Hydrocortisone

Identification

Summary

Hydrocortisone is a glucocorticoid used to treat corticosteroid-responsive dermatoses, endocrine disorders, immune conditions, and allergic disorders.

Brand Names
Ala-cort, Ala-scalp, Alcortin, Alkindi, Anusol HC, Aquanil HC, Casporyn HC, Cipro, Cipro HC, Colocort, Cortaid, Cortane-B, Cortef, Cortenema, Cortisporin, Cortizone-10, Dermacort, Dermarest Eczema, Dermazene, Home Papkit, Hydroskin, Monistat Itch Relief, Preparation H Hydrocortisone, Procto-med, Procto-pak, Proctocort, Proctol, Proctosedyl, Proctosol, Proctozone HC, Scalpicin Itch Relief, Texacort, Vanoxide-HC, Xerese
Generic Name
Hydrocortisone
DrugBank Accession Number
DB00741
Background

Hydrocortisone, or cortisol, is a glucocorticoid secreted by the adrenal cortex.7 Hydrocortisone is used to treat immune, inflammatory, and neoplastic conditions.14,15,16,17,18,19 It was discovered in the 1930s by Edward Kendall and named Compound F, or 17-hydroxycorticosterone.9

Hydrocortisone was granted FDA approval on 5 August 1952.20

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Weight
Average: 362.4599
Monoisotopic: 362.20932407
Chemical Formula
C21H30O5
Synonyms
  • (11β)-11,17,21-trihydroxypregn-4-ene-3,20-dione
  • 11beta-hydrocortisone
  • 11beta,17alpha,21-Trihydroxy-4-pregnene-3,20-dione
  • 11β-hydrocortisone
  • 17-Hydroxycorticosterone
  • 4-pregnen-11β,17α,21-triol-3,20-dione
  • Cortisol
  • Hidrocortisona
  • Hydrocortisone
  • Hydrocortisonum
  • Kendall's compound F
  • Reichstein's substance M
External IDs
  • NSC-10483

Pharmacology

Indication

Otic solutions are indicated for infections of the external auditory canal caused by susceptible organisms and with inflammation.14,15 Hydrocortisone tablets are indicated for certain endocrine, rheumatic, collagen, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, gastrointestinal, and other conditions.16 A hydrocortisone enema is indicated for ulcerative colitis,17 a topical ointment with antibiotics is indicated for corticosteroid responsive dermatoses with infections,18 and a topical cream with acyclovir is indicated to treat cold sores.19 Oral granules of hydrocortisone are used as a replacement therapy for Adrenocortical Insufficiency (AI) in children under 17 years of age.21

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofAcquired hemolytic anemia•••••••••••••••••••••••
Management ofAcute gouty arthritis••••••••••••••••••
Symptomatic treatment ofAcute leukemia•••••••••••••••••••••••••••
Used in combination to treatAcute otitis externaCombination Product in combination with: Ciprofloxacin (DB00537)•••••••••••••••••••• • •••••
Treatment ofAdrenal insufficiency••••••••••••••••••••••• ••••••••••••••••
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Hydrocortisone binds to the glucocorticoid receptor leading to downstream effects such as inhibition of phospholipase A2, NF-kappa B, other inflammatory transcription factors, and the promotion of anti-inflammatory genes.10 Hydrocortisone has a wide therapeutic index8 and a moderate duration of action.1,6 Patients should stop taking the medication if irritation or sensitization occurs.14,15,16,17,18,19

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.10 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.10

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-10.10

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.10 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.10

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
AAnnexin A1
agonist
Humans
Absorption

Oral hydrocortisone at a dose of 0.2-0.3mg/kg/day reached a mean Cmax of 32.69nmol/L with a mean AUC of 90.63h*nmol/L1 A 0.4-0.6mg/kg/day dose reached a mean Cmax of 70.81nmol/L with a mean AUC of 199.11h*nmol/L.1 However, the pharmacokinetics of hydrocortisone can vary by 10 times from patient to patient.1

Topical hydrocortisone cream is 4-19% bioavailable[8546995] with a Tmax of 24h.2

Hydrocortisone retention enemas are have a bioavailability of 0.810 for slow absorbers and 0.502 in rapid absorbers.4 Slow absorbers take up hydrocortisone at a rate of 0.361±0.255/h while fast absorbers take up hydrocortisone at a rate of 1.05±0.255/h.4

A 20mg IV dose of hydrocortisone has an AUC of 1163±277ng*h/mL.6

Volume of distribution

Total hydrocortisone has a volume of distribution of 39.82L, while the free fraction has a volume of distribution of 474.38L.1

Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin11 and serum albumin12 in plasma. Hydrocortisone is 90.1% bound to proteins in plasma, with 56.2% bound to albumin.5

Metabolism

Hydrocortisone is metabolised to 6-beta hydrocortisol via CYP3A, 5-beta tetrahydrocortisol via 3-oxo-5-beta-steroid 4-dehydrogenase, 5-alpha tetrahydrocortisol via 3-oxo-5-alpha-steroid 4-dehydrogenase 2, cortisone via Corticosteroid 11-beta-dehydrogenase isozyme 1 and Corticosteroid 11-beta-dehydrogenase isozyme 2, and glucuronide products.13 Cortisone is further metabolized to tetrahydrocortisone and dihydrocortisol.13

Hover over products below to view reaction partners

Route of elimination

Corticosteroids are eliminated predominantly in the urine.12 However, data regarding the exact proportion is not readily available.7

Half-life

Total hydrocortisone via the oral route has a half life of 2.15h while the free fraction has a half life of 1.39h.1 A 20mg IV dose of hydrocortisone has a terminal half life of 1.9±0.4h.6

Clearance

Total hydrocortisone by the oral route has a mean clearance of 12.85L/h, while the free fraction has a mean clearance of 235.78L/h.1 A 20mg IV dose of hydrocortisone has a clearance of 18.2±4.2L/h.6

Adverse Effects
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Toxicity

Data regarding acute overdoses of glucocorticoids are rare.14,15,16,17,18,19 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.8 Overdose may be treated by adjusting the dose or stopping the corticosteroid as well as initiating symptomatic and supportive treatment.8

Pathways
PathwayCategory
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia Due to 17 alpha-Hydroxylase DeficiencyDisease
Corticosterone Methyl Oxidase I Deficiency (CMO I)Disease
3-beta-Hydroxysteroid Dehydrogenase DeficiencyDisease
Corticotropin Activation of Cortisol ProductionSignaling
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAHDisease
11-beta-Hydroxylase Deficiency (CYP11B1)Disease
Apparent Mineralocorticoid Excess SyndromeDisease
SteroidogenesisMetabolic
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia Due to 21-Hydroxylase DeficiencyDisease
17-alpha-Hydroxylase Deficiency (CYP17)Disease
21-Hydroxylase Deficiency (CYP21)Disease
Corticosterone Methyl Oxidase II Deficiency (CMO II)Disease
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Hydrocortisone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Hydrocortisone can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Hydrocortisone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Hydrocortisone.
AcarboseThe risk or severity of hyperglycemia can be increased when Hydrocortisone is combined with Acarbose.
Food Interactions
  • Avoid alcohol.

