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Identification
NameDexamethasone
Accession NumberDB01234  (APRD00674)
Typesmall molecule
Groupsapproved, investigational
Description

An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
1-Dehydro-16α-methyl-9α-fluorohydrocortisoneNot AvailableNot Available
16α-Methyl-9α-fluoro-1-dehydrocortisolNot AvailableNot Available
9α-Fluoro-16α-methylprednisoloneNot AvailableNot Available
DexametasonaSpanishINN
DexamethasonumLatinINN
Salts
Name/CAS Structure Properties
Dexamethasone acetate
Thumb
  • InChI Key: AKUJBENLRBOFTD-RPRRAYFGSA-N
  • Monoisotopic Mass: 434.210466929
  • Average Mass: 434.4977
DBSALT000383
Dexamethasone sodium phosphate
Thumb
  • InChI Key: PLCQGRYPOISRTQ-FCJDYXGNSA-L
  • Monoisotopic Mass: 516.130121939
  • Average Mass: 516.4046
DBSALT000843
Brand names
NameCompany
BaycadronNot Available
DecadronSidus
MaxidexNot Available
OZURDEXNot Available
Brand mixtures
Brand NameIngredients
CiprodexCiprofloxacin (Ciprofloxacin Hydrochloride) + Dexamethasone
DioptrolDexamethasone + Neomycin Sulfate + Polymyxin B Sulfate
Endomethasone IvoryDexamethasone + Hydrocortisone Acetate + Paraformaldehyde + Thymol Iodide
MaxitrolDexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate
MethedexPolymyxin B Sulfate + Neomycin + Dexamethasone
NEO-POLY-DEXPolymyxin B Sulfate + Neomycin + Dexamethasone
Sandoz OpticortDexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin
Septomixine ForteDexamethasone + Halethazole Tartrate + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate + Tyrothricin
Sofracort Ear/Eye OintmentDexamethasone + Framycetin Sulfate + Gramicidin
Sofracort Eye/Ear DropsDexamethasone Sodium Metasulphobenzoate + Framycetin Sulfate + Gramicidin
Sofracort Sterile Ear/Eye DropsDexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin
Sofracort Sterile Ear/Eye OintmentDexamethasone + Framycetin Sulfate + Gramicidin
TobradexDexamethasone + Tobramycin
Categories
CAS number50-02-2
WeightAverage: 392.4611
Monoisotopic: 392.199902243
Chemical FormulaC22H29FO5
InChI KeyUREBDLICKHMUKA-CXSFZGCWSA-N
InChI
InChI=1S/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1
IUPAC Name
(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassLipids
ClassSteroids and Steroid Derivatives
SubclassGluco/mineralocorticoids, Progestogins and Derivatives
Direct parentGluco/mineralocorticoids, Progestogins and Derivatives
Alternative parentsHydroxysteroids; Ketosteroids; Halogenated Steroids; Iridoids and Derivatives; Cyclohexanols; Tertiary Alcohols; Cyclic Alcohols and Derivatives; Ketones; Fluorohydrins; Polyamines; Enolates; Primary Alcohols; Organofluorides; Alkyl Fluorides; Aldehydes
Substituents3-keto-steroid; 20-keto-steroid; 9-halo-steroid; 17-hydroxy-steroid; 11-hydroxy-steroid; 11-noriridane monoterpene; monoterpene; cyclohexanol; tertiary alcohol; cyclic alcohol; secondary alcohol; ketone; halohydrin; fluorohydrin; polyamine; enolate; primary alcohol; alcohol; organofluoride; organohalogen; carbonyl group; alkyl halide; alkyl fluoride; aldehyde
Classification descriptionThis compound belongs to the gluco/mineralocorticoids, progestogins and derivatives. These are steroids whose structure is based on an hydroxylated prostane moiety.
Pharmacology
IndicationInjection: 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.
Ophthalmic ointment and solution: for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.
Ophthalmic solution only: for the treatment of steroid responsive inflammatory conditions of the external auditory meatus
Topic cream: for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
Oral aerosol: for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy
Intranasal aerosol: for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps
PharmacodynamicsDexamethasone 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.
Mechanism of actionDexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. This complex binds to DNA elements (glucocorticoid response elements) which 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 A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Absorption80-90%
Volume of distributionNot Available
Protein binding70%
Metabolism

Hepatic.

