Fluorometholone

Identification

Summary

Fluorometholone is an ophthalmic corticosteroid used for the relief of inflammation located in both the palpebral and bulbar conjunctiva, the cornea, and the anterior segment of the globe of the eye.

Brand Names
FML, FML Forte Liquifilm, FML-S, Flarex, Fluor-OP
Generic Name
Fluorometholone
DrugBank Accession Number
DB00324
Background

A glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732)

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 376.4617
Monoisotopic: 376.204987621
Chemical Formula
C22H29FO4
Synonyms
  • (1R,2S,8S,10S,11S,14R,15S,17S)-14-acetyl-1-fluoro-14,17-dihydroxy-2,8,15-trimethyltetracyclo[8.7.0.02,7.011,15]heptadeca-3,6-dien-5-one
  • 9-Fluoro-11beta,17-dihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione
  • Fluorometholon
  • Fluorométholone
  • Fluorometholone
  • Fluorometholonum
  • Fluorometolona
External IDs
  • NSC 33001
  • U 17323

Pharmacology

Indication

For the ophthalmic treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAnterior chamber inflammationCombination Product in combination with: Tetryzoline (DB06764)••••••••••••••••••••• •••••••• • •••••
Adjunct therapy in treatment ofBacterial eye infection••• •••••
Used in combination to treatConjunctivitis allergicCombination Product in combination with: Tetryzoline (DB06764)••••••••••••••••••••• •••••••• • •••••
Used in combination to treatCorneal inflammationCombination Product in combination with: Tetryzoline (DB06764)••••••••••••••••••••• •••••••• • •••••
Treatment ofEye inflammation••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Corticosteroids such as fluorometholone inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.

Mechanism of action

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Their primary target is 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.

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Side effects may include acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids. LD50 = 234 mg/kg (rats)

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Fluorometholone can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Abatacept.
AcarboseThe risk or severity of hyperglycemia can be increased when Fluorometholone is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Fluorometholone is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Fluorometholone is combined with Acemetacin.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Fluorometholone acetate9I50C3I3OK3801-06-7YRFXGQHBPBMFHW-SBTZIJSASA-N
International/Other Brands
Efflumidex (Allergan) / Fluaton (Allergan) / Flumetholon (Ferron) / Flurolon (Allergan) / FML Liquifilm (Allergan) / Foxone (Winston) / Fucin (Mey See) / Fuluson (Dae Wo) / Fumelon (Han Lim) / Humetoron (Kuk Je) / Oxylone
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FlarexSuspension0.1 % w/vOphthalmicNovartis1987-12-31Not applicableCanada flag
FlarexSuspension / drops1 mg/1mLOphthalmicALCON LABORATORIES, INC.1992-02-06Not applicableUS flag
FlarexSuspension / drops1 mg/1mLOphthalmicEyevance Pharmaceuticals2019-03-05Not applicableUS flag
Fluor-OpSuspension0.1 mL/100mLOphthalmicNovartis Ophthalmics2006-05-11Not applicableUS flag
FMLSuspension0.1 %OphthalmicAbbvie1972-12-31Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FluorometholoneSolution / drops1 mg/1mLOphthalmicREMEDYREPACK INC.2019-03-012020-06-01US flag
FluorometholoneSolution / drops1 mg/1mLOphthalmicPacific Pharma, Inc.1997-10-31Not applicableUS flag
Fluorometholone Ophthalmic SuspensionSuspension / drops1 mg/1mLOphthalmicAmneal Pharmaceuticals NY LLC2023-01-09Not applicableUS flag
Fluorometholone Ophthalmic SuspensionSuspension / drops1 mg/1mLOphthalmicAmneal Pharmaceuticals NY LLC2023-01-09Not applicableUS flag
PMS-fluorometholoneSuspension0.1 %OphthalmicPharmascience Inc2001-07-162016-10-28Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
EFEMOLINE 5 ML DAMLAFluorometholone (1 mg/ml) + Tetrahydrozoline hydrochloride (0.25 mg/ml)Solution / dropsOphthalmicTHEA PHARMA İLAÇ TİC.LTD. ŞTİ.2011-11-18Not applicableTurkey flag
FLU-SURE T® SUSPENSIÓN OFTÁLMICAFluorometholone (1 mg) + Tetrahydrozoline hydrochloride (0.25 mg)SuspensionOphthalmicARBOFARMA S.A.S.2012-10-03Not applicableColombia flag
FML-neo Oph SusFluorometholone (0.1 %) + Neomycin sulfate (0.5 %)SuspensionOphthalmicAllergan1977-12-312011-08-04Canada flag
FML-SFluorometholone (1.0 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)SuspensionOphthalmicAllergan2007-02-20Not applicableUS flag
TobraflexFluorometholone acetate (1 mg/1mL) + Tobramycin (3 mg/1mL)SuspensionOphthalmicAlcon, Inc.1989-07-211989-07-21US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
FLUOROPOS GOZ DAMLASI 1MG/ML 5MLFluorometholone (1 mg/ml)Solution / dropsOphthalmicBİEM İLAÇ SAN. VE TİC. A.Ş.2020-08-142020-12-09Turkey flag

