Identification

Name
Dexamethasone
Accession Number
DB01234
Description

Dexamethasone, or MK-125, is a corticosteroid fluorinated at position 9 used to treat endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions.12 Developed in 1957, it is structurally similar to other corticosteroids like hydrocortisone and prednisolone.9

Dexamethasone was granted FDA approval on 30 October 1958.10 In a press release for the Randomized Evaluation of COVID-19 Therapy (RECOVERY) trial on 16 June 2020, dexamethasone was recommended for use in COVID-19 patients with severe respiratory symptoms. Dexamethasone reduced deaths by approximately one third in patients requiring ventilation and by one fifth in those requiring oxygen.21

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 392.4611
Monoisotopic: 392.199902243
Chemical Formula
C22H29FO5
Synonyms
  • 1-Dehydro-16alpha-methyl-9alpha-fluorohydrocortisone
  • 1-Dehydro-16α-methyl-9α-fluorohydrocortisone
  • 16alpha-Methyl-9alpha-fluoro-1-dehydrocortisol
  • 16α-Methyl-9α-fluoro-1-dehydrocortisol
  • 9alpha-Fluoro-16alpha-methylprednisolone
  • 9α-Fluoro-16α-methylprednisolone
  • Dexametasona
  • Dexamethasone
  • Dexaméthasone
  • Dexamethasonum
External IDs
  • ISV-305
  • NSC-34521
  • OTO-104

Pharmacology

Indication

Dexamethasone and ciprofloxacin otic suspension is indicated for bacterial infections with inflammation in acute otitis media and acute otitis externa.11 Intramuscular and intravenous injections are indicated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions.12 Oral tablets are indicated for the treatment of multiple myeloma.15 An intravitreal implant is indicated for some forms of macular edema and non-infectious posterior uveitis affecting the posterior of the eye.18 Various ophthalmic formulations are indicated for inflammatory conditions of the eye.13,14,16,17,19,20

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.3 Dexamethasone's duration of action varies depending on the route.11,12,13,14,15,16,17,18,19,20 Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces.3 Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.3

Mechanism of action

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.3 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.3

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.3

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.3 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.3

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
UNuclear receptor subfamily 0 group B member 1
stimulator
Humans
UAnnexin A1
agonist
Humans
UNitric oxide synthase, inducible
negative modulator
Humans
UNuclear receptor subfamily 1 group I member 2
agonist
Humans
Absorption

Absorption via the intramuscular route is slower than via the intravenous route.12 A 3mg intramuscular dose reaches a Cmax of 34.6±6.0ng/mL with a Tmax of 2.0±1.2h and an AUC of 113±38ng*h/mL.5 A 1.5mg oral dose reaches a Cmax of 13.9±6.8ng/mL with a Tmax of 2.0±0.5h and an AUC of 331±50ng*h/mL.5 Oral dexamethasone is approximately 70-78% bioavailable in healthy subjects.6

Volume of distribution

A 1.5mg oral dose of dexamethasone has a volume of distribution of 51.0L, while a 3mg intramuscular dose has a volume of distribution of 96.0L.5

Protein binding

Dexamethasone is approximately 77% protein bound in plasma.15 The majority of protein binding is with serum albumin.[A188559] Dexamethasone does not significantly bind to corticosteroid binding protein.[A188559]

Metabolism

Dexamethasone is 6-hydroxylated by CYP3A4 to 6α- and 6β-hydroxydexamethasone.1 Dexamethasone is reversibly metabolized to 11-dehydrodexamethasone by corticosteroid 11-beta-dehydrogenase isozyme 2 and can also be converted back to dexamethasone by Corticosteroid 11-beta-dehydrogenase isozyme 1.7,8

Hover over products below to view reaction partners

Route of elimination

Corticosteroids are generally eliminated predominantly in the urine.4 However, dexamethasone is <10% elminated in urine.15

Half-life

The mean terminal half life of a 20mg oral tablet is 4 hours.15 A 1.5mg oral dose of dexamethasone has a half life of 6.6±4.3h, while a 3mg intramuscular dose has a half life of 4.2±1.2h.5

Clearance

A 20mg oral tablet has a clearance of 15.7L/h.15 A 1.5mg oral dose of dexamethasone has a clearance of 15.6±4.9L/h while a 3.0mg intramuscular dose has a clearance of 9.9±1.4L/h.5

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

The oral LD50 in female mice was 6.5g/kg and 794mg/kg via the intravenous route.12

Overdoses are not expected with otic formulations.11 Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.2 Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.2

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Dexamethasone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Abatacept can be increased when combined with Dexamethasone.
AbemaciclibDexamethasone may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Dexamethasone.
AcalabrutinibThe metabolism of Dexamethasone can be increased when combined with Acalabrutinib.
AcarboseThe risk or severity of hyperglycemia can be increased when Dexamethasone is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Dexamethasone is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Dexamethasone is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Dexamethasone.
AcetaminophenDexamethasone may increase the hepatotoxic activities of Acetaminophen.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Products

