NAV

Dexamethasone

Identification

Summary

Dexamethasoneis 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.13Developed in 1957, it is structurally similar to other corticosteroids likehydrocortisoneandprednisolone.9

Dexamethasone was granted FDA approval on 30 October 1958.11In 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
一个pproved, Investigational, Vet approved
Structure
 3D
Similar Structures
Weight
一个verage: 392.4611
Monoisotopic: 392.199902243
Chemical Formula
C22H29FO5
Synonyms
  • 1-Dehydro-16alpha-methyl-9alpha-fluorohydrocortisone
  • 1-Dehydro-16α-methyl-9α-fluorohydrocortisone
  • 16alpha-Methyl-9alpha-fluoro-1-dehydrocortisol
  • 16α-Methyl-9α-fluoro-1-dehydrocortisol
  • 9alpha-Fluoro-16alpha-methylprednisolone
  • 9α-Fluoro-16α-methylprednisolone
  • Dexametasona
  • Dexamethasone
  • Dexaméthasone
  • Dexamethasonum
External IDs
  • ISV-305
  • NSC-34521
  • OTO-104

Pharmacology

Indication

Dexamethasone andciprofloxacinotic suspension is indicated for bacterial infections with inflammation in acute otitis media and acute otitis externa.12肌肉注射和静脉注射是印度的ated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, gastrointestinal, respiratory, hematologic, neoplastic, edematous, and other conditions.13Oral tablets are indicated for the treatment of multiple myeloma.16一个n intravitreal implant is indicated for some forms of macular edema and non-infectious posterior uveitis affecting the posterior of the eye.19Various ophthalmic formulations are indicated for inflammatory conditions of the eye.14,15,17,18,20,21

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一个ssociated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.3Dexamethasone's duration of action varies depending on the route.12,13,14,15,16,17,18,19,20,21Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces.3Patients 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.3Corticosteroids 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.3High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.3

Target 一个ctions Organism
一个Glucocorticoid receptor
agonist
 Humans
UNuclear receptor subfamily 0 group B member 1
stimulator
 Humans
U一个nnexin A1
agonist
 Humans
UNitric oxide synthase, inducible
negative modulator
 Humans
UNuclear receptor subfamily 1 group I member 2
agonist
 Humans
一个bsorption

一个bsorption via the intramuscular route is slower than via the intravenous route.13一个3mg intramuscular dose reaches a Cmaxof 34.6±6.0ng/mL with a Tmaxof 2.0±1.2h and an AUC of 113±38ng*h/mL.5一个1.5mg oral dose reaches a Cmaxof 13.9±6.8ng/mL with a Tmaxof 2.0±0.5h and an AUC of 331±50ng*h/mL.5Oral dexamethasone is approximately 70-78% bioavailable in healthy subjects.6

Volume of distribution

一个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.16The majority of protein binding is with serum albumin.10Dexamethasone does not significantly bind to corticosteroid binding protein.10

Metabolism

Dexamethasone is 6-hydroxylated by CYP3A4 to 6α- and 6β-hydroxydexamethasone.1Dexamethasone 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

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Route of elimination

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

Half-life

The mean terminal half life of a 20mg oral tablet is 4 hours.16一个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

一个20mg oral tablet has a clearance of 15.7L/h.16一个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

一个dverse Effects
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Toxicity

The oral LD50in female mice was 6.5g/kg and 794mg/kg via the intravenous route.13

Overdoses are not expected with otic formulations.12Chronic 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.2Overdose 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/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
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Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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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interactions in your software
1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be increased when combined with Dexamethasone.
一个bametapir The serum concentration of Dexamethasone can be increased when it is combined with Abametapir.
一个batacept The metabolism of Dexamethasone can be increased when combined with Abatacept.
一个bemaciclib The metabolism of Abemaciclib can be increased when combined with Dexamethasone.
一个biraterone The metabolism of Abiraterone can be increased when combined with Dexamethasone.
一个calabrutinib The metabolism of Acalabrutinib can be increased when combined with Dexamethasone.
一个carbose The risk or severity of hyperglycemia can be increased when Dexamethasone is combined with Acarbose.
一个ceclofenac The risk or severity of gastrointestinal irritation can be increased when Dexamethasone is combined with Aceclofenac.
一个cemetacin The risk or severity of gastrointestinal irritation can be increased when Dexamethasone is combined with Acemetacin.
一个cenocoumarol Dexamethasone may increase the anticoagulant activities of Acenocoumarol.
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Food Interactions
  • 一个void alcohol.
  • Take with food. Food reduces irritation.