Categories

ATC Codes
D07XB04 — FluorometholoneD07AB06 — FluorometholoneS01BA07 — FluorometholoneS01BB03 — Fluorometholone and mydriaticsC05AA06 — FluorometholoneD07CB03 — Fluorometholone and antibioticsS01CB05 — FluorometholoneS01CA07 — Fluorometholone and antiinfectivesD10AA01 — Fluorometholone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Pregnane steroids
Direct Parent
Gluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
20-oxosteroids / 11-beta-hydroxysteroids / 17-hydroxysteroids / Halogenated steroids / 3-oxo delta-1,4-steroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols / Fluorohydrins
show 6 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 9-halo-steroid / Alcohol / Aliphatic homopolycyclic compound / Alkyl fluoride
show 21 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid (CHEBI:31625)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
SV0CSG527L
CAS number
426-13-1
InChI Key
FAOZLTXFLGPHNG-KNAQIMQKSA-N
InChI
InChI=1S/C22H29FO4/c1-12-9-17-15-6-8-21(27,13(2)24)20(15,4)11-18(26)22(17,23)19(3)7-5-14(25)10-16(12)19/h5,7,10,12,15,17-18,26-27H,6,8-9,11H2,1-4H3/t12-,15-,17-,18-,19-,20-,21-,22-/m0/s1
IUPAC Name
(1R,3aS,3bS,5S,9aS,9bR,10S,11aS)-1-acetyl-9b-fluoro-1,10-dihydroxy-5,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES
[H][C@@]12CC[C@](O)(C(C)=O)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])C[C@H](C)C2=CC(=O)C=C[C@]12C

References

Synthesis Reference

Fried, J.; U.S. Patent 2,852,51 September 16,1958; assigned to Olin Mathieson Chemical Corporation. 
Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; US. Patent 2,867,637; January 6, 1959; assigned to The Upjohn Company
. Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; U.S. Patent 2,867,638; January 6, 1959; assigned to The Upjohn Company. 
Magerlein, B.J., Kagan, F. and Schlagel, C.A.; U.S. Patent 3,038,914; June 12, 1962; assigned to The Upjohn Company.

