Fludrocortisone is also a confirmation test for diagnosing Conn's syndrome (aldosterone-producing adrenal adenoma), the fludrocortisone suppression test. Loading the patient with fludrocortisone would suppress serum aldosterone level in a normal patient, whereas the level would remain elevated in a Conn's patient. The fludrocortisone suppression test is an alternative to the NaCl challenge (which would use normal saline or salt tablets).[medical citation needed]
Fludrocortisone is a corticosteroid and acts as a powerful mineralocorticoid, along with some additional but comparatively very weak glucocorticoid activity.[12] Relative to cortisol, it is said to have 10 times the glucocorticoid potency but 250 to 800 times the mineralocorticoid potency.[12][13] Fludrocortisone acetate is a prodrug of fludrocortisone, which is the active form of the drug.[14]
Plasma renin, sodium, and potassium are checked through blood tests to verify that the correct dosage is reached.[medical citation needed]
Fludrocortisone, also known as 9α-fluorocortisol (9α-fluorohydrocortisone) or as 9α-fluoro-11β,17α,21-trihydroxypregn-4-ene-3,20-dione, is a syntheticpregnanesteroid and a halogenatedderivativeofcortisol (11β,17α,21-trihydroxypregn-4-ene-3,20-dione).[1][2] Specifically, it is a modification of cortisol with a fluorine atom substituted in place of one hydrogen atom at the C9α position.[1][2] Fluorine is a good bioisostere for hydrogen because it is similar in size, with the major difference being in its electronegativity. The acetate form of fludrocortisone, fludrocortisone acetate, is the C21 acetateester of fludrocortisone,[1][2] and is hydrolyzed into fludrocortisone in the body.[14]
Fludrocortisone was described in the literature in 1953[15] and was introduced for medical use (as the acetate ester) in 1954.[13][16] It was the first synthetic corticosteroid to be marketed, and followed the introduction of cortisone in 1948 and hydrocortisone (cortisol) in 1951.[15][17] Fludrocortisone was also the first fluorine-containing pharmaceutical drug to be marketed.[18]
Fludrocortisone is the generic name of fludrocortisone and its INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, BANTooltip British Approved Name, DCFTooltip Dénomination Commune Française, and DCITTooltip Denominazione Comune Italiana, whereas fludrocortisone acetate is the generic name of fludrocortisone acetate and its USPTooltip United States Pharmacopeia, BANMTooltip British Approved Name and JANTooltip Japanese Accepted Name.[1][2][19]
Fludrocortisone is marketed mainly under the brand names Astonin and Astonin-H, whereas the more widely used fludrocortisone acetate is sold mainly as Florinef, but also under several other brand names including Cortineff, Florinefe, and Fludrocortison.[2][19]
^World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
^Freitas J, Santos R, Azevedo E, Costa O, Carvalho M, de Freitas AF (October 2000). "Clinical improvement in patients with orthostatic intolerance after treatment with bisoprolol and fludrocortisone". Clinical Autonomic Research. 10 (5): 293–299. doi:10.1007/BF02281112. PMID11198485. S2CID20843222.
^ abDe Groot LJ, Chrousos G, Dungan K, Feingold KR, Grossman A, Hershman JM, et al. (2000). "Glucocorticoid Therapy and Adrenal Suppression". In Feingold KR, Anawalt B, Blackman MR, Boyce A, Chrousos G, Corpas E, et al. (eds.). Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc. PMID25905379.
^Khan MO, Park KK, Lee HJ (2005). "Antedrugs: an approach to safer drugs". Current Medicinal Chemistry. 12 (19): 2227–2239. doi:10.2174/0929867054864840. PMID16178782.
^Walker MC, Chang MC (September 2014). "Natural and engineered biosynthesis of fluorinated natural products". Chemical Society Reviews. 43 (18): 6527–6536. doi:10.1039/c4cs00027g. PMID24776946. S2CID205904152.
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