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- 関
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- Florinef
WordNet
- a salt or ester of acetic acid (同)ethanoate
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- 酢酸(さくさん)塩;アセテート(酢酸人造絹糸)
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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
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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
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Clinical data |
AHFS/Drugs.com |
Monograph |
Pregnancy
category |
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Routes of
administration |
Oral |
Legal status |
Legal status |
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Pharmacokinetic data |
Protein binding |
High |
Metabolism |
Hepatic |
Biological half-life |
3.5 hours |
Identifiers |
CAS Number |
127-31-1 Y |
ATC code |
H02AA02 (WHO) |
PubChem |
CID 31378 |
IUPHAR/BPS |
2873 |
DrugBank |
DB00687 Y |
ChemSpider |
29111 Y |
UNII |
U0476M545B Y |
KEGG |
D07967 Y |
ChEBI |
CHEBI:50885 Y |
ChEMBL |
CHEMBL1201388 N |
Chemical data |
Formula |
C21H29FO5 |
Molar mass |
380.45 g/mol |
SMILES
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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
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InChI
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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 Y
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Key:AAXVEMMRQDVLJB-BULBTXNYSA-N Y
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NY (what is this?) (verify) |
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]
Contents
- 1 Medical uses
- 2 Side effects
- 3 Dosing
- 4 Chemical properties
- 5 References
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.
Mineralocorticoids and antimineralocorticoids (H02)
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Mineralocorticoids |
- 11-Deoxycorticosterone (desoxycortone)
- 11-Deoxycortisol (cortodoxone)
- Aldosterone
- Corticosterone
- Cortisol (hydrocortisone)
- Desoxycortone acetate
- Desoxycortone enanthate
- Fludrocortisone
- Fludrocortisone acetate
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Antimineralocorticoids |
- Amlodipine
- Benidipine
- Canrenoate potassium (potassium canrenoate)
- Canrenoic acid
- Canrenone
- Drospirenone
- Eplerenone
- Felodipine
- Finerenone
- Gestodene
- Nifedipine
- Nimodipine
- Nitrendipine
- Progesterone
- Spironolactone
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Synthesis modifiers |
- Acetoxolone
- Aminoglutethimide
- Carbenoxolone
- Enoxolone
- Ketoconazole
- Metyrapone
- Mitotane
- Trilostane
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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Glucocorticoid receptor modulators
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GR |
Agonists
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Mixed (SEGRAs)
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- Dagrocorat
- Fosdagrocorat
- Mapracorat
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Antagonists
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- 3α-Hydroxytibolone
- 3β-Hydroxytibolone
- Aglepristone
- Asoprisnil
- C108297
- C113176
- CORT-108297
- Cyproterone acetate
- Guggulsterone
- Ketoconazole
- Lilopristone
- LLY-2707
- Miconazole
- Mifepristone
- Onapristone
- ORG-34116
- ORG-34517 (SCH-900636)
- ORG-34850
- Pregnenolone 16α-carbonitrile
- Spironolactone
- Telapristone
- Tibolone
- Toripristone
- Ulipristal acetate
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Others |
Indirect
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- ACTH (corticotropin)
- CRH
- DHEA
- DHEA sulfate
- Plasma proteins (albumin, transcortin)
- Steroidogenesis modulators
- Vasopressin
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See also: Androgenics • Estrogenics • Mineralocorticoidics • Progestogenics • Steroid hormone metabolism modulators
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UpToDate Contents
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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
- 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)
- 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
Related Links
- Before taking fludrocortisone, tell your doctor and pharmacist if you are allergic to fludrocortisone, aspirin, tartrazine (a yellow dye in some processed foods and drugs), or any other drugs. tell your doctor and pharmacist ...
- Professional guide for Fludrocortisone Acetate. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more. ... Drugs.com provides accurate and independent information on more than ...
Related Pictures
★リンクテーブル★
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- 英
- fludrocortisone
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- 酢酸フルドロコルチゾン fludrocortisone acetate
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- フロリネフ
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- fludrocortisone acetate
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フルドロコルチゾン