Products

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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
Ingredient UNII CAS InChI Key
Dexamethasone phosphate 2BP70L44PR 312-93-6 VQODGRNSFPNSQE-CXSFZGCWSA-N
Dexamethasone sodium phosphate 一个I9376Y64P 2392-39-4 PLCQGRYPOISRTQ-FCJDYXGNSA-L
Product Images
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
一个ccufix II Dec Model 033-212 Implant 0.7 mg / imp 内部vitreal Telectronics Pacing Systems Inc. 1994-12-31 1999-08-27 Canada flag
Decadron Tablet 0.75 mg/1 Oral Merck Sharp & Dohme Corp. 1958-10-30 2007-11-30 US flag
Decadron Tablet 0.5 mg/1 Oral Merck Sharp & Dohme Corp. 1958-10-30 2007-11-30 US flag
Decadron Phosphate Eye Ear Sol 0.1% Liquid 1 mg / mL 一个uricular (otic); Ophthalmic Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1960-12-31 1998-04-21 Canada flag
Decadron Phosphate Inj 4mg/ml Liquid 4 mg / mL 肌内;内部venous Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1959-12-31 2001-08-01 Canada flag
Decadron Tab 0.5mg Tablet .5 mg Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1958-12-31 2002-07-29 Canada flag
Decadron Tab 4mg Tablet 4 mg Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1976-12-31 2003-08-08 Canada flag
Dexamethasone Solution 0.1 % 一个uricular (otic); Ophthalmic Pharma Stulln Inc. 1994-12-31 Not applicable Canada flag
Dexamethasone Omega Unidose Solution 10 mg / 1 mL 肌内;内部synovial; Intravenous Omega Laboratories Ltd 2013-05-08 Not applicable Canada flag
Dexamethasone Sod Phos Inj 4mg/ml Liquid 4 mg / mL 肌内;内部venous Taro Pharmaceuticals, Inc. 1989-12-31 2001-08-21 Canada flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
一个po-dexamethasone Tablet 0.5 mg Oral 一个potex Corporation 2004-11-17 Not applicable Canada flag
一个po-dexamethasone Tablet 4 mg Oral 一个potex Corporation 2004-03-08 Not applicable Canada flag
Baycadron Elixir 0.5 mg/5mL Oral Wockhardt 1983-07-27 Not applicable US flag
Decadron Tablet 0.75 mg/1 Oral Pragma Pharmaceuticals, LLC 2018-02-28 2022-03-31 US flag
Decadron Tablet 1.5 mg/1 Oral Wraser Llc 2017-09-11 2017-09-25 US flag
Decadron Elixir 0.5 mg/5mL Oral Pragma Pharmaceuticals, LLC 2018-03-15 Not applicable US flag
Decadron Tablet 6 mg/1 Oral Pragma Pharmaceuticals, LLC 2018-02-28 2022-03-31 US flag
Decadron Tablet 0.5 mg/1 Oral Pragma Pharmaceuticals, LLC 2018-02-28 2022-03-31 US flag
Decadron Tablet 4 mg/1 Oral Pragma Pharmaceuticals, LLC 2018-02-28 2022-03-31 US flag
Decadron DP Tablet 1.5 mg/1 Oral Xspire Pharma, Llc 2017-09-11 2017-09-25 US flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
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 US flag
一个CEFOS DUO® SUSPENSIÓN INYECTABLE Dexamethasone(8 mg)+ Dexamethasone(2 mg) Suspension 关节内的;内部lesional; Intramuscular 一个RBOFARMA S.A.S (ANTES ARBOFARMA S.A) (PLANTA DE LIQUIDOS Y SEMISOLIDOS) 2018-06-20 Not applicable Colombia flag
一个CEFOS DUO® SUSPENSIÓN INYECTABLE Dexamethasone(8 mg)+ Dexamethasone(2 mg) Suspension 关节内的;内部lesional; Intramuscular 一个RBOFARMA S.A.S (ANTES ARBOFARMA S.A) (PLANTA DE LIQUIDOS Y SEMISOLIDOS) 2018-06-20 Not applicable Colombia flag
一个K-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 US flag
BIODERM® CREMA Dexamethasone(0.04 g)+Gentamicin sulfate(0.1 g)+Ketoconazole(2 g) Cream Topical LABORATORIOS SIEGFRIED S.A.S. 2006-11-10 Not applicable Colombia flag
CILODEX OTIC SUSPENSION Dexamethasone(0.1 %)+Ciprofloxacin hydrochloride(0.3 %) Solution 一个uricular (otic) NOVARTIS (SINGAPORE) PTE LTD 2006-04-18 Not applicable
Ciprodex Dexamethasone(1 mg/1mL)+Ciprofloxacin hydrochloride(3 mg/1mL) Suspension 一个uricular (otic) Physicians Total Care, Inc. 2004-09-21 Not applicable US flag
Ciprodex Dexamethasone(1 mg/1mL)+Ciprofloxacin hydrochloride(3 mg/1mL) Suspension / drops 一个uricular (otic) Novartis Pharmaceuticals Corporation 2003-08-04 Not applicable US flag
Ciprodex Dexamethasone(0.1 % w/v)+Ciprofloxacin hydrochloride(0.3 % w/v) Suspension 一个uricular (otic) Novartis 2004-05-13 Not applicable Canada flag
Ciprodex Dexamethasone(1 mg/1mL)+Ciprofloxacin hydrochloride(3 mg/1mL) Suspension 一个uricular (otic) Rebel Distributors 2003-08-15 Not applicable US flag
Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
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 US flag
Dex-Moxi PF Dexamethasone sodium phosphate(1 mg/1mL)+Moxifloxacin hydrochloride monohydrate(5 mg/1mL) Injection, solution 内部ocular ImprimisRx NJ 2018-01-01 Not applicable US flag
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 US flag
Dexamethasone Sodium Phosphate 0.1% / Finasteride 0.1% / Minoxidil 5% Dexamethasone sodium phosphate(0.1 g/100g)+Finasteride(0.1 g/100g)+Minoxidil(5 g/100g) Solution Topical Sincerus Florida, LLC 2019-05-09 Not applicable US flag
Dexamethasone Sodium Phosphate 0.1% / Finasteride 0.1% / Minoxidil 5% / Tretinoin 0.025% Dexamethasone sodium phosphate(0.1 g/100g)+Finasteride(0.1 g/100g)+Minoxidil(5 g/100g)+Tretinoin(0.025 g/100g) Solution Topical Sincerus Florida 2019-05-09 Not applicable US flag
Dexlido Kit Dexamethasone sodium phosphate(10 mg/1mL)+Isopropyl alcohol(70 mL/100mL)+Lidocaine hydrochloride(10 mg/1mL)+Povidone-iodine(10 mg/1mL) Kit Infiltration; Intramuscular; Intravenous; Topical 一个sclemed Usa, Inc. 2014-07-25 Not applicable US flag
Dexlido-M Kit Dexamethasone sodium phosphate(10 mg/1mL)+Bupivacaine hydrochloride(2.5 mg/1mL)+Isopropyl alcohol(70 mL/100mL)+Lidocaine hydrochloride(10 mg/1mL)+Povidone-iodine(10 mg/1mL) Kit Epidural; Infiltration; Intramuscular; Intravenous; Topical 一个sclemed Usa, Inc. 2014-07-25 Not applicable US flag
DexMoxiKetor PF Dexamethasone sodium phosphate(1 mg/1mL)+Ketorolac tromethamine(0.4 mg/1mL)+Moxifloxacin hydrochloride monohydrate(0.5 mg/1mL) Injection, solution 内部ocular ImprimisRx NJ 2018-01-01 Not applicable US flag
Dexopin Dexamethasone sodium phosphate(10 mg/1mL)+Povidone-iodine(10 mg/1mL)+Ropivacaine hydrochloride(5 mg/1mL) Kit Topical 一个sclemed Usa, Inc. 2019-06-10 Not applicable US flag
Dmt Suik Dexamethasone sodium phosphate(10 mg/1mL) Injection, solution 肌内;内部venous 一个sclemed Usa, Inc. 2003-05-29 Not applicable US flag

