Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H29FO5 |
Molecular Weight | 380.4504 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@]12C[C@H](O)[C@@]3(F)[C@@H](CCC4=CC(=O)CC[C@]34C)[C@@H]1CC[C@]2(O)C(=O)CO
InChI
InChIKey=AAXVEMMRQDVLJB-BULBTXNYSA-N
InChI=1S/C21H29FO5/c1-18-7-5-13(24)9-12(18)3-4-15-14-6-8-20(27,17(26)11-23)19(14,2)10-16(25)21(15,18)22/h9,14-16,23,25,27H,3-8,10-11H2,1-2H3/t14-,15-,16-,18-,19-,20-,21-/m0/s1
DescriptionCurator's Comment: description was created based on several sources, including
http://www.2ndchance.info/addison's-florinef.pdf
Curator's Comment: description was created based on several sources, including
http://www.2ndchance.info/addison's-florinef.pdf
Fludrocortisone acetate (approved as Florinef) is a synthetic adrenocortical steroid possessing very potent mineralcorticoid properties and high glucocorticoid activity. Main indications are Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt losing adrenogenital syndrome.
Originator
Sources: http://pubs.acs.org/doi/abs/10.1021/ja01634a101
Curator's Comment: refernce was retrived from https://www.researchgate.net/publication/284208027_Fludrocortisone_Acetate
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P22199 Gene ID: 25672.0 Gene Symbol: Nr3c2 Target Organism: Rattus norvegicus (Rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/611629 |
1.07 nM [Kd] | ||
Target ID: P08235 Gene ID: 4306.0 Gene Symbol: NR3C2 Target Organism: Homo sapiens (Human) |
|||
Target ID: P06536 Gene ID: 24413.0 Gene Symbol: Nr3c1 Target Organism: Rattus norvegicus (Rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/611629 |
|||
Target ID: P04150 Gene ID: 2908.0 Gene Symbol: NR3C1 Target Organism: Homo sapiens (Human) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | FLORINEF Approved UseFludrocortisone acetate tablets USP, 0.1 mg are indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome. Launch Date1955 |
|||
Primary | FLORINEF Approved UseFludrocortisone acetate tablets USP, 0.1 mg are indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome. Launch Date1955 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1241.1 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25611194 |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.19 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27416887 |
50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3275.8 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25611194 |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.25 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27416887 |
50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25611194 |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27416887 |
50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25611194 |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
FLUDROCORTISONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
0.3 mg 1 times / day multiple, oral Highest studied dose Dose: 0.3 mg, 1 times / day Route: oral Route: multiple Dose: 0.3 mg, 1 times / day Sources: |
unhealthy |
Other AEs: Serum potassium decreased, Rise in blood pressure... Other AEs: Serum potassium decreased (5 patients) Sources: Rise in blood pressure (5 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Rise in blood pressure | 5 patients | 0.3 mg 1 times / day multiple, oral Highest studied dose Dose: 0.3 mg, 1 times / day Route: oral Route: multiple Dose: 0.3 mg, 1 times / day Sources: |
unhealthy |
Serum potassium decreased | 5 patients | 0.3 mg 1 times / day multiple, oral Highest studied dose Dose: 0.3 mg, 1 times / day Route: oral Route: multiple Dose: 0.3 mg, 1 times / day Sources: |
unhealthy |
PubMed
Title | Date | PubMed |
---|---|---|
Clinical improvement in patients with orthostatic intolerance after treatment with bisoprolol and fludrocortisone. | 2000 Oct |
|
[Addisonian myopathy]. | 2001 |
|
Hypoadrenocorticism in a cat. | 2001 Apr |
|
Steroids in sepsis--more effective than activated protein C? | 2001 Aug |
|
Mechanisms underlying the impairment in orthostatic tolerance after nocturnal recumbency in patients with autonomic failure. | 2001 Dec |
|
Endothelial cell dysfunction in mice after transgenic knockout of type 2, but not type 1, 11beta-hydroxysteroid dehydrogenase. | 2001 Dec 4 |
|
[An autopsy case of pure autonomic failure with pathological features of Parkinson's disease]. | 2001 Jan |
|
Aldosterone synthase deficiency type I with no documented homozygous mutations in the CYP11B2 gene. | 2001 Jan |
|
Fludrocortisone acetate to treat neurally mediated hypotension in chronic fatigue syndrome: a randomized controlled trial. | 2001 Jan 3 |
|
[Orthostatic intolerance syndromes]. | 2001 Jan-Mar |
|
Dysautonomia and neurocardiogenic syncope. | 2001 Mar |
|
Orthostatic hypotension and chronic fatigue syndrome. | 2001 Mar 21 |
|
Orthostatic hypotension and chronic fatigue syndrome. | 2001 Mar 21 |
|
Insulin and mineralocorticoids influence on extrarenal potassium metabolism in chronic hemodialysis patients. | 2001 Nov |
|
Congenital hyperreninemic hypoaldosteronism unlinked to the aldosterone synthase (CYP11B2) gene. | 2001 Nov |
|
[Adrenal insufficiency caused by treatment with levothyroxine]. | 2001 Nov 29 |
|
[Increasing pigmentation in Schmidt syndrome (polyglandular autoimmune syndrome type II]. | 2001 Oct |
|
Fludrocortisone treatment in a child with severe cerebral salt wasting. | 2001 Oct |
|
Adverse cardiac effects of salt with fludrocortisone in hypertension. | 2001 Oct |
|
Pharmacologic options available to treat symptomatic intradialytic hypotension. | 2001 Oct |
