fludrocortisone acetate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.522 Moderate 0.78
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.404 Moderate 0.78
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 36.813 10^-6 cm/s Moderate 0.78
dh-clint Dog hepatocyte intrinsic clearance 36.898 uL/min/10^6 cells Moderate 0.78
dppb Dog plasma protein binding (% unbound) 41.730 % Moderate 0.78
fcs-ppb Fetal calf serum protein binding (% unbound) 52.760 % Moderate 0.78
herg hERG pIC50 4.284 pIC50 Moderate 0.78
hh-clint Human hepatocyte intrinsic clearance 43.551 uL/min/10^6 cells Moderate 0.78
hlm-clint Human liver microsomal intrinsic clearance 57.677 uL/min/mg protein Moderate 0.78
hppb Human plasma protein binding (% unbound) 33.440 % Moderate 0.78
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK 14
kinase-selectivity-class GRK2 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 6.699 Moderate 0.78
mh-clint Mouse hepatocyte intrinsic clearance 177.419 Moderate 0.78
mppb Mouse plasma protein binding (% unbound) 44.160 Moderate 0.78
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 9.506 Moderate 0.78
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 48.330 % Moderate 0.78
rh-clint Rat hepatocyte intrinsic clearance 188.799 uL/min/10^6 cells Moderate 0.78
rh-fuinc Rat hepatocyte fraction unbound in incubation 88.520 % Moderate 0.78
rppb Rat plasma protein binding (% unbound) 35.680 % Moderate 0.78
solubility-dd Solubility at pH 7.4 in DMSO 790.679 uM Moderate 0.78

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 63.09 19.42 34 4487 41793 90582133
Syncope 49.98 19.42 46 4475 132617 90491309
Adrenocortical insufficiency acute 47.04 19.42 13 4508 2588 90621338
Serum amyloid A protein increased 40.80 19.42 9 4512 708 90623218
Fall 40.59 19.42 80 4441 481730 90142196
Dizziness 40.51 19.42 90 4431 589194 90034732
Blood pressure decreased 32.20 19.42 28 4493 74867 90549059
Postural orthostatic tachycardia syndrome 30.49 19.42 9 4512 2263 90621663
Presyncope 29.79 19.42 19 4502 31786 90592140
Loss of consciousness 22.21 19.42 31 4490 140207 90483719
Hypotension 21.49 19.42 49 4472 325348 90298578
Dyskinesia 20.60 19.42 16 4505 36518 90587408
Abdominal wall haemorrhage 20.57 19.42 4 4517 169 90623757
Urinary tract infection 20.15 19.42 46 4475 305586 90318340

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
Fall 66.95 20.99 93 3730 234427 42383085
Hypertransaminasaemia 57.71 20.99 24 3799 9203 42608309
Freezing phenomenon 52.45 20.99 15 3808 1874 42615638
Orthostatic hypotension 42.23 20.99 29 3794 30541 42586971
Confusional state 38.35 20.99 60 3763 167537 42449975
On and off phenomenon 35.86 20.99 13 3810 3454 42614058
Syncope 32.15 20.99 42 3781 99364 42518148
Hallucination 29.84 20.99 31 3792 57476 42560036
Loss of consciousness 29.83 20.99 39 3784 92315 42525197
Blood pressure increased 28.31 20.99 40 3783 101888 42515624
Dizziness 28.05 20.99 66 3757 249188 42368324
Dyskinesia 27.98 20.99 21 3802 25369 42592143
Hypotension 27.68 20.99 67 3756 257564 42359948
Epileptic encephalopathy 26.53 20.99 6 3817 291 42617221
Cerebrovascular accident 25.32 20.99 37 3786 97123 42520389
Stoma site discharge 24.95 20.99 8 3815 1468 42616044
Multiple system atrophy 23.81 20.99 5 3818 171 42617341
Adrenocortical insufficiency acute 21.77 20.99 8 3815 2207 42615305
Speech disorder 21.35 20.99 19 3804 29102 42588410
Wound necrosis 21.02 20.99 5 3818 303 42617209