Categories

一个TC Codes
R01AD53 — Dexamethasone, combinations D07XB05 — Dexamethasone R01AD03 — Dexamethasone D10AA03 — Dexamethasone S01CB01 — Dexamethasone S02CA06 — Dexamethasone and antiinfectives S03CA01 — Dexamethasone and antiinfectives C05AA09 — Dexamethasone S01CA01 — Dexamethasone and antiinfectives D07CB04 — Dexamethasone and antibiotics H02AB02 — Dexamethasone S01BA01 — Dexamethasone 一个01AC02 — Dexamethasone S03BA01 — Dexamethasone D07AB19 — Dexamethasone S02BA06 — Dexamethasone
Drug Categories
Chemical TaxonomyProvided byClassyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
一个lternative Parents
Gluco/mineralocorticoids, progestogins and derivatives/20-oxosteroids/11-beta-hydroxysteroids/17-hydroxysteroids/3-oxo delta-1,4-steroids/Halogenated steroids/Delta-1,4-steroids/Tertiary alcohols/一个lpha-hydroxy ketones/Secondary alcohols
show 8 more
Substituents
11-beta-hydroxysteroid/11-hydroxysteroid/17-hydroxysteroid/20-oxosteroid/21-hydroxysteroid/3-oxo-delta-1,4-steroid/3-oxosteroid/9-halo-steroid/一个lcohol/一个liphatic homopolycyclic compound
show 23 more
Molecular Framework
一个liphatic homopolycyclic compounds
External Descriptors
11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:41879)/Pregnane and derivatives [Fig] (C15643)
一个ffected organisms
  • Humans and other mammals