General References
  1. FDA Approved Drug Products: FML (fluorometholone) ophthalmic suspension [Link]
Human Metabolome Database
HMDB0014469
KEGG Drug
D01367
PubChem Compound
9878
PubChem Substance
46505984
ChemSpider
9494
BindingDB
50103631
RxNav
4491
ChEBI
31625
ChEMBL
CHEMBL1200600
ZINC
ZINC000118912517
Therapeutic Targets Database
DAP001047
PharmGKB
PA164781355
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Fluorometholone
FDA label
Download (64.7 KB)
MSDS
Download (72 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAdenoviral Keratoconjunctivitis1
4CompletedTreatmentIntraocular Pressure (IOP)1
4Not Yet RecruitingTreatmentFuchs' Endothelial Dystrophy / Intraocular Pressure (IOP) / Pseudophakic Bullous Keratopathy1
4Not Yet RecruitingTreatmentSteroid Ophthalmic Insert1
4Unknown StatusHealth Services ResearchDry Eye Syndrome (DES) / Inflammation / Microvessels1

Pharmacoeconomics

Manufacturers
  • Pharmacia and upjohn co
  • Allergan pharmaceutical
  • Novartis pharmaceuticals corp
  • Alcon laboratories inc
Packagers
  • Alcon Laboratories
  • Allergan Inc.
  • A-S Medication Solutions LLC
  • Bausch & Lomb Inc.
  • Dispensing Solutions
  • Novartis AG
  • OMJ Pharmaceuticals
  • Pacific Pharma Lp
  • Pharma Pac LLC
  • Pharmedix
  • Physicians Total Care Inc.
Dosage Forms
FormRouteStrength
SuspensionConjunctival; Ophthalmic1 mg
Solution / dropsOphthalmic
Solution / dropsOphthalmic0.1 %
SuspensionOphthalmic0.1 % w/v
SuspensionOphthalmic1 mg
OintmentOphthalmic
OintmentOphthalmic0.1 %
Solution / dropsOphthalmic0.2 %
SuspensionConjunctival; Ophthalmic100000 mg
SuspensionOphthalmic1.000 mg
SuspensionOphthalmic; Topical1 mg
SuspensionOphthalmic; Topical100000 mg
SuspensionOphthalmic0.1 mL/100mL
Solution / dropsOphthalmic1 mg/1mL
Solution / dropsOphthalmic1 mg/ml
OintmentOphthalmic1 mg/1g
SuspensionOphthalmic0.1 %
Suspension / dropsOphthalmic1 mg/1mL
Suspension / dropsOphthalmic2.5 mg/1mL
SuspensionOphthalmic0.25 %
SolutionOphthalmic1 mg/ml
Suspension / dropsConjunctival0.1 % w/v
SuspensionOphthalmic
Suspension / dropsOphthalmic0.1 %
SuspensionConjunctival; Ophthalmic
SuspensionConjunctival; Intraocular; Ophthalmic
Solution / dropsOphthalmic
Suspension / dropsConjunctival
LiquidOphthalmic1 mg/1ml
Prices
Unit descriptionCostUnit
FML Liquifilm 0.1% Suspension 15ml Bottle82.16USD bottle
FML Forte 0.25% Suspension 15ml Bottle60.98USD bottle
FML Liquifilm 0.1% Suspension 10ml Bottle60.17USD bottle
Flarex 0.1% Suspension 10ml Bottle50.7USD bottle
FML Forte 0.25% Suspension 10ml Bottle48.58USD bottle
Flarex 0.1% Suspension 5ml Bottle42.82USD bottle
FML Liquifilm 0.1% Suspension 5ml Bottle41.65USD bottle
FML-S Liquifilm 0.1-10% Suspension 10ml Bottle35.99USD bottle
Fluor-Op 0.1% Suspension 15ml Bottle30.99USD bottle
FML Forte 0.25% Suspension 5ml Bottle30.07USD bottle
Fluor-Op 0.1% Suspension 10ml Bottle25.99USD bottle
Fluor-Op 0.1% Suspension 5ml Bottle17.99USD bottle
Flarex 0.1% eye drops8.11USD ml
Fml liquifilm 0.1% eye drop6.27USD ml
Fml forte 0.25% eye drops5.09USD ml
Fluorometholone 0.1% drops3.25USD ml
Fml Forte 0.25 % Suspension2.96USD ml
Flarex 0.1 % Suspension1.96USD ml
Pms-Fluorometholone 0.1 % Suspension1.73USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)292-303Fried, J.; U.S. Patent 2,852,51 September 16,1958; assigned to Olin Mathieson Chemical Corporation. 
Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; US. Patent 2,867,637; January 6, 1959; assigned to The Upjohn Company
. Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; U.S. Patent 2,867,638; January 6, 1959; assigned to The Upjohn Company. 
Magerlein, B.J., Kagan, F. and Schlagel, C.A.; U.S. Patent 3,038,914; June 12, 1962; assigned to The Upjohn Company.