SubstrateEnzymesProduct
Dexamethasone
6-beta-hydroxydexamethasoneDetails
Route of eliminationNot Available
Half life36-54 hours
ClearanceNot Available
ToxicityOral, rat LD50: >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.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.992
Blood Brain Barrier + 0.9781
Caco-2 permeable + 0.8304
P-glycoprotein substrate Substrate 0.7862
P-glycoprotein inhibitor I Non-inhibitor 0.8112
P-glycoprotein inhibitor II Non-inhibitor 0.8134
Renal organic cation transporter Non-inhibitor 0.7971
CYP450 2C9 substrate Non-substrate 0.8733
CYP450 2D6 substrate Non-substrate 0.9115
CYP450 3A4 substrate Substrate 0.7315
CYP450 1A2 substrate Non-inhibitor 0.938
CYP450 2C9 substrate Non-inhibitor 0.9106
CYP450 2D6 substrate Non-inhibitor 0.9231
CYP450 2C19 substrate Non-inhibitor 0.9247
CYP450 3A4 substrate Non-inhibitor 0.8308
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9169
Ames test Non AMES toxic 0.9132
Carcinogenicity Non-carcinogens 0.9399
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.1482 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9558
hERG inhibition (predictor II) Inhibitor 0.5091
Pharmacoeconomics
Manufacturers
  • Allergan herbert div allergan inc
  • Merck and co inc
  • Roxane laboratories inc
  • Alpharma us pharmaceuticals division
  • Sti pharma llc
  • Wockhardt eu operations (swiss) ag
  • Organon usa inc
  • Allergan inc
  • Watson laboratories inc
  • Alcon laboratories inc
  • Ecr pharmaceuticals
  • Impax laboratories inc
  • Mutual pharmaceutical co inc
  • Par pharmaceutical inc
  • Phoenix laboratories inc
  • Private formulations inc
  • Sandoz inc
  • Upsher smith laboratories inc
  • Whiteworth towne paulsen inc
  • Solvay pharmaceuticals
  • Merck research laboratories div merck co inc
  • Ucb inc
  • Central pharmaceuticals inc
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Akorn inc
  • Akorn strides llc
  • Baxter healthcare corp anesthesia and critical care
  • Bel mar laboratories inc
  • Dell laboratories inc
  • International medication systems ltd
  • Luitpold pharmaceuticals inc
  • Teva parenteral medicines inc
  • Wyeth ayerst laboratories
  • Pharmafair inc
  • Sola barnes hind
  • Alcon universal ltd
  • Bausch and lomb pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
ElixirOral
LiquidIntramuscular
LiquidIntravenous
LiquidOral
OintmentOphthalmic
SolutionIntravenous
SolutionOphthalmic
Solution / dropsOphthalmic
TabletOral
Prices
Unit descriptionCostUnit
Ozurdex 0.7 mg implant1554.0USDimplant
Maxidex 0.1% Suspension 15ml Bottle97.96USDbottle
Maxitrol 0.1-5-10000 Ointment 3.5 gm Tube87.3USDtube
Maxitrol 5-10000-0.1 Suspension 5ml Bottle75.88USDbottle
Maxidex 0.1% Suspension 5ml Bottle53.57USDbottle
Dexamethasone Sodium Phosphate 4 mg/ml Solution (1 Box = 25x1ml Vials)41.99USDbox
