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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/08/20 09:54:24」(JST)

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Fluticasone propionate belongs to a class of drugs known as corticosteroids, specifically glucocorticoids, which are hormones that predominantly affect the metabolism of carbohydrate and, to a lesser extent, fat and protein. It is used to treat asthma, allergic rhinitis, nasal polyps, various skin disorders and Crohn’s disease and ulcerative colitis. It is also used to treat eosinophilic esophagitis.

Pharmacology

Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen, estrogen, or mineralocorticoid receptor thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (e.g. mast cell, eosinophil, neutrophil, macrophages, and lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation. Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability.

Medical uses & administration

Asthma

Fluticasone is used by powder or aerosol inhalation for the prophylaxis of asthma. Typical initial doses in the UK range from 100 to 250 micrograms twice daily in mild asthma up to 1 mg twice daily in severe asthma, adjusted according to response. Children over 4 years of age may be given initial doses of 50 to 100 micrograms twice daily, increased to 200 micrograms twice daily if necessary. The drug may also be given via a nebuliser in severe chronic asthma. Usual adult doses are 0.5 to 2 mg twice daily. Children aged 4 to 16 years may be given 1 mg twice daily.

Allergic rhinitis

Nasal spray preparation of Fluticasone propionate is used in the prophylaxis and treatment of allergic rhinitis. The usual dose is 100 micrograms into each nostril once daily, increased if necessary to 100 micrograms into each nostril twice daily. Children over 4 years of age may be given half these doses.

Nasal polyps

Fluticasone propionate nasal drops are used in the treatment of nasal polyps, 200 micrograms should be instilled into each nostril once or twice daily for at least 4 to 6 weeks.

Other

Creams and ointments containing 0.05% and 0.005% Fluticasone propionate, respectively, are available and applied topically in the treatment of various skin disorders. It can be given orally in the treatment of Crohn’s disease and ulcerative colitis. Some benefit was also reported in coeliac disease. The dose is 5 mg four times daily but some consider higher doses necessary.

References

UpToDate Contents

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1. 思春期および成人における間欠型喘息および軽症持続型喘息の治療 treatment of intermittent and mild persistent asthma in adolescents and adults
2. 好酸球性食道炎の治療 treatment of eosinophilic esophagitis
3. 12歳未満の小児における慢性喘息：持続性喘息の治療およびコントロール薬 asthma in children younger than 12 years treatment of persistent asthma with controller medications
4. 吸入ステロイドの主な副作用 major side effects of inhaled glucocorticoids
5. 慢性鼻副鼻腔炎のマネージメント management of chronic rhinosinusitis

English Journal

Preference evaluation and perceived sensory comparison of fluticasone furoate and mometasone furoate intranasal sprays in allergic rhinitis.

Yonezaki M1, Akiyama K2, Karaki M3, Goto R4, Inamoto R5, Samukawa Y4, Kobayashi R6, Kobayashi E7, Hoshikawa H5.
Auris, nasus, larynx.Auris Nasus Larynx.2016 Jun;43(3):292-7. doi: 10.1016/j.anl.2015.09.003. Epub 2015 Oct 21.
OBJECTIVE: Intranasal corticosteroid sprays (INCSs) are commonly used for therapy of allergic rhinitis (AR). Adherence to regular use of INCSs is influenced by patient perception and preferences of products. The study objective was to compare perceived sensory attributes of fluticasone furoate nasal
PMID 26498699

Assessment of lung deposition and analysis of the effect of fluticasone/salmeterol hydrofluoroalkane (HFA) pressurized metered dose inhaler (pMDI) in stable persistent asthma patients using functional respiratory imaging.

De Backer J1, Van Holsbeke C1, Vos W1, Vinchurkar S1, Dorinsky P2, Rebello J3, Mangale M3, Hajian B4, De Backer W4.
Expert review of respiratory medicine.Expert Rev Respir Med.2016 Jun 1:1-7. [Epub ahead of print]
BACKGROUND: Unambiguously for inhaled products, PK measures are best suited for ensuring that the total systemic exposure is equivalent for two products but cannot provide regional information about lung deposition and structural changes. Functional respiratory imaging (FRI) has been demonstrated to
PMID 27227384

Topical steroids in eosinophilic esophagitis: Systematic review and meta-analysis of placebo-controlled randomized clinical trials.

Murali AR1, Gupta A2, Attar BM3, Ravi V4, Koduru P4.
Journal of gastroenterology and hepatology.J Gastroenterol Hepatol.2016 Jun;31(6):1111-9. doi: 10.1111/jgh.13281.
BACKGROUND AND AIMS: Eosinophilic esophagitis (EoE) is a clinicopathologic condition characterized by symptoms of esophageal dysfunction in the presence of eosinophil-predominant inflammation of esophageal mucosa. Topical steroids are recommended as first line pharmacologic therapy in EoE. We aimed
PMID 26699695

Japanese Journal

羊水過多を呈し妊娠29週に無下顎耳頭症の診断に至った1例

超音波医学 42(6), 731-736, 2015
NAID 130005110974

羊水過多を呈し妊娠29週に無下顎耳頭症の診断に至った1例

超音波医学 advpub(0), 2015
NAID 130005103419

サルメテロール/フルチカゾンプロピオン酸エステル配合剤を導入した小児気管支喘息患者の特徴と有用性

日本小児アレルギー学会誌 29(1), 123-131, 2015
NAID 130005074492

「フルチカゾン」

Fluticasone propionate
Systematic (IUPAC) name
	S-(fluoromethyl)-6α,9-difluoro-11β, 17-dihydroxy-16α-methyl-3-oxoandrosta-1, 4-diene-17β-carbothioate, 17-propanoate
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	C (US) C for Intranasal and Inhaled
Legal status	POM (UK) Rx Only (US)
Routes	Intranasal, Inhaled, Topical Cream or Ointment
Pharmacokinetic data
Bioavailability	0.51% (Intranasal)
Protein binding	91%
Metabolism	Intranasal; Hepatic (CYP3A4-mediated)
Half-life	10 hours
Excretion	Renal
Identifiers
CAS number	80474-14-2
ATC code	D07AC17 & D07AC04 (topical)
PubChem	CID 444036
DrugBank	DB00588
ChemSpider	392059
UNII	O2GMZ0LF5W
ChEBI	CHEBI:31441
ChEMBL	CHEMBL1473
Chemical data
Formula	C25H31F3O5S
Mol. mass	500.57 g/mol
	SMILES O=C(SCF)[C@]3(OC(=O)CC)[C@]2(C[C@H](O)[C@]4(F)[C@@]/1(\C(=C/C(=O)\C=C\1)[C@@H](F)C[C@H]4[C@@H]2C[C@H]3C)C)C;
	InChI InChI=1S/C25H31F3O5S/c1-5-20(31)33-25(21(32)34-12-26)13(2)8-15-16-10-18(27)17-9-14(29)6-7-22(17,3)24(16,28)19(30)11-23(15,25)4/h6-7,9,13,15-16,18-19,30H,5,8,10-12H2,1-4H3/t13-,15+,16+,18+,19+,22+,23+,24+,25+/m1/s1 ; Key:WMWTYOKRWGGJOA-CENSZEJFSA-N ;
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英: fluticasone
化: プロピオン酸フルチカゾン fluticasone propionate
商: アドエア、アラミスト、キリガミール、スカイロン、ファビ、フルタイド、フルチカノーズ、フルナーゼ、フロラーズ、ミリカレット、フルナーゼ、Flonase, Flovent
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fluticasone propionate