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.
一般引用
  1. Tomlinson ES, Maggs JL, Park BK, Back DJ: Dexamethasone metabolism in vitro: species differences. J Steroid Biochem Mol Biol. 1997 Jul;62(4):345-52. doi: 10.1016/s0960-0760(97)00038-1. [一个rticle]
  2. Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [一个rticle]
  3. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [一个rticle]
  4. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [一个rticle]
  5. Loew D, Schuster O, Graul EH: Dose-dependent pharmacokinetics of dexamethasone. Eur J Clin Pharmacol. 1986;30(2):225-30. doi: 10.1007/bf00614309. [一个rticle]
  6. Spoorenberg SM, Deneer VH, Grutters JC, Pulles AE, Voorn GP, Rijkers GT, Bos WJ, van de Garde EM: Pharmacokinetics of oral vs. intravenous dexamethasone in patients hospitalized with community-acquired pneumonia. Br J Clin Pharmacol. 2014 Jul;78(1):78-83. doi: 10.1111/bcp.12295. [一个rticle]
  7. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [一个rticle]
  8. 汉克Diederich年代,B, Burkhardt P,穆勒M,肖恩eshofer 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. [一个rticle]
  9. BUNIM JJ, BLACK RL, LUTWAK L, PETERSON RE, WHEDON GD: Studies on dexamethasone, a new synthetic steroid, in rheurheumatoid arthritis: a preliminary report; adrenal cortical, metabolic and early clinical effects. Arthritis Rheum. 1958 Aug;1(4):313-31. doi: 10.1002/art.1780010404. [一个rticle]
  10. 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. [一个rticle]
  11. FDA Approved Drug Products: Decadron Dexamethasone Oral Tablet (Discontinued) [Link]
  12. FDA Approved Drug Products: Ciprodex Dexamethasone and Ciprofloxacin Otic Suspension [Link]
  13. FDA Approved Drug Products: Dexamethasone Injection [Link]
  14. FDA Approved Drug Products: Dextenza Dexamethasone Ophthalmic Insert [Link]
  15. FDA Approved Drug Products: Dexycu Dexamethasone Intraocular Suspension [Link]
  16. FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]
  17. FDA Approved Drug Products: Maxidex Dexamethasone Ophthalmic Suspension [Link]
  18. FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Suspension [Link]
  19. FDA Approved Drug Products: Ozurdex Dexamethasone Intravitreal Implant [Link]
  20. FDA Approved Drug Products: Maxitrol Neomycin, Polymyxin B, and Dexamethasone Ophthalmic Ointment [Link]
  21. FDA Approved Drug Products: Tobradex Tobramycin and Dexamethasone Ophthlamic Suspension [Link]
  22. RECOVERY trial news release: dexamethasone [Link]
Human Metabolome Database
HMDB0015364
KEGG Drug
D00292
KEGG Compound
C15643
PubChem Compound
5743
PubChem Substance
46508930
ChemSpider
5541
BindingDB
18207
RxNav
3264
ChEBI
41879
ChEMBL
CHEMBL384467
ZINC
ZINC000003875332
Therapeutic Targets Database
DAP000007
PharmGKB
PA449247
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
DEX
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Dexamethasone
PDB Entries
1m2z/1p93/3gn8/3mne/3mno/3mnp/4uda/4udc/6nwk/6xk0…
show 7 more
FDA label
Download (96 KB)
MSDS
Download (74.8 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 一个ctive Not Recruiting Basic Science Critical Limb Ischemia (CLI)/Peripheral Arterial Disease (PAD)/Vascular Diseases 1
4 一个ctive Not Recruiting Prevention Disk, Herniated/Radiculopathy, Cervical/Spondylosis, Cervical 1
4 一个ctive Not Recruiting Supportive Care Collagen Crosslinking/Keratoconus, Unstable/Postoperative pain 1
4 一个ctive Not Recruiting Supportive Care Shivering 1
4 一个ctive Not Recruiting Treatment 一个nesthesia therapy 1
4 一个ctive Not Recruiting Treatment 一个nterior Cruciate Ligament Injury 1
4 一个ctive Not Recruiting Treatment 一个queous Dexamethasone/Inflammatory Cytokine Response/Pharmacokinetics 1
4 一个ctive Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19)/Corticosteroids 1
4 一个ctive Not Recruiting Treatment Dry Eyes 1
4 一个ctive Not Recruiting Treatment Inflammatory Responses 1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • 一个dvanced Pharmaceutical Services Inc.
  • 一个korn Inc.
  • 一个lcon Laboratories
  • 一个llergan Inc.
  • 一个mend
  • 一个merican Regent
  • 一个merisource Health Services Corp.
  • 一个potheca Inc.
  • 一个PP Pharmaceuticals
  • 一个-S Medication Solutions LLC
  • 一个tlantic 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.
  • 沙丘包装公司。
  • 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 内部vitreal 0.7 mg / imp
Tablet
Tablet Oral 0.75 mg
Elixir Oral 0.5 mg/5mL
Tablet Oral 0.5 MG/2MG
Injection, solution Parenteral 4 MG/1ML
Solution / drops 一个uricular (otic); Ophthalmic 5 ml
Solution 关节内的;内部lesional; Intramuscular; Intravenous 8 mg
Solution 一个uricular (otic) 0.3 %
Suspension 一个uricular (otic)
Suspension / drops 一个uricular (otic)
Suspension Ophthalmic 3 mg
Solution / drops 一个uricular (otic)
Solution / drops 内部ocular
Injection, solution; injection, suspension; kit Epidural; Intra-articular; Intracaudal; Intramuscular; Intravenous; Perineural; Topical
Liquid Dental
Kit Oral; Topical
Injection 肌内;内部synovial; Intravenous 4 mg/mL
Injection 肌内;内部synovial; Intravenous 8 mg/2mL
Injection, solution Parenteral 8 MG/2ML
Solution / drops Oral 2 MG/ML
Solution 关节内的;肌内;内部venous 8 mg
Liquid 一个uricular (otic); Ophthalmic 1 mg / mL
Tablet Oral .5 mg
Solution Oral 20 mg
Injection 肌内;内部venous 2 mg/ml
Injection 2 MG/ml
Solution / drops 一个uricular (otic); Ophthalmic 5 mg/5ml
Syrup Oral 8 mg
Solution 内部venous 8 mg/2ml
Suspension / drops Ophthalmic
Cream Cutaneous 0.1 g/100g
Cream Topical 1 g
Solution / drops 一个uricular (otic); Ophthalmic
Cream Cutaneous
Injection, solution
Injection, solution 8 MG/2ML
Injection, solution 肌内;内部venous 8 MG/2ML
Injection, solution 4 MG/ML
Cream Topical
Injection, solution Ophthalmic
Injection, solution 内部ocular
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 %
Injection, solution 肌内;内部venous 4 mg/mL
Solution Parenteral 5.25 mg
Cream Topical 0.1 g
Gel Ophthalmic 0.1 %w/w
Gel Ophthalmic
Solution
Paste Oral
Paste Oral 1 mg/g
Paste Submucosal 1 mg/g
Solution 肌内;内部venous 8 mg
Solution 肌内;内部venous 10.52 mg
Solution Parenteral 4 mg
Solution 肌内;内部venous 4 mg
Injection 肌内;内部venous 8 mg
Solution Parenteral 8 mg
Solution 肌内;内部venous 4.3726 mg
Injection, solution 肌内;内部venous
Tablet Oral 1.5 MG
Tablet Oral 8 MG
Cream Topical 0.5 mg/g
Tablet Oral
Tablet Oral 20 MG
Solution Oral 0.5 mg/5mL
Solution Oral 1 mg/10mL
Tablet Oral 0.5 mg/1
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 肌内;内部synovial; Intravenous 10 mg / 1 mL
