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Idrocortisone [DCIT]
Brand Acticort
names Aeroseb HC
Aeroseb-HC
Ala-cort
Ala-Scalp
Alacort
Algicirtis
Alphaderm
Amberin
Anflam
Anusol HC
Aquacort
Aquanil HC
Balneol-hc
Barseb HC
Basan-Corti
Beta-hc
CaldeCORT Spray
Cetacort
Clear aid
Cleiton
Cobadex
Colocort
Compound F
Cort-Dome
Cort-Quin
Cortaid
Cortanal
Cortef
Cortef Acetate
Cortenema
Cortesal
Corticreme
Cortifan
Cortifoam
Cortiment
Cortisol
Cortisol alcohol
Cortisolonum
Cortisporin
Cortisporin Otico
Cortispray
Cortolotion
Cortonema
Cortoxide
Cortril
Cremesone
Cremicort-H
Cutisol
Delacort
Derm-Aid
Dermacort
Dermaspray
Dermil
Dermocortal
Dermolate
Dioderm
Dome-cort
Domolene-HC
Dricort
Drotic
EF corlin
Efcorbin
Efcortelan
Efcortelin
Eldecort
Eldercort
Epicort
Epiderm H
Esiderm H
Evacort
Ficortril
Fiocortril
Flexicort
Foille Insetti
Genacort
Glycort
Gyno-Cortisone
H-Cort
Heb Cort
Heb-Cort
Hemsol-HC
Hi-cor
Hidalone
Hidro-Colisona
Hycort
Hycortol
Hycortole
Hydracort
Hydrasson
Hydro-adreson
Hydro-colisona
Hydrocort
Hydrocortal
Hydrocortistab
Hydrocortisyl
Hydrocortone
Hydroskin
Hysone
Hytisone
Hytone
Hytone lotion
Incortin-H
Incortin-hydrogen
Kendall's compound F
Komed HC
Kyypakkaus
Lacticare HC
Lacticare-HC
Lactisona
Locoid
Locoid Lipocream
Lubricort
Maintasone
Medicort
Meusicort
Micort-hc
Mildison
Milliderm
Neosporin-H Ear
Nogenic HC
Nutracort
Nystaform-HC
Optef
Orabase HCA
Otalgine
Otobiotic
Otocort
Otosone-F
Pandel
Pediotic Suspension
Penecort
Permicort
Polcort H
Preparation H Hydrocortisone Cream
Prepcort
Prevex HC
Proctocort
Proctofoam
Protocort
Racet
Rectoid
Reichstein's Substance M
Remederm HC
Sanatison
Scalpicin Capilar
Schericur
Scheroson F
Sigmacort
Signef
Stie-cort
Stiefcorcil
Synacort
Systral Hydrocort
Tarcortin
Tetrahydro E
Tetrahydrocompound E
Texacort
Texacort lotion 25
THE
Thyrotropic-releasing factor
Timocort
Transderma H
Traumaide
Uniderm
Urocortisone
Vioform-Hydrocortisone
VoSol HC
Vytone
Westcort
Zenoxone
Brand Actinac Pwr (Allantoin + Butoxyethyl Nicotinate + Chloramphenicol
name + Hydrocortisone Acetate + Sulfur)
mixtures Actinac Pws (Allantoin + Butoxyethyl Nicotinate + Chloramphenicol
+ Hydrocortisone Acetate + Sulfur)
Calmurid Hc Crm (Hydrocortisone + Urea)
Cortisporin (Bacitracin Zinc + Hydrocortisone + Neomycin Sulfate +
Polymyxin B Sulfate)
Eye and Wound Powder (Chlorhexidine Hydrochloride +
Hydrocortisone Acetate + Penicillin G Procaine + Sulfathiazole)
Forte Topical Suspension (Hydrocortisone Acetate + Hydrocortisone
Sodium Succinate + Neomycin (Neomycin Sulfate) + Penicillin G
Procaine + Polymyxin B Sulfate)
Neo-Cortef Eye Ear Dps (Hydrocortisone Acetate + Neomycin
Sulfate)
Neo-Cortef Eye Ear Drops Sterile Suspension (Hydrocortisone
Acetate + Neomycin Sulfate)
Neo-Cortef Eye Ear Ont (Hydrocortisone Acetate + Neomycin
Sulfate)
Ophthocort Ont (Chloramphenicol + Hydrocortisone Acetate +
Polymyxin B (Polymyxin B Sulfate))
Otizol Hc Liq (Hydrocortisone (Hydrocortisone Acetate) + Lidocaine
(Lidocaine Hydrochloride) + Neomycin (Neomycin Sulfate))
Proctosedyl Ointment (Dibucaine Hydrochloride + Esculin +
Framycetin Sulfate + Hydrocortisone)
Proctosedyl Sup (Dibucaine Hydrochloride + Esculin + Framycetin
Sulfate + Hydrocortisone)
Proctosedyl Suppositories (Dibucaine Hydrochloride + Esculin +
Framycetin Sulfate + Hydrocortisone)
Proctosone Ont (Dibucaine Hydrochloride + Esculin +
Hydrocortisone Acetate + Neomycin Sulfate)
Proctosone Sup (Dibucaine Hydrochloride + Esculin +
Hydrocortisone Acetate + Neomycin Sulfate)
Sopamycetin/Hc Ointment (Chloramphenicol + Hydrocortisone
Acetate)
Sopamycetin/Hc Ont (Chloramphenicol + Hydrocortisone Acetate)
Sopamycetin/Hc Susp (Chloramphenicol + Hydrocortisone Acetate)
Ti-U-Lac Hc Lotion (Hydrocortisone + Urea)
Vioform + Hydrocortisone (Clioquinol + Hydrocortisone)
Vioform Hydrocortisone Cream (Clioquinol + Hydrocortisone)
Vioform Hydrocortisone Mild (Clioquinol + Hydrocortisone)
Ketones
Pharmacology
For the relief of the inflammatory and pruritic manifestations of
corticosteroid-responsive dermatoses. Also used to treat endocrine
Indication (hormonal) disorders (adrenal insufficiency, Addisons disease). It is also used
to treat many immune and allergic disorders, such as arthritis, lupus, severe
psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.
