4 N/A N/A N/A
No VIP available CA VA CYP2C9 *1 N/A N/A N/A
VIP No VIP available No VIP available CYP2C9 *2 N/A N/A N/A
VIP CA VA CYP2C9 *3 N/A N/A N/A
No VIP available CA VA CYP2C9 *8 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *59 N/A N/A N/A
rs1057910 NC_000010.10:g.96741053A=, NC_000010.10:g.96741053A>C, NC_000010.11:g.94981296A=, NC_000010.11:g.94981296A>C, NG_008385.1:g.47639A=, NG_008385.1:g.47639A>C, NM_000771.3:c.1075A=, NM_000771.3:c.1075A>C, NP_000762.2:p.Ile359=, NP_000762.2:p.Ile359Leu, XM_005269575.1:c.1075A=, XM_005269575.1:c.1075A>C, XP_005269632.1:p.Ile359=, XP_005269632.1:p.Ile359Leu, rs17847042, rs3198471, rs61212474
A > C
SNP
I359L
No VIP available CA VA
rs12746200 NC_000001.10:g.186849186A>G, NC_000001.11:g.186880054A>G, NG_012203.1:g.56155A>G, NM_001311193.1:c.115+9538A>G, NM_024420.2:c.115+9538A>G, XM_005245267.1:c.4+9310A>G, XM_005245267.2:c.4+9310A>G, XM_005245268.1:c.115+9538A>G, XM_011509641.1:c.136+9538A>G, XM_011509642.1:c.115+9538A>G, XM_011509643.1:c.115+9538A>G, XR_921838.1:n.176+9538A>G, rs17591911
A > G
SNP
VIP No Clinical Annotations available No Variant Annotations available
rs1799853 NC_000010.10:g.96702047C=, NC_000010.10:g.96702047C>T, NC_000010.11:g.94942290C=, NC_000010.11:g.94942290C>T, NG_008385.1:g.8633C=, NG_008385.1:g.8633C>T, NM_000771.3:c.430C=, NM_000771.3:c.430C>T, NP_000762.2:p.Arg144=, NP_000762.2:p.Arg144Cys, XM_005269575.1:c.430C=, XM_005269575.1:c.430C>T, XP_005269632.1:p.Arg144=, XP_005269632.1:p.Arg144Cys, rs17110268, rs28371674, rs33968134, rs60690363
C > T
SNP
R144C
No VIP available CA VA
rs1805034 NC_000018.10:g.62360008C>T, NC_000018.9:g.60027241C>T, NG_008098.1:g.39694C>T, NM_001270949.1:c.575C>T, NM_001270950.1:c.575C>T, NM_001270951.1:c.575C>T, NM_001278268.1:c.533C>T, NM_003839.2:c.575C>T, NM_003839.3:c.575C>T, NP_001257878.1:p.Ala192Val, NP_001257879.1:p.Ala192Val, NP_001257880.1:p.Ala192Val, NP_001265197.1:p.Ala178Val, NP_003830.1:p.Ala192Val, XM_005266777.1:c.575C>T, XM_011526244.1:c.590C>T, XM_011526245.1:c.467C>T, XP_005266834.1:p.Ala192Val, XP_011524546.1:p.Ala197Val, XP_011524547.1:p.Ala156Val, XR_935263.1:n.605C>T, rs57818955
C > T
SNP
A192V
No VIP available CA VA
rs2228246 NC_000020.10:g.39792063A>G, NC_000020.11:g.41163423A>G, NM_002660.2:c.835A>G, NM_182811.1:c.835A>G, NP_002651.2:p.Ser279Gly, NP_877963.1:p.Ser279Gly, XM_005260438.1:c.835A>G, XM_005260438.2:c.835A>G, XM_011528865.1:c.298A>G, XM_011528866.1:c.835A>G, XM_011528867.1:c.835A>G, XP_005260495.1:p.Ser279Gly, XP_011527167.1:p.Ser100Gly, XP_011527168.1:p.Ser279Gly, XP_011527169.1:p.Ser279Gly, XR_244143.1:n.956A>G, XR_936550.1:n.956A>G, rs52803627, rs57350391, rs8192707
A > G
SNP
S279G
VIP No Clinical Annotations available No Variant Annotations available
rs890293 NC_000001.10:g.60392494C>A, NC_000001.11:g.59926822C>A, NG_007931.1:g.4930G>T, NM_000775.3:c.-76G>T, NR_134981.1:n.-24G>T, NR_134982.1:n.-24G>T, XR_246240.1:n.-49G>T, XR_246240.2:n.-49G>T, XR_946558.1:n.-49G>T, rs3738475, rs60282769
C > A
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Diclofenac Acid
  • Diclofenac Potassium
  • Diclofenac Sodium
  • ISV-205
Trade Names
  • Allvoran
  • Apo-Diclo
  • Assaren
  • Benfofen
  • Cataflam
  • Delphimix
  • Dichlofenac
  • Dichronic
  • Diclo-Phlogont
  • Diclo-Puren
  • Diclobenin
  • Diclord
  • Dicloreum
  • Dolobasan
  • Duravolten
  • Dyloject
  • Ecofenac
  • Effekton
  • Kriplex
  • Neriodin
  • Novapirina
  • Novo-Difenac
  • Novo-Difenac SR
  • Nu-Diclo
  • Pennsaid
  • Primofenac
  • ProSorb-D
  • Prophenatin
  • Rhumalgan
  • Solaraze
  • Solaraze T
  • Tsudohmin
  • Valetan
  • Voldal
  • Voltaren
  • Voltaren Ophtha
  • Voltaren Ophthalmic
  • Voltaren Rapide
  • Voltaren SR
  • Voltaren-XR
  • Voltarol
  • Xenid
Brand Mixture Names