|
Serum cortisol and 17-hydroxyprogesterone interrelation in classic 21-hydroxylase deficiency: is current replacement therapy satisfactory? | 2001 Oct |
|
Pro/con clinical debate: are steroids useful in the management of patients with septic shock? | 2002 Apr |
|
Effect of treatment with low doses of hydrocortisone and fludrocortisone on mortality in patients with septic shock. | 2002 Aug 21 |
|
Hyperkalaemia and selective hypoaldosteronism in myotonic dystrophy. | 2002 Feb |
|
The aldosterone-renin ratio and primary aldosteronism. | 2002 Feb |
|
[Syncope - a systematic overview of classification, pathogenesis, diagnosis and management]. | 2002 Feb |
|
Hyporeninemic hypoaldosteronism associated with Sjögren's syndrome. | 2002 Feb 15 |
|
Corticosteroid supplementation for adrenal insufficiency. | 2002 Jan 9 |
|
A footnote on the origin of fluorosteroids. | 2002 Jul |
|
Screening and diagnosis of primary aldosteronism. | 2002 Jul-Aug |
|
Structural basis for the glucocorticoid response in a mutant human androgen receptor (AR(ccr)) derived from an androgen-independent prostate cancer. | 2002 Mar 28 |
|
Dysautonomias: clinical disorders of the autonomic nervous system. | 2002 Nov 5 |
|
The mineralocorticoid receptor may compensate for the loss of the glucocorticoid receptor at specific stages of mammary gland development. | 2002 Sep |
|
A pilot randomized trial of induced blood pressure elevation: effects on function and focal perfusion in acute and subacute stroke. | 2003 |
|
Sepsis clinical knowledge: a role of steroid treatment. | 2003 Apr |
|
Bench-to-bedside review: endothelial cell dysfunction in severe sepsis: a role in organ dysfunction? | 2003 Apr |
|
Diminished renal kallikrein responses to mineralocorticoid stimulation in African Americans: determinants of an intermediate phenotype for hypertension. | 2003 Apr |
|
Monozygotic twins with congenital adrenal hyperplasia: long-term endocrine evaluation and gene analysis. | 2003 Apr-May |
|
Association between supine hypertension and orthostatic hypotension in autonomic failure. | 2003 Aug |
|
Primary aldosteronism and hypertensive disease. | 2003 Aug |
|
Chronic fatigue syndrome and Addison's disease. | 2003 Feb |
|
Successful treatment of severe orthostatic hypotension with erythropoietin. | 2003 Jan |
|
Serum leptin levels in patients with 21-hydroxylase deficiency before and after treatment. | 2003 Jan-Mar |
|
Automated coupling of capillary-HPLC to matrix-assisted laser desorption/ionization mass spectrometry for the analysis of small molecules utilizing a reactive matrix. | 2003 Jul |
|
Neurologic complications following treatment of canine hypoadrenocorticism. | 2003 Jun |
|
Impact of smoking on the response to treatment of thyroid associated ophthalmopathy. | 2003 Jun |
|
[A 47-year-old man with "pure autonomic failure" and pernicious anemia]. | 2003 Jun 13 |
|
Combination therapy with hydrocortisone and fludrocortisone does not improve symptoms in chronic fatigue syndrome: a randomized, placebo-controlled, double-blind, crossover study. | 2003 Jun 15 |
|
Stability of fludrocortisone acetate solutions prepared from tablets and powder. | 2003 Mar |
|
Blood pressure in children and adolescents with congenital adrenal hyperplasia (21-hydroxylase deficiency): a preliminary report. | 2003 May |
Patents
Name | Type | Language | ||
---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
S03CA05
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-ATC |
S01CA06
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-ATC |
H02AA02
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-VATC |
QS03CA05
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-ATC |
S02CA07
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-VATC |
QS02CA07
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
NCI_THESAURUS |
C521
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
18.1
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-VATC |
QS01CA06
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
WHO-VATC |
QH02AA02
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
||
|
LIVERTOX |
422
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
2873
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
DB00687
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
100000080700
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
FLUDROCORTISONE
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
m5431
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | Merck Index | ||
|
D005438
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
204-833-2
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
U0476M545B
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
DTXSID7023061
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
C71629
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
U0476M545B
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
3332
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
460
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
SUB07684MIG
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
31378
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
4452
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | RxNorm | ||
|
CHEMBL1201010
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
127-31-1
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
50885
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY | |||
|
11318
Created by
admin on Mon Mar 31 18:34:43 GMT 2025 , Edited by admin on Mon Mar 31 18:34:43 GMT 2025
|
PRIMARY |
ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)