Products

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Product Images
International/Other Brands
Acticort / Aeroseb HC / Ala-Scalp / Algicirtis / Beta-HC / Cetacort / Cortaid / Delacort / Ficortril / Genacort / Glycort / Komed HC / Lacticare HC / Lubricort / Meusicort / Mildison / Nogenic HC / Nutracort / Penecort / Permicort / Polcort H / Preparation H Hydrocortisone Cream / Prevex HC / Proctocream / Remederm HC / Sanatison / Scalpicin Capilar / Schericur / Sigmacort / Synacort / Systral Hydrocort / Timocort
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alkindi5.0 mgOralDiurnal Europe B.V.2021-01-22Not applicableEU flag
Alkindi0.5 mgOralDiurnal Europe B.V.2021-01-22Not applicableEU flag
Alkindi2.0 mgOralDiurnal Europe B.V.2021-01-22Not applicableEU flag
Alkindi1.0 mgOralDiurnal Europe B.V.2021-01-22Not applicableEU flag
Alkindi SprinkleGranule1 mg/1OralEton Pharmaceuticals, Inc.2020-09-29Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ala-ScalpLotion20 mg/1mLTopicalLifsa Drugs Llc2021-02-05Not applicableUS flag
Ala-ScalpLotion20 mg/1mLTopicalDerm Ventures LLC2020-07-24Not applicableUS flag
AlacortCream25 mg/1gTopicalCrown Laboratories2016-01-06Not applicableUS flag
AlacortCream10 mg/1gTopicalCrown Laboratories1973-03-09Not applicableUS flag
Anusol HCCream25 mg/1gTopicalSalix Pharmaceuticals, Inc1984-06-06Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
1% HydrocortisoneCream1 g/100gTopicalYuyao Jessie Commodity Co.,Ltd.2015-12-01Not applicableUS flag
999 Itch RelievingOintment1 g/100gTopicalGuangdong CR. Shunfeng Pharmaceutical Co Ltd1989-07-20Not applicableUS flag
999 Itch RelievingOintment1 g/100gTopicalGuangdong CR. Shunfeng Pharmaceutical Co Ltd1989-07-20Not applicableUS flag
Advanced HydrocortisoneCream10 mg/1gTopicalUltra Seal Corporation2011-04-052024-07-01US flag
AFASSCO 1% HydrocortisoneOintment0.01 g/1gTopicalAfassco Inc.2018-12-07Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Acetasol HCHydrocortisone (1.1 g/100mL) + Acetic acid (2.41 g/100mL)SolutionAuricular (otic)Physicians Total Care, Inc.1994-12-152012-06-30US flag
Acetasol HCHydrocortisone (1.1 g/100mL) + Acetic acid (2.41 g/100mL)SolutionAuricular (otic)Actavis Pharma, Inc.2002-09-102017-05-31US flag
Activir Duo 50 mg/g + 10 mg/g CremeHydrocortisone (10 mg/g) + Acyclovir (50 mg/g)CreamTopicalGsk Gebro Consumer Healthcare Gmb H2010-02-09Not applicableAustria flag
Alumier MD Post Procedure Kit with HydrocortisoneHydrocortisone (10 mg/1mL) + Titanium dioxide (70 mg/1mL) + Zinc oxide (62.8 mg/1mL)KitTopicalAlumier Labs2022-03-22Not applicableUS flag
Antibiotic Ear (Neo/Polym/HC)Hydrocortisone (10 mg/1mL) + Neomycin sulfate (3.5 mg/1mL) + Polymyxin B sulfate (10000 [USP'U]/1mL)Solution / dropsAuricular (otic)Physicians Total Care, Inc.1995-12-29Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
141016 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%Hydrocortisone (0.5 g/100g) + Hydroquinone (4 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141017 Hydrocortisone 0.5% / Hydroquinone 6% / Tretinoin 0.025%Hydrocortisone (0.5 g/100g) + Hydroquinone (6 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141060 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%Hydrocortisone (0.5 g/100g) + Hydroquinone (4 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
141061 Hydrocortisone 0.5% / Hydroquinone 8% / Tretinoin 0.025%Hydrocortisone (0.5 g/100g) + Hydroquinone (8 g/100g) + Tretinoin (0.025 g/100g)EmulsionTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
Ala QuinHydrocortisone (5 mg/1g) + Clioquinol (30 mg/1g)CreamTopicalCrown Laboratories1970-08-192021-11-30US flag

Categories

ATC Codes
S01CB03 — HydrocortisoneA01AC03 — HydrocortisoneS01BA02 — HydrocortisoneS01CA03 — Hydrocortisone and antiinfectivesD07AA02 — HydrocortisoneS01BB01 — Hydrocortisone and mydriaticsD07XA01 — HydrocortisoneD07BA04 — Hydrocortisone and antisepticsS02CA03 — Hydrocortisone and antiinfectivesA07EA02 — HydrocortisoneS02BA01 — HydrocortisoneR01AD60 — Hydrocortisone, combinationsH02AB09 — HydrocortisoneD07CA01 — Hydrocortisone and antibioticsS03CA04 — Hydrocortisone and antiinfectivesC05AA01 — Hydrocortisone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
Alternative Parents
Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-4-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-4-steroids / Cyclohexenones / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols
show 4 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-hydroxy ketone
show 16 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
3-oxo steroid, 11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, 21-hydroxy steroid, C21-steroid (CHEBI:17650) / Pregnane and derivatives [Fig], Glucocorticoids, C21 steroids (gluco/mineralocorticoids, progestogens) and derivatives (C00735) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030001)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
WI4X0X7BPJ
CAS number
50-23-7
InChI Key
JYGXADMDTFJGBT-VWUMJDOOSA-N
InChI
InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1
IUPAC Name
(1R,3aS,3bS,9aR,9bS,10S,11aS)-1,10-dihydroxy-1-(2-hydroxyacetyl)-9a,11a-dimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

References

Synthesis Reference

Manfred Baumgarth, Dieter Orth, Jurgen Harting, Hans Schaefer, Achim Zesch, "Hydrocortisone orthoesters, pharmaceutical formulations thereof and processes for the preparation thereof." U.S. Patent US4264584, issued March, 1974.

