Dexamethasone

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Identification

Summary

Dexamethasone is a glucocorticoid available in various modes of administration that is used for the treatment of various inflammatory conditions, including bronchial asthma, as well as endocrine and rheumatic disorders.

Brand Names

Baycadron, Ciprodex, Decadron, Dexamethasone Intensol, Dextenza, Dioptrol, Hexadrol, Hidex 6-day Taper, Maxidex, Maxitrol, Neofordex, Ozurdex, Taperdex 12 Day Taper, Taperdex 6 Day Taper, Taperdex 7-day Taper, Tobradex, Zcort 7 Day Taper

Generic Name

Dexamethasone

DrugBank Accession Number

DB01234

Background

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.¹³ Developed in 1957, it is structurally similar to other corticosteroids like hydrocortisone and prednisolone.⁹

Dexamethasone was granted FDA approval on 30 October 1958.¹¹ 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.²²

Type

Small Molecule

Groups

Approved, Investigational, Vet approved

Structure

Similar Structures

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

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Pharmacology

Indication

Dexamethasone and ciprofloxacin otic suspension is indicated for bacterial infections with inflammation in acute otitis media and acute otitis externa.¹² Intramuscular and intravenous injections are indicated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions.¹³ Oral tablets are indicated for the treatment of multiple myeloma.¹⁶ An intravitreal implant is indicated for some forms of macular edema and non-infectious posterior uveitis affecting the posterior of the eye.¹⁹ Various ophthalmic formulations are indicated for inflammatory conditions of the eye.^{14,15,17,18,20,21}

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Dose Form
Management of	Acne rosacea		••••••••••••
Management of	Acquired hemolytic anemia		••••••••••••
Management of	Acute gouty arthritis		••••••••••••
Management of	Acute leukemia		••••••••••••
Used in combination to treat	Acute otitis externa	Combination Product in combination with: Ciprofloxacin (DB00537)	••••••••••••	•••••• •••••••••• •••••••	••••••••••

Contraindications & Blackbox Warnings

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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.^{12,13,14,15,16,17,18,19,20,21} 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

Target	Actions	Organism
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.¹³ A 3mg intramuscular dose reaches a C_max of 34.6±6.0ng/mL with a T_max of 2.0±1.2h and an AUC of 113±38ng*h/mL.⁵ A 1.5mg oral dose reaches a C_max of 13.9±6.8ng/mL with a T_max 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.¹⁶ The majority of protein binding is with serum albumin.¹⁰ Dexamethasone does not significantly bind to corticosteroid binding protein.¹⁰

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

Dexamethasone

Route of elimination

Corticosteroids are generally eliminated predominantly in the urine.⁴ However, dexamethasone is <10% elminated in urine.¹⁶

Half-life

The mean terminal half life of a 20mg oral tablet is 4 hours.¹⁶ 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.¹⁶ 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

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Toxicity

The oral LD₅₀ in female mice was 6.5g/kg and 794mg/kg via the intravenous route.¹³

Overdoses are not expected with otic formulations.¹² 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

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.

Drug	Interaction
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1,2-Benzodiazepine	The metabolism of 1,2-Benzodiazepine can be increased when combined with Dexamethasone.
Abametapir	The serum concentration of Dexamethasone can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Dexamethasone can be increased when combined with Abatacept.
Abemaciclib	The metabolism of Abemaciclib can be increased when combined with Dexamethasone.
Abiraterone	The metabolism of Abiraterone can be increased when combined with Dexamethasone.

Food Interactions

Avoid alcohol.
Take with food. Food reduces irritation.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Dexamethasone phosphate	2BP70L44PR	312-93-6	VQODGRNSFPNSQE-CXSFZGCWSA-N
Dexamethasone sodium phosphate	AI9376Y64P	2392-39-4	PLCQGRYPOISRTQ-FCJDYXGNSA-L

Product Images

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Accufix II Dec Model 033-212	Implant	0.7 mg / imp	Intravitreal	Telectronics Pacing Systems Inc.	1994-12-31	1999-08-27
Decadron	Tablet	0.75 mg/1	Oral	Merck Sharp & Dohme B.V.	1958-10-30	2007-11-30
Decadron	Tablet	0.5 mg/1	Oral	Merck Sharp & Dohme B.V.	1958-10-30	2007-11-30
Decadron Phosphate Eye Ear Sol 0.1%	Liquid	1 mg / mL	Auricular (otic); Ophthalmic	Merck Frosst Canada & Cie, Merck Frosst Canada & Co.	1960-12-31	1998-04-21
Decadron Phosphate Inj 4mg/ml	Liquid	4 mg / mL	Intramuscular; Intravenous	Merck Frosst Canada & Cie, Merck Frosst Canada & Co.	1959-12-31	2001-08-01

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo-dexamethasone	Tablet	0.5 mg	Oral	Apotex Corporation	2004-11-17	Not applicable
Apo-dexamethasone	Tablet	4 mg	Oral	Apotex Corporation	2004-03-08	Not applicable
Baycadron	Elixir	0.5 mg/5mL	Oral	Wockhardt	1983-07-27	Not applicable
Decadron	Tablet	0.75 mg/1	Oral	Pragma Pharmaceuticals, LLC	2018-02-28	2022-03-31
Decadron	Tablet	1.5 mg/1	Oral	Wraser Llc	2017-09-11	2017-09-25

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
999 Itch Relief	Dexamethasone (15 mg/20000mg) + Menthol (200 mg/20000mg) + Synthetic camphor (200 mg/20000mg)	Ointment	Topical	China Resources Sanjiu Medical & Pharmaceutical Co., Ltd.	2003-07-03	Not applicable
ACEFOS DUO® SUSPENSIÓN INYECTABLE	Dexamethasone (8 mg) + Dexamethasone (2 mg)	Suspension	Intra-articular; Intralesional; Intramuscular	ARBOFARMA S.A.S.	2018-06-20	Not applicable
ACEFOS DUO® SUSPENSIÓN INYECTABLE	Dexamethasone (8 mg) + Dexamethasone (2 mg)	Suspension	Intra-articular; Intralesional; Intramuscular	ARBOFARMA S.A.S.	2018-06-20	Not applicable
AK-Trol	Dexamethasone (1 mg/1g) + Neomycin sulfate (3.5 mg/1g) + Polymyxin B sulfate (10000 [USP'U]/1g)	Ointment	Ophthalmic	Physicians Total Care, Inc.	1996-01-05	2000-06-30
ALEGI	Dexamethasone (0.5 mg) + Dexchlorpheniramine maleate (2 mg)	Tablet		L API Laboratories	2019-01-24	2029-01-24

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Dex-Moxi	Dexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (5 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
Dex-Moxi PF	Dexamethasone sodium phosphate (1 mg/1mL) + Moxifloxacin hydrochloride monohydrate (5 mg/1mL)	Injection, solution	Intraocular	ImprimisRx NJ	2018-01-01	Not applicable
Dex-Moxi-Ketor	Dexamethasone sodium phosphate (1 mg/1mL) + Ketorolac tromethamine (0.4 mg/1mL) + Moxifloxacin hydrochloride monohydrate (0.5 mg/1mL)	Injection, solution	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
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)	Solution	Topical	Sincerus Florida, LLC	2019-05-09	Not applicable
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)	Solution	Topical	Sincerus Florida, LLC	2019-05-09	Not applicable