Dexamethasone micronized powd41.31USDg
Dexamethasone powder21.27USDg
Dexamethasone Sodium Phosphate 0.1% Solution 5ml Bottle19.99USDbottle
Dexamethasone acetate powd15.12USDg
Dexamethasone sod ph powder14.24USDg
Dexamethasone Sodium Phosphate 4 mg/ml Solution 5ml Vial13.99USDvial
Dexamethasone Sodium Phosphate 10 mg/ml4.78USDml
Dexamethasone Sodium Phosphate 4 mg/ml 1 Vial = 5ml4.0USDml
Dexamethasone 0.1% eye drop3.43USDml
Dexasol 0.1% eye drops3.38USDml
Maxidex 0.1 % Ointment2.69USDg
Dexamethasone 10 mg/ml vial2.56USDml
Maxidex 0.1% eye drops2.36USDml
Dexamethasone Sodium Phosphate 4 mg/ml1.77USDml
Maxidex 0.1 % Suspension1.73USDml
Sandoz Dexamethasone Sod. Phosphate 0.1 % Solution1.38USDml
Pms-Dexamethasone Sodium Phosp 10 mg/ml1.34USDml
Dexamethasone 4 mg/ml vial1.04USDml
Dexamethasone 6 mg tablet1.01USDtablet
Dexasone 4 mg Tablet0.86USDtablet
Apo-Dexamethasone 4 mg Tablet0.8USDtablet
Pms-Dexamethasone 4 mg Tablet0.8USDtablet
Ratio-Dexamethasone 4 mg Tablet0.8USDtablet
Dexamethasone 2 mg tablet0.68USDtablet
Dexamethasone 1 mg/1 ml soln0.65USDml
Dexamethasone 4 mg tablet0.6USDtablet
Dexamethasone 1 mg tablet0.49USDtablet
Pms-Dexamethasone 0.75 mg Tablet0.47USDtablet
Pms-Dexamethasone 2 mg Tablet0.43USDtablet
Dexamethasone 0.5 mg/5ml Elixir0.4USDml
Dexamethasone 0.75 mg tablet0.38USDtablet
Dexamethasone 1.5 mg tablet0.35USDtablet
Dexamethasone 0.5 mg tablet0.31USDtablet
Apo-Dexamethasone 0.5 mg Tablet0.21USDtablet
Pms-Dexamethasone 0.5 mg Tablet0.2USDtablet
Ratio-Dexamethasone 0.5 mg Tablet0.18USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States68997172003-11-012023-11-01
United States67269182000-10-202020-10-20
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point170-229Fried, J.; US. Patent 2,852.51 1; September 16, 1958; assigned to Olin Mathieson Chemical Corporation. Muller, G., Bardoneschi, R. and Jolly, J.; U.S. Patent 3,007,923; November 7, 1961; assigned to Les Laboratories Francais de Chimiotherapie, France.
water solubility89 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.83HANSCH,C ET AL. (1995)
logS-3.64ADME Research, USCD
Caco2 permeability-4.75ADME Research, USCD
Predicted Properties
PropertyValueSource
water solubility5.05e-02 g/lALOGPS
logP1.93ALOGPS
logP1.68ChemAxon
logS-3.9ALOGPS
pKa (strongest acidic)12.42ChemAxon
pKa (strongest basic)-3.3ChemAxon
physiological charge0ChemAxon
hydrogen acceptor count5ChemAxon
hydrogen donor count3ChemAxon
polar surface area94.83ChemAxon
rotatable bond count2ChemAxon
refractivity102.49ChemAxon
polarizability40.83ChemAxon
number of rings4ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Fried, J.; US. Patent 2,852.51 1; September 16, 1958; assigned to Olin Mathieson Chemical Corporation.
Muller, G., Bardoneschi, R. and Jolly, J.; U.S. Patent 3,007,923; November 7, 1961; assigned to Les Laboratories Francais de Chimiotherapie, France.

