florinef

同

fludrocortisone acetate

PrepTutorEJDIC

1. (1971年まで用いられた)英国のフロリン銀貨(2シリングに相当)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/04 23:47:14」(JST)

wiki en

[Wiki en表示]

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
Legal status	US: ℞-only
Routes of administration	Oral
Pharmacokinetic data
Protein binding	High
Metabolism	Hepatic
Biological half-life	3.5 hours
Identifiers
CAS Number	127-31-1 Y
ATC code	H02AA02
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
Molecular 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 Y Key:AAXVEMMRQDVLJB-BULBTXNYSA-N Y
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 U.S. 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.

Medical uses

Fludrocortisone has been used in the treatment of cerebral salt wasting syndrome. 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). 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

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 起立性低血圧および食後低血圧の治療 treatment of orthostatic and postprandial hypotension
• 2. 成人における副腎不全の治療 treatment of adrenal insufficiency in adults
• 3. シェーグレン症候群による全身および腺外症状の治療 treatment of systemic and extraglandular manifestations of sjogrens syndrome
• 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

• Hyponatremia in an Elderly Patient due to Isolated Hypoaldosteronism Occurring after Licorice Withdrawal.

• Hataya Y1, Oba A, Yamashita T, Komatsu Y.
• Internal medicine (Tokyo, Japan).Intern Med.2017;56(2):175-179. doi: 10.2169/internalmedicine.56.6438. Epub 2017 Jan 15.
• PMID 28090048

• Aerosolization, Drug Permeation and Cellular Interaction of Dry Powder Pulmonary Formulations of Corticosteroids with Hydroxypropyl-β-Cyclodextrin as a Solubilizer.

• Vartiainen V1, Bimbo LM2, Hirvonen J3, Kauppinen EI4, Raula J5.
• Pharmaceutical research.Pharm Res.2017 Jan;34(1):25-35. doi: 10.1007/s11095-016-2035-9. Epub 2016 Sep 7.
• PMID 27604893

• Corticosteroid Fludrocortisone Acetate Targets Multiple End Points in Zebrafish (Danio rerio) at Low Concentrations.

• Zhao Y1, Zhang K1, Fent K1,2.
• Environmental science & technology.Environ Sci Technol.2016 Sep 20;50(18):10245-54. doi: 10.1021/acs.est.6b03436. Epub 2016 Sep 12.
• PMID 27618422

Japanese Journal

• 塩類喪失型先天性副腎皮質過形成に対する Florinef の効果について

• 岩間 正文 [他]
• 小児科臨床 27(10), 1180-1182, 1974-10
• NAID 40017897307

Related Links

• フロリネフ (Florinef) - ドラッグ・エクスプレス-海外医薬品 ...

フロリネフ(Florinef)、酢酸フルドロコルチゾン錠(Fludrocortisone)、【2缶(200錠)/10480円】を購入するならこちらへ ... ＜注意＞こちらの商品は2 ～8 の貯蔵環境が必要ですが、EMS便は冷蔵便がありませんので、常温便でお届けします。

• 【フロリネフ】犬のアジソン病の薬にフロリネフ｜病院より ...

フロリネフの販売店 >>> 【オオサカ堂（送料無料で安心 ）】 病院では1錠で550円ですが、同じフロリネフを個人輸入で購入すると1錠で41円。病院が高すぎるのか？ネットが安すぎるのか？ これは、「動物病院の薬が保険対象外」だから ...

Related Pictures