514-36-3 Usage
Description
Fludrocortisone acetate, also known as 21-acetyloxy-9-fluoro-11β,17-dihydroxypregn-4-ene-3,20-dione or 9α-fluorohydrocortisone (Florinef Acetate), is a synthetic corticosteroid that serves as a potent mineralocorticoid receptor agonist. It is characterized by its high mineralocorticoid activity, which is approximately 800 times that of hydrocortisone, and its glucocorticoid activity, which is about 11 times as potent. Fludrocortisone acetate is primarily used for the treatment of Addison's disease and for the inhibition of endogenous adrenocortical secretions.
Uses
Used in Pharmaceutical Industry:
Fludrocortisone acetate is used as a medication for the treatment of Addison's disease, a condition characterized by insufficient production of adrenal hormones. Its potent mineralocorticoid activity promotes sodium retention and potassium excretion, helping to maintain electrolyte balance in patients with this condition.
Additionally, Fludrocortisone acetate is used as a partial replacement therapy for primary and secondary adrenocortical insufficiency, as well as for the treatment of salt-losing adrenal hyperplasia. Its glucocorticoid actions, which are about 10 times as potent as hydrocortisone, contribute to its effectiveness in these applications.
Biochem/physiol Actions
Fludrocortisone acetate is a synthetic corticosteroid with more mineralocorticoid than glucocorticoid activity.
Clinical Use
Replacement therapy in adrenal insufficiency
Veterinary Drugs and Treatments
Fludrocortisone is used in small animal medicine for the treatment
of adrenocortical
insufficiency (Addison’s disease). It can also be
used as adjunctive therapy in hyperkalemia.
Additionally, in humans, fludrocortisone has been used in saltlosing,
congenital adrenogenital syndrome
and in patients with severe
postural hypotension.
Drug interactions
Potentially hazardous interactions with other drugs
Aldesleukin: avoid concomitant use.
Antibacterials: metabolism accelerated by rifamycins;
metabolism possibly inhibited by erythromycin;
possibly reduce isoniazid concentration.
Anticoagulants: efficacy of coumarins and
phenindione may be altered.
Antiepileptics: metabolism accelerated by
carbamazepine, fosphenytoin, phenobarbital,
phenytoin and primidone.
Antifungals: increased risk of hypokalaemia with
amphotericin - avoid; metabolism possibly inhibited
by itraconazole and ketoconazole.
Antivirals: concentration possibly increased by
ritonavir.
Cobicistat: concentration of fludrocortisone
increased.
Vaccines: high dose corticosteroids can impair
immune response to vaccines - avoid concomitant
use with live vaccines
Metabolism
Fludrocortisone is hydrolysed to produce the nonesterified alcohol. In human volunteers, excretion through
urine was about 80%, and it was concluded that about
20% were excreted by a different route. It is likely that, as
for the metabolism of other steroids, excretion into the
bile is balanced by re-absorption in the intestine and some
part is excreted with the faeces
Check Digit Verification of cas no
The CAS Registry Mumber 514-36-3 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 5,1 and 4 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 514-36:
(5*5)+(4*1)+(3*4)+(2*3)+(1*6)=53
53 % 10 = 3
So 514-36-3 is a valid CAS Registry Number.
InChI:InChI=1/C23H31FO6/c1-13(25)30-12-19(28)22(29)9-7-16-17-5-4-14-10-15(26)6-8-20(14,2)23(17,24)18(27)11-21(16,22)3/h10,16-18,27,29H,4-9,11-12H2,1-3H3/t16-,17-,18-,20-,21-,22-,23-/m0/s1
514-36-3Relevant articles and documents
-
Hirschmann et al.
, p. 4956,4959 (1956)
-
Process and intermediates for the preparation of 17 alphahydroxyprogesterones and corticoids from an enol steroid
-
, (2008/06/13)
This invention discloses an improved process for the production of corticoids from 17α-hydroxy steroids utilizing peroxymonosulfate.