フルニソリド
- 同
- Aerobid, Nasalide, Nasarel
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/09/05 00:49:41」(JST)
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Flunisolide
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Systematic (IUPAC) name |
(1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
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Clinical data |
Trade names |
Aerobid |
AHFS/Drugs.com |
Monograph |
MedlinePlus |
a681048 |
Routes of
administration |
Inhaled |
Pharmacokinetic data |
Protein binding |
40% after oral inhalation |
Biological half-life |
1.8 hours |
Identifiers |
CAS Number |
3385-03-3 Y |
ATC code |
R01AD04 (WHO) R03BA03 (WHO) |
PubChem |
CID 82153 |
IUPHAR/BPS |
7076 |
DrugBank |
DB00180 Y |
ChemSpider |
74144 Y |
UNII |
78M02AA8KF Y |
KEGG |
D00324 N |
ChEBI |
CHEBI:5106 Y |
ChEMBL |
CHEMBL1512 Y |
Synonyms |
6α-Fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene-3,20-dione acetone cyclic 16,17-acetal |
Chemical data |
Formula |
C24H31FO6 |
Molar mass |
434.498 g/mol |
SMILES
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O=C\1\C=C/[C@]2(/C(=C/1)[C@@H](F)C[C@H]3[C@H]4[C@](C[C@H](O)[C@H]23)([C@@]5(OC(O[C@@H]5C4)(C)C)C(=O)CO)C)C
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InChI
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InChI=1S/C24H31FO6/c1-21(2)30-19-9-14-13-8-16(25)15-7-12(27)5-6-22(15,3)20(13)17(28)10-23(14,4)24(19,31-21)18(29)11-26/h5-7,13-14,16-17,19-20,26,28H,8-11H2,1-4H3/t13-,14-,16-,17-,19+,20+,22-,23-,24+/m0/s1 Y
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Key:XSFJVAJPIHIPKU-XWCQMRHXSA-N Y
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NY (what is this?) (verify) |
Flunisolide (marketed as AeroBid, Nasalide, Nasarel) is a corticosteroid often prescribed as treatment for allergic rhinitis.[1] Intranasal corticosteroids are the most effective medication for controlling symptoms. [2] In the United Kingdom it was formerly marketed as Syntaris, but this was recently discontinued by the manufacturers.[3]
The principal mechanism of action of flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action. The effects of topical corticosteroids is not immediate and requires regular use and at least a few days to start experiencing noticeable symptom relief. As-needed use has been shown to be not as effective as regular recommended use. [4] Flunisolide should not be used in the presence of nasal infection. It should not be continued if there is no relief of symptoms after regular use over two to three weeks. [5]
Side effects
Temporary nose and throat dryness, irritation, bleeding or unpleasant taste or smell may occur.[6] Nasal septum perforation is rarely reported. [7] Rare, but localized infections of the nose and pharynx with Candida albicans have been reported and long-term use may raise the chance of cataracts or glaucoma.[8]
Flunisolide nasal spray is absorbed into the circulatory system (blood).[9] Corticosteroid nasal sprays may affect the hypothalamic-pituitary-adrenal axis function in humans.[10] After the desired clinical effect is obtained, the maintenance dose should be reduced to the smallest amount necessary to control symptoms, which can be as low as 1 spray in each nostril a day. Utilizing the minimum effective dose will reduce possibility of side effects.[11]Recommended amounts of intranasal corticosteroids are generally not associated with systemic side effects.
Corticosteroids inhibit wound healing. Therefore, use of corticosteroid nasal sprays in patients who have experienced recent nasal septal ulcers, recurrent epistaxis, nasal surgery or trauma, a nasal corticosteroid should be used with caution until healing has occurred.[12] In pregnancy, recommended doses of intranasal corticosteroids are safe and effective.[13]
References
- ^ See http://www.drugbank.ca/drugs/DB00180
- ^ "The diagnosis and management of rhinitis: an updated practice parameter". Allergy and Clinical Immunology. 122: S1–84. Aug 2008. doi:10.1016/j.jaci.2008.06.003. PMID 18662584.
- ^ See http://www.pharphar.com/v/Syntaris
- ^ "The diagnosis and management of rhinitis: an updated practice parameter". Allergy and Clinical Immunology. 122: S1–84. Aug 2008. doi:10.1016/j.jaci.2008.06.003. PMID 18662584.
- ^ http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8ba9cc1c-55e5-40ed-9efe-f7abb73976ea
- ^ http://www.medicinenet.com/flunisolide-nasal/page2.htm
- ^ "The diagnosis and management of rhinitis: an updated practice parameter". Allergy and Clinical Immunology. 122: S1–84. Aug 2008. doi:10.1016/j.jaci.2008.06.003. PMID 18662584.
- ^ http://www-uptodate-com.ucsf.idm.oclc.org/contents/flunisolide-nasal-patient-drug-information?source=search_result&search=flunisolide&selectedTitle=3~14
- ^ http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8ba9cc1c-55e5-40ed-9efe-f7abb73976ea
- ^ http://www.rxlist.com/nasalide-drug/clinical-pharmacology.htm
- ^ http://www.rxlist.com/nasalide-drug/clinical-pharmacology.htm
- ^ http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8ba9cc1c-55e5-40ed-9efe-f7abb73976ea
- ^ "The diagnosis and management of rhinitis: an updated practice parameter". Allergy and Clinical Immunology. 122: S1–84. Aug 2008. doi:10.1016/j.jaci.2008.06.003. PMID 18662584.