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: [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

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

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. [Article]
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. [Article]
Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
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. [Article]
Loew D, Schuster O, Graul EH: Dose-dependent pharmacokinetics of dexamethasone. Eur J Clin Pharmacol. 1986;30(2):225-30. doi: 10.1007/bf00614309. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
FDA Approved Drug Products: Decadron Dexamethasone Oral Tablet (Discontinued) [Link]
FDA Approved Drug Products: Ciprodex Dexamethasone and Ciprofloxacin Otic Suspension [Link]
FDA Approved Drug Products: Dexamethasone Injection [Link]
FDA Approved Drug Products: Dextenza Dexamethasone Ophthalmic Insert [Link]
FDA Approved Drug Products: Dexycu Dexamethasone Intraocular Suspension [Link]
FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]
FDA Approved Drug Products: Maxidex Dexamethasone Ophthalmic Suspension [Link]
FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Suspension [Link]
FDA Approved Drug Products: Ozurdex Dexamethasone Intravitreal Implant [Link]
FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Ointment [Link]
FDA Approved Drug Products: Tobradex Tobramycin and Dexamethasone Ophthlamic Suspension [Link]
RECOVERY trial news release: dexamethasone [Link]

External Links

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

PDB Entries

1m2z / 1p93 / 3mne / 3mno / 3mnp / 4uda / 4udc / 6nwk / 6xk0 / 7krj …

show 8 more

FDA label

Download (96 KB)

MSDS

Download (74.8 KB)

Clinical Trials

Clinical Trials Clinical Trial & Rare Diseases Add-on Data Package Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package

Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
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Not Available	Active Not Recruiting	Not Available	Multiple Myeloma (MM)	2	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Basic Science	Hyperandrogenemia / Obesity / Polycystic Ovarian Syndrome (PCOS)	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Basic Science	Hyperandrogenism / Obesity / Polycystic Ovarian Syndrome (PCOS)	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Diagnostic	Lung Cancer, Nonsmall Cell, Stage IIIA / Recurrent Non-Small Cell Lung Carcinoma / Stage IIIB Non-Small Cell Lung Cancer / Stage IV Non-small Cell Lung Cancer (NSCLC)	1	somestatus	stop reason	just information to hide
Not Available	Active Not Recruiting	Supportive Care	Breast Cancer / Post Operative Nausea and Vomiting (PONV)	1	somestatus	stop reason	just information to hide