US4264584
General References
  1. Werumeus Buning J, Touw DJ, Brummelman P, Dullaart RPF, van den Berg G, van der Klauw MM, Kamp J, Wolffenbuttel BHR, van Beek AP: Pharmacokinetics of oral hydrocortisone - Results and implications from a randomized controlled trial. Metabolism. 2017 Jun;71:7-16. doi: 10.1016/j.metabol.2017.02.005. Epub 2017 Feb 13. [Article]
  2. Aalto-Korte K, Turpeinen M: Pharmacokinetics of topical hydrocortisone at plasma level after applications once or twice daily in patients with widespread dermatitis. Br J Dermatol. 1995 Aug;133(2):259-63. doi: 10.1111/j.1365-2133.1995.tb02625.x. [Article]
  3. Aalto-Korte K, Turpeinen M: Quantifying systemic absorption of topical hydrocortisone in erythroderma. Br J Dermatol. 1995 Sep;133(3):403-8. doi: 10.1111/j.1365-2133.1995.tb02668.x. [Article]
  4. Lima JJ, Jusko WJ: Bioavailability of hydrocortisone retention enemas in relation to absorption kinetics. Clin Pharmacol Ther. 1980 Aug;28(2):262-9. doi: 10.1038/clpt.1980.159. [Article]
  5. FLORINI JR, BUYSKE DA: Plasma protein binding of triamcinolone-H3 and hydrocortisone-4-C14. J Biol Chem. 1961 Jan;236:247-51. [Article]
  6. Derendorf H, Mollmann H, Barth J, Mollmann C, Tunn S, Krieg M: Pharmacokinetics and oral bioavailability of hydrocortisone. J Clin Pharmacol. 1991 May;31(5):473-6. doi: 10.1002/j.1552-4604.1991.tb01906.x. [Article]
  7. Jung C, Greco S, Nguyen HH, Ho JT, Lewis JG, Torpy DJ, Inder WJ: Plasma, salivary and urinary cortisol levels following physiological and stress doses of hydrocortisone in normal volunteers. BMC Endocr Disord. 2014 Nov 26;14:91. doi: 10.1186/1472-6823-14-91. [Article]
  8. 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]
  9. Simoni R, Hill R, Vaughan M: The Isolation of Thyroxine and Cortisone: the Work of Edward C. Kendall Journal of Biological Chemistry. 2002 May 24;277(21):e10. [Article]
  10. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
  11. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
  12. 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]
  13. Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]
  14. FDA Approved Drug Products: Vosol Hydrocortisone and Glacial Acetic Acid Otic Drops [Link]
  15. FDA Approved Drug Products: Casporyn Neomycin Sulfate, Polymixin B Sulfate, and Hydrocortisone Otic Drops [Link]
  16. FDA Approved Drug Products: Cortef Hydrocortisone Oral Tablets [Link]
  17. FDA Approved Drug Products: Cortenema Hydrocortisone Rectal Enema [Link]
  18. FDA Approved Drug Products: Bacitracin, Neomycin, Polymyxin B, and Hydrocortisone Topical Ointment [Link]
  19. FDA Approved Drug Products: Xerese (Acyclovir and Hydrocortisone) Topical Cream [Link]
  20. FDA Approved Drug Products: Hydrocortone Hydrocortisone Oral Tablets (Discontinued) [Link]
  21. FDA Approved Drug Products: ALKINDI SPRINKLE (hydrocortisone) oral granules [Link]
Human Metabolome Database
HMDB0000063
KEGG Drug
D00088
KEGG Compound
C00735
PubChem Compound
5754
PubChem Substance
46505089
ChemSpider
5551
BindingDB
13775
RxNav
5492
ChEBI
17650
ChEMBL
CHEMBL389621
ZINC
ZINC000013540519
Therapeutic Targets Database
DAP000718
PharmGKB
PA449905
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
HCY
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Hydrocortisone
PDB Entries
2v95 / 2vdy / 4c49 / 4p6x / 5hgc / 6hgf / 6hgg / 6itp / 6itq / 6nwl
show 2 more
FDA label
Download (30 KB)
MSDS
Download (73.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionPancreatic Fistula / Pancreatic Neoplasms1
4Active Not RecruitingTreatmentAtopic Dermatitis1
4Active Not RecruitingTreatmentCongenital Adrenal Hyperplasia (CAH)1
4CompletedNot AvailableBurns1
4CompletedBasic ScienceAnxiety1

