Tìm theo
Prednicarbate
anti inflammatory agents, corticosteroids, steroids
Thuốc Gốc
Small Molecule
CAS: 73771-04-7
ATC: D07AC18, V01AA07, V01AA03
ĐG : Dermik Labs
CTHH: C27H36O8
PTK: 488.5699
Prednicarbate is a relatively new topical corticosteroid drug. It is similar in potency to hydrocortisone. It is used in the treatment of inflammatory skin diseases, such as atopic dermatitis. It has a favorable benefit-risk ratio, with an inflammatory action similar to that of a medium potency corticosteroid, but with a low potential to cause skin atrophy. The anti-inflammation action of corticosteroids is associated with the inhibition of the interleukin 1-alpha cytokine within keratinocytes. IL-1a is also found in fibroblasts, where it is responsible for proliferation, collagenase induction and IL-6 synthesis, which are related to skin thickness.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H36O8
Phân tử khối
488.5699
Monoisotopic mass
488.241018128
InChI
InChI=1S/C27H36O8/c1-5-22(31)34-15-21(30)27(35-24(32)33-6-2)12-10-19-18-8-7-16-13-17(28)9-11-25(16,3)23(18)20(29)14-26(19,27)4/h9,11,13,18-20,23,29H,5-8,10,12,14-15H2,1-4H3
InChI Key
InChIKey=FNPXMHRZILFCKX-UHFFFAOYSA-N
IUPAC Name
2-{14-[(ethoxycarbonyl)oxy]-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl}-2-oxoethyl propanoate
Traditional IUPAC Name
2-{14-[(ethoxycarbonyl)oxy]-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl}-2-oxoethyl propanoate
SMILES
CCOC(=O)OC1(CCC2C3CCC4=CC(=O)C=CC4(C)C3C(O)CC12C)C(=O)COC(=O)CC
Độ hòa tan
5.62e-03 g/l
logP
2.9
logS
-4.9
pKa (strongest acidic)
14.82
pKa (Strongest Basic)
-2.9
PSA
116.2 Å2
Refractivity
127.8 m3·mol-1
Polarizability
51.39 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Corticosteroids diffuse across cell membranes and complex with specific cytoplasmic receptors. These complexes then enter the cell nucleus, bind to DNA (chromatin), and stimulate transcription of messenger RNA (mRNA) and subsequent protein synthesis of various inhibitory enzymes responsible for the anti-inflammatory effects of topical corticosteroids. These anti-inflammatory effects include inhibition of early processes such as edema, fibrin deposition, capillary dilatation, movement of phagocytes into the area, and phagocytic activities. Later processes, such as capillary production, collagen deposition, and keloid formation also are inhibited by corticosteroids.
Cơ Chế Tác Dụng : Prednicarbate is a relatively new topical corticosteroid drug. It is similar in potency to hydrocortisone. It is used in the treatment of inflammatory skin diseases, such as atopic dermatitis. It has a favorable benefit-risk ratio, with an inflammatory action similar to that of a medium potency corticosteroid, but with a low potential to cause skin atrophy. The anti-inflammation action of corticosteroids is associated with the inhibition of the interleukin 1-alpha cytokine within keratinocytes. IL-1a is also found in fibroblasts, where it is responsible for proliferation, collagenase induction and IL-6 synthesis, which are related to skin thickness. In common with other topical corticosteroids, prednicarbate has anti-inflammatory, antipruritic, and vasoconstrictive properties. In general, the mechanism of the anti-inflammatory activity of topical steroids is unclear. 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.
Dược Động Học :
▧ Absorption :
Absorbed systemically across the stratum corneum.
▧ Metabolism :
Primarily in skin
Chỉ Định : For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Liều Lượng & Cách Dùng : Cream - Topical
Liquid - Cutaneous
Liquid - Intradermal
Liquid - Subcutaneous
Ointment - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dermatop
  • Công ty :
    Sản phẩm biệt dược : Dermatop E Emollient
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01130
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=52421
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506799
ChemSpider
http://www.chemspider.com/Chemical-Structure.47402.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0066-0507-15
PharmGKB
http://www.pharmgkb.org/drug/PA164749394
Wikipedia
http://en.wikipedia.org/wiki/Prednicarbate
RxList
http://www.rxlist.com/cgi/generic2/prednicarbate.htm
Drugs.com
http://www.drugs.com/cdi/prednicarbate-cream.html
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