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

Form	Route	Strength
Implant	Intravitreal	0.7 mg / imp
Tablet	Oral	0.500 mg
Tablet
Tablet	Oral	0.75 mg
Elixir	Oral	0.5 mg/5mL
Cream		10 mg/g
Tablet	Oral	0.5 MG/2MG
Solution	Parenteral	8.745 mg
Solution / drops	Ophthalmic	3 mg
Injection, solution	Parenteral	4 MG/1ML
Solution / drops	Ophthalmic	1 mg/ml
Ointment	Ophthalmic	1 mg/g
Solution	Intra-articular; Intralesional; Intramuscular; Intravenous	8 mg
Solution	Auricular (otic)	0.3 %
Suspension	Auricular (otic)
Suspension / drops	Auricular (otic)
Solution / drops	Auricular (otic)
Solution	Intramuscular
Solution / drops	Intraocular
Injection, solution; injection, suspension; kit	Epidural; Intra-articular; Intracaudal; Intramuscular; Intravenous; Perineural; Topical
Liquid	Dental
Kit	Oral; Topical
Injection	Intramuscular; Intrasynovial; Intravenous	4 mg/mL
Injection	Intramuscular; Intrasynovial; Intravenous	8 mg/2mL
Injection, solution	Parenteral	8 MG/2ML
Solution / drops	Oral	2 MG/ML
Solution	Intra-articular; Intramuscular; Intravenous	8 mg
Liquid	Auricular (otic); Ophthalmic	1 mg / mL
Tablet	Oral	.5 mg
Solution	Oral	2000000 mg
Injection	Intramuscular; Intravenous	2 mg/ml
Injection		2 MG/ml
Solution	Parenteral	8.000 mg
Tablet	Oral	4.000 mg
Solution / drops	Auricular (otic); Ophthalmic	5 mg/5ml
Syrup	Oral	8 mg
Solution	Intravenous	8 mg/2ml
Suspension / drops	Ophthalmic
Cream	Cutaneous	0.1 g/100g
Cream	Topical	1 g
Solution / drops	Auricular (otic); Ophthalmic
Cream	Cutaneous
Injection, solution
Injection, solution		8 MG/2ML
Injection, solution	Intramuscular; Intravenous	4 MG/ML
Injection, solution	Intramuscular; Intravenous	8 MG/2ML
Injection, solution		4 MG/ML
Cream	Topical
Injection, solution	Ophthalmic
Injection, solution	Intraocular
Injection, solution	Parenteral	100 MG
Injection, solution	Parenteral	40 MG
Spray	Nasal	13.5 mcg/14mL
Solution	Ophthalmic	1 mg/ml
Ointment	Ophthalmic	0.3 mg/g
Solution	Ophthalmic	5 ml
Solution / drops	Ophthalmic	0.1 %
Solution	Oral	0.4 MG/ML
Solution	Oral	2 MG/ML
Solution	Oral	4 MG/ML
Solution	Parenteral	5.25 mg
Cream	Topical	0.1 g
Solution	Intramuscular; Intravenous	800000 mg
Solution	Ophthalmic	1.000 mg
Gel	Ophthalmic	0.1 %w/w
Gel	Ophthalmic	0985 mg/g
Solution
Paste	Oral	1 mg/g
Paste	Submucosal	1 mg/g
Solution	Parenteral	8 mg
Solution	Parenteral	4 mg
Solution	Intramuscular; Intravenous	10.52 mg
Solution	Intramuscular; Intravenous	8 mg
Solution	Intramuscular; Intravenous	4 mg
Injection	Intramuscular; Intravenous	8 mg
Solution	Intramuscular; Intravenous	4.3726 mg
Injection, solution	Intramuscular; Intravenous
Tablet	Oral	1.5 MG
Tablet	Oral	8 MG
Cream	Topical	0.5 mg/g
Tablet	Oral	20 MG
Tablet	Oral	40 MG
Injection
Solution	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	10 mg / mL
Solution	Oral	0.5 mg/5mL
Solution	Oral	1 mg/10mL
Tablet	Oral	0.5 mg/1
Tablet	Oral	0.5 mg/0.5mg
Tablet	Oral	0.75 mg/0.75mg
Tablet	Oral	0.75 mg/1
Tablet	Oral	1 mg/1
Tablet	Oral	1.5 mg/1
Tablet	Oral	2 mg/1
Tablet	Oral	4 mg/1
Tablet	Oral	6 mg/1
Solution, concentrate	Oral	1 mg/1mL
Solution	Intramuscular; Intrasynovial; Intravenous	10 mg / 1 mL
Liquid	Intramuscular; Intrasynovial; Intravenous	10 mg / 1 mL
Injection		5.45 mg
Injection		6.58 mg
Injection	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	10 mg/1mL
Injection	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	4 mg/1mL
Injection	Intramuscular	10 mg/1mL
Injection	Intramuscular; Intravenous	10 mg/1mL
Injection	Intramuscular; Intravenous	100 mg/10mL
Injection, emulsion	Intramuscular; Intravenous	10 mg/1mL
Injection, solution	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	4 mg/1mL
Injection, solution	Intramuscular	4 mg/1mL
Injection, solution	Intramuscular; Intravenous	10 mg/1mL
Injection, solution	Intramuscular; Intravenous	4 mg/1mL
Injection, solution	Intravenous	4 mg/1mL
Injection, suspension	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	4 mg/1mL
Solution	Ophthalmic	1 mg/1mL
Solution / drops	Ophthalmic	1 mg/1mL
Solution	Topical
Solution	Intramuscular; Intrasynovial; Intravenous	4 mg / mL
Solution	Intramuscular; Intrasynovial; Intravenous	10 mg / mL
Injection	Intramuscular; Intravenous	4 mg/ml
Solution	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	4 mg / mL
Solution	Intra-articular; Intramuscular; Intravenous	4 mg / mL
Solution	Intramuscular; Intravenous	10 mg / mL
Liquid	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	4 mg / mL
Liquid	Auricular (otic); Ophthalmic
Solution		4 mg/1ml
Injection	Intramuscular; Intravenous	5 mg/ml
Injection		5 MG/ml
Solution / drops	Auricular (otic); Ophthalmic	1 MG/ML
Injection	Intra-articular; Intramuscular; Intravenous; Intravitreal	8 mg/2ml
Kit	Infiltration; Intramuscular; Intravenous; Topical
Injection, solution; kit; solution; swab	Epidural; Infiltration; Intra-articular; Intracaudal; Intramuscular; Intrathecal; Intravascular; Intravenous; Perineural; Topical
Kit	Epidural; Infiltration; Intramuscular; Intravenous; Topical
Tablet		0.5 mg
Syrup	Oral	0.5 mg/5ml
Insert	Ophthalmic	0.4 mg/1
Solution	Conjunctival; Ophthalmic
Solution	Auricular (otic); Ophthalmic
Injection, suspension	Intraocular	517 ug/0.005mL
Kit	Intramuscular; Intravenous; Topical
Solution	Intramuscular	100.000 mg
Suspension	Intra-articular; Intralesional; Intramuscular
Implant	Intravitreal	.5 mg / unit
Implant	Intravitreal	0.5 mg / unit
Solution / drops	Ophthalmic	5 mg
Gel	Ophthalmic	1.5 MG/ML
Solution	Ophthalmic	1.140 mg
Solution / drops	Ophthalmic	1.5 MG/ML
Solution	Auricular (otic); Topical
Injection, solution	Intramuscular; Intravenous	100 mg/10ml
Injection, solution	Intramuscular; Intravenous	40 mg/5ml
Injection	Parenteral	100 mg
Injection	Parenteral	40 mg
Cream	Topical	200000 g
Tablet	Oral	20 mg/1
Injection, solution	Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue	10 mg/1mL
Liquid	Intramuscular; Intravenous	4 mg / mL
Solution	Oral	2 mg/5ml
Injection		8 mg/2ml
Suspension	Conjunctival; Ophthalmic	1 mg
Solution / drops	Auricular (otic)	10 ml
Cream	Cutaneous	1.000 g
Injection	Intravenous	4 mg/ml
Injection, solution; kit	Intra-articular; Intralesional; Intramuscular; Intravenous; Perineural; Soft tissue
Ointment	Ophthalmic	2 MG/G
Solution / drops	Ophthalmic	2 MG/ML
Kit	Topical
Ointment	Ophthalmic	0.1 % w/w
Ointment	Ophthalmic	0.5 mg/1g
Suspension	Ophthalmic	0.1 % w/v
Suspension	Ophthalmic	1 mg/1mL
Suspension / drops	Ophthalmic	1 mg/1mL
Suspension / drops	Ophthalmic	0.1 %
Suspension	Ophthalmic	0.1 %
Suspension	Ophthalmic
Ointment	Ophthalmic	0.1 %
Solution	Ophthalmic	0.1 %
Ointment	Ophthalmic	1.000 mg
Suspension	Ophthalmic	1.000 mg
Suspension	Conjunctival; Ophthalmic	1 mg
Solution	Parenteral	8.00 mg
Solution / drops	Ophthalmic
Syrup	Oral
Solution	Ophthalmic	0.1 % w/v
Solution / drops	Ophthalmic	1 mg/ml
Solution	Oral	20 mg
Ointment	Ophthalmic
Solution	Nasal
Solution	Intraocular; Ophthalmic
Suspension	Ophthalmic
Suspension / drops	Ophthalmic
Suspension / drops	Topical
Solution	Intramuscular	8.000 mg
Solution	Ophthalmic	3 mg
Gel	Conjunctival
Solution	Ophthalmic
Solution	Parenteral	200 mg
Injection, solution; kit	Epidural; Intracaudal; Intramuscular; Intravenous; Perineural; Topical
Solution	Ophthalmic; Topical
Liquid	Ophthalmic; Topical	.1 %
Solution	Auricular (otic); Ophthalmic	0.1 %
Ointment	Conjunctival; Ophthalmic
Solution / drops	Auricular (otic); Ophthalmic	5 ml
Solution	Conjunctival; Ophthalmic	1 mg
Solution	Ophthalmic	1 mg
Implant	Intraocular	700.000 mcg
Implant	Intravitreal	0.7 mg/1
Implant	Intravitreal	0.7 mg
Implant	Intravitreal	700 MICROGRAMMI
Implant	Intravitreal	700 mcg
Implant	Ophthalmic	0.7 mg
Intrauterine device	Intraocular; Intrauterine	0.7 mg
Injection		40 mg/10ml
Injection		4 MG/ML
Suspension	Intramuscular
Tablet	Oral	2 mg
Elixir	Oral	0.5 mg / 5 mL
Liquid	Intramuscular; Intravenous	10 mg / mL
Solution	Ophthalmic	1.3 mg
Solution / drops	Auricular (otic); Ophthalmic	.1 %
Kit	Intramuscular; Intravenous
Solution	Parenteral	8.0 mg
Injection, solution	Intramuscular
Kit	Epidural; Infiltration; Intramuscular; Intravenous; Perineural; Topical
Solution / drops	Auricular (otic); Ophthalmic	0.1 %
Solution	Intravenous	8.740 mg
Ointment	Auricular (otic); Ophthalmic
Ointment	Topical
Injection	Intramuscular; Intrasynovial; Intravenous	8 g
Injection, solution	Parenteral	4 MG/ML
Ointment	Ophthalmic	0.2 %
Solution / drops	Oral	0.2 %
Spray	Nasal	0.15 mg
Solution	Oral	0.02 %
Suspension	Conjunctival; Ophthalmic	2 mg
Tablet	Oral
Solution	Parenteral
Suspension	Conjunctival; Ophthalmic
Ointment	Ophthalmic	0.1 %
Suspension / drops	Ophthalmic	0.1 %
Ointment	Conjunctival; Ophthalmic	0.1 g
Suspension / drops	Intraocular
Cream	Rectal; Topical
Emulsion	Urethral
Solution / drops	Ophthalmic	0.15 %
Tablet, effervescent	Oral	2 MG
Tablet, effervescent	Oral	4 MG
Tablet, effervescent	Oral	8 MG
Ointment	Ophthalmic
Solution / drops	Ophthalmic
Liquid	Ophthalmic
Capsule
Liquid	Auricular (otic)
Injection, solution		4 mg/1ml
Solution / drops	Auricular (otic); Ophthalmic
Syrup		0.5 mg/5ml
Tablet, sugar coated	Oral	0.5 mg
Tablet	Oral	0.25 mg
Tablet, film coated		0.5 mg
Solution		5 mg/1ml
Tablet	Oral	0.5 mg
Tablet	Oral	4 mg
Implant	Intravitreal	0.7 mg/implant