Product Ingredients
IngredientUNIICASInChI Key
Dexamethasone phosphate2BP70L44PR312-93-6VQODGRNSFPNSQE-CXSFZGCWSA-N
Dexamethasone sodium phosphateAI9376Y64P2392-39-4PLCQGRYPOISRTQ-UHFFFAOYSA-L
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accufix II Dec Model 033-212ImplantTelectronics Pacing Systems Inc.1994-12-311999-08-27Canada flag
DecadronTablet0.5 mg/1OralMerck Sharp & Dohme Corp.1958-10-302007-11-30US flag
DecadronTablet0.75 mg/1OralMerck Sharp & Dohme Corp.1958-10-302007-11-30US flag
Decadron Phosphate Eye Ear Sol 0.1%LiquidAuricular (otic); OphthalmicMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1960-12-311998-04-21Canada flag
Decadron Phosphate Inj 4mg/mlLiquidIntramuscular; IntravenousMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1959-12-312001-08-01Canada flag
Decadron Tab 0.5mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1958-12-312002-07-29Canada flag
Decadron Tab 4mgTabletOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1976-12-312003-08-08Canada flag
DexamethasoneSolution0.1 %Auricular (otic); OphthalmicPharma Stulln Inc.1994-12-31Not applicableCanada flag
Dexamethasone Omega UnidoseSolutionIntramuscular; Intrasynovial; IntravenousOmega Laboratories Ltd2013-05-08Not applicableCanada flag
Dexamethasone Sod Phos Inj 4mg/mlLiquidIntramuscular; IntravenousTaro Pharmaceuticals, Inc.1989-12-312001-08-21Canada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-dexamethasoneTabletOralApotex Corporation2004-11-17Not applicableCanada flag
Apo-dexamethasoneTabletOralApotex Corporation2004-03-08Not applicableCanada flag
BaycadronElixir0.5 mg/5mLOralWockhardt1983-07-27Not applicableUS flag
DecadronTablet1.5 mg/1OralWraser Llc2017-09-112017-09-25US flag
DecadronTablet0.5 mg/1OralPragma Pharmaceuticals, LLC2018-02-28Not applicableUS flag
DecadronTablet4 mg/1OralPragma Pharmaceuticals, LLC2018-02-28Not applicableUS flag
DecadronElixir0.5 mg/5mLOralPragma Pharmaceuticals, LLC2018-03-15Not applicableUS flag
DecadronTablet0.75 mg/1OralPragma Pharmaceuticals, LLC2018-02-28Not applicableUS flag
DecadronTablet6 mg/1OralPragma Pharmaceuticals, LLC2018-02-28Not applicableUS flag
Decadron DPTablet1.5 mg/1OralXspire Pharma, Llc2017-09-112017-09-25US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
999 Itch ReliefDexamethasone (15 mg/20000mg) + Levomenthol (200 mg/20000mg) + Synthetic camphor (200 mg/20000mg)OintmentTopicalChina Resources Sanjiu Medical & Pharmaceutical Co., Ltd.2003-07-03Not applicableUS flag
AK-TrolDexamethasone (1 mg/1g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (10000 [USP'U]/1g)OintmentOphthalmicPhysicians Total Care, Inc.1996-01-052000-06-30US flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)Suspension / dropsAuricular (otic)Nucare Pharmaceuticals,inc.2003-08-04Not applicableUS flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)Suspension / dropsAuricular (otic)Novartis Pharmaceuticals Corporation2003-08-04Not applicableUS flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)SuspensionAuricular (otic)Rebel Distributors2003-08-15Not applicableUS flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)Suspension / dropsAuricular (otic)Proficient Rx LP2003-08-04Not applicableUS flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)Suspension / dropsAuricular (otic)Clinical Solutions Wholsesale2003-08-152017-06-28US flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)SuspensionAuricular (otic)Physicians Total Care, Inc.2004-09-21Not applicableUS flag
CiprodexDexamethasone (1 mg/1mL) + Ciprofloxacin hydrochloride (3 mg/1mL)Suspension / dropsAuricular (otic)ALCON LABORATORIES, INC.2003-08-04Not applicableUS flag
CiprodexDexamethasone (0.1 %) + Ciprofloxacin (0.3 %)SuspensionAuricular (otic)Novartis2004-05-13Not applicableCanada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Dex-MoxiDexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (5 mg/1mL)Injection, solutionOphthalmicImprimis Njof, Llc2018-01-05Not applicableUS flag
Dex-Moxi PFDexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (5 mg/1mL)Injection, solutionIntraocularImprimisRx NJ2018-01-01Not applicableUS flag
Dex-Moxi-KetorDexamethasone sodium phosphate (1 mg/1mL) + Ketorolac tromethamine (0.4 mg/1mL) + Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL)Injection, solutionOphthalmicImprimis Njof, Llc2018-01-05Not applicableUS flag
Dexamethasone Sodium Phosphate 0.1% / Finasteride 0.1% / Minoxidil 5%Dexamethasone sodium phosphate (0.1 g/100g) + Finasteride (0.1 g/100g) + Minoxidil (5 g/100g)SolutionTopicalSincerus Florida, LLC2019-05-09Not applicableUS flag
Dexamethasone Sodium Phosphate 0.1% / Finasteride 0.1% / Minoxidil 5% / Tretinoin 0.025%Dexamethasone sodium phosphate (0.1 g/100g) + Finasteride (0.1 g/100g) + Minoxidil (5 g/100g) + Tretinoin (0.025 g/100g)SolutionTopicalSincerus Florida2019-05-09Not applicableUS flag
Dexlido KitDexamethasone sodium phosphate (10 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitInfiltration; Intramuscular; Intravenous; TopicalAsclemed Usa, Inc.2014-07-25Not applicableUS flag
Dexlido-M KitDexamethasone sodium phosphate (10 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitEpidural; Infiltration; Intramuscular; Intravenous; TopicalAsclemed Usa, Inc.2014-07-25Not applicableUS flag
DexMoxiKetor PFDexamethasone sodium phosphate (1 mg/1mL) + Ketorolac tromethamine (0.4 mg/1mL) + Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL)Injection, solutionIntraocularImprimisRx NJ2018-01-01Not applicableUS flag
DexopinDexamethasone sodium phosphate (10 mg/1mL) + Povidone-iodine (10 mg/1mL) + Ropivacaine hydrochloride (5 mg/1mL)KitTopicalAsclemed Usa, Inc.2019-06-10Not applicableUS flag
Dmt SuikDexamethasone sodium phosphate (10 mg/1mL)Injection, solutionIntramuscular; IntravenousAsclemed Usa, Inc.2003-05-29Not applicableUS flag