Pharmacolo Hydrocortisone is the most important human glucocorticoid. It is essential for
gy life and regulates or supports a variety of important cardiovascular,
metabolic, immunologic and homeostatic functions. Topical hydrocortisone is
used for its anti-inflammatory or immunosuppressive properties to treat
inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids
are a class of steroid hormones characterised by an ability to bind with the
cortisol receptor and trigger a variety of important cardiovascular, metabolic,
immunologic and homeostatic effects. Glucocorticoids are distinguished from
mineralocorticoids and sex steroids by having different receptors, target cells,
and effects. Technically, the term corticosteroid refers to both glucocorticoids
and mineralocorticoids, but is often used as a synonym for glucocorticoid.
Glucocorticoids suppress cell-mediated immunity. They act by inhibiting
genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and
TNF-alpha, the most important of which is the IL-2. Reduced cytokine
production limits T cell proliferation. Glucocorticoids also suppress humoral
immunity, causing B cells to express lower amounts of IL-2 and IL-2
receptors. This diminishes both B cell clonal expansion and antibody
synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte
cells being activated.
Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding
the receptor the newly formed receptor-ligand complex translocates itself into
the cell nucleus, where it binds to many glucocorticoid response elements
(GRE) in the promoter region of the target genes. The DNA bound receptor
then interacts with basic transcription factors, causing the increase in
expression of specific target genes. The anti-inflammatory actions of
corticosteroids are thought to involve lipocortins, phospholipase A2
inhibitory proteins which, through inhibition arachidonic acid, control the
biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids
induce lipocortin-1 (annexin-1) synthesis, which then binds to cell
membranes preventing the phospholipase A2 from coming into contact with
its substrate arachidonic acid. This leads to diminished eicosanoid production.
Mechanism
The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed,
of action
potentiating the effect. In other words, the two main products in inflammation
Prostaglandins and Leukotrienes are inhibited by the action of
Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to
the extracellular space, where it binds to the leukocyte membrane receptors
and inhibits various inflammatory events: epithelial adhesion, emigration,
chemotaxis, phagocytosis, respiratory burst and the release of various
inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen
activator, chemokines etc.) from neutrophils, macrophages and mastocytes.
Additionally the immune system is suppressed by corticosteroids due to a
decrease in the function of the lymphatic system, a reduction in
immunoglobulin and complement concentrations, the precipitation of
lymphocytopenia, and interference with antigen-antibody binding.
Topical corticosteroids can be absorbed from normal intact skin.
Absorption Inflammation and/or other disease processes in the skin increase percutaneous
absorption.
Side effects include inhibition of bone formation, suppression of calcium
Toxicity
absorption and delayed wound healing
Protein
95%
binding
Biotransfor
Primarily hepatic via CYP3A4
mation
Half life 6-8 hours
Corticosteroids are metabolized primarily in the liver and are then excreted
Route of
by the kidneys. Some of the topical corticosteroids and their metabolites are
elimination
also excreted into the bile.