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 79.53 17.91 50 6761 66199 110516289
Fall 73.13 17.91 132 6679 603350 109979138
Syncope 68.72 17.91 73 6738 202463 110380025
Dizziness 47.64 17.91 121 6690 698072 109884416
Hypertransaminasaemia 44.17 17.91 24 6787 24231 110558257
Adrenocortical insufficiency acute 41.39 17.91 14 6797 4426 110578062
Loss of consciousness 39.04 17.91 54 6757 196252 110386236
Serum amyloid A protein increased 36.46 17.91 9 6802 933 110581555
Blood pressure decreased 36.39 17.91 40 6771 115051 110467437
Dyskinesia 36.23 17.91 28 6783 51418 110531070
Hypotension 33.81 17.91 89 6722 523760 110058728
On and off phenomenon 33.70 17.91 12 6799 4412 110578076
Freezing phenomenon 31.48 17.91 10 6801 2599 110579889
Presyncope 30.96 17.91 25 6786 48862 110533626
Cerebrovascular accident 27.59 17.91 44 6767 181240 110401248
Postural orthostatic tachycardia syndrome 26.00 17.91 8 6803 1874 110580614
Blood pressure increased 25.58 17.91 52 6759 258321 110324167
Confusional state 24.68 17.91 74 6737 468606 110113882
Hypoaldosteronism 23.93 17.91 6 6805 663 110581825
Epileptic encephalopathy 23.79 17.91 6 6805 679 110581809
Urinary tract infection 22.62 17.91 57 6754 326225 110256263
Death 21.88 17.91 93 6718 698776 109883712
Dehydration 20.61 17.91 50 6761 279461 110303027
Hallucination 20.29 17.91 28 6783 101404 110481084
Stoma site discharge 19.11 17.91 7 6804 2788 110579700
Wound necrosis 18.35 17.91 5 6806 763 110581725
Rhabdomyolysis 18.00 17.91 29 6782 120372 110462116

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:22587 antiviral agent
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:35472 anti-inflammatory drug
CHEBI has role CHEBI:37962 adrenergic agent

Related Drugs by ATC class:

H02AA Mineralocorticoids 2 drugs
aldosteronedesoxycortone
S01CA Corticosteroids and antiinfectives in combination 11 drugs
betamethasonechloroprednisoneclobetasone butyratedexamethasonefluocinolone acetonidefluocortolonefluorometholonehydrocortisoneloteprednol etabonatemethylprednisoloneprednisolone
S02CA Corticosteroids and antiinfectives in combination 6 drugs
dexamethasoneflumetasonefluocinolone acetonidehydrocortisoneprednisolonetriamcinolone
S03CA Corticosteroids and antiinfectives in combination 5 drugs
betamethasonedexamethasonehydrocortisonemethylprednisoloneprednisolone

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




🐶 Veterinary Drug Use

None

🐶 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
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
CHEBI:5102 CHEBI
CHEMBL1201388 ChEMBL_ID
225609 PUBCHEM_CID
127-31-1 SECONDARY_CAS_RN
31378 PUBCHEM_CID
2873 IUPHAR_LIGAND_ID
V47IF0PVH4 UNII
460 INN_ID
D005438 MESH_DESCRIPTOR_UI
U0476M545B UNII
CHEBI:50885 CHEBI
U0476M545B INXIGHT DRUGS
V47IF0PVH4 INXIGHT DRUGS

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 0615-6562 TABLET 0.10 mg ORAL ANDA 20 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0904-7317 TABLET 0.10 mg ORAL ANDA 21 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 51407-705 TABLET 0.10 mg ORAL ANDA 16 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 55154-2644 TABLET 0.10 mg ORAL ANDA 21 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 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 70771-1893 TABLET 0.10 mg ORAL ANDA 16 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 71335-2454 TABLET 0.10 mg ORAL ANDA 21 sections
fludrocortisone acetate Human Prescription Drug Label 1 71930-088 TABLET 0.10 mg ORAL ANDA 24 sections
Fludrocortisone acetate HUMAN PRESCRIPTION DRUG LABEL 1 72578-164 TABLET 0.10 mg ORAL ANDA 16 sections
Fludrocortisone Acetate HUMAN PRESCRIPTION DRUG LABEL 1 72603-170 TABLET 0.10 mg ORAL ANDA 21 sections