PharmGKB Accession Id

PA449293

Type(s):

Drug

Description

A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Source: Drug Bank

Indication

For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.

Source: Drug Bank

Pharmacology

Diclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis

Source: Drug Bank

Food Interaction

Avoid alcohol.|Take with food to reduce irritation.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

More than 99%

Source: Drug Bank

Absorption

Completely absorbed from the gastrointestinal tract.

Source: Drug Bank

Half-Life

2 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD 50=390mg/kg (orally in mice)

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites.

Source: Drug Bank

Volume of Distribution

  • 1.3 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C14H11Cl2NO2

Source: Drug Bank

Isomeric SMILES

c1ccc(c(c1)CC(=O)O)Nc2c(cccc2Cl)Cl

Source: OpenEye

Canonical SMILES

OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl

Source: Drug Bank

Average Molecular Weight

296.149

Source: Drug Bank

Monoisotopic Molecular Weight

295.016684015

Source: Drug Bank

SMILES

OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl

Source: Drug Bank

InChI String

InChI=1S/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19)

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
PTGS1 (source: Drug Bank)
PTGS2 (source: Drug Bank)
TTR (source: Drug Bank)

Drug Interactions

Interaction Description
cyclosporine - diclofenac Monitor for nephrotoxicity (source: Drug Bank)
cyclosporine - diclofenac Monitor for nephrotoxicity (source: Drug Bank)
diclofenac - alendronate Increased risk of gastric toxicity (source: Drug Bank)
diclofenac - alendronate Increased risk of gastric toxicity (source: Drug Bank)
diclofenac - anisindione The NSAID, diclofenac, may increase the anticoagulant effect of anisindione. (source: Drug Bank)
diclofenac - cyclosporine Monitor for nephrotoxicity (source: Drug Bank)
diclofenac - cyclosporine Monitor for nephrotoxicity (source: Drug Bank)
diclofenac - dicumarol The NSAID increases the anticoagulant effect (source: Drug Bank)
diclofenac - dicumarol The NSAID, diclofenac, may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
diclofenac - rifampin Decreased levels/effect of the NSAID (source: Drug Bank)
diclofenac - rifampin Rifampin, a CYP2C9 inducer, may increase the metabolism of diclofenac. (source: Drug Bank)
diclofenac - warfarin The NSAID increases the anticoagulant effect (source: Drug Bank)
diclofenac - warfarin The NSAID, diclofenac, may increase the anticoagulant effect of warfarin. (source: Drug Bank)
ginkgo biloba - diclofenac Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. (source: Drug Bank)
lithium - diclofenac The NSAID increases serum levels of lithium (source: Drug Bank)
lithium - diclofenac The NSAID, diclofenac, may decrease the renal excretion of lithium. Increased risk of lithium toxicity. (source: Drug Bank)
methotrexate - diclofenac The NSAID increases the effect and toxicity of methotrexate (source: Drug Bank)
methotrexate - diclofenac The NSAID, diclofenac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity. (source: Drug Bank)
rifampin - diclofenac Decreased levels/effect of the NSAID (source: Drug Bank)
tacrine - diclofenac The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Diclofenac, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Diclofenac is initiated, discontinued or if the dose is changed. (source: Drug Bank)
telmisartan - diclofenac Concomitant use of Telmisartan and Diclofenac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment. (source: Drug Bank)
telmisartan - diclofenac Concomitant use of Telmisartan and Diclofenac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment. (source: Drug Bank)
timolol - diclofenac The NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol. (source: Drug Bank)
timolol - diclofenac The NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol. (source: Drug Bank)
tizanidine - diclofenac Diclofenac may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. (source: Drug Bank)
trandolapril - diclofenac The NSAID, Diclofenac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Diclofenac is initiated, discontinued or dose changed. (source: Drug Bank)
treprostinil - diclofenac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy. (source: Drug Bank)
voriconazole - diclofenac Voriconazole, a strong CYP2C9 inhibitor, may increase the serum concentration of diclofenac by decreasing its metabolism. Renal impairment may increase the risk of diclofenac adverse effects. Monitor for changes in therapeutic and adverse effects of diclofenac if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
warfarin - diclofenac The antiplatelet effects of oral diclofenac may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to diclofenac: 26