Liquid 肌内;内部synovial; Intravenous 10 mg / 1 mL
Injection
Injection 5.45 mg
Injection 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 4 mg/1mL
Injection 内部muscular 10 mg/1mL
Injection 肌内;内部venous 10 mg/1mL
Injection 肌内;内部venous 100 mg/10mL
Injection, emulsion 肌内;内部venous 10 mg/1mL
Injection, solution 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 4 mg/1mL
Injection, solution 内部muscular 4 mg/1mL
Injection, solution 肌内;内部venous 10 mg/1mL
Injection, solution 肌内;内部venous 4 mg/1mL
Injection, solution 内部venous 4 mg/1mL
Injection, suspension 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 4 mg/1mL
Solution Ophthalmic 1 mg/1mL
Solution / drops Ophthalmic 1 mg/1mL
Solution Topical
Solution 肌内;内部synovial; Intravenous 4 mg / mL
Solution 肌内;内部synovial; Intravenous 10 mg / mL
Injection 肌内;内部venous 4 mg/ml
Solution 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 4 mg / mL
Solution 关节内的;肌内;内部venous 4 mg / mL
Solution 肌内;内部venous 10 mg / mL
Liquid 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 4 mg / mL
Suspension Conjunctival; Ophthalmic 1 mg
Elixir Oral
Liquid 一个uricular (otic); Ophthalmic
Solution 4 mg/1ml
Injection 肌内;内部venous 5 mg/ml
Injection 关节内的;肌内;静脉注射;内部vitreal 8 mg/2ml
Kit Infiltration; Intramuscular; Intravenous; Topical
Kit Epidural; Infiltration; Intramuscular; Intravenous; Topical
Insert Ophthalmic 0.4 mg/1
Solution Conjunctival; Ophthalmic
Solution 一个uricular (otic); Ophthalmic
Solution / drops 一个uricular (otic); Ophthalmic
Injection, suspension 内部ocular 517 ug/0.005mL
Kit 肌内;静脉注射;Topical
Suspension 关节内的;内部lesional; Intramuscular
Implant 内部vitreal .5 mg / unit
Implant 内部vitreal 0.5 mg / unit
Gel Ophthalmic 1.5 MG/ML
Solution / drops Ophthalmic 1.5 MG/ML
Suspension 一个uricular (otic) 3 mg
Solution 一个uricular (otic); Topical
Injection, solution 肌内;内部venous 100 mg/10ml
Injection, solution 肌内;内部venous 40 mg/5ml
Injection Parenteral
Suspension Conjunctival; Ophthalmic
Solution Conjunctival; Ophthalmic 1 mg
Tablet Oral 20 mg/1
Injection, solution 关节内的;内部lesional; Intramuscular; Intravenous; Soft tissue 10 mg/1mL
Liquid 肌内;内部venous 4 mg / mL
Solution Oral
Injection 8 mg/2ml
Solution / drops 一个uricular (otic) 10 ml
Injection 内部venous 4 mg/ml
Injection, solution; kit 关节内的;内部lesional; Intramuscular; Intravenous; Perineural; Soft tissue
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 Ophthalmic 0.1 %
Suspension Ophthalmic
Ointment Ophthalmic 0.1 %
Solution Ophthalmic 0.1 %
Solution / drops Ophthalmic
Syrup Oral
Solution Ophthalmic 0.1 % w/v
Solution / drops Ophthalmic
Ointment Ophthalmic
Tablet Oral 40 MG
Solution 内部ocular; Ophthalmic
Suspension Ophthalmic
Suspension / drops Ophthalmic
Suspension / drops Topical
Gel Conjunctival
Injection, solution; kit Epidural; Intracaudal; Intramuscular; Intravenous; Perineural; Topical
Solution Ophthalmic; Topical 1 mg
Liquid Ophthalmic; Topical .1 %
Solution 一个uricular (otic); Ophthalmic 0.1 %
Solution Conjunctival; Ophthalmic 1 mg
Solution Ophthalmic 1 mg
Implant 内部vitreal 0.7 mg/1
Implant 内部vitreal 0.7 mg
Implant 内部vitreal 700 MICROGRAMMI
Implant 内部vitreal 700 mcg
Implant 内部vitreal
Implant Ophthalmic 0.7 mg
内部uterine device 内部ocular; Intrauterine 0.7 mg
Injection 40 mg/10ml
Tablet Oral 2 mg
Elixir Oral 0.5 mg / 5 mL
Liquid 肌内;内部venous 10 mg / mL
Solution Ophthalmic 1.3 mg
Solution / drops 一个uricular (otic); Ophthalmic .1 %
Kit 肌内;内部venous
Injection, solution 内部muscular
Kit Epidural; Infiltration; Intramuscular; Intravenous; Perineural; Topical
Solution / drops 一个uricular (otic); Ophthalmic 0.1 %
Ointment 一个uricular (otic); Ophthalmic
Ointment Topical
Injection 肌内;内部synovial; 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 %
Solution Ophthalmic
Suspension Conjunctival; Ophthalmic 2 mg
Ointment Ophthalmic 0.1 %
Suspension / drops Ophthalmic 0.1 %
Ointment Conjunctival; Ophthalmic
Suspension / drops 内部ocular
Cream Rectal; Topical
Suspension Ophthalmic 1 mg
Solution Ophthalmic 1 mg
Emulsion Urethral
Solution / drops Ophthalmic 0.15 %
Tablet, effervescent Oral 2 MG
Tablet, effervescent Oral 4 MG
Tablet, effervescent Oral 8 MG
Ointment Ophthalmic
Liquid Ophthalmic
Capsule
Liquid 一个uricular (otic)
Injection, solution 4 mg/1ml
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 内部vitreal 0.7 mg/implant
Prices
Unit description Cost Unit
Ozurdex 0.7毫克植入 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
地塞米松磷酸钠4毫克/毫升1瓶= 5米l 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
一个po-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
一个po-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不卖也不买毒品。定价信息rmation is supplied for informational purposes only.
Patents
Patent Number Pediatric Extension 一个pproved Expires (estimated) Region
US8846650 No 2014-09-30 2025-06-04 US flag
US9149486 No 2015-10-06 2022-09-13 US flag
US6359016 No 2002-03-19 2020-08-10 US flag
US6284804 No 2001-09-04 2020-08-10 US flag
US6726918 No 2004-04-27 2020-10-20 US flag
US6899717 No 2005-05-31 2023-11-01 US flag
US8034366 No 2011-10-11 2023-01-09 US flag
US8506987 No 2013-08-13 2023-01-09 US flag
US9012437 No 2015-04-21 2020-10-20 US flag
US8043628 No 2011-10-25 2020-10-20 US flag
US8088407 No 2012-01-03 2020-10-20 US flag
US9283178 No 2016-03-15 2020-10-20 US flag
US9192511 No 2015-11-24 2023-01-09 US flag
US8063031 No 2011-11-22 2020-10-20 US flag
US7033605 No 2006-04-25 2020-10-20 US flag
US7767223 No 2010-08-03 2021-11-28 US flag
US8034370 No 2011-10-11 2023-01-09 US flag
US7795316 No 2010-09-14 2028-08-03 US flag
US8101582 No 2012-01-24 2027-12-19 US flag
US8450287 No 2013-05-28 2027-12-19 US flag
US9345714 No 2016-05-24 2022-09-13 US flag
US9402805 No 2016-08-02 2022-09-13 US flag
US9592242 No 2017-03-14 2020-10-20 US flag
US9775849 No 2017-10-03 2020-10-20 US flag
US6960346 No 2005-11-01 2023-07-03 US flag
US7560120 No 2009-07-14 2022-09-05 US flag
US10028965 No 2018-07-24 2034-05-23 US flag
US10022502 No 2018-07-17 2020-09-12 US flag
US10076526 No 2018-09-18 2023-01-09 US flag
US8563027 No 2013-10-22 2030-02-12 US flag
US8409606 No 2013-04-02 2030-05-14 US flag
US10159683 No 2018-12-25 2034-05-23 US flag
US9254267 No 2016-02-09 2024-09-11 US flag
US10537585 No 2020-01-21 2037-12-18 US flag
US10702539 No 2020-07-07 2023-01-09 US flag
US10799642 No 2020-10-13 2032-05-11 US flag
US11304961 No 2017-12-18 2037-12-18 US flag
US11097061 No 2019-06-23 2039-06-23 US flag
US11458041 No 2017-11-16 2037-11-16 US flag

