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) 0.14 mg/mL Benet LZ, Broccatelli F, Oprea TI
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 58.90 20.82 31 3087 29450 50572556
Adrenocortical insufficiency acute 42.10 20.82 11 3107 1433 50600573
Syncope 32.97 20.82 36 3082 102966 50499040
Dizziness 30.18 20.82 66 3052 346303 50255703
Fall 29.38 20.82 64 3054 334868 50267138
Blood pressure decreased 22.29 20.82 22 3096 55887 50546119

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 75.40 21.59 24 3168 3582 29567753
Fall 55.66 21.59 81 3111 177097 29394238
Confusional state 36.51 21.59 56 3136 127821 29443514
Orthostatic hypotension 33.36 21.59 24 3168 22605 29548730
Freezing phenomenon 33.11 21.59 10 3182 1253 29570082
Loss of consciousness 30.96 21.59 39 3153 74017 29497318
Epileptic encephalopathy 30.80 21.59 6 3186 115 29571220
Dizziness 27.44 21.59 62 3130 189622 29381713
Cerebrovascular accident 26.73 21.59 37 3155 76874 29494461
Syncope 26.58 21.59 38 3154 81333 29490002
Blood pressure increased 26.39 21.59 36 3156 73767 29497568
Hallucination 24.39 21.59 27 3165 44685 29526650
Multiple system atrophy 22.67 21.59 5 3187 179 29571156

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
Hypertransaminasaemia 66.06 19.19 24 5161 7167 64486380
Orthostatic hypotension 63.29 19.19 42 5143 46696 64446851
Fall 56.04 19.19 111 5074 416715 64076832
Syncope 47.76 19.19 61 5124 157574 64335973
Adrenocortical insufficiency acute 41.09 19.19 13 5172 2552 64490995
Dizziness 36.97 19.19 96 5089 430067 64063480
Loss of consciousness 35.18 19.19 51 5134 148314 64345233
Confusional state 34.32 19.19 69 5116 261075 64232472
Dyskinesia 27.82 19.19 24 5161 39364 64454183
Hypoaldosteronism 26.54 19.19 6 5179 325 64493222
Blood pressure decreased 25.50 19.19 33 5152 86166 64407381
Freezing phenomenon 25.45 19.19 8 5177 1538 64492009
Epileptic encephalopathy 25.26 19.19 6 5179 404 64493143
Hypotension 23.90 19.19 76 5109 380898 64112649
Cerebrovascular accident 23.87 19.19 41 5144 137542 64356005
Hypertension 23.38 19.19 59 5126 259202 64234345
On and off phenomenon 21.62 19.19 8 5177 2511 64491036
Presyncope 20.09 19.19 19 5166 35070 64458477
Blood pressure increased 19.60 19.19 43 5142 172509 64321038

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
2873 IUPHAR_LIGAND_ID
127-31-1 SECONDARY_CAS_RN
V47IF0PVH4 UNII
225609 PUBCHEM_CID
31378 PUBCHEM_CID
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
460 INN_ID
D005438 MESH_DESCRIPTOR_UI
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 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 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 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 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