フルメタゾン
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- flumetasone、flumetasone pivalate
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/02/25 17:37:03」(JST)
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Flumetasone
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Systematic (IUPAC) name |
(1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.02,7.011,15]heptadeca-3,6-dien-5-one
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Clinical data |
AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
Routes of
administration |
Topical |
Pharmacokinetic data |
Metabolism |
Hepatic, CYP3A4-mediated |
Identifiers |
CAS Number |
2135-17-3 Y |
ATC code |
D07AB03 , D07XB01 (combinations), QH02AB90 |
PubChem |
CID 16490 |
UNII |
LR3CD8SX89 N |
KEGG |
D04208 Y |
ChEMBL |
CHEMBL1201392 N |
Synonyms |
Flumethasone |
Chemical data |
Formula |
C22H28F2O5 |
Molar mass |
410.452 g/mol |
NY (what is this?) (verify) |
Flumetasone (INN; or flumethasone) is a corticosteroid for topical use. Trade names include Locacorten, Locorten, and Orsalin. It is available in combination with clioquinol, under the trade name Locacorten-Vioform (in some countries Locorten-Vioform), for the treatment of otitis externa and otomycosis. It is usually formulated as the pivalic acid ester prodrug flumetasone pivalate.
Flumethasone is 420 times as potent as cortisone in an animal model for anti-inflammatory activity.[citation needed]
See also
- Glucocorticoid
- Corticosteroid
- Triamcinolone acetonide
References
Glucocorticoids and antiglucocorticoids (H02)
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Glucocorticoids |
Pregnene |
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Pregnenedione |
- Hydrocortisone (cortisol)# (Hydrocortisone aceponate
- Hydrocortisone buteprate
- Hydrocortisone butyrate)
- Budesonide
- Ciclesonide
- Deflazacort
- Medrysone
- Tixocortol
- Halogenated at 6: Cloprednol
- Halogenated, with FG at 16: Halcinonide
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Pregnadiene |
- Rimexolone
- Halogenated, with FG at 16: Flunisolide
- Triamcinolone
- Amcinonide
- Fluocinolone acetonide (Fluocinonide)
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Pregnadienediol |
- Prednisone (Meprednisone)
- Halogenated at 9: Fluorometholone
- Halogenated, with FG at 16: Fluocortolone (Clocortolone
- Diflucortolone
- Fluocortin)
- Desoximetasone
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Pregnadienetriol |
- Prednisolone# (Methylprednisolone
- Methylprednisolone aceponate
- Prednicarbate
- Prednylidene)
- Desonide
- Halogenated: Fluprednisolone (Difluprednate
- Fluperolone)
- Halogenated, with FG at 16: Dexamethasone#
- Betamethasone (Clobetasol
- Clobetasone
- Diflorasone
- Halometasone
- Ulobetasol)
- Beclometasone
- Paramethasone
- Alclometasone
- Fluclorolone acetonide
- Flumetasone
- Fluprednidene
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Pregnatriene |
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Androstene |
- Halogenated, with FG at 16: Fluticasone (Fluticasone propionate
- Fluticasone furoate)
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Others/unsorted |
- Halogenated: Loteprednol
- Halogenated, with FG at 16: Fludroxycortide
- Formocortal
- Mometasone furoate
- Promestriene
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Antiglucocorticoids |
- SGRMs: Dagrocorat§
- Fosdagrocorat§
- Mapracorat†
- Antagonists: Ketoconazole
- Mifepristone
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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 signaling
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Receptor
(ligands) |
GR
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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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Enzyme |
Modulators
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- See here instead (modulators of 20,22-desmolase, 17α-hydroxylase/17,20-lyase, 3β-HSD, 11β-HSD, 21-hydroxylase, 11β-hydroxylase, and 18-hydroxylase).
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Others |
Precursors
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- Cholesterol
- 22R-Hydroxycholesterol
- 20α,22R-Dihydroxycholesterol
- Pregnenolone
- Pregnenolone sulfate
- 17-Hydroxypregnenolone
- Progesterone
- 17-Hydroxyprogesterone
- 11-Deoxycorticosterone
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Indirect
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- ACTH (corticotropin)
- CRH
- DHEA
- DHEA sulfate
- Plasma proteins (albumin, transcortin)
- Vasopressin
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See also: Androgenics • Estrogenics • Mineralocorticoids • Progestogenics
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English Journal
- Synthesis and structure-activity relationships of novel cationic lipids with anti-inflammatory and antimicrobial activities.