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 一个DME Research, USCD
Caco2 permeability -4.75 一个DME Research, USCD
Predicted Properties
Property Value Source
Water Solubility 0.0505 mg/mL 一个LOGPS
logP 1.93 一个LOGPS
logP 1.68 Chemaxon
logS -3.9 一个LOGPS
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
一个mes 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
一个DMET data is predicted usingadmetSAR, 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 Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available
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 - 0 - a4r - 0696000000 - 1 - df7921eb1369fef69c4
MS/MS Spectrum - , positive LC-MS/MS splash10-00dj-3960000000-e9ee044790c0655981b1

Targets

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Details 1.Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
一个ctions
一个gonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
分子量
85658.57 Da
References
  1. 约翰·沃恩JP CD,基督教HC,莫里斯摩根富林明,花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. [一个rticle]
  2. Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. [一个rticle]
  3. Funato H, Kobayashi A, Watanabe Y: Differential effects of antidepressants on dexamethasone-induced nuclear translocation and expression of glucocorticoid receptor. Brain Res. 2006 Oct 30;1117(1):125-34. Epub 2006 Sep 7. [一个rticle]
  4. Vaitkuviene A, Ulinskaite A, Meskys R, Duburs G, Klusa V, Liutkevicius E: Study of the interaction of 1,4-dihydropyridine derivatives with glucocorticoid hormone receptors from the rat liver. Pharmacol Rep. 2006 Jul-Aug;58(4):551-8. [一个rticle]
  5. Wang D, Zhang H, Lang F, Yun CC: Acute activation of NHE3 by dexamethasone correlates with activation of SGK1 and requires a functional glucocorticoid receptor. Am J Physiol Cell Physiol. 2007 Jan;292(1):C396-404. Epub 2006 Sep 13. [一个rticle]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [一个rticle]
Details 2.Nuclear receptor subfamily 0 group B member 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Stimulator
General Function
Transcription factor binding
Specific Function
Orphan nuclear receptor. Component of a cascade required for the development of the hypothalamic-pituitary-adrenal-gonadal axis. Acts as a coregulatory protein that inhibits the transcriptional act...
Gene Name
NR0B1
Uniprot ID
P51843
Uniprot Name
Nuclear receptor subfamily 0 group B member 1
分子量
51717.185 Da
References
  1. Gummow BM, Scheys JO, Cancelli VR, Hammer GD: Reciprocal regulation of a glucocorticoid receptor-steroidogenic factor-1 transcription complex on the Dax-1 promoter by glucocorticoids and adrenocorticotropic hormone in the adrenal cortex. Mol Endocrinol. 2006 Nov;20(11):2711-23. Epub 2006 Jul 20. [一个rticle]
  2. Yu CC, Li PH: In vivo inhibition of steroidogenic acute regulatory protein expression by dexamethasone parallels induction of the negative transcription factor DAX-1. Endocrine. 2006 Dec;30(3):313-23. [一个rticle]
Details 3.一个nnexin A1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
一个gonist
General Function
Structural molecule activity
Specific Function
Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
Gene Name
一个NXA1
Uniprot ID
P04083
Uniprot Name
一个nnexin A1
分子量
38713.855 Da
References
  1. Morand EF, Hall P, Hutchinson P, Yang YH: Regulation of annexin I in rheumatoid synovial cells by glucocorticoids and interleukin-1. Mediators Inflamm. 2006;2006(2):73835. [一个rticle]
  2. John CD, Theogaraj E, Christian HC, Morris JF, Smith SF, Buckingham JC: Time-specific effects of perinatal glucocorticoid treatment on anterior pituitary morphology, annexin 1 expression and adrenocorticotrophic hormone secretion in the adult female rat. J Neuroendocrinol. 2006 Dec;18(12):949-59. [一个rticle]
  3. Davies E, Omer S, Buckingham JC, Morris JF, Christian HC: Expression and externalization of annexin 1 in the adrenal gland: structure and function of the adrenal gland in annexin 1-null mutant mice. Endocrinology. 2007 Mar;148(3):1030-8. Epub 2006 Dec 7. [一个rticle]
  4. Wang C, Wang J, Guo HF, Liu RY: Involvement of annexin I in the dexamethasone-mediated upregulation of A549 cells phagocytosis of apoptotic eosinophils. Immunol Lett. 2007 Aug 15;111(2):103-10. Epub 2007 Jul 2. [一个rticle]
Details 4.Nitric oxide synthase, inducible
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Negative modulator
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
Gene Name
NOS2
Uniprot ID
P35228
Uniprot Name
Nitric oxide synthase, inducible
分子量
131116.3 Da
References
  1. Soderberg M, Raffalli-Mathieu F, Lang MA: Regulation of the murine inducible nitric oxide synthase gene by dexamethasone involves a heterogeneous nuclear ribonucleoprotein I (hnRNPI) dependent pathway. Mol Immunol. 2007 May;44(12):3204-10. Epub 2007 Mar 26. [一个rticle]
  2. Huang H, Lavoie-Lamoureux A, Moran K, Lavoie JP: IL-4 stimulates the expression of CXCL-8, E-selectin, VEGF, and inducible nitric oxide synthase mRNA by equine pulmonary artery endothelial cells. Am J Physiol Lung Cell Mol Physiol. 2007 May;292(5):L1147-54. [一个rticle]
  3. Nandi J, Saud B, Zinkievich JM, Palma DT, Levine RA: 5-aminosalicylic acid improves indomethacin-induced enteropathy by inhibiting iNOS transcription in rats. Dig Dis Sci. 2008 Jan;53(1):123-32. Epub 2007 May 15. [一个rticle]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [一个rticle]
Details 5.Nuclear receptor subfamily 1 group I member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
一个gonist
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
分子量
49761.245 Da
References
  1. Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [一个rticle]

