Tìm theo
Flunisolide
Các tên gọi khác (3) :
  • Flunisolida
  • Flunisolide anhydrous
  • Flunisolidum
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 3385-03-3
ATC: R01AD04, R03BA03
ĐG : 3M Health Care , http://www.3m.com
CTHH: C24H31FO6
PTK: 434.4977
Flunisolide (marketed as AeroBid, Nasalide, Nasarel) is a corticosteroid often prescribed as treatment for allergic rhinitis. The principle mechanism of action of flunisolide is to activate glucocorticoid receptors. It also has anti-inflammatory action.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H31FO6
Phân tử khối
434.4977
Monoisotopic mass
434.210466929
InChI
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
InChI Key
InChIKey=XSFJVAJPIHIPKU-XWCQMRHXSA-N
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[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one
Traditional IUPAC Name
flunisolide
SMILES
[H][C@@]12C[C@@]3([H])[C@]4([H])C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@@]4([H])[C@@H](O)C[C@]3(C)[C@@]1(OC(C)(C)O2)C(=O)CO
Độ tan chảy
226-230
Độ hòa tan
Practically insoluble
logP
1.1
logS
-4.1
pKa (strongest acidic)
13.73
pKa (Strongest Basic)
-2.9
PSA
93.06 Å2
Refractivity
111.89 m3·mol-1
Polarizability
44.88 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Flunisolide is a synthetic corticosteroid. It is administered either as an oral metered-dose inhaler for the treatment of asthma or as a nasal spray for treating allergic rhinitis. Corticosteroids are naturally occurring hormones that prevent or suppress inflammation and immune responses. When given as an intranasal spray, flunisolide reduces watery nasal discharge (rhinorrhea), nasal congestion, postnasal drip, sneezing, and itching oat the back of the throat that are common allergic symptoms.
Cơ Chế Tác Dụng : Flunisolide (marketed as AeroBid, Nasalide, Nasarel) is a corticosteroid often prescribed as treatment for allergic rhinitis. The principle mechanism of action of flunisolide is to activate glucocorticoid receptors. It also has anti-inflammatory action. Flunisolide is a glucocorticoid receptor agonist. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Flunisolide binds to plasma transcortin, and it becomes active when it is not bound to transcortin.
Dược Động Học :
▧ Absorption :
Absorbed rapidly
▧ Protein binding :
Approximately 40% after oral inhalation
▧ Metabolism :
Primarily hepatic, converted to the S beta-OH metabolite.
▧ Half Life :
1.8 hours
Chỉ Định : For the maintenance treatment of asthma as a prophylactic therapy.
Tương Tác Thuốc :
  • Telithromycin Telithromycin may reduce clearance of Flunisolide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flunisolide if Telithromycin is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of flunisolide by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of flunisolide if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Spray - Nasal
Spray, metered - Nasal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Roche
    Sản phẩm biệt dược : AeroBid
  • Công ty :
    Sản phẩm biệt dược : Aerospan
  • Công ty : Krewel
    Sản phẩm biệt dược : Bronalide
  • Công ty : Teva Santé
    Sản phẩm biệt dược : Nasalide
  • Công ty :
    Sản phẩm biệt dược : Nasarel
  • Công ty : Syntex
    Sản phẩm biệt dược : Rhinalar
  • Công ty : Teva
    Sản phẩm biệt dược : Syntaris
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00180
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=82153
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507894
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00324
ChemSpider
http://www.chemspider.com/Chemical-Structure.74144.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-0672-99
PharmGKB
http://www.pharmgkb.org/drug/PA449661
Wikipedia
http://en.wikipedia.org/wiki/Flunisolide
RxList
http://www.rxlist.com/cgi/generic/flunisolide.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/aer1009.shtml
Drugs.com
http://www.drugs.com/cdi/flunisolide-spray.html
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