Prices

Unit description	Cost	Unit
Ozurdex 0.7 mg implant	1554.0USD	implant
Maxidex 0.1% Suspension 15ml Bottle	97.96USD	bottle
Maxitrol 0.1-5-10000 Ointment 3.5 gm Tube	87.3USD	tube
Maxitrol 5-10000-0.1 Suspension 5ml Bottle	75.88USD	bottle
Maxidex 0.1% Suspension 5ml Bottle	53.57USD	bottle
Dexamethasone Sodium Phosphate 4 mg/ml Solution (1 Box = 25x1ml Vials)	41.99USD	box
Dexamethasone micronized powd	41.31USD	g
Dexamethasone powder	21.27USD	g
Dexamethasone Sodium Phosphate 0.1% Solution 5ml Bottle	19.99USD	bottle
Dexamethasone acetate powd	15.12USD	g
Dexamethasone sod ph powder	14.24USD	g
Dexamethasone Sodium Phosphate 4 mg/ml Solution 5ml Vial	13.99USD	vial
Dexamethasone Sodium Phosphate 10 mg/ml	4.78USD	ml
Dexamethasone Sodium Phosphate 4 mg/ml 1 Vial = 5ml	4.0USD	ml
Dexamethasone 0.1% eye drop	3.43USD	ml
Dexasol 0.1% eye drops	3.38USD	ml
Maxidex 0.1 % Ointment	2.69USD	g
Dexamethasone 10 mg/ml vial	2.56USD	ml
Maxidex 0.1% eye drops	2.36USD	ml
Dexamethasone Sodium Phosphate 4 mg/ml	1.77USD	ml
Maxidex 0.1 % Suspension	1.73USD	ml
Sandoz Dexamethasone Sod. Phosphate 0.1 % Solution	1.38USD	ml
Pms-Dexamethasone Sodium Phosp 10 mg/ml	1.34USD	ml
Dexamethasone 4 mg/ml vial	1.04USD	ml
Dexamethasone 6 mg tablet	1.01USD	tablet
Dexasone 4 mg Tablet	0.86USD	tablet
Apo-Dexamethasone 4 mg Tablet	0.8USD	tablet
Pms-Dexamethasone 4 mg Tablet	0.8USD	tablet
Ratio-Dexamethasone 4 mg Tablet	0.8USD	tablet
Dexamethasone 2 mg tablet	0.68USD	tablet
Dexamethasone 1 mg/1 ml soln	0.65USD	ml
Dexamethasone 4 mg tablet	0.6USD	tablet
Dexamethasone 1 mg tablet	0.49USD	tablet
Pms-Dexamethasone 0.75 mg Tablet	0.47USD	tablet
Pms-Dexamethasone 2 mg Tablet	0.43USD	tablet
Dexamethasone 0.5 mg/5ml Elixir	0.4USD	ml
Dexamethasone 0.75 mg tablet	0.38USD	tablet
Dexamethasone 1.5 mg tablet	0.35USD	tablet
Dexamethasone 0.5 mg tablet	0.31USD	tablet
Apo-Dexamethasone 0.5 mg Tablet	0.21USD	tablet
Pms-Dexamethasone 0.5 mg Tablet	0.2USD	tablet
Ratio-Dexamethasone 0.5 mg Tablet	0.18USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US8846650	No	2014-09-30	2025-06-04
US9149486	No	2015-10-06	2022-09-13
US6359016	No	2002-03-19	2020-08-10
US6284804	No	2001-09-04	2020-08-10
US6726918	No	2004-04-27	2020-10-20
US6899717	No	2005-05-31	2023-11-01
US8034366	No	2011-10-11	2023-01-09
US8506987	No	2013-08-13	2023-01-09
US9012437	No	2015-04-21	2020-10-20
US8043628	No	2011-10-25	2020-10-20
US8088407	No	2012-01-03	2020-10-20
US9283178	No	2016-03-15	2020-10-20
US9192511	No	2015-11-24	2023-01-09
US8063031	No	2011-11-22	2020-10-20
US7033605	No	2006-04-25	2020-10-20
US7767223	No	2010-08-03	2021-11-28
US8034370	No	2011-10-11	2023-01-09
US7795316	No	2010-09-14	2028-08-03
US8101582	No	2012-01-24	2027-12-19
US8450287	No	2013-05-28	2027-12-19
US9345714	No	2016-05-24	2022-09-13
US9402805	No	2016-08-02	2022-09-13
US9592242	No	2017-03-14	2020-10-20
US9775849	No	2017-10-03	2020-10-20
US6960346	No	2005-11-01	2023-07-03
US7560120	No	2009-07-14	2022-09-05
US10028965	No	2018-07-24	2034-05-23
US10022502	No	2018-07-17	2020-09-12
US10076526	No	2018-09-18	2023-01-09
US8563027	No	2013-10-22	2030-02-12
US8409606	No	2013-04-02	2030-05-14
US10159683	No	2018-12-25	2034-05-23
US9254267	No	2016-02-09	2024-09-11
US10537585	No	2020-01-21	2037-12-18
US10702539	No	2020-07-07	2023-01-09
US10799642	No	2020-10-13	2032-05-11
US11304961	No	2017-12-18	2037-12-18
US11097061	No	2021-08-24	2039-06-23
US11458041	No	2017-11-16	2037-11-16

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	260-264	ChemSpider
water solubility	89 mg/L (at 25 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	1.83	HANSCH,C ET AL. (1995)
logS	-3.64	ADME Research, USCD
Caco2 permeability	-4.75	ADME Research, USCD

Predicted Properties

Property	Value	Source
Water Solubility	0.0505 mg/mL	ALOGPS
logP	1.93	ALOGPS
logP	1.68	Chemaxon
logS	-3.9	ALOGPS
pKa (Strongest Acidic)	12.42	Chemaxon
pKa (Strongest Basic)	-3.3	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	5	Chemaxon
Hydrogen Donor Count	3	Chemaxon
Polar Surface Area	94.83 Å²	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	102.49 m³·mol^-1	Chemaxon
Polarizability	40.71 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