General ReferenceNot Available
External Links
ResourceLink
KEGG DrugD00292
PubChem Compound5743
PubChem Substance46508930
ChemSpider5541
BindingDB18207
ChEBI41879
ChEMBLCHEMBL384467
Therapeutic Targets DatabaseDAP000007
PharmGKBPA449247
IUPHAR2768
Guide to Pharmacology2768
HETDEX
Drug Product Database664227
RxListhttp://www.rxlist.com/cgi/generic/dexameth.htm
Drugs.comhttp://www.drugs.com/cdi/dexamethasone-drops.html
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dec1118.shtml
WikipediaDexamethasone
ATC CodesA01AC02C05AA09D07AB19D07XB05D10AA03H02AB02R01AD03S01BA01S01CB01S02BA06S03BA01
AHFS Codes
  • 52:08.08
  • 68:04.00
PDB EntriesNot Available
FDA labelshow(96 KB)
MSDSshow(74.8 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe corticosteroid, dexamethasone, alters the anticoagulant effect, acenocoumarol.
Acetylsalicylic acidThe corticosteroid, dexamethasone, may decrease the effect of the salicylate, acetylsalicylic acid.
AmbenoniumThe corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, ambenonium.
AminoglutethimideAminoglutethimide may decrease the effect of dexamethasone.
AmobarbitalThe barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
AnisindioneThe corticosteroid, dexamethasone, alters the anticoagulant effect of anisindione.
AprepitantAprepitant may increase the effect and toxicity of dexamethasone.
AprobarbitalThe barbiturate, aprobarbital, may decrease the effect of the corticosteroid, dexamethasone.
ButabarbitalThe barbiturate, butabarbital, may decrease the effect of the corticosteroid, dexamethasone.
ButalbitalThe barbiturate, butalbital, may decrease the effect of the corticosteroid, dexamethasone.
ButethalThe barbiturate, butethal, may decrease the effect of the corticosteroid, dexamethasone.
Dabigatran etexilateP-Glycoprotein inducers such as dexamethasone may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
DicoumarolThe corticosteroid, dexamethasone, alters the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturateThe barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
EdrophoniumThe corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, edrophonium.
Estradiol valerate/DienogestAffects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
EthotoinThe enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, dexamethasone.
FosphenytoinThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, dexamethasone.
HeptabarbitalThe barbiturate, heptabarbital, may decrease the effect of the corticosteroid, dexamethasone.
HexobarbitalThe barbiturate, hexobarbital, may decrease the effect of the corticosteroid, dexamethasone.
ImatinibDexamethasone may decrease levels of imatinib.
LurasidoneConcomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated. Will decrease Cmax of lurasidone by 85%.
Magnesium salicylateThe corticosteroid, dexamethasone, may decrease the effect of magnesium salicylate.
MephenytoinThe enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, dexamethasone.
MethohexitalThe barbiturate, methohexital, may decrease the effect of the corticosteroid, dexamethasone.
MethylphenobarbitalThe barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
MidodrineIncreased arterial pressure
NeostigmineThe corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine.
PentobarbitalThe barbiturate, pentobarbital, may decrease the effect of the corticosteroid, dexamethasone.
PhenobarbitalThe barbiturate, phenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
PhenytoinThe enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, dexamethasone.
PrimidoneThe barbiturate, primidone, may decrease the effect of the corticosteroid, dexamethasone.
PyridostigmineThe corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Quinidine barbiturateThe barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
RifampicinThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, dexamethasone.
RilpivirineStrong inducers of CYP3A4 decrease the exposure of rilpivirine thus decreasing efficacy.
RoflumilastAffects CYP3A4 metabolism, decreases level or effect of roflumilast.
SalsalateThe corticosteroid, dexamethasone, may decrease the effect of the salicylate, salsalate.
SecobarbitalThe barbiturate, secobarbital, may decrease the effect of the corticosteroid, dexamethasone.
SunitinibPossible decrease in sunitinib levels
TacrineTacrine and Dexamethasone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
TalbutalThe barbiturate, talbutal, may decrease the effect of the corticosteroid, dexamethasone.
TelithromycinCo-administration may cause decreased Telithromycin and increased Dexamethasone plasma concentrations. Consider alternate therapy.
TemsirolimusDexamethasone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
ThalidomideIncreased risk of dermatologic adverse effects and venous thromboembolic events (VTE). Consider VTE prophylaxis during concomitant therapy and monitor for adverse dematologic effects.
TramadolDexamethasone may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
TrazodoneThe CYP3A4 inducer, Dexamethasone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Dexamethasone is initiated, discontinued or dose changed.
VandetanibDecreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
VecuroniumVecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Dexamethasone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of dexamethasone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of dexamethasone if voriconazole is initiated, discontinued or dose changed.
WarfarinThe corticosteroid, dexamethasone, alters the anticoagulant effect of warfarin.
Food Interactions
  • Avoid alcohol.
  • Avoid taking with grapefruit juice.
  • Take with food to reduce irritation.