Pharmacoeconomics

Manufacturers
  • Hi tech pharmacal co inc
  • Allergan herbert div allergan inc
  • Del ray laboratories inc
  • Salix pharmaceuticals inc
  • Bayer pharmaceuticals corp
  • Monarch pharmaceuticals inc
  • Valeant pharmaceuticals international
  • Westwood squibb pharmaceuticals inc
  • C and m pharmacal inc
  • Pharmaceutical assoc inc div beach products
  • Actavis mid atlantic llc
  • Alpharma us pharmaceuticals division
  • Altana inc
  • Ambix laboratories div organics corp america
  • Everylife
  • E fougera div altana inc
  • G and w laboratories inc
  • Ingram pharmaceutical co
  • Ivax pharmaceuticals inc
  • Naska pharmacal co inc div rugby darby group cosmetics
  • Perrigo new york inc
  • Pharmaderm div altana inc
  • Pharmafair inc
  • Stiefel laboratories inc
  • Syosset laboratories inc
  • Taro pharmaceuticals usa inc
  • Teva pharmaceuticals usa inc
  • Topiderm inc
  • Usl pharma inc
  • Vintage pharmaceuticals inc
  • Whiteworth towne paulsen inc
  • Sanofi aventis us llc
  • Coria laboratories ltd
  • Medicis pharmaceutical corp
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  • Ani pharmaceuticals inc
  • Teva pharmaceuticals usa
  • Healthpoint ltd
  • Allergan herbert skin care div allergan inc
  • Pharmacia and upjohn co
  • Baker norton pharmaceuticals inc
  • Solvay pharmaceuticals
  • Beta dermaceuticals inc
  • Bluline laboratories inc
  • Heran pharmaceutical inc
  • Mericon industries inc
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  • Dermik laboratories div aventis pharmaceuticals inc
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  • Jsj pharmaceuticals llc
  • Pfizer laboratories div pfizer inc
  • Barr laboratories inc
  • Elkins sinn div ah robins co inc
  • John j ferrante
  • Impax laboratories inc
  • Inwood laboratories inc sub forest laboratories inc
  • Lannett co inc
  • Nexgen pharma inc
  • Panray corp sub ormont drug and chemical co inc
  • Parke davis div warner lambert co
  • Purepac pharmaceutical co
  • Roxane laboratories inc
  • Sandoz inc
  • Stiefel a gsk co
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Merck and co inc
  • Pfipharmecs div pfizer inc
  • Schwarz pharma inc
  • Able laboratories inc
  • Hr cenci laboratories inc
  • Ferndale laboratories inc
  • Akorn inc
  • Bel mar laboratories inc
  • Colgate oral pharmaceuticals inc
  • Taro pharmaceutical industries ltd
  • Triax pharmaceuticals llc
  • Yamanouchi europe bv
  • Savage laboratories inc div altana inc
  • Abbott laboratories pharmaceutical products div
  • Abbott laboratories hosp products div
  • Hospira inc
  • Abraxis pharmaceutical products
  • Baxter healthcare corp anesthesia and critical care
  • International medication systems ltd
  • Taro pharmaceuticals inc
  • Ranbaxy laboratories inc
Packagers
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • AG Marin Pharmaceuticals
  • Alaven Pharmaceutical
  • Alcon Laboratories
  • Amerisource Health Services Corp.
  • Ani Pharmaceuticals
  • Anip Acquisition Co.
  • Arbor Pharmaceuticals Incorporated
  • A-S Medication Solutions LLC
  • Avidas Pharmaceuticals
  • Bay Pharma Inc.
  • Bayer Healthcare
  • Bergen Brunswig
  • Beta Dermaceuticals
  • Bio Pharm Inc.
  • Bristol-Myers Squibb Co.
  • C.O. Truxton Inc.
  • Cardinal Health
  • Carlisle Laboratories Inc.
  • Carolina Medical Products Co.
  • Chattem Chemicals Inc.
  • Co Med Pharmaceuticals Inc.
  • Colgate Oral
  • Combe Inc.
  • Consolidated Midland Corp.
  • Contract Pharm
  • Crown Laboratories Inc.
  • Cutis Pharma Inc.
  • Cypress Pharmaceutical Inc.
  • Darby Dental Supply Co. Inc.
  • Del Ray Dermatology
  • Dermik Labs
  • DispenseXpress Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Dofs Laboratories
  • DPT Laboratories Ltd.
  • DSC Laboratories
  • E. Fougera and Co.
  • ECR Pharmaceuticals
  • Elkins-Sinn Inc.
  • Enterprises Importfab Inc.
  • Ferndale Labs
  • G & W Labs
  • Genesis Pharmaceutical Inc.
  • Gertz
  • H and H Laboratories
  • H.J. Harkins Co. Inc.
  • Harmony Laboratories Inc.
  • Hi Tech Pharmacal Co. Inc.
  • Hospira Inc.
  • Inyx Usa Ltd.
  • JHP Pharmaceuticals LLC
  • Johnson & Johnson Healthcare
  • JSJ Pharmaceuticals Inc.
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Lehigh Valley Technologies Inc.
  • Lyne Laboratories Inc.
  • Major Pharmaceuticals
  • Mallinckrodt Inc.
  • Martin Surgical Supply
  • Meda AB
  • Mikart Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • National Vitamin Company
  • Nexgen Pharma Inc.
  • Nycomed Inc.
  • Paddock Labs
  • Palmetto Pharmaceuticals Inc.
  • Patheon Inc.
  • Perrigo Co.
  • Person & Covey
  • Pfizer Inc.
  • Pharmacia Inc.
  • Pharmaderm
  • Pharmedix
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Professional Co.
  • Prometic Pharma Inc.
  • Qualitest
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Resource Optimization and Innovation LLC
  • Rising Pharmaceuticals
  • River's Edge Pharmaceuticals
  • Rouses Point Pharmaceuticals LLC
  • Salix Pharmaceuticals
  • Sandhills Packaging Inc.
  • Sandoz
  • Sanofi-Aventis Inc.
  • Schwarz Pharma Inc.
  • Solvay Pharmaceuticals
  • Southwood Pharmaceuticals
  • Stanley Pharmaceuticals Ltd.
  • Stat Rx Usa
  • Stat Scripts LLC
  • Summers Labs
  • Suppositoria Laboratories Inc.
  • Taro Pharmaceuticals USA
  • Teva Pharmaceutical Industries Ltd.
  • Topiderm Inc.
  • Triax Pharmaceuticals LLC
  • UCB Pharma
  • United Pharmaceuticals
  • United Research Laboratories Inc.
  • Universal Laboratories Inc.
  • Upsher Smith Laboratories
  • Veratex Corp.
  • Vertical Pharmaceuticals Inc.
  • Vintage Pharmaceuticals Inc.
  • West-Ward Pharmaceuticals
  • Wockhardt Ltd.
  • WraSer Pharmaceuticals
  • Wyeth Pharmaceuticals
Dosage Forms
FormRouteStrength
SolutionAuricular (otic)
OintmentTopical0.01 g/1g
LotionTopical20 mg/1mL
GelTopical
GranuleOral0.5 MG
GranuleOral1.0 MG
GranuleOral2.0 MG
GranuleOral5.0 MG
GranuleOral0.5 mg/1
GranuleOral1 mg/1
GranuleOral2 mg/1
GranuleOral5 mg/1
CreamTopical0.57 g/57g