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 inhibitor	Non-inhibitor	0.9106
CYP450 2D6 inhibitor	Non-inhibitor	0.9231
CYP450 2C19 inhibitor	Non-inhibitor	0.9247
CYP450 3A4 inhibitor	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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-02ai-2923000000-e31987dc12e5a702a42e
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-0a4r-0696000000-1df7921eb1369fef69c4
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-00dj-3960000000-e9ee044790c0655981b1
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-01ot-0904000000-dbbc479b104fbe981ce7
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0903000000-c84b561c97b1277fed56
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0903000000-b498846e21073040b905
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0900000000-b04e175289861dc518f1
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0900000000-b04e175289861dc518f1
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-01ot-0904000000-dbbc479b104fbe981ce7
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0903000000-c84b561c97b1277fed56
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0002-0903000000-b498846e21073040b905
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-006w-0719000000-d4feef3f83ca022aa94d
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0002-0913000000-3c8e5afb526637f1e822
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0002-0910000000-57f268bed9b190ee6066
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0002-0900000000-cfdda545a27ec16c8b76
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0002-0900000000-c70817ad99741f01b675
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00di-0009000000-ecbabc9fe90444b14afe
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05fr-0019000000-4161bdd8f3deed25b9bc
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-002r-0594000000-bf4495b7906d53ad019d
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00ds-0980000000-c4e88ec70fa28252f6f7
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05fs-0930000000-8022e38d862953c2551b
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05fs-1920000000-6f1a7ac153a363c2aa73
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00tf-1910000000-e34981c957b125a39447
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05fr-0019000000-285cd2de8c812f1c5e55
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-002r-0593000000-bd52212afb3af2380901
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00ds-0980000000-ff265e4738c79efad9e3
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00dj-0940000000-818b114d12290dc23743
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05fs-1930000000-9e4283fb9c2780729f55
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-05dm-1920000000-0f41e220b5d3d1abe699
LC-MS/MS Spectrum - LC-ESI-ITFT , positive	LC-MS/MS	splash10-00di-0009000000-cf986616b1138d5569c7
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-00dl-0009000000-431895662c53cadb563c
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-0a4r-0498000000-233b2490f89112ad539e
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-000j-0791000000-c83a21019f43596e6804
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-00dj-0970000000-36eebd63d78f040ae67f
LC-MS/MS Spectrum - LC-ESI-QTOF , positive	LC-MS/MS	splash10-00dj-0940000000-730013951a30cf080ad4
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0a4r-0696000000-1df7921eb1369fef69c4
MS/MS Spectrum - , positive	LC-MS/MS	splash10-00dj-3960000000-e9ee044790c0655981b1
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0a4i-0009000000-00003435b133eaf070c7
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03dl-0009000000-03c14b3aebaeee922b19
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0690-0249000000-4facfeec7ee2fb2f8aac
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0536-9008000000-1e2c2d71c74539debecb
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0k9x-1109000000-05ef731b82e7f2a91eff
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-053i-0891000000-500d64044bb025597c6d
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	200.5607403	predicted	DarkChem Lite v0.1.0
[M-H]-	183.1403496	predicted	DarkChem Lite v0.1.0
[M-H]-	193.32462	predicted	DeepCCS 1.0 (2019)
[M+H]+	205.0308403	predicted	DarkChem Lite v0.1.0
[M+H]+	191.0385409	predicted	DarkChem Lite v0.1.0
[M+H]+	195.22002	predicted	DeepCCS 1.0 (2019)
[M+Na]+	200.8533403	predicted	DarkChem Lite v0.1.0
[M+Na]+	203.5742586	predicted	DarkChem Lite v0.1.0
[M+Na]+	201.1668	predicted	DeepCCS 1.0 (2019)

Targets

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Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	1	N/A	N/A	A29113 / A29577
EC 50 (nM)	5.01	N/A	N/A	A29114 / A29119
EC 50 (nM)	2.5	N/A	N/A	A29155 / A29584 / A29158
EC 50 (nM)	1.1	N/A	N/A	A29155 / A29584 / A29158
EC 50 (nM)	4.2	N/A	N/A	A29155 / A29158
EC 50 (nM)	7.2	N/A	N/A	A28052
EC 50 (nM)	4.5	N/A	N/A	A29584
EC 50 (nM)	7.94	N/A	N/A	A29586
EC 50 (nM)	5	N/A	N/A	A29158
EC 50 (nM)	1.8	N/A	N/A	A29164
EC 50 (nM)	17	N/A	N/A	A29164
EC 50 (nM)	9.7	N/A	N/A	A29588
EC 50 (nM)	13	N/A	N/A	A29588
EC 50 (nM)	3.7	N/A	N/A	A29588
IC 50 (nM)	7.94	N/A	N/A	A29114 / A29119
IC 50 (nM)	>10000	N/A	N/A	A29114 / A29119
IC 50 (nM)	1.17	N/A	N/A	A29114 / A29119
IC 50 (nM)	3.4	N/A	N/A	A29578 / A29157
IC 50 (nM)	3	N/A	N/A	A29151 / A29579 / A29164
IC 50 (nM)	7.6	N/A	N/A	A29117
IC 50 (nM)	1	N/A	N/A	A29117 / A29582 / A29587
IC 50 (nM)	5	N/A	N/A	A29580 / A29581 / A29583 / A27831
IC 50 (nM)	11.4	N/A	N/A	A29121
IC 50 (nM)	2.51	N/A	N/A	A29586
IC 50 (nM)	1.58	N/A	N/A	A29586
IC 50 (nM)	12.59	N/A	N/A	A29586 / A29587
IC 50 (nM)	0.51	N/A	N/A	A29157 / A29164
IC 50 (nM)	0.508	N/A	N/A	A28962
IC 50 (nM)	3.98	N/A	N/A	A29587
Kd (nM)	19	N/A	N/A	A29585
Ki (nM)	5.5	N/A	N/A	A28035
Ki (nM)	1.1	N/A	N/A	A29155 / A29121 / A29158
Ki (nM)	1.2	N/A	N/A	A29584

Details1. Glucocorticoid receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Receptor for glucocorticoids (GC) (PubMed:27120390, PubMed:37478846). 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 modulator of other transcription factors (PubMed:28139699). Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:9590696). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (PubMed:25775514). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
Specific Function: core promoter sequence-specific DNA binding
Gene Name: NR3C1
Uniprot ID: P04150
Uniprot Name: Glucocorticoid receptor
Molecular Weight: 85658.57 Da

References

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Details2. Nuclear receptor subfamily 0 group B member 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Stimulator

General 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 activity of other nuclear receptors through heterodimeric interactions. May also have a role in the development of the embryo and in the maintenance of embryonic stem cell pluripotency (By similarity)
Specific Function: AF-2 domain binding
Gene Name: NR0B1
Uniprot ID: P51843
Uniprot Name: Nuclear receptor subfamily 0 group B member 1
Molecular Weight: 51717.185 Da

References

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. [Article]
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. [Article]

