Fludrocortisone
Clinical data | |
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Trade names | Astonin, Astonin-H, others |
Other names | StC-1400; 9α-Fluorohydrocortisone; 9α-Fluorocortisol; 9α-Fluoro-17α-hydroxycorticosterone; 9α-Fluoro-11β,17α,21-trihydroxypregn-4-ene-3,20-dione |
AHFS/Drugs.com | Monograph |
Pregnancy category |
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Routes of administration | By mouth |
Drug class | Corticosteroid; glucocorticoid; mineralocorticoid |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Protein binding | High |
Metabolism | Liver |
Elimination half-life | 3.5 hours |
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Clinical data | |
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Trade names | Cortineff, Florinef, Florinefe, Fludrocortison, others |
Other names | Fluorohydrocortisone acetate; 9α-Fluorohydrocortisone 21-acetate; 9α-Fluoro-17α-hydroxycorticosterone 21-acetate; 9α-Fluoro-11β,17α,21-trihydroxypregn-4-ene-3,20-dione 21-acetate |
Routes of administration | By mouth |
Drug class | Corticosteroid; glucocorticoid; mineralocorticoid |
Pharmacokinetic data | |
Metabolism | Liver |
Identifiers | |
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JSmol) | |
Melting point | 260 to 262 °C (500 to 504 °F) (dec.) |
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Fludrocortisone, sold under the brand name Florinef, among others, is a
Common side effects of fludrocortisone include
Fludrocortisone was patented in 1953.[6] It is on the World Health Organization's List of Essential Medicines.[7]
Medical uses
Fludrocortisone has been used in the treatment of
Fludrocortisone is also a confirmation test for diagnosing
Side effects
Use of Fludrocortisone can lead to one or more of the following side effects:[11]
- Sodium and water retention
- Swelling due to fluid retention (edema)
- High blood pressure (hypertension)
- Headache
- Low blood potassium level (hypokalemia)
- Muscle weakness
- Fatigue
- Increased susceptibility to infection
- Impaired wound healing
- Increased sweating
- Increased hair growth (hirsutism)
- Thinning of skin and stretch marks
- Disturbances of the gut such as indigestion (peptic ulcer)
- Decreased bone density and increased risk of fractures of the bones
- Difficulty in sleeping (insomnia)
- Depression
- Weight gain
- Raised blood sugar level
- Changes to the menstrual cycle
- Partial loss of vision due to opacity in the lens of the eye (cataracts)
- Raised pressure in the eye (glaucoma)
- Increased pressure in the skull (intracranial pressure)
Pharmacology
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]
Chemistry
Fludrocortisone, also known as 9α-fluorocortisol (9α-fluorohydrocortisone) or as 9α-fluoro-11β,17α,21-trihydroxypregn-4-ene-3,20-dione, is a
History
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]
Society and culture
Generic name
Fludrocortisone is the
Brand names
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]
Availability
Fludrocortisone is marketed in Austria, Croatia, Denmark, Germany, Luxembourg, Romania, and Spain, whereas fludrocortisone acetate is more widely available throughout the world and is marketed in the United States, Canada, the United Kingdom, various other European countries, Australia, Japan, China, Brazil, and many other countries.[2][19]
References
- ^ ISBN 978-1-4757-2085-3. Archivedfrom the original on 5 November 2017.
- ^ ISBN 978-3-88763-075-1. Archivedfrom the original on 2017-11-05.
- ^ a b c d e f "Fludrocortisone Acetate". The American Society of Health-System Pharmacists. Archived from the original on 5 July 2017. Retrieved 8 December 2016.
- ISBN 978-3-7643-7726-7. Archivedfrom the original on 5 November 2017.
- ^ "Fludrocortisone Use During Pregnancy | Drugs.com". www.drugs.com. Archived from the original on 24 December 2016. Retrieved 24 December 2016.
- ISBN 9783527607495. Archivedfrom the original on 2017-11-05.
- hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- S2CID 28871495.
- S2CID 20843222.
- PMID 34000076.
- ^ "Fludrocortisone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD". www.webmd.com. Retrieved 2023-09-05.
- ^ PMID 25905379.
- ^ ISBN 978-0-7817-6879-5. Archivedfrom the original on 2017-11-05.
- ^ PMID 27416887.
- ^ PMID 13875857.
- ISBN 978-0-8155-1856-3. Archivedfrom the original on 5 November 2017.
- PMID 16178782.
- S2CID 205904152.
- ^ a b c "Fludrocortisone Uses, Side Effects & Warnings". Archived from the original on 2015-05-13. Retrieved 2017-07-16.
External links
- "Fludrocortisone". Drug Information Portal. U.S. National Library of Medicine.