Categories

ATC Codes
R01AD53 — Dexamethasone, combinationsD07XB05 — DexamethasoneR01AD03 — DexamethasoneD10AA03 — DexamethasoneS01CB01 — DexamethasoneS02CA06 — Dexamethasone and antiinfectivesS03CA01 — Dexamethasone and antiinfectivesC05AA09 — DexamethasoneS01CA01 — Dexamethasone and antiinfectivesD07CB04 — Dexamethasone and antibioticsH02AB02 — DexamethasoneS01BA01 — DexamethasoneA01AC02 — DexamethasoneS03BA01 — DexamethasoneD07AB19 — DexamethasoneS02BA06 — Dexamethasone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
Alternative Parents
Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 11-beta-hydroxysteroids / 17-hydroxysteroids / 3-oxo delta-1,4-steroids / Halogenated steroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols
show 8 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 9-halo-steroid / Alcohol / Aliphatic homopolycyclic compound
show 23 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:41879) / Pregnane and derivatives [Fig] (C15643)

Chemical Identifiers

UNII
7S5I7G3JQL
CAS number
50-02-2
InChI Key
UREBDLICKHMUKA-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,2R,3aS,3bS,9aS,9bR,10S,11aS)-9b-fluoro-1,10-dihydroxy-1-(2-hydroxyacetyl)-2,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES

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 References
  1. Tomlinson ES, Maggs JL, Park BK, Back DJ: Dexamethasone metabolism in vitro: species differences. J Steroid Biochem Mol Biol. 1997 Jul;62(4):345-52. doi: 10.1016/s0960-0760(97)00038-1. [PubMed:9408089]
  2. Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [PubMed:24347992]
  3. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  4. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [PubMed:15634032]
  5. Loew D, Schuster O, Graul EH: Dose-dependent pharmacokinetics of dexamethasone. Eur J Clin Pharmacol. 1986;30(2):225-30. doi: 10.1007/bf00614309. [PubMed:3709651]
  6. Spoorenberg SM, Deneer VH, Grutters JC, Pulles AE, Voorn GP, Rijkers GT, Bos WJ, van de Garde EM: Pharmacokinetics of oral vs. intravenous dexamethasone in patients hospitalized with community-acquired pneumonia. Br J Clin Pharmacol. 2014 Jul;78(1):78-83. doi: 10.1111/bcp.12295. [PubMed:24400953]
  7. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [PubMed:9141556]
  8. Diederich S, Hanke B, Burkhardt P, Muller M, Schoneshofer M, Bahr V, Oelkers W: Metabolism of synthetic corticosteroids by 11 beta-hydroxysteroid-dehydrogenases in man. Steroids. 1998 May-Jun;63(5-6):271-7. doi: 10.1016/s0039-128x(98)00039-7. [PubMed:9618784]
  9. BUNIM JJ, BLACK RL, LUTWAK L, PETERSON RE, WHEDON GD: Studies on dexamethasone, a new synthetic steroid, in rheurheumatoid arthritis: a preliminary report; adrenal cortical, metabolic and early clinical effects. Arthritis Rheum. 1958 Aug;1(4):313-31. doi: 10.1002/art.1780010404. [PubMed:13560344]
  10. FDA Approved Drug Products: Decadron Dexamethasone Oral Tablet (Discontinued) [Link]
  11. FDA Approved Drug Products: Ciprodex Dexamethasone and Ciprofloxacin Otic Suspension [Link]
  12. FDA Approved Drug Products: Dexamethasone Injection [Link]
  13. FDA Approved Drug Products: Dextenza Dexamethasone Ophthalmic Insert [Link]
  14. FDA Approved Drug Products: Dexycu Dexamethasone Intraocular Suspension [Link]
  15. FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]
  16. FDA Approved Drug Products: Maxidex Dexamethasone Ophthalmic Suspension [Link]
  17. FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Suspension [Link]
  18. FDA Approved Drug Products: Ozurdex Dexamethasone Intravitreal Implant [Link]
  19. FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Ointment [Link]
  20. FDA Approved Drug Products: Tobradex Tobramycin and Dexamethasone Ophthlamic Suspension [Link]
  21. RECOVERY trial news release: dexamethasone [Link]
Human Metabolome Database
HMDB0015364
KEGG Drug
D00292
KEGG Compound
C15643
PubChem Compound
5743
PubChem Substance
46508930
ChemSpider
5541
BindingDB
18207
RxNav
3264
ChEBI
41879
ChEMBL
CHEMBL384467
ZINC
ZINC000003875332
Therapeutic Targets Database
DAP000007
PharmGKB
PA449247
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
DEX
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Dexamethasone
AHFS Codes
  • 68:04.00 — Adrenals
  • 52:08.00 — Anti-inflammatory Agents
  • 52:08.08 — Corticosteroids
PDB Entries
1m2z / 1p93 / 3gn8 / 3mne / 3mno / 3mnp / 4uda / 4udc / 6nwk / 6xk0
FDA label
Download (96 KB)
MSDS
Download (74.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionDry Eye Syndromes1
4Active Not RecruitingTreatmentColorectal Cancers / Crohn's Disease (CD) / Digestive System Diseases / Gastrointestinal Cancers / Gastrointestinal Diseases / Inflammatory Bowel Diseases (IBD) / Intestinal Diseases / Pain / Pain, Neuropathic / Postoperative pain1
4Active Not RecruitingTreatmentExacerbation of Ulcerative Colitis / Granulomatous Colitis / Ulcerative Colitis, Active Severe1
4Active Not RecruitingTreatmentMacular Edema / Retinal Vein Occlusion1
4Active Not RecruitingTreatmentMultiple Myeloma (MM)2
4Active Not RecruitingTreatmentPain, Radiating1
4Active Not RecruitingTreatmentRadiculopathy, Cervical1
4Active Not RecruitingTreatmentRelapsed and/or Refractory Multiple Myeloma1
4CompletedNot AvailablePain1
4CompletedNot AvailablePostoperative pain1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Akorn Inc.
  • Alcon Laboratories
  • Allergan Inc.
  • Amend
  • American Regent
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bausch & Lomb Inc.
  • Baxter International Inc.
  • Bimeda Inc.
  • Blansett Pharmacal Co. Inc.
  • Bryant Ranch Prepack
  • C.O. Truxton Inc.
  • Cardinal Health
  • Carlisle Laboratories Inc.
  • Clint Pharmaceutical Inc.
  • Consolidated Midland Corp.
  • Darby Dental Supply Co. Inc.
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • ECR Pharmaceuticals
  • Falcon Pharmaceuticals Ltd.
  • General Injectables and Vaccines Inc.
  • Generics Puerto Rico Inc.
  • Keene Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Luitpold Pharmaceuticals Inc.
  • Major Pharmaceuticals
  • Martica Enterprises Inc.
  • Martin Surgical Supply
  • Medisca Inc.
  • Merck & Co.
  • Merit Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • MWI Veterinary Supply Co.
  • National Pharmaceuticals
  • Neuman Distributors Inc.
  • Nord Ost Corp.
  • Nucare Pharmaceuticals Inc.
  • Ocusoft
  • Paddock Labs
  • Par Pharmaceuticals
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • Primedics Laboratories
  • Qualitest
  • Raz Co. Inc.
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Robar Inc.
  • Roxane Labs
  • San Jose Surgical Supply Inc.
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Stat Rx Usa
  • Strides Arcolab Limited
  • Teva Pharmaceutical Industries Ltd.
  • Veratex Corp.
  • Wa Butler Co.
  • Wockhardt Ltd.
Dosage Forms
FormRouteStrength
OintmentTopical
SuspensionIntra-articular; Intralesional; Intramuscular8 mg
TabletOral0.75 mg
ElixirOral0.5 mg/5mL
Injection, solutionParenteral4 MG/1ML
Solution / dropsAuricular (otic); Ophthalmic5 ml
Solution / dropsOphthalmic
SolutionIntra-articular; Intralesional; Intramuscular; Intravenous8 mg
SuspensionOphthalmic3 mg
SuspensionAuricular (otic)
Suspension / dropsAuricular (otic)
SuspensionConjunctival; Ophthalmic3 mg
Suspension3 mg/ml
SolutionDental100 mg/100g
LiquidDental
KitOral; Topical
Injection, solution4 MG/1ML
Injection, solution8 MG/2ML
Solution / dropsOral2 MG/ML
Tablet0.75 MG
Tablet500 mcg
SolutionIntra-articular; Intramuscular; Intravenous8 mg
LiquidAuricular (otic); Ophthalmic