Targets

1. Glucocorticoid receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Glucocorticoid receptor P04150 Details

References:

  1. Warne JP, John CD, Christian HC, Morris JF, Flower RJ, Sugden D, Solito E, Gillies GE, Buckingham JC: Gene deletion reveals roles for annexin A1 in the regulation of lipolysis and IL-6 release in epididymal adipose tissue. Am J Physiol Endocrinol Metab. 2006 Dec;291(6):E1264-73. Epub 2006 Jul 11. Pubmed
  2. Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. Pubmed
  3. Funato H, Kobayashi A, Watanabe Y: Differential effects of antidepressants on dexamethasone-induced nuclear translocation and expression of glucocorticoid receptor. Brain Res. 2006 Oct 30;1117(1):125-34. Epub 2006 Sep 7. Pubmed
  4. Vaitkuviene A, Ulinskaite A, Meskys R, Duburs G, Klusa V, Liutkevicius E: Study of the interaction of 1,4-dihydropyridine derivatives with glucocorticoid hormone receptors from the rat liver. Pharmacol Rep. 2006 Jul-Aug;58(4):551-8. Pubmed
  5. Wang D, Zhang H, Lang F, Yun CC: Acute activation of NHE3 by dexamethasone correlates with activation of SGK1 and requires a functional glucocorticoid receptor. Am J Physiol Cell Physiol. 2007 Jan;292(1):C396-404. Epub 2006 Sep 13. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Nuclear receptor subfamily 0 group B member 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: stimulator

Components

Name UniProt ID Details
Nuclear receptor subfamily 0 group B member 1 P51843 Details

References:

  1. Gummow BM, Scheys JO, Cancelli VR, Hammer GD: Reciprocal regulation of a glucocorticoid receptor-steroidogenic factor-1 transcription complex on the Dax-1 promoter by glucocorticoids and adrenocorticotropic hormone in the adrenal cortex. Mol Endocrinol. 2006 Nov;20(11):2711-23. Epub 2006 Jul 20. Pubmed
  2. Yu CC, Li PH: In vivo inhibition of steroidogenic acute regulatory protein expression by dexamethasone parallels induction of the negative transcription factor DAX-1. Endocrine. 2006 Dec;30(3):313-23. Pubmed

3. Annexin A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
Annexin A1 P04083 Details

References:

  1. Morand EF, Hall P, Hutchinson P, Yang YH: Regulation of annexin I in rheumatoid synovial cells by glucocorticoids and interleukin-1. Mediators Inflamm. 2006;2006(2):73835. Pubmed
  2. John CD, Theogaraj E, Christian HC, Morris JF, Smith SF, Buckingham JC: Time-specific effects of perinatal glucocorticoid treatment on anterior pituitary morphology, annexin 1 expression and adrenocorticotrophic hormone secretion in the adult female rat. J Neuroendocrinol. 2006 Dec;18(12):949-59. Pubmed
  3. Davies E, Omer S, Buckingham JC, Morris JF, Christian HC: Expression and externalization of annexin 1 in the adrenal gland: structure and function of the adrenal gland in annexin 1-null mutant mice. Endocrinology. 2007 Mar;148(3):1030-8. Epub 2006 Dec 7. Pubmed
  4. Wang C, Wang J, Guo HF, Liu RY: Involvement of annexin I in the dexamethasone-mediated upregulation of A549 cells phagocytosis of apoptotic eosinophils. Immunol Lett. 2007 Aug 15;111(2):103-10. Epub 2007 Jul 2. Pubmed

