NR3C2 binds fludrocortisone

Stable Identifier
R-HSA-9726509
Type
Reaction [binding]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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Fludrocortisone is a synthetic mineralocorticoid used in conjunction with hydrocortisone to replace missing endogenous corticosteroids in patients with adrenal insufficiency. It is functionally similar to aldosterone, the body's primary endogenous mineralocorticoid, and is structurally analogous to cortisol, differing only by a fluorine atom at the 9-position of the steroid structure and having similar affinity for the mineralocorticoid receptor (NR3C2) as aldosterone (Rupprecht et al. 1993, Oelkers et al. 1994).

Fludrocortisone is indicated as partial replacement therapy for primary or secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing androgenital syndrome (Charmandari et al. 2014, Hamitouche et al. 2017). Fludrocortisone has also shown to be effective in the treatment of cerebral salt-wasting syndrome (Taplin et al. 2006, Misra et al. 2018). Common side effects of fludrocortisone include high blood pressure, swelling, heart failure, and low blood potassium.
Literature References
PubMed ID Title Journal Year
8282004 Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands

Berning, B, van Steensel, B, Damm, K, Söder, M, Holsboer, F, Reul, JM, Spengler, D, Rupprecht, R

Eur. J. Pharmacol. 1993
8157723 Impaired renal 11 beta-oxidation of 9 alpha-fluorocortisol: an explanation for its mineralocorticoid potency

Diederich, S, Buchen, S, Muhme, S, Krain, J, Schöneshöfer, M, Oelkers, W

J Clin Endocrinol Metab 1994
28083797 Population Pharmacokinetic-Pharmacodynamic Model of Oral Fludrocortisone and Intravenous Hydrocortisone in Healthy Volunteers

Alvarez, JC, Comets, E, Laviolle, B, Ribot, M, Bellissant, E, Hamitouche, N

AAPS J 2017
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