SolutionOral20 mg
Solution / dropsAuricular (otic); Ophthalmic5 mg/5ml
Injection, solutionIntramuscular; Intravenous8 mg/2ml
Syrup8 mg
SolutionIntravenous8 mg/2ml
Suspension / dropsOphthalmic1 mg/ml
CreamCutaneous0.1 g/100g
CreamTopical0.04 g
Injection, solutionOphthalmic
Injection, solutionIntraocular
Injection, solutionParenteral100 MG
Injection, solutionParenteral40 MG
Capsule500 mcg
SprayNasal13.5 mcg/14mL
Solution5 ml
Solution / dropsOphthalmic0.1 %
SolutionParenteral5.25 mg
GelOphthalmic100 mcg/1g
GelOphthalmic0.985 mg/g
Solution
PasteOral100 mg/100g
SolutionIntramuscular; Intravenous4 mg
SolutionIntramuscular; Intravenous8 mg
SolutionIntramuscular; Intravenous10.52 mg
SolutionIntramuscular; Intravenous4.3726 mg
Tablet0.5 MG
Tablet1.5 MG
Tablet4 MG
Tablet8 MG
CreamTopical0.5 mg/g
Tablet20 MG
Tablet40 MG
MouthwashOral10 g/100mL
MouthwashOral50 mg/100mL
SolutionAuricular (otic); Ophthalmic0.1 %
SolutionOral0.5 mg/5mL
SolutionOral5 mg/5mL
Solution / dropsOphthalmic50 mg/100mL
Syrup500 mcg/5mL
Tablet200 mcg
Tablet250 mcg
TabletOral0.5 mg/1
TabletOral0.75 mg/1
TabletOral1 mg/1
TabletOral1.5 mg/1
TabletOral2 mg/1
TabletOral4 mg/1
TabletOral6 mg/1
Solution / dropsOphthalmic5 mg/100mL
Solution, concentrateOral1 mg/1mL
LiquidIntramuscular; Intrasynovial; Intravenous
InjectionIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue4 mg/1mL
InjectionIntramuscular10 mg/1mL
InjectionIntramuscular; Intravenous10 mg/1mL
InjectionIntramuscular; Intravenous100 mg/10mL
Injection, emulsionIntramuscular; Intravenous10 mg/1mL
Injection, solutionIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue4 mg/1mL
Injection, solutionIntramuscular4 mg/1mL
Injection, solutionIntramuscular; Intravenous10 mg/1mL
Injection, solutionIntramuscular; Intravenous4 mg/1mL
Injection, solutionIntravenous4 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue4 mg/1mL
SolutionOphthalmic1 mg/1mL
Solution / dropsOphthalmic1 mg/1mL
SolutionTopical
SolutionIntramuscular; Intrasynovial; Intravenous
LiquidIntra-articular; Intramuscular; Intravenous
SolutionIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue
SolutionIntramuscular; Intravenous
LiquidIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue
SolutionOral500 mcg/5mL
Solution / dropsAuricular (otic); Ophthalmic100 mg/100mL
Injection
Tablet, coatedOral500 mcg
KitInfiltration; Intramuscular; Intravenous; Topical
KitEpidural; Infiltration; Intramuscular; Intravenous; Topical
InsertOphthalmic0.4 mg/1
Injection, powder, for solution4 mg/1mL
SolutionConjunctival; Ophthalmic1 mg
Injection, suspensionIntraocular517 ug/0.005mL
KitIntramuscular; Intravenous; Topical
Implant
SolutionAuricular (otic); Topical1 mg
SuspensionConjunctival; Ophthalmic3.5 mg
Tablet2 MG
InjectionParenteral100 mg
InjectionParenteral40 mg
SolutionConjunctival; Ophthalmic0.05 mg
TabletOral20 mg/1
Ointment100 mg/100g
Injection, solutionIntra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue10 mg/1mL
SolutionOral2 mg/5ml
Injection8 mg/2ml
Solution / dropsAuricular (otic)10 ml
Injection, emulsion4 mg/1mL
KitTopical
OintmentOphthalmic0.5 mg/1g
SuspensionOphthalmic1 mg/1mL
OintmentOphthalmic0.1 %
SuspensionOphthalmic0.1 %
OintmentOphthalmic1 mg/1g
Suspension / dropsOphthalmic1 mg/1mL
Solution / dropsOphthalmic
SyrupOral
Solution / dropsOphthalmic1 mg/ml
TabletOral4 mg
OintmentOphthalmic
LiquidAuricular (otic); Ophthalmic
Cream50 mg/100g
TabletOral40 mg
SuspensionOphthalmic
Suspension / dropsOphthalmic
SolutionOphthalmic
Solution / dropsOphthalmic1 mg
Solution / dropsOphthalmic5 mg/5mL
LiquidOphthalmic; Topical
SolutionOphthalmic1.3 mg
SolutionAuricular (otic); Ophthalmic
Solution / dropsOphthalmic0.3 %
Solution / drops5 ml
SolutionConjunctival; Ophthalmic1.3 mg
Injection, solution5 mg/1mL
SuspensionAuricular (otic)3 mg
ImplantIntravitreal0.7 mg/1
ImplantIntravitreal0.7 mg
ImplantIntravitreal700 MICROGRAMMI
ImplantIntravitreal700 mcg
TabletOral
ElixirOral
LiquidIntramuscular; Intravenous
SolutionIntra-articular; Intramuscular; Intravenous
Solution / dropsAuricular (otic); Ophthalmic
KitIntramuscular; Intravenous
KitEpidural; Infiltration; Intramuscular; Intravenous; Perineural; Topical
SolutionAuricular (otic); Ophthalmic
Solution / dropsAuricular (otic)0.3 %
Solution / dropsAuricular (otic); Ophthalmic
Solution / dropsTopical
OintmentAuricular (otic); Ophthalmic
Solution / dropsAuricular (otic); Ophthalmic50 mg/100mL
InjectionIntramuscular; Intrasynovial; Intravenous8 g
Injection, solution4 MG/ML
Ointment0.2 %
Solution / dropsOral0.2 %
SprayNasal0.15 mg
SolutionOral0.02 %
SolutionOphthalmic3 mg
Solution / dropsOphthalmic500 mg/100mL
SuspensionConjunctival; Ophthalmic2 mg
Solution / dropsOphthalmic100 mg/100mL
OintmentOphthalmic300 mg/100g
Suspension / dropsOphthalmic100 mg/100mL
OintmentOphthalmic0.3 %
SuspensionOphthalmic1 mg
SuspensionConjunctival; Ophthalmic1 mg
Suspension / dropsOphthalmic0.3 %
Capsule100 mcg
SolutionOphthalmic1 mg
CreamTopical1 %
CreamTopical1 g
CreamTopical2.04 g
Tablet
OintmentOphthalmic1 g
OintmentConjunctival; Ophthalmic0.1 g
Injection, solution40 mg/10mL
Prices
Unit descriptionCostUnit
Ozurdex 0.7 mg implant1554.0USD implant
Maxidex 0.1% Suspension 15ml Bottle97.96USD bottle
Maxitrol 0.1-5-10000 Ointment 3.5 gm Tube87.3USD tube
Maxitrol 5-10000-0.1 Suspension 5ml Bottle75.88USD bottle
Maxidex 0.1% Suspension 5ml Bottle53.57USD bottle
Dexamethasone Sodium Phosphate 4 mg/ml Solution (1 Box = 25x1ml Vials)41.99USD box
Dexamethasone micronized powd41.31USD g
Dexamethasone powder21.27USD g
Dexamethasone Sodium Phosphate 0.1% Solution 5ml Bottle19.99USD bottle
Dexamethasone acetate powd15.12USD g
Dexamethasone sod ph powder14.24USD g
Dexamethasone Sodium Phosphate 4 mg/ml Solution 5ml Vial13.99USD vial
Dexamethasone Sodium Phosphate 10 mg/ml4.78USD ml
Dexamethasone Sodium Phosphate 4 mg/ml 1 Vial = 5ml4.0USD ml
Dexamethasone 0.1% eye drop3.43USD ml
Dexasol 0.1% eye drops3.38USD ml
Maxidex 0.1 % Ointment2.69USD g
Dexamethasone 10 mg/ml vial2.56USD ml
Maxidex 0.1% eye drops2.36USD ml
Dexamethasone Sodium Phosphate 4 mg/ml1.77USD ml
Maxidex 0.1 % Suspension1.73USD ml
Sandoz Dexamethasone Sod. Phosphate 0.1 % Solution1.38USD ml
Pms-Dexamethasone Sodium Phosp 10 mg/ml1.34USD ml
Dexamethasone 4 mg/ml vial1.04USD ml
Dexamethasone 6 mg tablet1.01USD tablet