Details3. Annexin A1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Agonist

General 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). Plays a role in glucocorticoid-mediated down-regulation of the early phase of the inflammatory response (By similarity). Contributes to the adaptive immune response by enhancing signaling cascades that are triggered by T-cell activation, regulates differentiation and proliferation of activated T-cells (PubMed:17008549). Promotes the differentiation of T-cells into Th1 cells and negatively regulates differentiation into Th2 cells (PubMed:17008549). Has no effect on unstimulated T cells (PubMed:17008549). Negatively regulates hormone exocytosis via activation of the formyl peptide receptors and reorganization of the actin cytoskeleton (PubMed:19625660). Has high affinity for Ca(2+) and can bind up to eight Ca(2+) ions (By similarity). Displays Ca(2+)-dependent binding to phospholipid membranes (PubMed:2532504, PubMed:8557678). Plays a role in the formation of phagocytic cups and phagosomes. Plays a role in phagocytosis by mediating the Ca(2+)-dependent interaction between phagosomes and the actin cytoskeleton (By similarity)
Specific Function: cadherin binding involved in cell-cell adhesion
Gene Name: ANXA1
Uniprot ID: P04083
Uniprot Name: Annexin A1
Molecular Weight: 38713.855 Da

References

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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details4. Nitric oxide synthase, inducible

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Negative modulator

General Function: Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body (PubMed:7504305, PubMed:7531687, PubMed:7544004, PubMed:7682706). In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity and mediates cysteine S-nitrosylation of cytoplasmic target proteins such PTGS2/COX2 (By similarity). As component of the iNOS-S100A8/9 transnitrosylase complex involved in the selective inflammatory stimulus-dependent S-nitrosylation of GAPDH on 'Cys-247' implicated in regulation of the GAIT complex activity and probably multiple targets including ANXA5, EZR, MSN and VIM (PubMed:25417112). Involved in inflammation, enhances the synthesis of pro-inflammatory mediators such as IL6 and IL8 (PubMed:19688109)
Specific Function: arginine binding
Gene Name: NOS2
Uniprot ID: P35228
Uniprot Name: Nitric oxide synthase, inducible
Molecular Weight: 131116.3 Da

References

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. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details5. Nuclear receptor subfamily 1 group I member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Agonist

General 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 and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes
Specific Function: DNA-binding transcription activator activity, RNA polymerase II-specific
Gene Name: NR1I2
Uniprot ID: O75469
Uniprot Name: Nuclear receptor subfamily 1 group I member 2
Molecular Weight: 49761.245 Da

References

Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [Article]

Enzymes

Details1. 11-beta-hydroxysteroid dehydrogenase type 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Catalyzes the conversion of biologically active 11beta-hydroxyglucocorticoids (11beta-hydroxysteroid) such as cortisol, to inactive 11-ketoglucocorticoids (11-oxosteroid) such as cortisone, in the presence of NAD(+) (PubMed:10497248, PubMed:12788846, PubMed:17314322, PubMed:22796344, PubMed:27927697, PubMed:30902677, PubMed:33387577, PubMed:7859916, PubMed:8538347). Functions as a dehydrogenase (oxidase), thereby decreasing the concentration of active glucocorticoids, thus protecting the nonselective mineralocorticoid receptor from occupation by glucocorticoids (PubMed:10497248, PubMed:12788846, PubMed:17314322, PubMed:33387577, PubMed:7859916). Plays an important role in maintaining glucocorticoids balance during preimplantation and protects the fetus from excessive maternal corticosterone exposure (By similarity). Catalyzes the oxidation of 11beta-hydroxytestosterone (11beta,17beta-dihydroxyandrost-4-ene-3-one) to 11-ketotestosterone (17beta-hydroxyandrost-4-ene-3,11-dione), a major bioactive androgen (PubMed:22796344, PubMed:27927697). Catalyzes the conversion of 11beta-hydroxyandrostenedione (11beta-hydroxyandrost-4-ene-3,17-dione) to 11-ketoandrostenedione (androst-4-ene-3,11,17-trione), which can be further metabolized to 11-ketotestosterone (PubMed:27927697). Converts 7-beta-25-dihydroxycholesterol to 7-oxo-25-hydroxycholesterol in vitro (PubMed:30902677). 7-beta-25-dihydroxycholesterol (not 7-oxo-25-hydroxycholesterol) acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration (PubMed:30902677). May protect ovulating oocytes and fertilizing spermatozoa from the adverse effects of cortisol (By similarity)
Specific Function: 11-beta-hydroxysteroid dehydrogenase (NAD+) activity
Gene Name: HSD11B2
Uniprot ID: P80365
Uniprot Name: 11-beta-hydroxysteroid dehydrogenase type 2
Molecular Weight: 44126.06 Da

References

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. [Article]
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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>50000	N/A	N/A	A15818

Details2. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
Specific Function: 1,8-cineole 2-exo-monooxygenase activity
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
Dexamethasone monograph, Boehringer Ingelheim [Link]
Flockhart Table of Drug Interactions [Link]
FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]

Details3. 11-beta-hydroxysteroid dehydrogenase 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Controls the reversible conversion of biologically active glucocorticoids such as cortisone to cortisol, and 11-dehydrocorticosterone to corticosterone in the presence of NADP(H) (PubMed:10497248, PubMed:12460758, PubMed:14973125, PubMed:15152005, PubMed:15280030, PubMed:17593962, PubMed:21453287, PubMed:27927697, PubMed:30902677). Participates in the corticosteroid receptor-mediated anti-inflammatory response, as well as metabolic and homeostatic processes (PubMed:10497248, PubMed:12414862, PubMed:15152005, PubMed:21453287). Plays a role in the secretion of aqueous humor in the eye, maintaining a normotensive, intraocular environment (PubMed:11481269). Bidirectional in vitro, predominantly functions as a reductase in vivo, thereby increasing the concentration of active glucocorticoids (PubMed:10497248, PubMed:11481269, PubMed:12414862, PubMed:12460758). It has broad substrate specificity, besides glucocorticoids, it accepts other steroid and sterol substrates (PubMed:15095019, PubMed:15152005, PubMed:17593962, PubMed:21453287). Interconverts 7-oxo- and 7-hydroxy-neurosteroids such as 7-oxopregnenolone and 7beta-hydroxypregnenolone, 7-oxodehydroepiandrosterone (3beta-hydroxy-5-androstene-7,17-dione) and 7beta-hydroxydehydroepiandrosterone (3beta,7beta-dihydroxyandrost-5-en-17-one), among others (PubMed:17593962). Catalyzes the stereo-specific conversion of the major dietary oxysterol, 7-ketocholesterol (7-oxocholesterol), into the more polar 7-beta-hydroxycholesterol metabolite (PubMed:15095019, PubMed:15152005). 7-oxocholesterol is one of the most important oxysterols, it participates in several events such as induction of apoptosis, accumulation in atherosclerotic lesions, lipid peroxidation, and induction of foam cell formation (PubMed:15095019). Mediates the 7-oxo reduction of 7-oxolithocholate mainly to chenodeoxycholate, and to a lesser extent to ursodeoxycholate, both in its free form and when conjugated to glycine or taurine, providing a link between glucocorticoid activation and bile acid metabolism (PubMed:21453287). Catalyzes the synthesis of 7-beta-25-dihydroxycholesterol from 7-oxo-25-hydroxycholesterol in vitro, which acts as a ligand for the G-protein-coupled receptor (GPCR) Epstein-Barr virus-induced gene 2 (EBI2) and may thereby regulate immune cell migration (PubMed:30902677)
Specific Function: 11-beta-hydroxysteroid dehydrogenase (NADP+) activity
Gene Name: HSD11B1
Uniprot ID: P28845
Uniprot Name: 11-beta-hydroxysteroid dehydrogenase 1
Molecular Weight: 32400.665 Da