CreamTopical1 g/1mL
SolutionTopical1 g/100g
CreamTopical.05 mg/1g
LotionTopical0.01 g/1g
OintmentTopical1 g/100g
Cream; jellyTopical1 %
CreamTopical0.01 g/1g
CreamTopical0.284 g/28.4g
SuspensionAuricular (otic)
SolutionAuricular (otic)0.2 %
CreamCutaneous1.000 mg
CreamTopical0.5 g
SprayTopical10 g/1mL
LotionTopical
OintmentTopical10 mg / g
TabletOral20 mg
EnemaRectal100 mg / 60 mL
Enema; suspensionRectal100 mg / 60 mL
OintmentTopical100 g/1g
CreamTopical1.116 g
Cream0.5 %
CreamTopical5 MG/G
LotionTopical0.5 g
CreamTopical10 mg/1g
OintmentTopical
SuspensionTopical
LotionTopical10 mg/1g
Solution / dropsOphthalmic
GelTopical1 mg/1g
LotionTopical1 mg/1mL
Kit
LotionTopical0.75 g/100mL
LotionTopical0.45 mg/45mL
CreamTopical.284 g/28.4g
CreamTopical.284 g/287.4g
CreamTopical2.5 mg/g
CreamTopical10 mg/g
SprayOral5 mg/mL
CreamTopical1 g/100mL
CapsuleOral10 MG
CapsuleOral20 MG
CapsuleOral5 MG
Capsule, extended releaseOral10 mg
Capsule, extended releaseOral20 mg
Capsule, extended releaseOral5 mg
CreamTopical2.5 %
SolutionTopical2.5 %
CreamTopical0.25 %
KitOral
OintmentTopical10 mg/1mL
InjectionIntramuscular; Intravenous2 G
Injection, powder, for solutionIntravenous; Parenteral1 G/10ML
Injection, powder, for solutionIntravenous; Parenteral500 MG/5ML
Powder, for solutionParenteral; Rectal; Respiratory (inhalation)100 MG/2ML
Powder, for solutionParenteral; Rectal; Respiratory (inhalation)25 MG/2ML
SolutionIntravenous100.000 mg
SolutionParenteral500.000 mg
TabletOral
CreamTopical0.5 g/100g
ShampooTopical10.2 mg/1mL
CreamTopical1 % w/w
OintmentTopical1 % w/w
GelTopical10 mg/1g
OintmentTopical10 mg/1g
CreamTopical0.59 mg/59mL
OintmentRectal10 mg/1g
StickTopical.01 g/1g
CreamTopical100000 g
LotionTopical0.505 g
CreamTopical2.5 mg
CreamTopical5 mg
CreamTopical10 mg
TabletOral15 mg
TabletOral2.5 mg
SprayOral5 mg
TabletOral10.0 mg
Aerosol, sprayTopical1.13 g/113g
CreamTopical1 h/100g
CreamTopical1 mg/100g
CreamTopical10 mg/1mL
CreamTopical25 mg/1g
CreamTopical5 mg/1g
EnemaRectal100 mg/60mL
GelTopical1 g/100g
LiquidTopical10 mg/1mL
LiquidTopical10 mg/1g
LotionTopical1 g/1mL
LotionTopical1 g/100.65mL
LotionTopical1.14 g/114g
LotionTopical10 mg/1mL
LotionTopical25 mg/1mL
OintmentTopical0.0102 g/1g
OintmentTopical25 mg/1g
OintmentTopical5 mg/1g
PowderNot applicable1 g/1g
ShampooTopical1 g/100mL
SuspensionRectal100 mg/60mL
TabletOral10 mg/1
TabletOral20 mg/1
TabletOral5 mg/1
EmulsionTopical
CreamTopical1 % w/w
OintmentTopical10 mg/1
Cream
Aerosol, sprayTopical10 mg/1g
CreamTopical500 mg / 100 g
CreamTopical1 g / 100 g
CreamTopical0.5 %
CreamTopical5 mg / g
CreamTopical10 mg / g
OintmentTopical0.5 %
OintmentTopical1 %
CreamTopical140 mg/14g
CreamTopical10.2 mg/1g
OintmentTopical10 g/100g
Ointment10 mg
SolutionOral10 mg
EmulsionTopical10 mg
LotionTopical1 g/100mL
GelTopical2 g/100g
OintmentTopical
Ointment
Solution / drops
Solution / dropsOphthalmic
OintmentOphthalmic
SprayTopical1 g/100g
LotionTopical1.02 g/100g
KitOral; Topical
Tablet, chewableOral; Topical
LotionTopical1 g/100g
LotionTopical5 mg
CreamTopical1 %
KitTopical
CreamCutaneous1 %
Cream0.1 %
EmulsionTopical0.1 %
Ointment0.1 %
SolutionTopical0.1 %
LiquidTopical5 mg/1mL
LiquidTopical9 mg/1mL
SprayTopical10 mg/1mL
OintmentTopical1.02 g/100g
CreamTopical1.02 g/100g
CreamTopical1 g/100g
CreamTopical0.009 g/1
Solution / dropsConjunctival
CreamCutaneous1.000 g
SprayTopical1 g/1g
CreamTopical1 g/100g
Solution / dropsAuricular (otic)
SuspensionOphthalmic
Suspension / dropsAuricular (otic)
OintmentOphthalmic
SolutionParenteral100.00 mg
LotionTopical5 mg/1g
CreamCutaneous1.0000 g
SolutionCutaneous1.0000 g
LiquidAuricular (otic)
KitTopical20 mg/1mL
SprayTopical1.12 g/112g
LipstickTopical0.005 g/1g
LotionTopical0.025 mg/2.5mL
TabletOral5 MG
Tablet, multilayer, extended releaseOral20 mg
Tablet, multilayer, extended releaseOral5 mg
CreamTopical7.5 g/100mL
CreamTopical1 mg/1g
LiquidTopical0.28 mg/100mL
Aerosol, foamRectal
OintmentRectal
OintmentRectal; Topical
Injection, powder, for solutionIntravenous; Parenteral100 MG/2ML
CreamTopical.01 mg/1g
CreamTopical0.51 g/100g
SprayTopical500 g/1g
CreamTopical1 mg/100mL
CreamTopical0.33 %
Ointment0.33 %
Ointment1 %
CreamTopical2.5 % w/w
LotionTopical2.5 %
Aerosol, foamTopical10 mg/1g
Solution
LiquidTopical1 g/100mL
LiquidTopical
Injection, powder, for solutionIntravenous; Parenteral
SolutionParenteral100.000 mg
SprayOral5 mg/g
CreamTopical
LotionTopical1 g
EmulsionTopical2.5 mg/g
Ointment
SolutionTopical25 mg/1mL
LotionTopical1 %
LotionTopical1 mL/100mL
SolutionParenteral100. mg
CreamTopical0.5 % w/w
ShampooTopical10 mg/1mL
CreamTopical1 g
CreamTopical
CreamTopical10 mg/1L
SprayTopical10 g/1L
InjectionIntramuscular; Intravenous
Cream
SuppositoryRectal
TabletOral10 mg
Ointment1 %w/w
Cream1 %w/w
Prices
Unit descriptionCostUnit
Locoid Lipocream 0.1% Cream 60 gm Tube335.36USD tube
Cortifoam 90 mg Foam 15 gm Can239.99USD can
Locoid 0.1% Solution 60ml Bottle233.15USD bottle
Locoid Lipocream 0.1% Cream 45 gm Tube200.98USD tube
Locoid 0.1% Cream 45 gm Tube183.83USD tube
Locoid 0.1% Ointment 45 gm Tube174.86USD tube
Pandel 0.1% Cream 45 gm Tube161.37USD tube
Pandel 0.1% Cream 15 gm Tube138.56USD tube
Proctocort 1% Cream 28.35 gm Tube127.51USD tube
Anusol-HC 2.5% Cream 30 gm Tube106.45USD tube
Locoid Lipocream 0.1% Cream 15 gm Tube85.41USD tube
Texacort 2.5% Solution 30ml Bottle85.41USD bottle
Cortisporin 3.5-10000-1 Solution 10ml Bottle84.33USD bottle
Proctofoam HC 1-1% Foam 10 gm Can81.9USD can
Cortisporin 3.5-10000-1 Suspension 10ml Bottle79.55USD bottle
Locoid 0.1% Solution 20ml Bottle79.28USD bottle
Cortisporin 1% Ointment 15 gm Tube75.09USD tube
Locoid 0.1% Cream 15 gm Tube67.49USD tube
Hydrocortisone Ace-Pramoxine 2.5-1% Cream 28.35 gm Tube64.75USD tube
Locoid 0.1% Ointment 15 gm Tube62.04USD tube
Hydrocortisone Valerate 0.2% Ointment 60 gm Tube56.74USD tube
Hydrocortisone 2.5% Lotion 59 gm Bottle55.61USD bottle
Westcort 0.2% Ointment 60 gm Tube55.0USD tube
Cortisporin 0.5-0.5-10000 Cream 7.5 gm Tube54.37USD tube
Westcort 0.2% Ointment 15 gm Tube50.99USD tube
