fluorometholone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
steroids not used as glucocorticosteroids 1208 426-13-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluorometholone
  • fluormetholon
  • flumetholone
  • flumetholon
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)
  • Molecular weight: 376.47
  • Formula: C22H29FO4
  • CLOGP: 2.11
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 74.60
  • ALOGS: -4.36
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 12, 1972 FDA ALLERGAN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 100.90 24.71 52 1430 93035 46591545
Eye irritation 84 24.71 28 1454 16586 46667994
Eye pain 59.56 24.71 25 1457 27915 46656665
Keratitis 43.44 24.71 11 1471 2472 46682108
Corneal erosion 39.91 24.71 7 1475 265 46684315
Ocular hyperaemia 36.57 24.71 16 1466 19694 46664886
Corneal perforation 29.57 24.71 6 1476 500 46684080
Corneal disorder 27.12 24.71 7 1475 1696 46682884

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Corneal disorder 64.16 33.03 12 769 802 29950895
Treatment failure 55.94 33.03 24 757 34655 29917042
Intraocular pressure increased 51.40 33.03 14 767 5106 29946591

Pharmacologic Action:

SourceCodeDescription
ATC C05AA06 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Corticosteroids
ATC D07AB06 DERMATOLOGICALS
CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
CORTICOSTEROIDS, PLAIN
Corticosteroids, moderately potent (group II)
ATC D07XB04 DERMATOLOGICALS
CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
CORTICOSTEROIDS, OTHER COMBINATIONS
Corticosteroids, moderately potent, other combinations
ATC D10AA01 DERMATOLOGICALS
ANTI-ACNE PREPARATIONS
ANTI-ACNE PREPARATIONS FOR TOPICAL USE
Corticosteroids, combinations for treatment of acne
ATC S01BA07 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIINFLAMMATORY AGENTS
Corticosteroids, plain
ATC S01CB05 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
Corticosteroids/antiinfectives/mydriatics in combination
ATC D07CB03 DERMATOLOGICALS
CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS
Corticosteroids, moderately potent, combinations with antibiotics
ATC S01BB03 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIINFLAMMATORY AGENTS
Corticosteroids and mydriatics in combination
ATC S01CA07 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
Corticosteroids and antiinfectives in combination
FDA MoA N0000175450 Corticosteroid Hormone Receptor Agonists
FDA EPC N0000175576 Corticosteroid
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D005938 Glucocorticoids
MeSH PA D006728 Hormones
CHEBI has role CHEBI:35472 anti-inflammatory drugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Cyclitis indication 17657000
Iritis indication 65074000 DOID:1406
Iridocyclitis indication 77971008
Corneal abrasion indication 85848002
Corneal ulcer indication 91514001 DOID:8463
Uveitis indication 128473001 DOID:13141
Punctate keratopathy indication 246936005
Herpes zoster keratitis indication 397573005
Rosacea indication 398909004 DOID:8881
Allergic conjunctivitis indication 473460002 DOID:11204
Post-Op Ocular Inflammation indication
Otitis externa off-label use 3135009
Allergic otitis externa off-label use 405821001
Otitis Externa Seborrhea off-label use
Otitis Externa Eczema off-label use
Ocular hypertension contraindication 4210003 DOID:9282
Herpes simplex keratitis contraindication 9389005
Herpes simplex dendritic keratitis contraindication 29943008
Fungal infection of eye contraindication 31194008
Severe myopia contraindication 34187009
Tuberculosis of eye contraindication 49107007
Diabetes mellitus contraindication 73211009 DOID:9351
Open-angle glaucoma contraindication 84494001 DOID:1067
Krukenberg spindle contraindication 85430004
Anemia due to enzyme deficiency contraindication 111577008
Deficiency of glucose-6-phosphate dehydrogenase contraindication 124134002 DOID:2862
Eye infection contraindication 128351009
Bacterial infection of eye contraindication 128984004
Viral eye infection contraindication 312132001
Vaccinia keratitis contraindication 397552005
Porphyria contraindication 418470004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.06 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucocorticoid receptor Nuclear hormone receptor AGONIST Ki 8.80 DRUG MATRIX CHEMBL
Androgen receptor Transcription factor Ki 6.07 DRUG MATRIX
Progesterone receptor Transcription factor Ki 6.97 DRUG MATRIX

External reference:

IDSource
4018212 VUID
N0000146545 NUI
D01367 KEGG_DRUG
4018212 VANDF
C0016351 UMLSCUI
CHEBI:31625 CHEBI
CHEMBL1200600 ChEMBL_ID
DB00324 DRUGBANK_ID
D005469 MESH_DESCRIPTOR_UI
7079 IUPHAR_LIGAND_ID
803 INN_ID
SV0CSG527L UNII
9878 PUBCHEM_CID
4491 RXNORM
4744 MMSL
6193 MMSL
7403 MMSL
002194 NDDF
108851006 SNOMEDCT_US
2925007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FML HUMAN PRESCRIPTION DRUG LABEL 1 0023-0316 OINTMENT 1 mg OPHTHALMIC NDA 18 sections
FML HUMAN PRESCRIPTION DRUG LABEL 1 11980-211 SUSPENSION/ DROPS 1 mg OPHTHALMIC NDA 17 sections
FML FORTE HUMAN PRESCRIPTION DRUG LABEL 1 11980-228 SUSPENSION/ DROPS 2.50 mg OPHTHALMIC NDA 17 sections
FLUOROMETHOLONE HUMAN PRESCRIPTION DRUG LABEL 1 60758-880 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA AUTHORIZED GENERIC 16 sections