PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
dexamethasone

2D structure

Overview

Generic Names: DEX; DXM; Desametasone; Desametasone [Dcit]; Desamethasone; Dexametasona [INN-Spanish]; Dexamethasone Acetate; Dexamethasone Alcohol; Dexamethasone Base; Dexamethasone Sodium Phosphate; Dexamethasonum [INN-Latin]; Dexamethazone; Dxms; Fluormethylprednisolone; dexamethasone
Trade Names: Adexone; Aeroseb-D; Aeroseb-Dex; Anaflogistico; Aphtasolon; Aphthasolone; Auxiron; Azium; Bisu Ds; Calonat; Corson; Corsone; Cortisumman; Decacort; Decacortin; Decaderm; Decadron; Decadron Tablets, Elixir; Decadron-La; Decagel; Decalix; Decasone; Decaspray; Dectancyl; Dekacort; Deltafluorene; Dergramin; Deronil; Desadrene; Desameton; Deseronil; Dex-Ide; Dexa; Dexa Mamallet; Dexa-Cortidelt; Dexa-Cortisyl; Dexa-Mamallet; Dexa-Scheroson; Dexa-Sine; Dexacen-4; Dexacidin; Dexacort; Dexacortal; Dexacortin; Dexadeltone; Dexafarma; Dexair; Dexalona; Dexaltin; Dexameth; Dexamethasone Intensol; Dexamonozon; Dexapolcort; Dexapos; Dexaprol; Dexason; Dexasone; Dexinolon; Dexinoral; Dexone; Dexone 0.5; Dexone 0.75; Dexone 1.5; Dexone 4; Dexonium; Dextelan; Dezone; Dinormon; Fluormone; Fluorocort; Fortecortin; Gammacorten; Hexadecadrol; Hexadrol; Hexadrol Elixir; Hexadrol Tablets; Hl-Dex; IontoDex; Isopto-Dex; Lokalison F; Loverine; Luxazone; Maxidex; Maxitrol; Mediamethasone; Mexidex; Millicorten; Mymethasone; Ocu-Trol; Oradexon; Pet Derm Iii; Pet-Derm Iii; Policort; Posurdex; Prednisolon F; Prednisolone F; Sk-Dexamethasone; Spoloven; Sunia Sol D; Superprednol; Turbinaire; Visumetazone
Brand Mixtures: Ak Trol Suspension (Dexamethasone + Neomycin Sulfate + Polymyxin B Sulfate); Ciprodex (Ciprofloxacin (Ciprofloxacin Hydrochloride) + Dexamethasone); Cresophene Liq (Camphor + Chlorophenol + Dexamethasone + Thymol); Dioptrol Ointment (Dexamethasone + Neomycin Sulfate + Polymyxin B Sulfate); Dioptrol Suspension (Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate); Endomethasone Ivory (Dexamethasone + Hydrocortisone Acetate + Paraformaldehyde + Thymol Iodide); Maxitrol (Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate); Maxitrol Ont (Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate); Naquasone Bolus (Dexamethasone + Trichlormethiazide); Naquasone Inj (Dexamethasone + Trichlormethiazide); Neodecadron Eye Ear Soln 0.1% (Dexamethasone Phosphate (Dexamethasone Sodium Phosphate) + Neomycin Sulfate); Pendamine (Chlorpheniramine Maleate + Dexamethasone + Dihydrostreptomycin Sulfate + Penicillin G Procaine); Sandoz Opticort (Dexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin); Septomixine Forte (Dexamethasone + Halethazole Tartrate + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate + Tyrothricin); Sofracort Ear/Eye Ointment (Dexamethasone + Framycetin Sulfate + Gramicidin); Sofracort Eye/Ear Drops (Dexamethasone Sodium Metasulphobenzoate + Framycetin Sulfate + Gramicidin); Sofracort Sterile Ear/Eye Drops (Dexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin); Sofracort Sterile Ear/Eye Ointment (Dexamethasone + Framycetin Sulfate + Gramicidin); Tobradex Oph Ointment (Dexamethasone + Tobramycin); Tobradex Oph Sus (Dexamethasone + Tobramycin); Tresaderm Dermatologic Solution (Dexamethasone + Neomycin (Neomycin Sulfate) + Thiabendazole)
PharmGKB Accession Id: PA449247

Description

An anti-inflammatory 9-fluoro-glucocorticoid. PubChem (source: Drug Bank)

Indication

<B>Injection:</B> for the treatment of endocrine disorders, rheumatic D=disorders, collagen diseases, dermatologic diseases, allergic statesc, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, cerebral edema.
<br><B>Ophthalmic ointment and solution:</B> for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.
<br><B>Ophthalmic solution only:</B> for the treatment of steroid responsive inflammatory conditions of the external auditory meatus
<br><B>Topic cream:</B> for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
<br><B>Oral aerosol:</B> for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy
<br><B>Intranasal aerosol:</B> for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps (source: Drug Bank)

ATC Therapeutic Categories

  • A01AC:Corticosteroids for local oral treatment
  • C05AA:Corticosteroids
  • D07AB:Corticosteroids, moderately potent (group II)
  • D07XB:Corticosteroids, moderately potent, other combinations
  • D10AA:Corticosteroids, combinations for treatment of acne
  • H02AB:Glucocorticoids
  • R01AD:Corticosteroids
  • S01BA:Corticosteroids, plain
  • S01CB:Corticosteroids/antiinfectives/mydriatics in combination
  • S02BA:Corticosteroids
  • S03BA:Corticosteroids