4. Nitric oxide synthase, inducible

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: negative modulator

Components

Name UniProt ID Details
Nitric oxide synthase, inducible P35228 Details

References:

  1. Soderberg M, Raffalli-Mathieu F, Lang MA: Regulation of the murine inducible nitric oxide synthase gene by dexamethasone involves a heterogeneous nuclear ribonucleoprotein I (hnRNPI) dependent pathway. Mol Immunol. 2007 May;44(12):3204-10. Epub 2007 Mar 26. Pubmed
  2. Huang H, Lavoie-Lamoureux A, Moran K, Lavoie JP: IL-4 stimulates the expression of CXCL-8, E-selectin, VEGF, and inducible nitric oxide synthase mRNA by equine pulmonary artery endothelial cells. Am J Physiol Lung Cell Mol Physiol. 2007 May;292(5):L1147-54. Pubmed
  3. Nandi J, Saud B, Zinkievich JM, Palma DT, Levine RA: 5-Aminosalicylic Acid Improves Indomethacin-Induced Enteropathy by Inhibiting iNOS Transcription in Rats. Dig Dis Sci. 2007 May 15;. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. Pubmed

2. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inducer

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cholesterol side-chain cleavage enzyme, mitochondrial

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cholesterol side-chain cleavage enzyme, mitochondrial P05108 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Steroid 17-alpha-hydroxylase/17,20 lyase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Steroid 17-alpha-hydroxylase/17,20 lyase P05093 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 19A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 19A1 P11511 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 1B1 Q16678 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

11. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

12. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

13. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

14. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

15. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

16. Cytochrome P450 3A43

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A43 Q9HB55 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

17. Cytochrome P450 4A11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 4A11 Q02928 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Transporters

1. Bile salt export pump

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Bile salt export pump O95342 Details

References:

  1. Fardel O, Payen L, Courtois A, Vernhet L, Lecureur V: Regulation of biliary drug efflux pump expression by hormones and xenobiotics. Toxicology. 2001 Oct 5;167(1):37-46. Pubmed

2. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. Pubmed
  2. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. Pubmed
  3. Schuetz JD, Silverman JA, Thottassery JV, Furuya KN, Schuetz EG: Divergent regulation of the class II P-glycoprotein gene in primary cultures of hepatocytes versus H35 hepatoma by glucocorticoids. Cell Growth Differ. 1995 Oct;6(10):1321-32. Pubmed
  4. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. Pubmed
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. Pubmed
  6. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. Pubmed
  7. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. Pubmed
  8. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, Borst P: Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest. 1995 Oct;96(4):1698-705. Pubmed

3. Canalicular multispecific organic anion transporter 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 1 Q92887 Details

References:

  1. Demeule M, Jodoin J, Beaulieu E, Brossard M, Beliveau R: Dexamethasone modulation of multidrug transporters in normal tissues. FEBS Lett. 1999 Jan 15;442(2-3):208-14. Pubmed
  2. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. Pubmed

4. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

References:

  1. Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. Pubmed
  2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. Pubmed

5. ATP-binding cassette sub-family G member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. Elahian F, Kalalinia F, Behravan J: Evaluation of indomethacin and dexamethasone effects on BCRP-mediated drug resistance in MCF-7 parental and resistant cell lines. Drug Chem Toxicol. 2010 Apr;33(2):113-9. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on April 10, 2014 13:59