Enzymes

Details 1.Corticosteroid 11-beta-dehydrogenase isozyme 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
General Function
Steroid binding
Specific Function
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. Modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation...
Gene Name
HSD11B2
Uniprot ID
P80365
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 2
分子量
44126.06 Da
References
  1. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [一个rticle]
  2. 汉克Diederich年代,B, Burkhardt P,穆勒M,肖恩eshofer 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. [一个rticle]
Details 2.Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
分子量
57342.67 Da
References
  1. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [一个rticle]
  2. Lampen A, Christians U, Guengerich FP, Watkins PB, Kolars JC, Bader A, Gonschior AK, Dralle H, Hackbarth I, Sewing KF: Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions, and interindividual variability. Drug Metab Dispos. 1995 Dec;23(12):1315-24. [一个rticle]
  3. Christians U, Schmidt G, Bader A, Lampen A, Schottmann R, Linck A, Sewing KF: Identification of drugs inhibiting the in vitro metabolism of tacrolimus by human liver microsomes. Br J Clin Pharmacol. 1996 Mar;41(3):187-90. [一个rticle]
  4. Miranda SR, Meyer SA: Cytotoxicity of chloroacetanilide herbicide alachlor in HepG2 cells independent of CYP3A4 and CYP3A7. Food Chem Toxicol. 2007 May;45(5):871-7. doi: 10.1016/j.fct.2006.11.011. Epub 2006 Nov 26. [一个rticle]
  5. Yamaguchi Y, Kirita S, Baba T, Aoyama J, Touchi A, Tukey RH, Guengerich FP, Matsubara T: Identification of rat and human cytochrome P450 forms involved in the metabolism of the thromboxane A2 receptor antagonist (+)-S-145. Drug Metab Dispos. 1997 Jan;25(1):75-80. [一个rticle]
  6. Gomez-Lechon MJ, Donato T, Jover R, Rodriguez C, Ponsoda X, Glaise D, Castell JV, Guguen-Guillouzo C: Expression and induction of a large set of drug-metabolizing enzymes by the highly differentiated human hepatoma cell line BC2. Eur J Biochem. 2001 Mar;268(5):1448-59. [一个rticle]
  7. Berson A, Wolf C, Chachaty C, Fisch C, Fau D, Eugene D, Loeper J, Gauthier JC, Beaune P, Pompon D, et al.: Metabolic activation of the nitroaromatic antiandrogen flutamide by rat and human cytochromes P-450, including forms belonging to the 3A and 1A subfamilies. J Pharmacol Exp Ther. 1993 Apr;265(1):366-72. [一个rticle]
  8. McCune JS, Hawke RL, LeCluyse EL, Gillenwater HH, Hamilton G, Ritchie J, Lindley C: In vivo and in vitro induction of human cytochrome P4503A4 by dexamethasone. Clin Pharmacol Ther. 2000 Oct;68(4):356-66. doi: 10.1067/mcp.2000.110215. [一个rticle]
  9. Dexamethasone monograph, Boehringer Ingelheim [Link]
  10. Flockhart Table of Drug Interactions [Link]
  11. FDA Approved Drug Products: Hemady Dexamethasone Oral Tablets [Link]
Details 3.Corticosteroid 11-beta-dehydrogenase isozyme 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
General Function
11-beta-hydroxysteroid dehydrogenase [nad(p)] activity
Specific Function
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea...
Gene Name
HSD11B1
Uniprot ID
P28845
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 1
分子量
32400.665 Da
References
  1. Diederich S, Hanke B, Oelkers W, Bahr V: Metabolism of dexamethasone in the human kidney: nicotinamide adenine dinucleotide-dependent 11beta-reduction. J Clin Endocrinol Metab. 1997 May;82(5):1598-602. [一个rticle]
  2. 汉克Diederich年代,B, Burkhardt P,穆勒M,肖恩eshofer 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. [一个rticle]
Details 4.Cytochrome P450 3A5
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
分子量
57108.065 Da
References
  1. Hukkanen J, Lassila A, Paivarinta K, Valanne S, Sarpo S, Hakkola J, Pelkonen O, Raunio H: Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. Am J Respir Cell Mol Biol. 2000 Mar;22(3):360-6. [一个rticle]
  2. Hukkanen J, Vaisanen T, Lassila A, Piipari R, Anttila S, Pelkonen O, Raunio H, Hakkola J: Regulation of CYP3A5 by glucocorticoids and cigarette smoke in human lung-derived cells. J Pharmacol Exp Ther. 2003 Feb;304(2):745-52. [一个rticle]
  3. Flockhart Table of Drug Interactions [Link]
Details 5.Cytochrome P450 3A7
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
分子量
57525.03 Da
References
  1. Miranda SR, Meyer SA: Cytotoxicity of chloroacetanilide herbicide alachlor in HepG2 cells independent of CYP3A4 and CYP3A7. Food Chem Toxicol. 2007 May;45(5):871-7. doi: 10.1016/j.fct.2006.11.011. Epub 2006 Nov 26. [一个rticle]
  2. Flockhart Table of Drug Interactions [Link]
Details 6.Steroid 17-alpha-hydroxylase/17,20 lyase
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inhibitor
General Function
Steroid 17-alpha-monooxygenase activity
Specific Function
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation ...
Gene Name
CYP17A1
Uniprot ID
P05093
Uniprot Name
Steroid 17-alpha-hydroxylase/17,20 lyase
分子量
57369.995 Da
References
  1. Trzeciak WH, LeHoux JG, Waterman MR, Simpson ER: Dexamethasone inhibits corticotropin-induced accumulation of CYP11A and CYP17 messenger RNAs in bovine adrenocortical cells. Mol Endocrinol. 1993 Feb;7(2):206-13. doi: 10.1210/mend.7.2.8385739. [一个rticle]
Details 7.Cytochrome P450 1A1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inhibitor
Inducer
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
分子量
58164.815 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [一个rticle]
  2. Monostory K, Kohalmy K, Prough RA, Kobori L, Vereczkey L: The effect of synthetic glucocorticoid, dexamethasone on CYP1A1 inducibility in adult rat and human hepatocytes. FEBS Lett. 2005 Jan 3;579(1):229-35. doi: 10.1016/j.febslet.2004.11.080. [一个rticle]
Details 8.Cytochrome P450 2A6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
分子量
56501.005 Da
References
  1. Onica T, Nichols K, Larin M, Ng L, Maslen A, Dvorak Z, Pascussi JM, Vilarem MJ, Maurel P, Kirby GM: Dexamethasone-mediated up-regulation of human CYP2A6 involves the glucocorticoid receptor and increased binding of hepatic nuclear factor 4 alpha to the proximal promoter. Mol Pharmacol. 2008 Feb;73(2):451-60. Epub 2007 Oct 31. [一个rticle]
  2. Meunier V, Bourrie M, Julian B, Marti E, Guillou F, Berger Y, Fabre G: Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: a 10-year follow-up. Xenobiotica. 2000 Jun;30(6):589-607. doi: 10.1080/004982500406426 . [一个rticle]
  3. Waxman DJ, Chang TK: Spectrofluorometric analysis of CYP2A6-catalyzed coumarin 7-hydroxylation. Methods Mol Biol. 2006;320:91-6. doi: 10.1385/1-59259-998-2:91. [一个rticle]
Details 9.Cytochrome P450 2B6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
分子量
56277.81 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [一个rticle]
  2. Wang H, Tompkins LM: CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme. Curr Drug Metab. 2008 Sep;9(7):598-610. [一个rticle]
Details 10.Cytochrome P450 2C19
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
分子量
55930.545 Da
References
  1. Raucy JL, Mueller L, Duan K, Allen SW, Strom S, Lasker JM: Expression and induction of CYP2C P450 enzymes in primary cultures of human hepatocytes. J Pharmacol Exp Ther. 2002 Aug;302(2):475-82. doi: 10.1124/jpet.102.033837. [一个rticle]
  2. 斯科特•SA Sangkuhl K, Shuldiner AR,洛JS,托尔n 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. [一个rticle]
Details 11.Cytochrome P450 2C8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
分子量
55824.275 Da
References
  1. 后方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. [一个rticle]
  2. Pascussi JM, Gerbal-Chaloin S, Fabre JM, Maurel P, Vilarem MJ: Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: consequences on cytochrome P450 gene regulation. Mol Pharmacol. 2000 Dec;58(6):1441-50. doi: 10.1124/mol.58.6.1441. [一个rticle]
  3. Gerbal-Chaloin S, Pascussi JM, Pichard-Garcia L, Daujat M, Waechter F, Fabre JM, Carrere N, Maurel P: Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metab Dispos. 2001 Mar;29(3):242-51. [一个rticle]
Details 12.Cytochrome P450 2E1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
分子量
56848.42 Da
References
  1. Baron JM, Holler D, Schiffer R, Frankenberg S, Neis M, Merk HF, Jugert FK: Expression of multiple cytochrome p450 enzymes and multidrug resistance-associated transport proteins in human skin keratinocytes. J Invest Dermatol. 2001 Apr;116(4):541-8. doi: 10.1046/j.1523-1747.2001.01298.x. [一个rticle]
  2. Sampol E, Mirrione A, Villard PH, Piccerelle P, Scoma H, Berbis P, Barra Y, Durand A, Lacarelle B: Evidence for a tissue-specific induction of cutaneous CYP2E1 by dexamethasone. Biochem Biophys Res Commun. 1997 Jun 27;235(3):557-61. doi: 10.1006/bbrc.1997.6829. [一个rticle]
  3. Monostory K, Vereczkey L: Combined action of phenobarbital and dexamethasone on the activity of rat liver P450 system. Acta Pharm Hung. 1993 Sep;63(5):296-300. [一个rticle]
Details 13.Cytochrome P450 3A43
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Monooxygenase activity
Specific Function
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name
CYP3A43
Uniprot ID
Q9HB55
Uniprot Name
Cytochrome P450 3A43
分子量
57669.21 Da
References
  1. Krusekopf S, Roots I, Kleeberg U: Differential drug-induced mRNA expression of human CYP3A4 compared to CYP3A5, CYP3A7 and CYP3A43. Eur J Pharmacol. 2003 Apr 11;466(1-2):7-12. doi: 10.1016/s0014-2999(03)01481-x. [一个rticle]
Details 14.Cytochrome P450 4A11
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Leukotriene-b4 20-monooxygenase activity
Specific Function
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 2...
Gene Name
CYP4A11
Uniprot ID
Q02928
Uniprot Name
Cytochrome P450 4A11
分子量
59347.31 Da
References
  1. Cummings BS, Lasker JM, Lash LH: Expression of glutathione-dependent enzymes and cytochrome P450s in freshly isolated and primary cultures of proximal tubular cells from human kidney. J Pharmacol Exp Ther. 2000 May;293(2):677-85. [一个rticle]
  2. 萨瓦河U,许MH,约翰逊EF:微分处于三峡on 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. [一个rticle]
Details 15.Cytochrome P450 11B1, mitochondrial
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inhibitor
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
Gene Name
CYP11B1
Uniprot ID
P15538
Uniprot Name
Cytochrome P450 11B1, mitochondrial
分子量
57572.44 Da
References
  1. Fardella CE, Pinto M, Mosso L, Gomez-Sanchez C, Jalil J, Montero J: Genetic study of patients with dexamethasone-suppressible aldosteronism without the chimeric CYP11B1/CYP11B2 gene. J Clin Endocrinol Metab. 2001 Oct;86(10):4805-7. doi: 10.1210/jcem.86.10.7920. [一个rticle]