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. This results in a modification of transcription and, hence, protein synthesis in order to achieve inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of dexamethasone are thought to involve phospholipase A<sub>2</sub> inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. (source: Drug Bank)

Pharmacology

Dexamethasone and its derivatives, dexamethasone sodium phosphate and dexamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties and ability to penetrate the CNS, dexamethasone is used alone to manage cerebral edema and with tobramycin to treat corticosteroid-responsive inflammatory ocular conditions. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid taking with grapefruit juice.
Take with food to reduce irritation. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. (source: Drug Bank)

Protein Binding

70% (source: Drug Bank)

Absorption

80-90% (source: Drug Bank)

Toxicity

Oral, rat LD<sub>50</sub>: >3 gm/kg. Signs of overdose include retinal toxicity, glaucoma, subcapsular cataract, gastrointestinal bleeding, pancreatitis, aseptic bone necrosis, osteoporosis, myopathies, obesity, edemas, hypertension, proteinuria, diabetes, sleep disturbances, psychiatric syndromes, delayed wound healing, atrophy and fragility of the skin, ecchymosis, and pseudotumor cerebri. (source: Drug Bank)

Isomeric SMILES Code:

C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@]1(C(=O)CO)O)C)O)F)C (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs2032582 at chr7:86998554 in ABCB1
    In multiple myeloma patients treated with dexamethasone, doxorubicin, and vincristine, followed by autologous stem cell transformation (ASCT), treatment efficacy was not related to this variant. However, the overall survival of patients with the G/G genotype of this variant was significantly lower than that of patients carrying T/T or G/T alleles. In ASCT nonresponders, diplotype analysis of this variant together with another variant (ABCB1 C3435T) showed that GC/GC patients survived for less time than GC/TT and TT/TT patients.
    Variant Name:
    MDR1 G2677T/A, MDR1 (2677G, 893 Ala), MDR1 (2677T, 893 Ser), MDR1 (2677A, 893 Thr)
    Related Drugs:
    dexamethasone, doxorubicin, vincristine
    Related Diseases:
    Multiple Myeloma
    Evidence:
    PMID:18408561
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 Has annotations
ABCB1
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
BIRC3
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
CYP2A6
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2B6
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP2C8
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP2E1
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP3A43
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP3A7
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GSTM1
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
GSTP1
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GSTT1
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
IL10
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL13
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
IL1A
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
IL3
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL5
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
IL6
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
MTHFR
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
NR3C1
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
Phenotype data available No genotype data Literature annotations available Has annotations
PTGS2
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SAA1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SAA2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
SLC19A1
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
TNF
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
TPMT
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
TYMS
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
UGT1A1
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
VDR
  • CO
  • PD
  • PK
  •   
  • GN
Publications

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

Drug Targets

Gene Description
ANXA1 Uncurated Annotation (source: Drug Bank)
CXCL12 Uncurated Annotation (source: Drug Bank)
NOS2 Uncurated Annotation (source: Drug Bank)
NFKB1 Uncurated Annotation (source: Drug Bank)
NR0B1 Uncurated Annotation (source: Drug Bank)
NR3C1 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
cyclophosphamide
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
erythromycin
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
sorafenib
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
testosterone
  •   
  •   
  • PK
  •   
  •   
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 corticosteroid alters the anticoagulant effect (source: Drug Bank)
aminoglutethimide Uncurated Annotation Aminogluthetimide decreases the effect of dexamethasone (source: Drug Bank)
amobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
aspirin Uncurated Annotation The corticosteroid decreases the effect of salicylates (source: Drug Bank)
butalbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
dicumarol Uncurated Annotation The corticosteroid alters the anticoagulant effect (source: Drug Bank)
edrophonium Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
hexobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
imatinib Uncurated Annotation Decreases levels of imatinib (source: Drug Bank)
mephenytoin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
methylphenobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
neostigmine Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
pentobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
phenobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
phenytoin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
primidone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pyridostigmine Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
rifampin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
salicylate-magnesium Uncurated Annotation The corticosteroid decreases the effect of salicylates (source: Drug Bank)
sunitinib Uncurated Annotation Possible decrease in sunitinib levels (source: Drug Bank)
warfarin Uncurated Annotation The corticosteroid alters the anticoagulant effect (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Amyloidosis
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Asthma
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Fatigue Syndrome, Chronic
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Glaucoma
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
HIV Seropositivity
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Meningitis, Bacterial
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Multiple Myeloma
  • CO
  •   
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Precursor Cell Lymphoblastic Leukemia-Lymphoma
  • CO
  • PD
  • PK
  •   
  • 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. Pharmacogenetic Risk Factors for Osteonecrosis of the Hip Among Children With Leukemia
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • CO
    Submitted by Mary Relling, PharmD involving ABCB1, CYP3A4, CYP3A5, GSTM1, GSTP1, GSTT1, MTHFR, NR3C1, SLC19A1, TPMT, TYMS, UGT1A1, VDR, dexamethasone, methotrexate, prednisone, , Osteonecrosis and Precursor Cell Lymphoblastic Leukemia-Lymphoma

Additional Datasets

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

  1. Osteonecrosis in Children with Acute Lymphoblastic Leukemia: A Report from the Children's Oncology Group
  2. Physicochemical determinants of human renal clearance
  3. SWI/SNF chromatin-remodeling complex and glucocorticoid resistance in acute lymphoblastic leukemia
  4. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01234
KEGG Drug ID:
D00292
PubChem Compound ID:
5743

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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