Tìm theo
Desoximetasone
Các tên gọi khác (7 ) :
  • (11beta,16alpha)-9-Fluoro-11,21-dihydroxy-16-methylpregna-1,4-diene-3,20-dione
  • 9alpha-Fluoro-16alpha-methyl-delta(1)-corticosterone
  • Desoximetason
  • Desoximetasona
  • Désoximétasone
  • Desoximetasonum
  • Desoxymethasone
Thuốc Gốc
Small Molecule
CAS: 382-67-2
ATC: D07AC03, D07XC02
ĐG : Dispensing Solutions , http://www.drxdispensing.com
CTHH: C22H29FO4
PTK: 376.4617
A topical anti-inflammatory glucocorticoid used in dermatoses, skin allergies, psoriasis, etc. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H29FO4
Phân tử khối
376.4617
Monoisotopic mass
376.204987621
InChI
InChI=1S/C22H29FO4/c1-12-8-16-15-5-4-13-9-14(25)6-7-21(13,3)22(15,23)18(27)10-20(16,2)19(12)17(26)11-24/h6-7,9,12,15-16,18-19,24,27H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,18+,19-,20+,21+,22+/m1/s1
InChI Key
InChIKey=VWVSBHGCDBMOOT-IIEHVVJPSA-N
IUPAC Name
(1R,2S,10S,11S,13R,14S,15S,17S)-1-fluoro-17-hydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
desoximetasone
SMILES
[H][C@@]12C[C@@H](C)[C@H](C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Độ tan chảy
217 °C
Độ hòa tan
42.1 mg/L
logP
2.35
logS
-4.1
pKa (strongest acidic)
13.44
pKa (Strongest Basic)
-3.3
PSA
74.6 Å2
Refractivity
101.17 m3·mol-1
Polarizability
40.09 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Like other topical corticosteroids, desoximetasone has anti-inflammatory, antipruritic, and vasoconstrictive properties. Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Desoximetasone is a potent topical corticosteroid that should not be used with occlusive dressings. It is recommended that treatment should be limited to 2 consecutive weeks and therapy should be discontinued when adequate results have been achieved.
Cơ Chế Tác Dụng : A topical anti-inflammatory glucocorticoid used in dermatoses, skin allergies, psoriasis, etc. [PubChem] The precise mechanism of the antiinflammatory activity of topical steroids in the treatment of steroid-responsive dermatoses, in general, is uncertain. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. This is achieved first by the drug binding to the glucocorticoid receptors which then translocates into the nucleus and binds to DNA causing various activations and repressions of genes. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Dược Động Học :
▧ Absorption :
Topical corticosteroids can be absorbed from intact healthy skin. The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle and the integrity of the epidermal barrier. Occlusion, inflammation and/or other disease processes in the skin may also increase percutaneous absorption.
▧ Protein binding :
Bound to plasma proteins in varying degrees.
▧ Metabolism :
Metabolized, primarily in the liver, and then excreted by the kidneys.
▧ Route of Elimination :
Corticosteroids are bound to plasma proteins in varying degrees, are metabolized primarily in the liver and excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.Pharmacokinetic studies in men with Desoximetasone Cream USP, 0.25% with tagged desoximetasone showed a total of 5.2% ± 2.9% excretion in urine (4.1% ± 2.3%) and feces (1.1% ± 0.6%)
▧ Half Life :
The half-life of the material was 15 ± 2 hours (for urine) and 17 ± 2 hours (for feces) between the third and fifth trial day.
Độc Tính : Topically applied desoximetasone can be absorbed in sufficient amounts to produce systemic effects. Symptoms of overdose include thinning of skin and suppression of adrenal cortex (decreased ability to respond to stress).
Chỉ Định : 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
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00547
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5311067
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506793
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470604.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/51672-1271-1
PharmGKB
http://www.pharmgkb.org/drug/PA164746011
Wikipedia
http://en.wikipedia.org/wiki/Desoximetasone
RxList
http://www.rxlist.com/cgi/generic3/desoximeta.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/top1452.shtml
Drugs.com
http://www.drugs.com/cdi/desoximetasone-cream.html
... loading
... loading