Dexasone 4 mg Tablet0.86USD tablet
Apo-Dexamethasone 4 mg Tablet0.8USD tablet
Pms-Dexamethasone 4 mg Tablet0.8USD tablet
Ratio-Dexamethasone 4 mg Tablet0.8USD tablet
Dexamethasone 2 mg tablet0.68USD tablet
Dexamethasone 1 mg/1 ml soln0.65USD ml
Dexamethasone 4 mg tablet0.6USD tablet
Dexamethasone 1 mg tablet0.49USD tablet
Pms-Dexamethasone 0.75 mg Tablet0.47USD tablet
Pms-Dexamethasone 2 mg Tablet0.43USD tablet
Dexamethasone 0.5 mg/5ml Elixir0.4USD ml
Dexamethasone 0.75 mg tablet0.38USD tablet
Dexamethasone 1.5 mg tablet0.35USD tablet
Dexamethasone 0.5 mg tablet0.31USD tablet
Apo-Dexamethasone 0.5 mg Tablet0.21USD tablet
Pms-Dexamethasone 0.5 mg Tablet0.2USD tablet
Ratio-Dexamethasone 0.5 mg Tablet0.18USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8846650No2014-09-302025-06-04US flag
US9149486No2015-10-062022-09-13US flag
US6359016No2002-03-192020-08-10US flag
US6284804No2001-09-042020-08-10US flag
US6726918No2004-04-272020-10-20US flag
US6899717No2005-05-312023-11-01US flag
US8034366No2011-10-112023-01-09US flag
US8506987No2013-08-132023-01-09US flag
US9012437No2015-04-212020-10-20US flag
US8043628No2011-10-252020-10-20US flag
US8088407No2012-01-032020-10-20US flag
US9283178No2016-03-152020-10-20US flag
US9192511No2015-11-242023-01-09US flag
US8063031No2011-11-222020-10-20US flag
US7033605No2006-04-252020-10-20US flag
US7767223No2010-08-032021-11-28US flag
US8034370No2011-10-112023-01-09US flag
US7795316No2010-09-142028-08-03US flag
US8101582No2012-01-242027-12-19US flag
US8450287No2013-05-282027-12-19US flag
US9345714No2016-05-242022-09-13US flag
US9402805No2016-08-022022-09-13US flag
US9592242No2017-03-142020-10-20US flag
US9775849No2017-10-032020-10-20US flag
US6960346No2005-11-012023-07-03US flag
US7560120No2009-07-142022-09-05US flag
US10028965No2018-07-242034-05-23US flag
US10022502No2018-07-172020-09-12US flag
US10076526No2018-09-182023-01-09US flag
US8563027No2013-10-222030-02-12US flag
US8409606No2013-04-022030-05-14US flag
US10159683No2018-12-252034-05-23US flag
US9254267No2016-02-092024-09-11US flag
US10537585No2017-12-182037-12-18US flag
US10702539No2003-01-092023-01-09US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)260-264ChemSpider
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 Solubility0.0505 mg/mLALOGPS
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 Area94.83 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity102.49 m3·mol-1ChemAxon
Polarizability40.71 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.992
Blood Brain Barrier+0.9781
Caco-2 permeable+0.8304
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor INon-inhibitor0.8112
P-glycoprotein inhibitor IINon-inhibitor0.8134
Renal organic cation transporterNon-inhibitor0.7971
CYP450 2C9 substrateNon-substrate0.8733
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7315
CYP450 1A2 substrateNon-inhibitor0.938
CYP450 2C9 inhibitorNon-inhibitor0.9106
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9247
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9169
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9399
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.1482 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9558
hERG inhibition (predictor II)Inhibitor0.5091
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-01ot-0904000000-dbbc479b104fbe981ce7
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0903000000-c84b561c97b1277fed56
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0903000000-b498846e21073040b905
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0900000000-b04e175289861dc518f1
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0900000000-b04e175289861dc518f1
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-01ot-0904000000-dbbc479b104fbe981ce7
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0903000000-c84b561c97b1277fed56
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-0903000000-b498846e21073040b905
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-006w-0719000000-d4feef3f83ca022aa94d
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0002-0913000000-3c8e5afb526637f1e822
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0002-0910000000-57f268bed9b190ee6066
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0002-0900000000-cfdda545a27ec16c8b76
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0002-0900000000-c70817ad99741f01b675
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0009000000-ecbabc9fe90444b14afe
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05fr-0019000000-4161bdd8f3deed25b9bc
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-002r-0594000000-bf4495b7906d53ad019d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00ds-0980000000-c4e88ec70fa28252f6f7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05fs-0930000000-8022e38d862953c2551b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05fs-1920000000-6f1a7ac153a363c2aa73
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00tf-1910000000-e34981c957b125a39447
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05fr-0019000000-285cd2de8c812f1c5e55
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-002r-0593000000-bd52212afb3af2380901
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00ds-0980000000-ff265e4738c79efad9e3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0940000000-818b114d12290dc23743
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05fs-1930000000-9e4283fb9c2780729f55
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05dm-1920000000-0f41e220b5d3d1abe699
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0009000000-cf986616b1138d5569c7
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00dl-0009000000-431895662c53cadb563c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4r-0498000000-233b2490f89112ad539e
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000j-0791000000-c83a21019f43596e6804
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00dj-0970000000-36eebd63d78f040ae67f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00dj-0940000000-730013951a30cf080ad4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4r-0696000000-1df7921eb1369fef69c4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dj-3960000000-e9ee044790c0655981b1

