fludrocortisone acetate ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
corticosteroids, except prednisolone derivatives 1191 514-36-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alflorone acetate
  • fludrocortisone 21-acetate
  • fluorocortisol acetate
  • fluorohydrocortisone acetate
  • fludrocortisone acetate
  • florinef acetate
A synthetic mineralocorticoid with anti-inflammatory activity.
  • Molecular weight: 422.49
  • Formula: C23H31FO6
  • CLOGP: 2.27
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 100.90
  • ALOGS: -3.94
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.04 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Aug. 18, 1955 FDA

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
Orthostatic hypotension 58.54 20.59 32 3516 36128 63449346
Adrenocortical insufficiency acute 46.19 20.59 12 3536 1686 63483788
Syncope 40.86 20.59 41 3507 117344 63368130
Dizziness 32.50 20.59 73 3475 429852 63055622
Fall 31.20 20.59 68 3480 392266 63093208
Blood pressure decreased 26.91 20.59 25 3523 64997 63420477

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
Hypertransaminasaemia 66.85 20.79 24 3465 5582 34947860
Fall 59.25 20.79 86 3403 202799 34750643
Freezing phenomenon 44.90 20.79 13 3476 1523 34951919
Orthostatic hypotension 36.66 20.79 26 3463 25893 34927549
Confusional state 36.12 20.79 57 3432 144103 34809339
Loss of consciousness 31.54 20.79 40 3449 82627 34870815
Syncope 28.37 20.79 40 3449 91411 34862031
Dizziness 28.06 20.79 65 3424 218456 34734986
Epileptic encephalopathy 28.03 20.79 6 3483 202 34953240
On and off phenomenon 27.18 20.79 10 3479 2487 34950955
Blood pressure increased 26.53 20.79 38 3451 88064 34865378
Hallucination 26.40 20.79 29 3460 51469 34901973
Hypotension 26.36 20.79 64 3425 221585 34731857
Cerebrovascular accident 26.16 20.79 37 3452 84774 34868668
Multiple system atrophy 22.87 20.79 5 3484 186 34953256
Cerebral hypoperfusion 22.51 20.79 6 3483 518 34952924
Dyskinesia 21.81 20.79 18 3471 22395 34931047
Wound necrosis 20.90 20.79 5 3484 279 34953163

FDA Adverse Event Reporting System (Geriatric)

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
Orthostatic hypotension 67.48 17.74 45 5716 56119 79682508
Fall 60.47 17.74 118 5643 487511 79251116
Hypertransaminasaemia 56.76 17.74 24 5737 11900 79726727
Syncope 56.27 17.74 67 5694 179382 79559245
Adrenocortical insufficiency acute 44.39 17.74 14 5747 3029 79735598
Dizziness 39.03 17.74 104 5657 526337 79212290
Loss of consciousness 38.91 17.74 54 5707 167889 79570738
Confusional state 31.16 17.74 70 5691 317927 79420700
Dyskinesia 29.40 17.74 25 5736 44748 79693879
Blood pressure decreased 29.27 17.74 36 5725 99430 79639197
Freezing phenomenon 28.73 17.74 9 5752 1905 79736722
Hypoaldosteronism 26.26 17.74 6 5755 380 79738247
Hypotension 24.87 17.74 79 5682 440238 79298389
Epileptic encephalopathy 24.76 17.74 6 5755 490 79738137
Cerebrovascular accident 24.75 17.74 42 5719 155250 79583377
On and off phenomenon 24.09 17.74 9 5752 3231 79735396
Hypertension 21.11 17.74 62 5699 330930 79407697
Blood pressure increased 20.08 17.74 46 5715 211314 79527313
Presyncope 19.28 17.74 19 5742 41035 79697592
Wound necrosis 18.33 17.74 5 5756 653 79737974
Dehydration 18.28 17.74 49 5712 248138 79490489
Rhabdomyolysis 17.90 17.74 29 5732 103102 79635525