References

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. [Article]
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. [Article]

Details4. Cytochrome P450 3A5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
Specific Function: aromatase activity
Gene Name: CYP3A5
Uniprot ID: P20815
Uniprot Name: Cytochrome P450 3A5
Molecular Weight: 57108.065 Da

References

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. [Article]
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. [Article]
Flockhart Table of Drug Interactions [Link]

Details5. Cytochrome P450 3A7

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
Specific Function: all-trans retinoic acid 18-hydroxylase activity
Gene Name: CYP3A7
Uniprot ID: P24462
Uniprot Name: Cytochrome P450 3A7
Molecular Weight: 57469.95 Da

References

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. [Article]
Flockhart Table of Drug Interactions [Link]

Details6. Steroid 17-alpha-hydroxylase/17,20 lyase

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: A cytochrome P450 monooxygenase involved in corticoid and androgen biosynthesis (PubMed:22266943, PubMed:25301938, PubMed:27339894, PubMed:9452426). Catalyzes 17-alpha hydroxylation of C21 steroids, which is common for both pathways. A second oxidative step, required only for androgen synthesis, involves an acyl-carbon cleavage. The 17-alpha hydroxy intermediates, as part of adrenal glucocorticoids biosynthesis pathway, are precursors of cortisol (Probable) (PubMed:25301938, PubMed:9452426). Hydroxylates steroid hormones, pregnenolone and progesterone to form 17-alpha hydroxy metabolites, followed by the cleavage of the C17-C20 bond to form C19 steroids, dehydroepiandrosterone (DHEA) and androstenedione (PubMed:22266943, PubMed:25301938, PubMed:27339894, PubMed:36640554, PubMed:9452426). Has 16-alpha hydroxylase activity. Catalyzes 16-alpha hydroxylation of 17-alpha hydroxy pregnenolone, followed by the cleavage of the C17-C20 bond to form 16-alpha-hydroxy DHEA (PubMed:36640554). Also 16-alpha hydroxylates androgens, relevant for estriol synthesis (PubMed:25301938, PubMed:27339894). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:22266943, PubMed:25301938, PubMed:27339894, PubMed:9452426)
Specific Function: heme binding
Gene Name: CYP17A1
Uniprot ID: P05093
Uniprot Name: Steroid 17-alpha-hydroxylase/17,20 lyase
Molecular Weight: 57369.995 Da

References

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. [Article]

Details7. Cytochrome P450 1A1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor
Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15041462, PubMed:15805301, PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15041462, PubMed:15805301, PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C15-alpha and C16-alpha positions (PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15805301). Displays different regioselectivities for polyunsaturated fatty acids (PUFA) hydroxylation (PubMed:15041462, PubMed:18577768). Catalyzes the epoxidation of double bonds of certain PUFA (PubMed:15041462, PubMed:19965576, PubMed:20972997). Converts arachidonic acid toward epoxyeicosatrienoic acid (EET) regioisomers, 8,9-, 11,12-, and 14,15-EET, that function as lipid mediators in the vascular system (PubMed:20972997). Displays an absolute stereoselectivity in the epoxidation of eicosapentaenoic acid (EPA) producing the 17(R),18(S) enantiomer (PubMed:15041462). May play an important role in all-trans retinoic acid biosynthesis in extrahepatic tissues. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195)
Specific Function: arachidonic acid monooxygenase activity
Gene Name: CYP1A1
Uniprot ID: P04798
Uniprot Name: Cytochrome P450 1A1
Molecular Weight: 58164.815 Da

References

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. [Article]
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. [Article]

Details8. Cytochrome P450 2A6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General 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. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity
Specific Function: arachidonic acid epoxygenase activity
Gene Name: CYP2A6
Uniprot ID: P11509
Uniprot Name: Cytochrome P450 2A6
Molecular Weight: 56517.005 Da

References

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. [Article]
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 . [Article]
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. [Article]

Details9. Cytochrome P450 2B6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids (PubMed:12865317, PubMed:21289075). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:21289075). Hydroxylates steroid hormones, including testosterone at C-16 and estrogens at C-2 (PubMed:12865317, PubMed:21289075). Plays a role in the oxidative metabolism of xenobiotics, including plant lipids and drugs (PubMed:11695850, PubMed:22909231). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850)
Specific Function: anandamide 11,12 epoxidase activity
Gene Name: CYP2B6
Uniprot ID: P20813
Uniprot Name: Cytochrome P450 2B6
Molecular Weight: 56277.81 Da

References

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. [Article]
Wang H, Tompkins LM: CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme. Curr Drug Metab. 2008 Sep;9(7):598-610. [Article]

Details10. Cytochrome P450 2C19

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). 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 imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
Specific Function: (R)-limonene 6-monooxygenase activity
Gene Name: CYP2C19
Uniprot ID: P33261
Uniprot Name: Cytochrome P450 2C19
Molecular Weight: 55944.565 Da

References

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. [Article]
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. [Article]

Details11. Cytochrome P450 2C8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond (PubMed:15766564, PubMed:19965576, PubMed:7574697). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form (PubMed:11093772). Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1) (PubMed:14559847). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol) (PubMed:26427316)
Specific Function: arachidonic acid epoxygenase activity
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

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. [Article]
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. [Article]
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. [Article]

Details12. Cytochrome P450 2E1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of fatty acids (PubMed:10553002, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10553002, PubMed:18577768). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates fatty acids specifically at the omega-1 position displaying the highest catalytic activity for saturated fatty acids (PubMed:10553002, PubMed:18577768). May be involved in the oxidative metabolism of xenobiotics (Probable)
Specific Function: 4-nitrophenol 2-monooxygenase activity
Gene Name: CYP2E1
Uniprot ID: P05181
Uniprot Name: Cytochrome P450 2E1
Molecular Weight: 56848.42 Da

References

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. [Article]
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. [Article]
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. [Article]

Details13. Cytochrome P450 3A43

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: Exhibits low testosterone 6-beta-hydroxylase activity
Specific Function: aromatase activity
Gene Name: CYP3A43
Uniprot ID: Q9HB55
Uniprot Name: Cytochrome P450 3A43
Molecular Weight: 57669.21 Da

References

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. [Article]