Targets

Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
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:16835395]
  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:16891588]
  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:16956592]
  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:16963802]
  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:16971495]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Stimulator
General Function
Transcription factor binding
Specific Function
Orphan nuclear receptor. Component of a cascade required for the development of the hypothalamic-pituitary-adrenal-gonadal axis. Acts as a coregulatory protein that inhibits the transcriptional act...
Gene Name
NR0B1
Uniprot ID
P51843
Uniprot Name
Nuclear receptor subfamily 0 group B member 1
Molecular Weight
51717.185 Da
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:16857744]
  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:17526944]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Structural molecule activity
Specific Function
Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
Gene Name
ANXA1
Uniprot ID
P04083
Uniprot Name
Annexin A1
Molecular Weight
38713.855 Da
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:16883066]
  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:17076770]
  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:17158208]
  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:17644190]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Negative modulator
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
Gene Name
NOS2
Uniprot ID
P35228
Uniprot Name
Nitric oxide synthase, inducible
Molecular Weight
131116.3 Da
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:17379310]
  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:17494951]
  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. 2008 Jan;53(1):123-32. Epub 2007 May 15. [PubMed:17503181]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
Molecular Weight
49761.245 Da
References
  1. Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [PubMed:16054614]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. Modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation...
Gene Name
HSD11B2
Uniprot ID
P80365
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 2
Molecular Weight
44126.06 Da
References
  1. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [PubMed:9141556]
  2. Diederich S, Hanke B, Burkhardt P, Muller M, Schoneshofer M, Bahr V, Oelkers W: Metabolism of synthetic corticosteroids by 11 beta-hydroxysteroid-dehydrogenases in man. Steroids. 1998 May-Jun;63(5-6):271-7. doi: 10.1016/s0039-128x(98)00039-7. [PubMed:9618784]
Details
2. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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:10490933]
  2. Lampen A, Christians U, Guengerich FP, Watkins PB, Kolars JC, Bader A, Gonschior AK, Dralle H, Hackbarth I, Sewing KF: Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions, and interindividual variability. Drug Metab Dispos. 1995 Dec;23(12):1315-24. [PubMed:8689938]
  3. Christians U, Schmidt G, Bader A, Lampen A, Schottmann R, Linck A, Sewing KF: Identification of drugs inhibiting the in vitro metabolism of tacrolimus by human liver microsomes. Br J Clin Pharmacol. 1996 Mar;41(3):187-90. [PubMed:8866917]
  4. Miranda SR, Meyer SA: Cytotoxicity of chloroacetanilide herbicide alachlor in HepG2 cells independent of CYP3A4 and CYP3A7. Food Chem Toxicol. 2007 May;45(5):871-7. doi: 10.1016/j.fct.2006.11.011. Epub 2006 Nov 26. [PubMed:17207564]
  5. Yamaguchi Y, Kirita S, Baba T, Aoyama J, Touchi A, Tukey RH, Guengerich FP, Matsubara T: Identification of rat and human cytochrome P450 forms involved in the metabolism of the thromboxane A2 receptor antagonist (+)-S-145. Drug Metab Dispos. 1997 Jan;25(1):75-80. [PubMed:9010633]
  6. Gomez-Lechon MJ, Donato T, Jover R, Rodriguez C, Ponsoda X, Glaise D, Castell JV, Guguen-Guillouzo C: Expression and induction of a large set of drug-metabolizing enzymes by the highly differentiated human hepatoma cell line BC2. Eur J Biochem. 2001 Mar;268(5):1448-59. [PubMed:11231298]
  7. Berson A, Wolf C, Chachaty C, Fisch C, Fau D, Eugene D, Loeper J, Gauthier JC, Beaune P, Pompon D, et al.: Metabolic activation of the nitroaromatic antiandrogen flutamide by rat and human cytochromes P-450, including forms belonging to the 3A and 1A subfamilies. J Pharmacol Exp Ther. 1993 Apr;265(1):366-72. [PubMed:8386241]
  8. McCune JS, Hawke RL, LeCluyse EL, Gillenwater HH, Hamilton G, Ritchie J, Lindley C: In vivo and in vitro induction of human cytochrome P4503A4 by dexamethasone. Clin Pharmacol Ther. 2000 Oct;68(4):356-66. doi: 10.1067/mcp.2000.110215. [PubMed:11061575]
  9. Dexamethasone monograph, Boehringer Ingelheim [Link]
  10. Flockhart Table of Drug Interactions [Link]
  11. FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
11-beta-hydroxysteroid dehydrogenase [nad(p)] activity
Specific Function
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea...
Gene Name
HSD11B1
Uniprot ID
P28845
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 1
Molecular Weight
32400.665 Da
References
  1. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [PubMed:9141556]
  2. Diederich S, Hanke B, Burkhardt P, Muller M, Schoneshofer M, Bahr V, Oelkers W: Metabolism of synthetic corticosteroids by 11 beta-hydroxysteroid-dehydrogenases in man. Steroids. 1998 May-Jun;63(5-6):271-7. doi: 10.1016/s0039-128x(98)00039-7. [PubMed:9618784]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Hukkanen J, Lassila A, Paivarinta K, Valanne S, Sarpo S, Hakkola J, Pelkonen O, Raunio H: Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. Am J Respir Cell Mol Biol. 2000 Mar;22(3):360-6. [PubMed:10696073]
  2. Hukkanen J, Vaisanen T, Lassila A, Piipari R, Anttila S, Pelkonen O, Raunio H, Hakkola J: Regulation of CYP3A5 by glucocorticoids and cigarette smoke in human lung-derived cells. J Pharmacol Exp Ther. 2003 Feb;304(2):745-52. [PubMed:12538830]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Miranda SR, Meyer SA: Cytotoxicity of chloroacetanilide herbicide alachlor in HepG2 cells independent of CYP3A4 and CYP3A7. Food Chem Toxicol. 2007 May;45(5):871-7. doi: 10.1016/j.fct.2006.11.011. Epub 2006 Nov 26. [PubMed:17207564]
  2. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 17-alpha-monooxygenase activity
Specific Function
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation ...
Gene Name
CYP17A1
Uniprot ID
P05093
Uniprot Name
Steroid 17-alpha-hydroxylase/17,20 lyase
Molecular Weight
57369.995 Da
References
