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a salt or ester of acetic acid (同)ethanoate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/26 16:00:04」(JST)

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Fludrocortisone (also called 9α-fluorocortisol or 9α-fluorohydrocortisone) is a synthetic corticosteroid with moderate glucocorticoid potency and much greater mineralocorticoid potency. Therapeutically, it is used for its mineralocorticoid activity and not for its glucocorticoid activity.

The brand name in the EU, USA, and Canada is Florinef. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.^[1]

Medical uses

Fludrocortisone has been used in the treatment of cerebral salt wasting syndrome.^[2] It is used primarily to replace the missing hormone aldosterone in various forms of adrenal insufficiency such as Addison's disease and the classic salt wasting (21-hydroxylase deficiency) form of congenital adrenal hyperplasia. Due to its effects on increasing Na+ levels, and therefore blood volume, fludrocortisone is the first line of treatment for orthostatic intolerance and postural orthostatic tachycardia syndrome (POTS).^[3] It can be used to treat low blood pressure.

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 will not be altered in a Conns patient.

Side effects

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 (dyspepsia), distention of the abdomen and ulceration (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)

Dosing

Renin plasma, sodium, and potassium is checked through blood tests in order to verify that the correct dosage is reached.

Chemical properties

Chemically, fludrocortisone is identical to cortisol except for the substitution of fluorine in place of one hydrogen. Fluorine is a good bioisostere for hydrogen because it is similar in size. The major difference is in its electronegativity.

References

^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ Taplin CE, Cowell CT, Silink M, Ambler GR (December 2006). "Fludrocortisone therapy in cerebral salt wasting". Pediatrics 118 (6): e1904–8. doi:10.1542/peds.2006-0702. PMID 17101713.
^ Freitas J, Santos R, Azevedo E, Costa O, Carvalho M, Falcão de Freitas A (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.

UpToDate Contents

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1. まれな先天性副腎過形成 uncommon congenital adrenal hyperplasias
2. 起立性低血圧および食後低血圧の治療 treatment of orthostatic and postprandial hypotension
3. 成人における副腎不全の治療 treatment of adrenal insufficiency in adults
4. 低アルドステロン症（4型RTA）の病因、診断、および治療 etiology diagnosis and treatment of hypoaldosteronism type 4 rta
5. 体位性頻脈症候群 postural tachycardia syndrome

English Journal

Influence of drug content, type of semi-solid vehicle and rheological properties on the skin penetration of the model drug fludrocortisone acetate.

Nagelreiter C, Raffeiner S, Geyerhofer C, Klang V, Valenta C.SourceUniversity of Vienna, Department of Pharmaceutical Technology and Biopharmaceutics, Althanstraße 14, 1090 Vienna, Austria.
International journal of pharmaceutics.Int J Pharm.2013 Mar 28. pii: S0378-5173(13)00261-5. doi: 10.1016/j.ijpharm.2013.03.042. [Epub ahead of print]
Throughout Europe, topical creams containing corticosteroids are diluted with various neutral cream bases to meet the specific needs of patients. Even though this practice has been common for years, its effect has not been thoroughly investigated and so the effectiveness of the diluted topical stero
PMID 23541986

Early inhibition of natriuresis suppresses symptomatic cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage.

Nakagawa I, Hironaka Y, Nishimura F, Takeshima Y, Matsuda R, Yamada S, Motoyama Y, Park YS, Nakase H.SourceDepartment of Neurosurgery, Nara Medical University, Kashihara, Japan.
Cerebrovascular diseases (Basel, Switzerland).Cerebrovasc Dis.2013;35(2):131-7. doi: 10.1159/000346586. Epub 2013 Feb 7.
Background: Hyponatremia is a common complication occurring in one third of patients after subarachnoid hemorrhage (SAH). One mechanism that likely mediates the development of hyponatremia in SAH is cerebral salt wasting syndrome (CSWS), which induces natriuresis and reduces total blood volume, resu
PMID 23406891

Human plasma quantification of fludrocortisone using liquid chromatography coupled with atmospheric pressure chemical ionization mass spectrometry after low-dosage administration.

Ribot M, Polito A, Grassin-Delyle S, Annane D, Alvarez JC.SourceLaboratoire de Pharmacologie-Toxicologie, Centre Hospitalier Universitaire Raymond Poincaré, AP-HP, 104 Boulevard R. Poincaré, 92380 Garches et Université Versailles Saint-Quentin, France.
Clinica chimica acta; international journal of clinical chemistry.Clin Chim Acta.2012 Dec 7. pii: S0009-8981(12)00566-9. doi: 10.1016/j.cca.2012.11.026. [Epub ahead of print]
BACKGROUND: Fludrocortisone acetate is given at very low dosage (50μg) to patients suffering from septic shock with controversial clinical results. However, it is not clear if absorption is effective in these patients.METHODS: An analytical method based upon liquid chromatography coupled to triple
PMID 23228845

Japanese Journal

Hypersensitivity to Fludrocortisone Acetate in a Recipient of Bone Marrow Transplantation

Allergology International 60(4), 557-558, 2011
NAID 130004477121

合成ミネラロコルチコイド (特集合成ステロイドホルモン--最新の基礎・臨床研究) -- (各種合成ステロイドの薬理と臨床--種類,作用機序,副作用)

日本臨床 66(1), 125-129, 2008-01
NAID 40015772109

グリセロールキナーゼ欠損症を伴った先天性副腎低形成の1症例

Journal of Nara Medical Association 54(5-6), 305-311, 2003-12-31
NAID 120004972847

Related Pictures

★リンクテーブル★

リンク元	「フルドロコルチゾン」「florinef」
関連記事	「fludrocortisone」

「フルドロコルチゾン」

Fludrocortisone
Systematic (IUPAC) name
	9-fluoro-11,17-dihydroxy-17- (2-hydroxyacetyl)- 10,13-dimethyl- 1,2,6,7,8,9,10,11,12, 13,14,15,16,17- tetradecahydrocyclopenta[a]phenanthren-3-one
Clinical data
AHFS/Drugs.com	Monograph
Pregnancy; category	C;
Routes of; administration	Oral
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Protein binding	High
Metabolism	Hepatic
Biological half-life	3.5 hours
Identifiers
CAS Number	127-31-1
ATC code	H02AA02 (WHO)
PubChem	CID 31378
IUPHAR/BPS	2873
DrugBank	DB00687
ChemSpider	29111
UNII	U0476M545B
KEGG	D07967
ChEBI	CHEBI:50885
ChEMBL	CHEMBL1201388
Chemical data
Formula	C21H29FO5
Molar mass	380.45 g/mol
	SMILES O=C(CO)[C@]3(O)[C@]2(C[C@H](O)[C@]4(F)[C@@]1(/C(=C\C(=O)CC1)CC[C@H]4[C@@H]2CC3)C)C ;
	InChI 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 ; Key:AAXVEMMRQDVLJB-BULBTXNYSA-N ;
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