Details14. Cytochrome P450 4A11

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: A cytochrome P450 monooxygenase involved in the metabolism of fatty acids and their oxygenated derivatives (oxylipins) (PubMed:10553002, PubMed:10660572, PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:10553002, PubMed:10660572, PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). Catalyzes predominantly the oxidation of the terminal carbon (omega-oxidation) of saturated and unsaturated fatty acids, the catalytic efficiency decreasing in the following order: dodecanoic > tetradecanoic > (9Z)-octadecenoic > (9Z,12Z)-octadecadienoic > hexadecanoic acid (PubMed:10553002, PubMed:10660572). Acts as a major omega-hydroxylase for dodecanoic (lauric) acid in liver (PubMed:15611369, PubMed:1739747, PubMed:7679927, PubMed:8914854). Participates in omega-hydroxylation of (5Z,8Z,11Z,14Z)-eicosatetraenoic acid (arachidonate) to 20-hydroxyeicosatetraenoic acid (20-HETE), a signaling molecule acting both as vasoconstrictive and natriuretic with overall effect on arterial blood pressure (PubMed:10620324, PubMed:10660572, PubMed:15611369). Can also catalyze the oxidation of the penultimate carbon (omega-1 oxidation) of fatty acids with lower efficiency (PubMed:7679927). May contribute to the degradation of saturated very long-chain fatty acids (VLCFAs) such as docosanoic acid, by catalyzing successive omega-oxidations to the corresponding dicarboxylic acid, thereby initiating chain shortening (PubMed:18182499). Omega-hydroxylates (9R,10S)-epoxy-octadecanoate stereoisomer (PubMed:15145985). Plays a minor role in omega-oxidation of long-chain 3-hydroxy fatty acids (PubMed:18065749). Has little activity toward prostaglandins A1 and E1 (PubMed:7679927)
Specific Function: alkane 1-monooxygenase activity
Gene Name: CYP4A11
Uniprot ID: Q02928
Uniprot Name: Cytochrome P450 4A11
Molecular Weight: 59347.31 Da

References

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. [Article]
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. [Article]

Details15. Cytochrome P450 11B1, mitochondrial

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: A cytochrome P450 monooxygenase involved in the biosynthesis of adrenal corticoids (PubMed:12530636, PubMed:1518866, PubMed:1775135, PubMed:18215163, PubMed:23322723). Catalyzes a variety of reactions that are essential for many species, including detoxification, defense, and the formation of endogenous chemicals like steroid hormones. Steroid 11beta, 18- and 19-hydroxylase with preferred regioselectivity at 11beta, then 18, and lastly 19 (By similarity). Catalyzes the hydroxylation of 11-deoxycortisol and 11-deoxycorticosterone (21-hydroxyprogesterone) at 11beta position, yielding cortisol or corticosterone, respectively, but cannot produce aldosterone (PubMed:12530636, PubMed:1518866, PubMed:1775135, PubMed:18215163, PubMed:23322723). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate for hydroxylation and reducing the second into a water molecule. Two electrons are provided by NADPH via a two-protein mitochondrial transfer system comprising flavoprotein FDXR (adrenodoxin/ferredoxin reductase) and nonheme iron-sulfur protein FDX1 or FDX2 (adrenodoxin/ferredoxin) (PubMed:18215163). Due to its lack of 18-oxidation activity, it is incapable of generating aldosterone (PubMed:23322723). Could also be involved in the androgen metabolic pathway (Probable)
Specific Function: corticosterone 18-monooxygenase activity
Gene Name: CYP11B1
Uniprot ID: P15538
Uniprot Name: Cytochrome P450 11B1, mitochondrial
Molecular Weight: 57572.44 Da

References

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. [Article]

Carriers

Details1. Albumin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
Specific Function: antioxidant activity
Gene Name: ALB
Uniprot ID: P02768
Uniprot Name: Albumin
Molecular Weight: 69365.94 Da

References

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. [Article]

Transporters

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>50000	N/A	N/A	A15818

Details1. ATP-dependent translocase ABCB1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor
Inducer

General Function: Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
Specific Function: ABC-type xenobiotic transporter activity
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: ATP-dependent translocase ABCB1
Molecular Weight: 141477.255 Da

References

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details2. Organic anion transporter 3

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient (PubMed:14586168, PubMed:15644426, PubMed:15846473, PubMed:16455804, PubMed:31553721). Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) (PubMed:14586168, PubMed:15846473, PubMed:15864504, PubMed:22108572, PubMed:23832370). Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain (PubMed:11306713, PubMed:14586168, PubMed:15846473). E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange (PubMed:26377792). Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule (PubMed:11907186). Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate (PubMed:22108572, PubMed:23832370). Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins (PubMed:28534121). May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside (PubMed:15644426). May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate (PubMed:11669456, PubMed:15846473, PubMed:16455804). Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) (PubMed:14675047). May contribute to the release of cortisol in the adrenals (PubMed:15864504). Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB). In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Specific Function: organic anion transmembrane transporter activity
Gene Name: SLC22A8
Uniprot ID: Q8TCC7
Uniprot Name: Organic anion transporter 3
Molecular Weight: 59855.585 Da

References

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. [Article]

Details3. Bile salt export pump

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner (PubMed:15791618, PubMed:16332456, PubMed:18985798, PubMed:19228692, PubMed:20010382, PubMed:20398791, PubMed:22262466, PubMed:24711118, PubMed:29507376, PubMed:32203132). Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts (PubMed:16332456). Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion (PubMed:15901796, PubMed:18245269)
Specific Function: ABC-type bile acid transporter activity
Gene Name: ABCB11
Uniprot ID: O95342
Uniprot Name: Bile salt export pump
Molecular Weight: 146405.83 Da

References

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. [Article]

Details4. ATP-binding cassette sub-family C member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inducer

General Function: ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports a wide variety of conjugated organic anions such as sulfate-, glucuronide- and glutathione (GSH)-conjugates of endo- and xenobiotics substrates (PubMed:10220572, PubMed:10421658, PubMed:11500505, PubMed:16332456). Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification (PubMed:10421658). Mediates also hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 (PubMed:11500505). Transports sulfated bile salt such as taurolithocholate sulfate (PubMed:16332456). Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors (PubMed:10220572, PubMed:11500505, PubMed:12441801). Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine (PubMed:10220572, PubMed:11500505)
Specific Function: ABC-type glutathione S-conjugate transporter activity
Gene Name: ABCC2
Uniprot ID: Q92887
Uniprot Name: ATP-binding cassette sub-family C member 2
Molecular Weight: 174205.64 Da

References

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. [Article]
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. [Article]

Details5. Broad substrate specificity ATP-binding cassette transporter ABCG2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells (PubMed:11306452, PubMed:12958161, PubMed:19506252, PubMed:20705604, PubMed:28554189, PubMed:30405239, PubMed:31003562). Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme (PubMed:20705604, PubMed:23189181). Also mediates the efflux of sphingosine-1-P from cells (PubMed:20110355). Acts as a urate exporter functioning in both renal and extrarenal urate excretion (PubMed:19506252, PubMed:20368174, PubMed:22132962, PubMed:31003562, PubMed:36749388). In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates (PubMed:12682043, PubMed:28554189, PubMed:30405239). Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux (PubMed:11306452, PubMed:12477054, PubMed:15670731, PubMed:18056989, PubMed:31254042). In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity)
Specific Function: ABC-type xenobiotic transporter activity
Gene Name: ABCG2
Uniprot ID: Q9UNQ0
Uniprot Name: Broad substrate specificity ATP-binding cassette transporter ABCG2
Molecular Weight: 72313.47 Da

References

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. [Article]

Details6. Solute carrier organic anion transporter family member 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Specific Function: bile acid transmembrane transporter activity
Gene Name: SLCO1A2
Uniprot ID: P46721
Uniprot Name: Solute carrier organic anion transporter family member 1A2
Molecular Weight: 74144.105 Da

References

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. [Article]
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. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 17, 2024 17:30

Dexamethasone

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Structure for Dexamethasone (DB01234)

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