  1. Trzeciak WH, LeHoux JG, Waterman MR, Simpson ER: Dexamethasone inhibits corticotropin-induced accumulation of CYP11A and CYP17 messenger RNAs in bovine adrenocortical cells. Mol Endocrinol. 1993 Feb;7(2):206-13. doi: 10.1210/mend.7.2.8385739. [PubMed:8385739]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [PubMed:11286621]
  2. Monostory K, Kohalmy K, Prough RA, Kobori L, Vereczkey L: The effect of synthetic glucocorticoid, dexamethasone on CYP1A1 inducibility in adult rat and human hepatocytes. FEBS Lett. 2005 Jan 3;579(1):229-35. doi: 10.1016/j.febslet.2004.11.080. [PubMed:15620718]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Onica T, Nichols K, Larin M, Ng L, Maslen A, Dvorak Z, Pascussi JM, Vilarem MJ, Maurel P, Kirby GM: Dexamethasone-mediated up-regulation of human CYP2A6 involves the glucocorticoid receptor and increased binding of hepatic nuclear factor 4 alpha to the proximal promoter. Mol Pharmacol. 2008 Feb;73(2):451-60. Epub 2007 Oct 31. [PubMed:17978169]
  2. Meunier V, Bourrie M, Julian B, Marti E, Guillou F, Berger Y, Fabre G: Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: a 10-year follow-up. Xenobiotica. 2000 Jun;30(6):589-607. doi: 10.1080/004982500406426 . [PubMed:10923861]
  3. Waxman DJ, Chang TK: Spectrofluorometric analysis of CYP2A6-catalyzed coumarin 7-hydroxylation. Methods Mol Biol. 2006;320:91-6. doi: 10.1385/1-59259-998-2:91. [PubMed:16719377]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [PubMed:11286621]
  2. Wang H, Tompkins LM: CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme. Curr Drug Metab. 2008 Sep;9(7):598-610. [PubMed:18781911]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Raucy JL, Mueller L, Duan K, Allen SW, Strom S, Lasker JM: Expression and induction of CYP2C P450 enzymes in primary cultures of human hepatocytes. J Pharmacol Exp Ther. 2002 Aug;302(2):475-82. doi: 10.1124/jpet.102.033837. [PubMed:12130704]
  2. Scott SA, Sangkuhl K, Shuldiner AR, Hulot JS, Thorn CF, Altman RB, Klein TE: PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 19. Pharmacogenet Genomics. 2012 Feb;22(2):159-65. doi: 10.1097/FPC.0b013e32834d4962. [PubMed:22027650]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
  2. Pascussi JM, Gerbal-Chaloin S, Fabre JM, Maurel P, Vilarem MJ: Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: consequences on cytochrome P450 gene regulation. Mol Pharmacol. 2000 Dec;58(6):1441-50. doi: 10.1124/mol.58.6.1441. [PubMed:11093784]
  3. Gerbal-Chaloin S, Pascussi JM, Pichard-Garcia L, Daujat M, Waechter F, Fabre JM, Carrere N, Maurel P: Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metab Dispos. 2001 Mar;29(3):242-51. [PubMed:11181490]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [PubMed:11286621]
  2. Sampol E, Mirrione A, Villard PH, Piccerelle P, Scoma H, Berbis P, Barra Y, Durand A, Lacarelle B: Evidence for a tissue-specific induction of cutaneous CYP2E1 by dexamethasone. Biochem Biophys Res Commun. 1997 Jun 27;235(3):557-61. doi: 10.1006/bbrc.1997.6829. [PubMed:9207195]
  3. Monostory K, Vereczkey L: Combined action of phenobarbital and dexamethasone on the activity of rat liver P450 system. Acta Pharm Hung. 1993 Sep;63(5):296-300. [PubMed:8249615]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Monooxygenase activity
Specific Function
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name
CYP3A43
Uniprot ID
Q9HB55
Uniprot Name
Cytochrome P450 3A43
Molecular Weight
57669.21 Da
References
  1. Krusekopf S, Roots I, Kleeberg U: Differential drug-induced mRNA expression of human CYP3A4 compared to CYP3A5, CYP3A7 and CYP3A43. Eur J Pharmacol. 2003 Apr 11;466(1-2):7-12. doi: 10.1016/s0014-2999(03)01481-x. [PubMed:12679136]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Leukotriene-b4 20-monooxygenase activity
Specific Function
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 2...
Gene Name
CYP4A11
Uniprot ID
Q02928
Uniprot Name
Cytochrome P450 4A11
Molecular Weight
59347.31 Da
References
  1. Cummings BS, Lasker JM, Lash LH: Expression of glutathione-dependent enzymes and cytochrome P450s in freshly isolated and primary cultures of proximal tubular cells from human kidney. J Pharmacol Exp Ther. 2000 May;293(2):677-85. [PubMed:10773044]
  2. Savas U, Hsu MH, Johnson EF: Differential regulation of human CYP4A genes by peroxisome proliferators and dexamethasone. Arch Biochem Biophys. 2003 Jan 1;409(1):212-20. doi: 10.1016/s0003-9861(02)00499-x. [PubMed:12464261]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
Gene Name
CYP11B1
Uniprot ID
P15538
Uniprot Name
Cytochrome P450 11B1, mitochondrial
Molecular Weight
57572.44 Da
References
  1. Fardella CE, Pinto M, Mosso L, Gomez-Sanchez C, Jalil J, Montero J: Genetic study of patients with dexamethasone-suppressible aldosteronism without the chimeric CYP11B1/CYP11B2 gene. J Clin Endocrinol Metab. 2001 Oct;86(10):4805-7. doi: 10.1210/jcem.86.10.7920. [PubMed:11600544]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Cummings DM, Larijani GE, Conner DP, Ferguson RK, Rocci ML Jr: Characterization of dexamethasone binding in normal and uremic human serum. DICP. 1990 Mar;24(3):229-31. doi: 10.1177/106002809002400301. [PubMed:2316228]

Transporters

Details
1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
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:11297522]
  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:12387747]
  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:8845310]
  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:11602674]
  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:12699389]
  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:11785684]
  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:14661924]
  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:7560060]
  9. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [PubMed:19953504]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
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:11557128]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
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:9929003]
  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:11323161]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
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. doi: 10.3109/01480540903390000. [PubMed:20307139]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
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:9539145]
  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:8786566]

Drug created on June 13, 2005 07:24 / Updated on October 27, 2020 11:13

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