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association study of genetic variants in PLA2G4A, PLCG1, LAT, SYK, and TNFRS11A genes in NSAIDs-induced urticaria and/or angioedema patients. Pharmacogenetics and genomics. 2015. Ayuso Pedro, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Identification and Functional Assessment of a New CYP2C9 Allelic Variant CYP2C9*59. Drug metabolism and disposition: the biological fate of chemicals. 2015. Dai Da-Peng, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Interethnic differences in the relevance of CYP2C9 genotype and environmental factors for diclofenac metabolism in Hispanics from Cuba and Spain. The pharmacogenomics journal. 2013. Llerena 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
Pharmacogenomics of acetylsalicylic acid and other nonsteroidal anti-inflammatory agents: clinical implications. European journal of clinical pharmacology. 2013. Yiannakopoulou Eugenia. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP2C9 polymorphism analysis in Han Chinese populations: building the largest allele frequency database. The pharmacogenomics journal. 2013. Dai D-P, 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
Effect of non-steroidal anti-inflammatory drugs and new fenamate analogues on TRPC4 and TRPC5 channels. Biochemical pharmacology. 2012. Jiang Hongni, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: cytochrome P450, family 2, subfamily J, polypeptide 2: CYP2J2. Pharmacogenetics and genomics. 2010. Berlin Dorit 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
Polymorphic human prostaglandin H synthase-2 proteins and their interactions with cyclooxygenase substrates and inhibitors. The pharmacogenomics journal. 2010. Liu W, 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
Drug-induced liver injury: past, present and future. Pharmacogenomics. 2010. Daly Ann K. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Cytochrome P450 2C9-CYP2C9. Pharmacogenetics and genomics. 2010. Van Booven Derek, 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
Risk of myocardial infarction and death associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs) among healthy individuals: a nationwide cohort study. Clinical pharmacology and therapeutics. 2009. Fosbøl E L, 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
Genetically based impairment in CYP2C8- and CYP2C9-dependent NSAID metabolism as a risk factor for gastrointestinal bleeding: is a combination of pharmacogenomics and metabolomics required to improve personalized medicine?. Expert opinion on drug metabolism & toxicology. 2009. Agúndez José A G, 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
Prediction of the effects of genetic polymorphism on the pharmacokinetics of CYP2C9 substrates from in vitro data. Pharmaceutical research. 2009. Kusama Makiko, 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
Relationship between CYP2C8 genotypes and diclofenac 5-hydroxylation in healthy Spanish volunteers. European journal of clinical pharmacology. 2008. Dorado P, 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
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic susceptibility to nonsteroidal anti-inflammatory drug-related gastroduodenal bleeding: role of cytochrome P450 2C9 polymorphisms. Gastroenterology. 2007. Pilotto Alberto, 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
Genetic susceptibility to diclofenac-induced hepatotoxicity: contribution of UGT2B7, CYP2C8, and ABCC2 genotypes. Gastroenterology. 2007. Daly Ann K, 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
Enzyme source effects on CYP2C9 kinetics and inhibition. Drug metabolism and disposition: the biological fate of chemicals. 2006. Kumar Vikas, 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
Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clinical pharmacokinetics. 2005. Kosoglou Teddy, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic predisposition to acute gastrointestinal bleeding after NSAIDs use. British journal of pharmacology. 2004. Martínez Carmen, 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
Pharmacogenetics of codeine metabolism in an urban population of children and its implications for analgesic reliability. British journal of anaesthesia. 2002. Williams D G, 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
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, 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
Clinical pharmacokinetics of fluvastatin. Clinical pharmacokinetics. 2001. Scripture C D, 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
Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica; the fate of foreign compounds in biological systems. 1998. Tassaneeyakul W, 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
In vivo inhibition profile of cytochrome P450TB (CYP2C9) by (+/-)-fluvastatin. Clinical pharmacology and therapeutics. 1995. Transon C, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0781-5017-01
DrugBank:
DB00586
PDB:
DIF
ChEBI:
4507
KEGG Compound:
C01690
PubChem Compound:
3033
PubChem Substance:
46504644
4831
Drugs Product Database (DPD):
2241225
BindingDB:
13066
ChemSpider:
2925
HET:
DIF
Therapeutic Targets Database:
DAP000620
FDA Drug Label at DailyMed:
a0a86ecf-e6fe-4c85-ac60-f62fd63e2590

Clinical Trials

These are trials that mention diclofenac 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.