Volume of
Not Available
distribution
Clearance Not Available
Form Route Strength
Aerosol Rectal
Cream Topical
Enema Rectal
Liquid Topical
Dosages Lotion Topical
Ointment Ophthalmic
Ointment Topical
Powder, for solution Intramuscular
Powder, for solution Intravenous
Tablet Oral
Affected
Humans and other mammals
organisms
Pharmacoeconomics
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
Manufactur Hi tech pharmacal co inc
ers 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
Paddock laboratories inc
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
Perrigo co
Pfizer global research development
Carolina medical products co
Dermik laboratories div aventis pharmaceuticals inc
Torch laboratories inc
X gen pharmaceuticals inc
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
S02BA01
52:08.08
AHFS 84:06.00
Codes
68:04.00
PDB
Not Available
Entries
FDA label show (30 KB)
MSDS show (73.6 KB)
Interactions
Drug Drug Interaction
Interactions The corticosteroid, hydrocortisone, alters the
Acenocoumarol
anticoagulant effect, acenocoumarol.
The corticosteroid, hydrocortisone, may decrease the
Acetylsalicylic acid
effect of the salicylate, acetylsalicylic acid.
The corticosteroid, hydrocortisone, may decrease the
Ambenonium
effect of the anticholinesterase, ambenonium.
Amobarbital The barbiturate, amobarbital, may decrease the effect
of the corticosteroid, hydrocortisone.
The corticosteroid, hydrocortisone, alters the
Anisindione
anticoagulant effect of anisindione.
The barbiturate, aprobarbital, may decrease the effect
Aprobarbital
of the corticosteroid, hydrocortisone.
Bismuth The corticosteroid, hydrocortisone, may decrease the
Subsalicylate effect of the salicylate, bismuth subsalicylate.
The barbiturate, butabarbital, may decrease the effect
Butabarbital
of the corticosteroid, hydrocortisone.
The barbiturate, butalbital, may decrease the effect of
Butalbital
the corticosteroid, hydrocortisone.
The barbiturate, butethal, may decrease the effect of
Butethal
the corticosteroid, hydrocortisone.
Cholestyramine Cholestyramine decreases the effect of hydrocortisone
Cholestyramine Decreases the effect of hydrocortisone
Colestipol Cholestyramine decreases the effect of hydrocortisone
The corticosteroid, hydrocortisone, alters the
Dicumarol
anticoagulant effect of dicumarol.
The barbiturate, dihydroquinidine barbiturate, may
Dihydroquinidine
decrease the effect of the corticosteroid,
barbiturate
hydrocortisone.
The corticosteroid, hydrocortisone, may decrease the
Edrophonium
effect of the anticholinesterase, edrophonium.
The enzyme inducer, ethotoin, may decrease the effect
Ethotoin
of the corticosteroid, hydrocortisone.
The enzyme inducer, fosphenytoin, may decrease the
Fosphenytoin
effect of the corticosteroid, hydrocortisone.
The barbiturate, heptabarbital, may decrease the effect
Heptabarbital
of the corticosteroid, hydrocortisone.
The barbiturate, hexobarbital, may decrease the effect
Hexobarbital
of the corticosteroid, hydrocortisone.
Magnesium The corticosteroid, hydrocortisone, may decrease the
salicylate effect of magnesium salicylate.
The enzyme inducer, mephenytoin, may decrease the
Mephenytoin
effect of the corticosteroid, hydrocortisone.
The barbiturate, methohexital, may decrease the effect
Methohexital
of the corticosteroid, hydrocortisone.
The barbiturate, methylphenobarbital, may decrease
Methylphenobarbital
the effect of the corticosteroid, hydrocortisone.
Midodrine Increased arterial pressure
The corticosteroid, hydrocortisone, may decrease the
Neostigmine
effect of the anticholinesterase, neostigmine.
The barbiturate, pentobarbital, may decrease the effect
Pentobarbital
of the corticosteroid, hydrocortisone.
The barbiturate, phenobarbital, may decrease the effect
Phenobarbital
of the corticosteroid, hydrocortisone.
The enzyme inducer, phenytoin, may decrease the
Phenytoin
effect of the corticosteroid, hydrocortisone.
The barbiturate, primidone, may decrease the effect of
Primidone
the corticosteroid, hydrocortisone.
The corticosteroid, hydrocortisone, may decrease the
Pyridostigmine
effect of the anticholinesterase, pyridostigmine.
Quinidine The barbiturate, quinidine barbiturate, may decrease
barbiturate the effect of the corticosteroid, hydrocortisone.
The enzyme inducer, rifampin, may decrease the effect
Rifampin
of the corticosteroid, hydrocortisone.
The corticosteroid, hydrocortisone, may decrease the
Salicylate-sodium
effect of the salicylate, salicylate-sodium.
The corticosteroid, hydrocortisone, may decrease the
Salsalate
effect of the salicylate, salsalate.
The barbiturate, secobarbital, may decrease the effect
Secobarbital
of the corticosteroid, hydrocortisone.
Tacrine and Hydrocortisone may independently
Tacrine exacerbate muscle weakness in myasthenia gravis
patients. Monitor for additive muscle weakness effects.
The barbiturate, talbutal, may decrease the effect of the
Talbutal
corticosteroid, hydrocortisone.
