Tìm theo
Clobetasol propionate
Các tên gọi khác (3) :
  • 21-chloro-9-fluoro-11β,17-dihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17-propionate
  • clobetasol 17-propanoate
  • clobetasol 17-propionate
Thuốc điều trị bệnh da liễu
Thuốc Gốc
Small Molecule
CAS: 25122-46-7
ATC: D07AD01
ĐG : Accra Pac Inc.
CTHH: C25H32ClFO5
PTK: 466.97
A derivative of prednisolone with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than fluocinonide, it is used topically in treatment of psoriasis but may cause marked adrenocortical suppression. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H32ClFO5
Phân tử khối
466.97
Monoisotopic mass
466.192230046
InChI
InChI=1/C25H32ClFO5/c1-5-21(31)32-25(20(30)13-26)14(2)10-18-17-7-6-15-11-16(28)8-9-22(15,3)24(17,27)19(29)12-23(18,25)4/h8-9,11,14,17-19,29H,5-7,10,12-13H2,1-4H3/t14-,17-,18-,19-,22-,23-,24-,25-/s2
InChI Key
InChIKey=CBGUOGMQLZIXBE-KBUOYLHWNA-N
IUPAC Name
(1R,2S,10S,11S,13S,14R,15S,17S)-14-(2-chloroacetyl)-1-fluoro-17-hydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-3,6-dien-14-yl propanoate
Traditional IUPAC Name
temovate
SMILES
[H][C@@]12C[C@H](C)[C@](OC(=O)CC)(C(=O)CCl)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Độ tan chảy
226
Độ hòa tan
3.86 mg/L
logP
3.50
logS
-5
pKa (strongest acidic)
13.63
pKa (Strongest Basic)
-3.4
PSA
80.67 Å2
Refractivity
119.32 m3·mol-1
Polarizability
48.28 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Like other topical corticosteroids, clobetasol has anti-inflammatory, antipruritic, and vasoconstrictive properties. It is a very high potency 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 derivative of prednisolone with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than fluocinonide, it is used topically in treatment of psoriasis but may cause marked adrenocortical suppression. [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. 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. Initially, however, clobetasol, like other corticosteroids, bind to the glucocorticoid receptor, which complexes, enteres the cell nucleus and modifies genetic transcription (transrepression/transactivation).
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.
▧ Metabolism :
Metabolized, primarily in the liver, and then excreted by the kidneys.
▧ Route of Elimination :
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids, including clobetasol propionate and its metabolites, are also excreted into the bile.
Độc Tính : Oral LD50 in rat and mouse is >3000 mg/kg. Topically applied clobetasol 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 short-term topical treatment of the inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp.
Tương Tác Thuốc :
  • Aldesleukin Corticosteroids such as clobetasol may diminish the antineoplastic effect of aldesleukin. Avoid conccurent use of corticosteroids with aldesleukin.
  • Telaprevir Corticosteroids such as clobetasol may decrease the serum concentration of telaprevir. Telaprevir may increase the serum concentration of corticosteroids. Concurrent use of telaprevir and systemic corticosteroids is not recommended. When possible, consider alternatives, and if such a combination is necessary, use extra caution, monitoring patients for excessive systemic steroid effects as well as for diminished telaprevir effects.
Liều Lượng & Cách Dùng : Cream - Topical
Liquid - Topical
Lotion - Topical
Ointment - Topical
Shampoo - Topical
Solution - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Clobesol
  • Công ty : Galderma
    Sản phẩm biệt dược : Clobex
  • Công ty : Hi-Tech
    Sản phẩm biệt dược : Cormax
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Dermovate
  • Công ty : Hi-Tech
    Sản phẩm biệt dược : Embeline
  • Công ty : Hi-Tech
    Sản phẩm biệt dược : Embeline E
  • Công ty : Mipharm
    Sản phẩm biệt dược : Olux
  • Công ty :
    Sản phẩm biệt dược : OLUX-E
  • Công ty : Fougera
    Sản phẩm biệt dược : Temovate
  • Công ty : Fougera
    Sản phẩm biệt dược : Temovate E
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01013
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01272
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0462-0269-50
PharmGKB
http://www.pharmgkb.org/drug/PA164744375
Wikipedia
http://en.wikipedia.org/wiki/Clobetasol_propionate
RxList
http://www.rxlist.com/cgi/generic/olux.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tem1431.shtml
Drugs.com
http://www.drugs.com/cdi/clobetasol-cream.html
... loading
... loading