Tìm theo
Fluocinonide
Các tên gọi khác (5 ) :
  • Fluocinonide
  • Fluocinonido
  • Fluocinonidum
  • Lidex
  • Vanos
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 356-12-7
ATC: C05AA11, D07AC08
ĐG : Actavis Group , http://www.actavis.com
CTHH: C26H32F2O7
PTK: 494.5249
A topical glucocorticoid used in the treatment of eczema. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H32F2O7
Phân tử khối
494.5249
Monoisotopic mass
494.211609788
InChI
InChI=1S/C26H32F2O7/c1-13(29)33-12-20(32)26-21(34-22(2,3)35-26)10-15-16-9-18(27)17-8-14(30)6-7-23(17,4)25(16,28)19(31)11-24(15,26)5/h6-8,15-16,18-19,21,31H,9-12H2,1-5H3/t15-,16-,18-,19-,21+,23-,24-,25-,26+/m0/s1
InChI Key
InChIKey=WJOHZNCJWYWUJD-IUGZLZTKSA-N
IUPAC Name
2-[(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-6,6,9,13-tetramethyl-16-oxo-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-8-yl]-2-oxoethyl acetate
Traditional IUPAC Name
fluocinonide
SMILES
[H][C@@]12C[C@@]3([H])[C@]4([H])C[C@]([H])(F)C5=CC(=O)C=C[C@]5(C)[C@@]4(F)[C@@H](O)C[C@]3(C)[C@@]1(OC(C)(C)O2)C(=O)COC(C)=O
Độ tan chảy
309 °C
Độ hòa tan
4.74 mg/L
logP
3.19
logS
-4.5
pKa (strongest acidic)
13.55
pKa (Strongest Basic)
-3.4
PSA
99.13 Å2
Refractivity
120.56 m3·mol-1
Polarizability
49.12 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
5
Bioavailability
1
Rule of Five
true
Dược Lực Học : Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. It relieves itching, redness, dryness, crusting, scaling, inflammation, and discomfort. [Wikipedia]
Cơ Chế Tác Dụng : A topical glucocorticoid used in the treatment of eczema. [PubChem] Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. It relieves itching, redness, dryness, crusting, scaling, inflammation, and discomfort. Fluocinonide binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. Cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In another words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally 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. Like other glucocorticoid agents Fluocinolone acetonide acts as a physiological antagonist to insulin by decreasing glycogenesis (formation of glycogen). It also promotes the breakdown of lipids (lipolysis), and proteins, leading to the mobilization of extrahepatic amino acids and ketone bodies. This leads to increased circulating glucose concentrations (in the blood). There is also decreased glycogen formation in the liver.
Dược Động Học :
▧ Absorption :
The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings. In general, percutaneous absorption is minimal.
▧ Route of Elimination :
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
Độc Tính : Side effects may include acne-like eruptions, burning, dryness, excessive hair growth, infection of the skin, irritation, itching, lack of skin color, prickly heat, skin inflammation, skin loss or softening, stretch marks
Chỉ Định : A topical anti-inflammatory product for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Liều Lượng & Cách Dùng : Cream - Topical
Gel - Topical
Ointment - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Fluonex
  • Công ty : Medicis
    Sản phẩm biệt dược : Lidex
  • Công ty : Medicis
    Sản phẩm biệt dược : Lidex-E
  • Công ty :
    Sản phẩm biệt dược : Lonide
  • Công ty : Taro
    Sản phẩm biệt dược : Lyderm
  • Công ty : Bioglan
    Sản phẩm biệt dược : Metosyn
  • Công ty :
    Sản phẩm biệt dược : Topsymin
  • Công ty : Syntex
    Sản phẩm biệt dược : Topsyn
  • Công ty : Medicis
    Sản phẩm biệt dược : Vanos
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01047
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9642
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504523
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00325
ChemSpider
http://www.chemspider.com/Chemical-Structure.9265.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0168-0139-15
PharmGKB
http://www.pharmgkb.org/drug/PA449664
Wikipedia
http://en.wikipedia.org/wiki/Fluocinonide
RxList
http://www.rxlist.com/cgi/generic2/fluocin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/lid1227.shtml
Drugs.com
http://www.drugs.com/cdi/fluocinonide-cream.html
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