Trastuzumab may increase the risk of neutropenia and
Trastuzumab anemia. Monitor closely for signs and symptoms of
adverse events.
The corticosteroid, hydrocortisone, may decrease the
Trisalicylate-choline
effect of the salicylate, trisalicylate-choline.
Vecuronium may increase the adverse neuromuscular
effects of systemic corticosteroids, such as
Vecuronium
Hydrocortisone. Monitor for increased muscle
weakness and signs of polyneuropathies and myopathy.
The corticosteroid, hydrocortisone, alters the
Warfarin
anticoagulant effect of warfarin.
Food Take with food to reduce irritation. Calcium, phosphorous, potassium,
Interactions Vitamin A, C, D and zinc needs increased with long term use.
Biology
Pathways Not Available
Enzyme Metabolite Reaction Km Vmax
Metabolism Cytochrome P450 6-beta- 6-beta-
15.2 0.0064
3A4 hydrocortisol hydroxylation
Targets
1. Glucocorticoid receptor
Receptor for glucocorticoids (GC). Has a dual mode of action:as a transcription factor that
binds to glucocorticoid response elements (GRE) and as a modulator of other transcription
factors. Affects inflammatory responses, cellular proliferation and differentiation in target
tissues. Could act as a coactivator for STAT5-dependent transcription upon growth
hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control
of body growth
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. Pubmed
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. Pubmed
3. Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin
Endocrinol Metab. 2006 Sep;20(3):337-53. Pubmed
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. Pubmed
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. Pubmed
2. Annexin A1
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. Pubmed
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. Pubmed
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.
Pubmed
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. Pubmed
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. Pubmed
Enzymes
1. Cytochrome P450 3A4
References:
1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table.
Indiana University School of Medicine (2007). Accessed May 28, 2010.
2. S. Ekins, et al. 3D-QSAR Analysis of Cytochrome P-450 3A4 Substrates. JPET
291:424-433, 1999. Source
3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S,
Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database
on Cytochrome P450 enzymes including a tool for analysis of CYP-drug
interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009
Nov 24. Pubmed
Actions: substrate
UniProt ID: P20815
Gene: CYP3A5
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table.
Indiana University School of Medicine (2007). Accessed May 28, 2010.
Actions: substrate
UniProt ID: P24462
Gene: CYP3A7
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table.
Indiana University School of Medicine (2007). Accessed May 28, 2010.
4. Cytochrome P450 11B1, mitochondrial
Actions: substrate
UniProt ID: P15538
Gene: CYP11B1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S,
Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database
on Cytochrome P450 enzymes including a tool for analysis of CYP-drug
interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009
Nov 24. Pubmed
Actions: substrate
UniProt ID: P19099
Gene: CYP11B2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S,
Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database
on Cytochrome P450 enzymes including a tool for analysis of CYP-drug
interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009
Nov 24. Pubmed
Actions: inducer
UniProt ID: P10632
Gene: CYP2C8
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S,
Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database
on Cytochrome P450 enzymes including a tool for analysis of CYP-drug
interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009
Nov 24. Pubmed
Transporters
1. Multidrug resistance protein 1
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. Pubmed
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. Pubmed
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. Pubmed
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. Pubmed
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. Pubmed
Xenobiotic transporter that may play an important role in the exclusion of xenobiotics
from the brain. May be involved in brain-to-blood efflux. Appears to play a major role in
the multidrug resistance phenotype of several cancer cell lines. When overexpressed, the
transfected cells become resistant to mitoxantrone, daunorubicin and doxorubicin, display
diminished intracellular accumulation of daunorubicin, and manifest an ATP- dependent
increase in the efflux of rhodamine 123
Actions: inhibitor
UniProt ID: Q9UNQ0
Gene: ABCG2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
1. Imai Y, Asada S, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Breast cancer
resistance protein exports sulfated estrogens but not free estrogens. Mol
Pharmacol. 2003 Sep;64(3):610-8. Pubmed
Actions: inhibitor
UniProt ID: P46721
Gene: SLCO1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
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. Pubmed
2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid
clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp
Ther. 1996 Mar;276(3):891-6. Pubmed
Carriers
1. Sex hormone-binding globulin
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, and 17-beta-estradiol. Regulates the plasma metabolic
clearance rate of steroid hormones by controlling their plasma concentration
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. Pubmed
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. Pubmed
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. Pubmed
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 May 15;. Pubmed
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. Pubmed
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Craig Knox 14 hours ago
From DrugBank feedback: "It is stated that logP for HC is 0.5 and there is a link
to PhysProp where there is different (correct) value - 1.61. It is not a big deal of
course but could be misleading."
We have corrected the issue, the experimental logP is now "1.61 [HANSCH,C ET
AL. (1995)]"
Drug created on June 13, 2005 07:24 / Updated on February 11, 2011 09:04