- Myint M1, Bucki R2, Janmey PA3, Diamond SL4.
- Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2015 Jul 15;25(14):2837-43. doi: 10.1016/j.bmcl.2015.04.104. Epub 2015 May 11.
- Certain membrane-active cationic steroids are known to also possess both anti-inflammatory and antimicrobial properties. This combined functionality is particularly relevant for potential therapies of infections associated with elevated tissue damage, for example, cystic fibrosis airway disease, a c
- PMID 26004577
- Novel spectrophotometric determination of flumethasone pivalate and clioquinol in their binary mixture and pharmaceutical formulation.
- Abdel-Aleem EA1, Hegazy MA2, Sayed NW1, Abdelkawy M2, Abdelfatah RM3.
- Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2015 Feb 5;136 Pt B:707-13. doi: 10.1016/j.saa.2014.09.085. Epub 2014 Sep 30.
- This work is concerned with development and validation of three simple, specific, accurate and precise spectrophotometric methods for determination of flumethasone pivalate (FP) and clioquinol (CL) in their binary mixture and ear drops. Method A is a ratio subtraction spectrophotometric one (RSM). M
- PMID 25448970
- Effect-based detection of synthetic glucocorticoids in bovine urine.
- Pitardi D1, Cini B, Paleologo M, Brouwer A, Behnisch P, van der Linden S, Vincenti M, Capra P, Gili M, Pezzolato M, Meloni D, Bozzetta E.
- Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.Food Addit Contam Part A Chem Anal Control Expo Risk Assess.2015;32(2):194-204. doi: 10.1080/19440049.2014.996788. Epub 2015 Jan 8.
- Challenges to testing for the illicit use of anabolic substances in meat-producing animals stem from the production of new synthetic compounds and the administration of low-dose cocktails to circumvent detection by the surveillance schemes of European Union member states. This work evaluated for the
- PMID 25569131
Japanese Journal
- Determination of flumethasone in calf urine and serum by liquid chromatography-tandem mass spectrometry
- BRAMBILLA G.,BUIARELLI F.,CARTONI G. P.,COCCIOLI F.,COLAMONICI C.,FAGIOLO A.,GIANNINI C.,NERI B.
- Journal of chromatography. B, Biomedical sciences and applications 755(1), 265-278, 2001-05-05
- NAID 10012245142
- Quantitative determination of several synthetic corticosteroids by gas chromatography-mass spectrometry after purification by immunoaffinity chromatography
- DELAHAUT Ph.,JACQUEMIN P.,COLEMONTS Y.,DUBOIS M.,DE GRAEVE J.,DELUYKER H.
- Journal of chromatography. B, Biomedical sciences and applications 696(2), 203-215, 1997-08-29
- NAID 10024519107
- 副腎皮質ホルモン外用剤の皮膚におよぼす影響:—とくに皮膚萎縮とDNA合成抑制との関連について—
- 野本 正志
- 西日本皮膚科 43(5), 797-803, 1981
- コルチコステロイドの皮膚萎縮作用とDNA合成抑制作用の関連についてラットおよび培養ラット皮膚線維芽細胞を用いて検討した。その結果,flmethasons pivarate,triamcinolone acetonide,clobectasal propionsteでは皮膚萎縮作用もDNA合成抑制作用も強く,hydrocortisone butyrate,betamethasone valerate …
- NAID 130004472751
Related Links
- Sigma-Aldrich offers Sigma-F9507, Flumethasone for your research needs. Find product specific information including CAS, MSDS, protocols and references. ... Packaging Bottomless glass bottle. Contents are inside inserted fused ...
- Identification Name Flumethasone Pivalate Accession Number DB00663 (APRD00975) Type Small Molecule Groups Approved Description Flumethasone pivalate is a moderately potent difluorinated corticosteroid ester with anti ...
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フルメタゾン
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- flumetasone pivalate、flumethasone