Hydrocortisone Butyrate 0.1% Cream 45 gm Tube49.43USD tube
Hydrocortisone Valerate 0.2% Ointment 45 gm Tube48.73USD tube
Hydrocortisone 2.5% Lotion 59ml Bottle47.47USD bottle
Westcort 0.2% Ointment 45 gm Tube46.97USD tube
Hydrocortisone Valerate 0.2% Cream 60 gm Tube44.99USD tube
Hydrocortisone Valerate 0.2% Cream 45 gm Tube33.99USD tube
Ala Scalp 2% Lotion 29.6ml Bottle30.99USD bottle
Hydrocortisone Valerate 0.2% Ointment 15 gm Tube30.56USD tube
Westcort 0.2% Cream 15 gm Tube25.99USD tube
Hydrocortisone Valerate 0.2% Cream 15 gm Tube19.99USD tube
Cortisporin eye drops19.74USD ml
Solu-Cortef 1 g/vial17.55USD vial
Hydrocortisone 1% Lotion 118ml Bottle15.99USD bottle
Hydrocortisone Acetate 12 25 mg Suppository Box15.01USD box
Hydrocortisone 2.5% Ointment 28.35 gm Tube13.68USD tube
Hydrocortisone 2.5% Cream 30 gm Tube13.67USD tube
Colocort 100 mg/60ml Enema 60ml Bottle13.15USD bottle
Hydrocortisone 100 mg/60ml Enema 60ml Bottle12.6USD bottle
Hydrocortisone 0.5% Cream 28.35 gm Tube11.99USD tube
Hydrocortisone 1% Cream 15 gm Tube11.99USD tube
Hydrocortisone 1% Cream 28 gm Tube11.99USD tube
Hydrocortisone Acetate 1-1% Ointment 30 gm Tube11.99USD tube
Solu-Cortef 500 mg/vial10.47USD vial
Hydrocortisone hemisucc powder9.9USD g
Cortifoam 10% aerosol9.35USD g
Hydrocortisone Sod. Succinate 1 g/vial9.01USD vial
Solu-cortef (pf) 250 mg vial8.58USD vial
Cortisporin-tc ear susp8.3USD ml
Cortisporin ear suspension7.86USD ml
Solu-Cortef 250 mg/vial7.05USD vial
Cortenema (100 mg/60Ml) 100 mg/enm Enema6.96USD enema
Proctofoam-hc foam6.77USD g
Cortifoam 10 % Foam6.14USD g
Hycort (100 mg/60Ml) 100 mg/enm Enema5.79USD enema
Cortamed 2.5 % Ointment5.67USD g
Hydrocortisone Sod. Succinate 500 mg/vial5.34USD vial
Hydrocortisone powder5.19USD g
Solu-cortef (pf) 100 mg vial4.85USD vial
Solu-cortef 100 mg vial4.63USD vial
Proctocort 1% cream4.37USD g
Pandel 0.1% cream4.34USD g
Locoid 0.1% lipocream4.3USD g
Solu-Cortef 100 mg/vial4.07USD vial
Locoid 0.1% cream3.92USD g
Hydrocortisone Sod. Succinate 250 mg/vial3.56USD vial
Hydrocortisone ss 250 mg vial3.5USD vial
Anusol-hc 2.5% cream3.45USD g
Hydrocortisone acet powder3.15USD g
Proctofoam2.89USD g
A-hydrocort 100 mg vial2.42USD each
Proctocream-hc 2.5% cream2.17USD g
Hydrocortisone Sod. Succinate 100 mg/vial2.1USD vial
Hydrocortisone val 0.2% cream2.07USD g
Hytone 2.5% cream1.46USD g
Hydrocortisone buty 0.1% cream1.31USD g
First hydrocort 10% gel1.18USD g
Westcort 0.2% cream1.17USD g
Procto-kit 1% cream1.08USD g
Ala-scalp hp 2% lotion1.03USD ml
Cortef 20 mg tablet0.9USD tablet
Proctosol-hc 2.5% cream0.89USD g
Proctozone-hc 2.5% cream0.83USD g
Orabase plain paste0.77USD g
Hydrocortisone 2.5% lotion0.6USD ml
Cortef 10 mg tablet0.55USD tablet
Orabase-b 20% gel0.55USD g
Hydrocortisone 2.5% cream0.53USD g
Hydrocortisone 10 mg tablet0.52USD tablet
Cortef 5 mg tablet0.45USD tablet
Ala-cort 1% cream0.43USD g
Hydrocortisone 5 mg tablet0.38USD tablet
Corticaine 0.5% cream0.37USD g
Hydrocortisone 20 mg tablet0.32USD tablet
Prevex Hc 1 % Occlusive Cream0.3USD g
Emo-Cort 2.5 % Cream0.26USD g
Preparation h 1% cream0.24USD g
Tucks hydrocortisone ointment0.24USD g
Emo-Cort 2.5 % Lotion0.23USD g
Emo-Cort Scalp 2.5 % Lotion0.22USD g
Colocort 100 mg enema0.21USD ml
Cortenema 100 mg enema0.21USD ml
Sarna Hc 2.5 % Lotion0.2USD g
Emo-Cort 1 % Cream0.19USD g
Balneol lotion0.18USD ml
Emo-Cort 1 % Lotion0.18USD g
Lanacort 1% cool creme0.18USD g
Hyderm 0.5 % Cream0.18USD g
Hytone 1% cream0.17USD g
Cortoderm Mild 0.5 % Ointment0.15USD g
Beta hc 1% lotion0.14USD ml
Cortizone-10 1% spray0.14USD ml
Hydroval 0.2 % Cream0.13USD g
Hydroval 0.2 % Ointment0.13USD g
Aquanil hc 1% lotion0.12USD ml
Hydrocortisone plus 12 1% crm0.12USD g
Scalpicin 3% liquid0.12USD ml
Slender cortisol capsule0.12USD capsule
Cortaid 1% spray0.1USD ml
Sarna Hc 1 % Lotion0.1USD g
Hydrocortisone 0.5% cream0.08USD g
Hydrocortisone 1% cream0.08USD g
Uniderm moisturizer0.05USD ml
Cortoderm Regular 1 % Ointment0.04USD g
Hyderm 1 % Cream0.04USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5635497No1997-06-032014-06-03US flag
US7378405No2008-05-272026-12-19US flag
US7981877No2011-07-192025-01-23US flag
USRE39264No2006-09-052016-08-02US flag
US6514980No2003-02-042019-01-24US flag
US7223387No2007-05-292021-07-24US flag
US9717740No2017-08-012032-11-19US flag
US9675559No2017-06-132033-01-10US flag
US9649280No2017-05-162034-05-12US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)220 °CPhysProp
water solubility320 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.61HANSCH,C ET AL. (1995)
logS-2.97ADME Research, USCD
Caco2 permeability-4.66ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.199 mg/mLALOGPS
logP1.79ALOGPS
logP1.28Chemaxon
logS-3.3ALOGPS
pKa (Strongest Acidic)12.59Chemaxon
pKa (Strongest Basic)-2.8Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area94.83 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity97.4 m3·mol-1Chemaxon
Polarizability39.45 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9918
Blood Brain Barrier+0.9383
Caco-2 permeable-0.5096
P-glycoprotein substrateSubstrate0.7861
P-glycoprotein inhibitor INon-inhibitor0.7847
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.7463
CYP450 2C9 substrateNon-substrate0.8496
CYP450 2D6 substrateNon-substrate0.9138
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9406
CYP450 2C9 inhibitorNon-inhibitor0.9072
CYP450 2D6 inhibitorNon-inhibitor0.9418
CYP450 2C19 inhibitorNon-inhibitor0.9253
CYP450 3A4 inhibitorNon-inhibitor0.8902
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9095
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9597
BiodegradationNot ready biodegradable0.925
Rat acute toxicity1.8914 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.95
hERG inhibition (predictor II)Non-inhibitor0.584
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (2.96 KB)
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-MS (2 MEOX; 3 TMS)GC-MSsplash10-0f7o-3930000000-b7b43b2fc9f20acfd20b
GC-MS Spectrum - GC-MSGC-MSsplash10-0f7o-3930000000-b7b43b2fc9f20acfd20b