Carriers

Details 1.Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
一个LB
Uniprot ID
P02768
Uniprot Name
Serum albumin
分子量
69365.94 Da
References
  1. Cummings DM, Larijani GE, Conner DP, Ferguson RK, Rocci ML Jr: Characterization of dexamethasone binding in normal and uremic human serum. DICP. 1990 Mar;24(3):229-31. doi: 10.1177/106002809002400301. [一个rticle]

Transporters

Details 1.P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
Inhibitor
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
一个BCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
分子量
141477.255 Da
References
  1. Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. [一个rticle]
  2. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. [一个rticle]
  3. Schuetz JD, Silverman JA, Thottassery JV, Furuya KN, Schuetz EG: Divergent regulation of the class II P-glycoprotein gene in primary cultures of hepatocytes versus H35 hepatoma by glucocorticoids. Cell Growth Differ. 1995 Oct;6(10):1321-32. [一个rticle]
  4. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [一个rticle]
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [一个rticle]
  6. 一个dachi 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. [一个rticle]
  7. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [一个rticle]
  8. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, Borst P: Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest. 1995 Oct;96(4):1698-705. [一个rticle]
  9. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [一个rticle]
Details 2.Solute carrier family 22 member 8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
分子量
59855.585 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [一个rticle]
Details 3.Bile salt export pump
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
一个BCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
分子量
146405.83 Da
References
  1. Fardel O, Payen L, Courtois A, Vernhet L, Lecureur V: Regulation of biliary drug efflux pump expression by hormones and xenobiotics. Toxicology. 2001 Oct 5;167(1):37-46. [一个rticle]
Details 4.Canalicular multispecific organic anion transporter 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
一个BCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
分子量
174205.64 Da
References
  1. Demeule M, Jodoin J, Beaulieu E, Brossard M, Beliveau R: Dexamethasone modulation of multidrug transporters in normal tissues. FEBS Lett. 1999 Jan 15;442(2-3):208-14. [一个rticle]
  2. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [一个rticle]
Details 5.一个TP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
一个BCG2
Uniprot ID
Q9UNQ0
Uniprot Name
一个TP-binding cassette sub-family G member 2
分子量
72313.47 Da
References
  1. Elahian F, Kalalinia F, Behravan J: Evaluation of indomethacin and dexamethasone effects on BCRP-mediated drug resistance in MCF-7 parental and resistant cell lines. Drug Chem Toxicol. 2010 Apr;33(2):113-9. doi: 10.3109/01480540903390000. [一个rticle]
Details 6.Solute carrier organic anion transporter family member 1A2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
一个ctions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
介导的Na(+)独立的运输组织形式c anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
分子量
74144.105 Da
References
  1. Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. [一个rticle]
  2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [一个rticle]

Drug created at June 13, 2005 13:24 / Updated at February 17, 2023 22:44