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H02AA02 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CORTICOSTEROIDS FOR SYSTEMIC USE
CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN
Mineralocorticoids
ATC S01CA06 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
Corticosteroids and antiinfectives in combination
ATC S02CA07 SENSORY ORGANS
OTOLOGICALS
CORTICOSTEROIDS AND ANTIINFECTIVES IN COMBINATION
Corticosteroids and antiinfectives in combination
ATC S03CA05 SENSORY ORGANS
OPHTHALMOLOGICAL AND OTOLOGICAL PREPARATIONS
CORTICOSTEROIDS AND ANTIINFECTIVES IN COMBINATION
Corticosteroids and antiinfectives in combination
MeSH PA D000893 Anti-Inflammatory Agents
CHEBI has role CHEBI:35472 anti-inflammatory drugs
CHEBI has role CHEBI:37962 adrenergic agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Adrenogenital disorder indication 267395000 DOID:0050811
Primary adrenocortical insufficiency indication 373662000
Orthostatic hypotension off-label use 28651003
Inactive tuberculosis contraindication 11999007
Peptic ulcer contraindication 13200003 DOID:750
Glaucoma contraindication 23986001 DOID:1686
Acute tuberculosis contraindication 25629007
Hypertensive disorder contraindication 38341003 DOID:10763
Hypothyroidism contraindication 40930008 DOID:1459
Hypokalemia contraindication 43339004
Hypercortisolism contraindication 47270006
Chronic heart failure contraindication 48447003
Osteoporosis contraindication 64859006 DOID:11476
Diabetes mellitus contraindication 73211009 DOID:9351
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Bilateral cataracts contraindication 95722004
Disease of liver contraindication 235856003 DOID:409
Peripheral edema contraindication 271809000




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.18 acidic
pKa2 13.23 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
Mineralocorticoid receptor Nuclear hormone receptor AGONIST IC50 9.92 IUPHAR CHEMBL
Glucocorticoid receptor Nuclear hormone receptor EC50 8.20 WOMBAT-PK
Annexin A1 Cytosolic other WOMBAT-PK

External reference:

IDSource
4017621 VUID
N0000180849 NUI
D00986 KEGG_DRUG
4017621 VANDF
4019758 VANDF
CHEBI:5102 CHEBI
CHEBI:50885 CHEBI
CHEMBL1201010 ChEMBL_ID
C034635 MESH_SUPPLEMENTAL_RECORD_UI
DB00687 DRUGBANK_ID
165516 RXNORM
1846 MMSL
43145 MMSL
4735 MMSL
d00608 MMSL
002210 NDDF
004953 NDDF
116586002 SNOMEDCT_US
116587006 SNOMEDCT_US
89192008 SNOMEDCT_US
C0616274 UMLSCUI
C0016280 UMLSCUI
CHEMBL1201388 ChEMBL_ID
225609 PUBCHEM_CID
460 INN_ID
127-31-1 SECONDARY_CAS_RN
31378 PUBCHEM_CID
D005438 MESH_DESCRIPTOR_UI
2873 IUPHAR_LIGAND_ID
V47IF0PVH4 UNII
U0476M545B UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0115-7033 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0115-7033 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0143-1246 TABLET 0.10 mg ORAL ANDA 24 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0555-0997 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0615-6562 TABLET 0.10 mg ORAL ANDA 23 sections
FLUDROCORTISONE ACETATE HUMAN PRESCRIPTION DRUG LABEL 1 42291-529 TABLET 0.10 mg ORAL ANDA 23 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 42291-764 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 42291-764 TABLET 0.10 mg ORAL ANDA 20 sections
FLUDROCORTISONE ACETATE HUMAN PRESCRIPTION DRUG LABEL 1 50268-330 TABLET 0.10 mg ORAL ANDA 23 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 54868-5446 TABLET 0.10 mg ORAL ANDA 11 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 55154-6645 TABLET 0.10 mg ORAL ANDA 22 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 55154-6645 TABLET 0.10 mg ORAL ANDA 22 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 63629-7780 TABLET 0.10 mg ORAL ANDA 21 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 63629-8806 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 63629-8806 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68084-288 TABLET 0.10 mg ORAL ANDA 22 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68084-288 TABLET 0.10 mg ORAL ANDA 22 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 68084-288 TABLET 0.10 mg ORAL ANDA 22 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 69238-7033 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 69238-7033 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate Human Prescription Drug Label 1 70954-252 TABLET 0.10 mg ORAL ANDA 21 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 71335-0976 TABLET 0.10 mg ORAL ANDA 20 sections