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-052f-2910000000-2625335a031486ecb302
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-03di-0759000000-b337a46ecfd6de91776b
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-05fs-3940000000-2bf712a915c3a2c100a2
LC-MS/MS Spectrum - LC-ESI-IT , negativeLC-MS/MSsplash10-015a-0189000000-61afe49a8d4a96aae3f9
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-00lu-0149000000-b95a11b27f7e7d44dd51
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-001l-0019000000-4c4924e6ac472ad52886
MS/MS Spectrum - , negativeLC-MS/MSsplash10-001j-0259000000-fda4e876e9ef04015946
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0009000000-cc8188e19dbdd6210b77
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-07r1-1985000000-b6d756bd554367393be3
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00dj-1930000000-120dc8893cc4709c1f6b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00dm-2910000000-d1f01e1bce5fe0108f40
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05tf-3900000000-4ffd79c22013fe5479b6
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-054o-4900000000-fdbed869a0cadc21b64b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-002f-7900000000-dac7b2c5b3f8e8b85086
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-016u-7900000000-3a770c3819f82ea45841
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-016r-9800000000-d261cf7141fbf30715f5
MS/MS Spectrum - Linear Ion Trap , positiveLC-MS/MSsplash10-056r-0289000000-9a48511b5c3d5fa404e9
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-0759000000-b337a46ecfd6de91776b
MS/MS Spectrum - , positiveLC-MS/MSsplash10-05fs-3940000000-2bf712a915c3a2c100a2
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-01t9-0009000000-4093ca5af0da3685f238
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-0009000000-de7025f83ad3d5bbe454
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-054k-0629000000-50050ee94d788235c6dd
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-01q9-1009000000-156b042ede0b08bd0272
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0gw3-1039000000-ba4294bc29ac2df09c71
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-05mo-0940000000-7b25c8eeb717ba66538b
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-194.2512151
predicted
DarkChem Lite v0.1.0
[M-H]-194.2854151
predicted
DarkChem Lite v0.1.0
[M-H]-194.4778151
predicted
DarkChem Lite v0.1.0
[M-H]-195.5972151
predicted
DarkChem Lite v0.1.0
[M-H]-188.46715
predicted
DeepCCS 1.0 (2019)
[M+H]+194.7928151
predicted
DarkChem Lite v0.1.0
[M+H]+181.5477861
predicted
DarkChem Standard v0.1.0
[M+H]+196.1118151
predicted
DarkChem Lite v0.1.0
[M+H]+196.0463151
predicted
DarkChem Lite v0.1.0
[M+H]+190.36255
predicted
DeepCCS 1.0 (2019)
[M+Na]+194.2409151
predicted
DarkChem Lite v0.1.0
[M+Na]+191.3158269
predicted
DarkChem Standard v0.1.0
[M+Na]+195.0088151
predicted
DarkChem Lite v0.1.0
[M+Na]+196.90793
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. 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]
  2. Rautanen A, Eriksson JG, Kere J, Andersson S, Osmond C, Tienari P, Sairanen H, Barker DJ, Phillips DI, Forsen T, Kajantie E: Associations of body size at birth with late-life cortisol concentrations and glucose tolerance are modified by haplotypes of the glucocorticoid receptor gene. J Clin Endocrinol Metab. 2006 Nov;91(11):4544-51. Epub 2006 Aug 8. [Article]
  3. Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. [Article]
  4. Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. [Article]
  5. Sher L: Combined dexamethasone suppression-corticotropin-releasing hormone stimulation test in studies of depression, alcoholism, and suicidal behavior. ScientificWorldJournal. 2006 Oct 31;6:1398-404. [Article]
  6. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Structural molecule activity
Specific Function
Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
Gene Name
ANXA1
Uniprot ID
P04083
Uniprot Name
Annexin A1
Molecular Weight
38713.855 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Sato-Matsumura KC, Matsumura T, Nakamura H, Sawa H, Nagashima K, Koizumi H: Membrane expression of annexin I is enhanced by calcium and TPA in cultured human keratinocytes. Arch Dermatol Res. 2000 Oct;292(10):496-9. [Article]
  4. White MV, Igarashi Y, Lundgren JD, Shelhamer J, Kaliner M: Hydrocortisone inhibits rat basophilic leukemia cell mediator release induced by neutrophil-derived histamine releasing activity as well as by anti-IgE. J Immunol. 1991 Jul 15;147(2):667-73. [Article]
  5. Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [Article]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [Article]
  2. El-Sankary W, Bombail V, Gibson GG, Plant N: Glucocorticoid-mediated induction of CYP3A4 is decreased by disruption of a protein: DNA interaction distinct from the pregnane X receptor response element. Drug Metab Dispos. 2002 Sep;30(9):1029-34. [Article]
  3. El-Sankary W, Plant NJ, Gibson GG, Moore DJ: Regulation of the CYP3A4 gene by hydrocortisone and xenobiotics: role of the glucocorticoid and pregnane X receptors. Drug Metab Dispos. 2000 May;28(5):493-6. [Article]
  4. Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
  5. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
  2. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Abel SM, Back DJ: Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32. doi: 10.1016/0960-0760(93)90325-q. [Article]
  2. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
Gene Name
CYP11B1
Uniprot ID
P15538
Uniprot Name
Cytochrome P450 11B1, mitochondrial
Molecular Weight
57572.44 Da
References
  1. Freel EM, Shakerdi LA, Friel EC, Wallace AM, Davies E, Fraser R, Connell JM: Studies on the origin of circulating 18-hydroxycortisol and 18-oxocortisol in normal human subjects. J Clin Endocrinol Metab. 2004 Sep;89(9):4628-33. doi: 10.1210/jc.2004-0379. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
Gene Name
CYP11B2
Uniprot ID
P19099
Uniprot Name
Cytochrome P450 11B2, mitochondrial