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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Decongestants and other nasal preparations (R01)
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Topical |
Sympathomimetics, plain
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- Cyclopentamine
- Ephedrine
- Epinephrine
- Fenoxazoline
- Levomethamphetamine
- Metizoline
- Naphazoline
- Oxymetazoline
- Phenylephrine
- Propylhexedrine
- Tetryzoline
- Tramazoline
- Tuaminoheptane
- Tymazoline
- Xylometazoline
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Antiallergic agents,
excluding corticosteroids
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- histamine antagonists (Levocabastine
- Antazoline
- Thonzylamine)
- mast cell stabilizer (some are also antihistamines) (Cromoglicic acid
- Nedocromil
- Azelastine
- Olopatadine
- Lodoxamide)
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Corticosteroids
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- Beclometasone dipropionate
- Betamethasone
- Budesonide
- Ciclesonide
- Dexamethasone
- Flunisolide
- Fluticasone
- Mometasone furoate
- Prednisolone
- Tixocortol
- Triamcinolone
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Other nasal preparations
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- Cafaminol
- Calcium hexamine thiocyanate
- Eucalyptus oil
- Framycetin
- Hexamidine
- Hyaluronan
- Ipratropium bromide
- Mupirocin
- Retinol
- Ritiometan
- Saline water
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Systemic use:
Sympathomimetics |
- Phenylephrine
- Phenylpropanolamine
- Phenylpropylamine
- Pseudoephedrine (+loratadine)
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Drugs for obstructive airway diseases: asthma/COPD (R03)
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Adrenergics, inhalants |
Short-acting β2 agonists |
- Bitolterol
- Carbuterol
- Fenoterol
- Isoetarine
- Pirbuterol
- Procaterol
- Reproterol
- Rimiterol
- Salbutamol (albuterol)#/Levosalbutamol (levalbuterol)
- Terbutaline
- Tulobuterol
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Long-acting β2 agonists |
- Bambuterol
- Clenbuterol
- Formoterol/Arformoterol
- Salmeterol
- Salmefamol
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Ultra-long-acting β2 agonists |
- Abediterol
- Carmoterol
- Indacaterol
- Olodaterol
- Vilanterol
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Other |
- Epinephrine#
- Hexoprenaline
- Isoprenaline (isoproterenol)
- Orciprenaline (metaproterenol)
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Glucocorticoids |
- Beclometasone#
- Betamethasone
- Budesonide
- Ciclesonide
- Flunisolide
- Fluticasone
- Mometasone
- Triamcinolone
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Anticholinergics/
muscarinic antagonist |
- Aclidinium bromide
- Glycopyrronium bromide
- Ipratropium bromide#
- Oxitropium bromide
- Tiotropium bromide
- Umeclidinium bromide
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Mast cell stabilizers |
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Xanthines |
- Acefylline
- Ambuphylline
- Bamifylline
- Doxofylline
- Enprofylline
- Etamiphylline
- Proxyphylline
- Theophylline/Aminophylline/Choline theophyllinate
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Eicosanoid inhibition |
Leukotriene antagonists |
- Montelukast
- Pranlukast
- Zafirlukast
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Arachidonate 5-lipoxygenase inhibitors |
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Thromboxane receptor antagonists |
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Non-xanthine PDE4 inhibitors |
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Others/unknown |
- Amlexanox
- Eprozinol
- Fenspiride
- Omalizumab
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Combination products |
- Aclidinium/formoterol
- Beclometasone/formoterol
- Budesonide/formoterol
- Fluticasone furoate/vilanterol
- Fluticasone propionate/salmeterol
- Indacaterol/glycopyrronium bromide
- Ipratropium bromide/salbutamol
- Mometasone/formoterol
- Umeclidinium bromide/vilanterol
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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
- Telapristone
- Tibolone
- Toripristone
- Ulipristal acetate
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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
- Late (≥ 7 days) inhalation corticosteroids to reduce bronchopulmonary dysplasia in preterm infants.
- Onland W1, Offringa M, van Kaam A.
- The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2017 Aug 24;8:CD002311. doi: 10.1002/14651858.CD002311.pub4.
- PMID 28836266
- Dilemmas, Confusion, and Misconceptions Related to Small Airways Directed Therapy.
- Lavorini F1, Pedersen S2, Usmani OS3; Aerosol Drug Management Improvement Team (ADMIT).
- Chest.Chest.2017 Jun;151(6):1345-1355. doi: 10.1016/j.chest.2016.07.035. Epub 2016 Aug 11.
- PMID 27522955
- Inhaled corticosteroids: Effects on growth and bone health.
- Skoner DP1.
- Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology.Ann Allergy Asthma Immunol.2016 Dec;117(6):595-600. doi: 10.1016/j.anai.2016.07.043.
- PMID 27979015
Japanese Journal
- Degradation of Corticosteroids during Activated Sludge Processing
- Evidence of remodeling in peripheral airways of patients with mild to moderate asthma : Effect of hydrofluoroalkane-flunisolide
Related Links
- Flunisolide nasal spray may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: headache nasal irritation, burning, stuffiness, or dryness sore throat sneezing severe or frequent nosebleeds
- Flunisolide official prescribing information for healthcare professionals. Includes: indications, dosage, adverse reactions, pharmacology and more. ... Indications and Usage for Flunisolide Flunisolide Nasal Solution is indicated for the ...
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