water solubility30 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.00HANSCH,C ET AL. (1995)
logS-4.1ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0166 mg/mLALOGPS
logP2.34ALOGPS
logP2.42Chemaxon
logS-4.4ALOGPS
pKa (Strongest Acidic)12.65Chemaxon
pKa (Strongest Basic)-3.4Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area74.6 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity100.87 m3·mol-1Chemaxon
Polarizability39.94 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9956
Blood Brain Barrier+0.9716
Caco-2 permeable+0.8169
P-glycoprotein substrateSubstrate0.7834
P-glycoprotein inhibitor INon-inhibitor0.6791
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.8397
CYP450 2C9 substrateNon-substrate0.8762
CYP450 2D6 substrateNon-substrate0.907
CYP450 3A4 substrateSubstrate0.7663
CYP450 1A2 substrateNon-inhibitor0.9149
CYP450 2C9 inhibitorNon-inhibitor0.8345
CYP450 2D6 inhibitorNon-inhibitor0.9232
CYP450 2C19 inhibitorNon-inhibitor0.9285
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9452
Ames testNon AMES toxic0.9025
CarcinogenicityNon-carcinogens0.9404
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3393 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9694
hERG inhibition (predictor II)Non-inhibitor0.5956
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-01qd-2923000000-d51e17b0fa8439e2bc18
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-0079-2960000000-57c1831d283834b32701
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0079-2960000000-57c1831d283834b32701
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4r-0009000000-25b8222bd2f625ea8997
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0009000000-c8b4ec260ee10a8925df
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4l-0679000000-8599023096391eb0b98d
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00q9-0009000000-746f8fcb6c72dcf07f6f
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-01q9-0309000000-1e71037542f90a1ec9fd
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00dr-0392000000-6017694a59839e4c9217
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]-193.454293
predicted
DarkChem Lite v0.1.0
[M-H]-178.7936128
predicted
DarkChem Lite v0.1.0
[M-H]-190.0317
predicted
DeepCCS 1.0 (2019)
[M+H]+195.074593
predicted
DarkChem Lite v0.1.0
[M+H]+186.1119747
predicted
DarkChem Lite v0.1.0
[M+H]+191.92708
predicted
DeepCCS 1.0 (2019)
[M+Na]+194.054393
predicted
DarkChem Lite v0.1.0
[M+Na]+185.2282366
predicted
DarkChem Lite v0.1.0
[M+Na]+197.5807
predicted
DeepCCS 1.0 (2019)

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Learn more
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. Samudre SS, Lattanzio FA Jr, Williams PB, Sheppard JD Jr: Comparison of topical steroids for acute anterior uveitis. J Ocul Pharmacol Ther. 2004 Dec;20(6):533-47. [Article]
  2. Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. [Article]
  3. 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]
  4. Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. [Article]
  5. 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]
  6. 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]

Enzymes

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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
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. 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]
  2. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Moisan MP, Castanon N: Emerging Role of Corticosteroid-Binding Globulin in Glucocorticoid-Driven Metabolic Disorders. Front Endocrinol (Lausanne). 2016 Dec 19;7:160. doi: 10.3389/fendo.2016.00160. eCollection 2016. [Article]
  2. 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]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48