Molecular Weight
57559.62 Da
References
  1. Freel EM, Shakerdi LA, Friel EC, Wallace AM, Davies E, Fraser R, Connell JM: Studies on the origin of circulating 18-hydroxycortisol and 18-oxocortisol in normal human subjects. J Clin Endocrinol Metab. 2004 Sep;89(9):4628-33. doi: 10.1210/jc.2004-0379. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Bauersachs J, Christ M, Ertl G, Michaelis UR, Fisslthaler B, Busse R, Fleming I: Cytochrome P450 2C expression and EDHF-mediated relaxation in porcine coronary arteries is increased by cortisol. Cardiovasc Res. 2002 Jun;54(3):669-75. [Article]
  2. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
Efficiently catalyzes the reduction of progesterone, androstenedione, 17-alpha-hydroxyprogesterone and testosterone to 5-beta-reduced metabolites. The bile acid intermediates 7-alpha,12-alpha-dihyd...
Gene Name
AKR1D1
Uniprot ID
P51857
Uniprot Name
3-oxo-5-beta-steroid 4-dehydrogenase
Molecular Weight
37376.615 Da
References
  1. Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sterol 5-alpha reductase activity
Specific Function
Converts testosterone (T) into 5-alpha-dihydrotestosterone (DHT) and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation...
Gene Name
SRD5A2
Uniprot ID
P31213
Uniprot Name
3-oxo-5-alpha-steroid 4-dehydrogenase 2
Molecular Weight
28393.015 Da
References
  1. Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. Modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation...
Gene Name
HSD11B2
Uniprot ID
P80365
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 2
Molecular Weight
44126.06 Da
References
  1. Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
  2. Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
11-beta-hydroxysteroid dehydrogenase [nad(p)] activity
Specific Function
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea...
Gene Name
HSD11B1
Uniprot ID
P28845
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 1
Molecular Weight
32400.665 Da
References
  1. Finken MJ, Andrews RC, Andrew R, Walker BR: Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases. J Clin Endocrinol Metab. 1999 Sep;84(9):3316-21. doi: 10.1210/jcem.84.9.6009. [Article]
  2. Sarkar U, Rivera-Burgos D, Large EM, Hughes DJ, Ravindra KC, Dyer RL, Ebrahimkhani MR, Wishnok JS, Griffith LG, Tannenbaum SR: Metabolite profiling and pharmacokinetic evaluation of hydrocortisone in a perfused three-dimensional human liver bioreactor. Drug Metab Dispos. 2015 Jul;43(7):1091-9. doi: 10.1124/dmd.115.063495. Epub 2015 Apr 29. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
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
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. 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]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Androgen binding
Specific Function
Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
Gene Name
SHBG
Uniprot ID
P04278
Uniprot Name
Sex hormone-binding globulin
Molecular Weight
43778.755 Da
References
  1. Khoromi S, Muniyappa R, Nackers L, Gray N, Baldwin H, Wong KA, Matheny LA, Moquin B, Rainer A, Hill S, Remaley A, Johnson LL, Max MB, Blackman MR: Effects of chronic osteoarthritis pain on neuroendocrine function in men. J Clin Endocrinol Metab. 2006 Nov;91(11):4313-8. Epub 2006 Aug 15. [Article]
  2. Stroud LR, Solomon C, Shenassa E, Papandonatos G, Niaura R, Lipsitt LP, Lewinn K, Buka SL: Long-term stability of maternal prenatal steroid hormones from the National Collaborative Perinatal Project: still valid after all these years. Psychoneuroendocrinology. 2007 Feb;32(2):140-50. Epub 2007 Jan 31. [Article]
  3. Lombardi G, Mondaini N, Macchiarella A, Del Popolo G: Female sexual dysfunction and hormonal status in spinal cord injured (SCI) patients. J Androl. 2007 Sep-Oct;28(5):722-6. Epub 2007 May 9. [Article]
  4. Shifren JL, Desindes S, McIlwain M, Doros G, Mazer NA: A randomized, open-label, crossover study comparing the effects of oral versus transdermal estrogen therapy on serum androgens, thyroid hormones, and adrenal hormones in naturally menopausal women. Menopause. 2007 Nov-Dec;14(6):985-94. [Article]
  5. Rizzo L, Dobrovsky V, Danilowicz K, Kral M, Cross G, Serra HA, Bruno OD: Low-dose glucocorticoids in hyperandrogenism. Medicina (B Aires). 2007;67(3):247-52. [Article]
  6. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Steroid binding
Specific Function
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name
SERPINA6
Uniprot ID
P08185
Uniprot Name
Corticosteroid-binding globulin
Molecular Weight
45140.49 Da
References
  1. Henley DE, Lightman SL: New insights into corticosteroid-binding globulin and glucocorticoid delivery. Neuroscience. 2011 Apr 28;180:1-8. doi: 10.1016/j.neuroscience.2011.02.053. Epub 2011 Mar 1. [Article]
  2. 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]

Transporters

Details
1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. 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]
  2. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [Article]
  3. 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]
  4. Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, Komano T, Hori R: Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone. J Biol Chem. 1992 Dec 5;267(34):24248-52. [Article]
  5. Orlowski S, Mir LM, Belehradek J Jr, Garrigos M: Effects of steroids and verapamil on P-glycoprotein ATPase activity: progesterone, desoxycorticosterone, corticosterone and verapamil are mutually non-exclusive modulators. Biochem J. 1996 Jul 15;317 ( Pt 2):515-22. [Article]
  6. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Kanai N, Lu R, Bao Y, Wolkoff AW, Schuster VL: Transient expression of oatp organic anion transporter in mammalian cells: identification of candidate substrates. Am J Physiol. 1996 Feb;270(2 Pt 2):F319-25. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Cortisol demonstrated substrate activity in vitro using human OAT3 expressed on Xenopus Laevis.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55