fludrocortisone acetate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| corticosteroids, except prednisolone derivatives | 1191 | 514-36-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic mineralocorticoid with anti-inflammatory activity.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 18, 1955 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |