Tìm theo
Calcipotriol
Các tên gọi khác (4 ) :
  • Calcipotriene
  • Calcipotriol
  • Daivonex
  • Dovonex
Thuốc điều trị bệnh da liễu
Thuốc Gốc
Small Molecule
CAS: 112965-21-6
ATC: D05AX02
ĐG : Contract Pharm , http://www.contractpharma.com
CTHH: C27H40O3
PTK: 412.6047
Calcipotriol (INN) or calcipotriene (USAN) is a sythetic derivative of calcitriol or Vitamin D.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H40O3
Phân tử khối
412.6047
Monoisotopic mass
412.297745146
InChI
InChI=1S/C27H40O3/c1-17(6-13-25(29)20-8-9-20)23-11-12-24-19(5-4-14-27(23,24)3)7-10-21-15-22(28)16-26(30)18(21)2/h6-7,10,13,17,20,22-26,28-30H,2,4-5,8-9,11-12,14-16H2,1,3H3/b13-6+,19-7+,21-10-/t17-,22-,23-,24+,25-,26+,27-/m1/s1
InChI Key
InChIKey=LWQQLNNNIPYSNX-UROSTWAQSA-N
IUPAC Name
(1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R,3E,5S)-5-cyclopropyl-5-hydroxypent-3-en-2-yl]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol
Traditional IUPAC Name
calcipotriol
SMILES
O[C@H](\C=C\[C@@H](C)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C)C1CC1
Độ hòa tan
1.35e-02 g/l
logP
3.84
logS
-4.5
pKa (strongest acidic)
14.39
pKa (Strongest Basic)
-1.6
PSA
60.69 Å2
Refractivity
125.45 m3·mol-1
Polarizability
49.59 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Calcipotriene is a synthetic analog of vitamin D. In humans, the natural supply of vitamin D depends mainly on exposure to the ultraviolet rays of the sun for conversion of 7-dehydrocholesterol to vitamin D3 (cholecalciferol) in the skin.
Cơ Chế Tác Dụng : Calcipotriol (INN) or calcipotriene (USAN) is a sythetic derivative of calcitriol or Vitamin D. The precise mechanism of calcipotriol in remitting psoriasis is not well-understood. However, it has been shown to have comparable affinity with calcitriol for the Vitamin D receptor, while being less than 1% as active as the calcitriol in regulating calcium metabolism. The Vitamin D receptor (VDR) belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. T cells are known to play a role in psoriasis, and it is thought that the binding of calcipotriol to the VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes.
Dược Động Học :
▧ Absorption :
Clinical studies with radiolabeled ointment indicate that approximately 6% (+3%, SD) of the applied dose of calcipotriene is absorbed systemically when the ointment is applied topically to psoriasis plaques or 5% (+2.6%, SO) when applied to normal skin.
▧ Metabolism :
Hepatic. Calcipotriene metabolism following systemic uptake is rapid, and occurs via a similar pathway to the natural hormone. The primary metabolites are much less potent than the parent compound.
▧ Route of Elimination :
The active form of the vitamin, 1,25-dihydroxy vitamin D3 (calcitriol), is known to be recycled via the liver and excreted in the bile. There is evidence that maternal 1,25-dihydroxy vitamin D3 (calcitriol) may enter the fetal circulation, but it is not known whether it is excreted in human milk.
Độc Tính : Topically applied calcipotriene can be absorbed in sufficient amounts to produce systemic effects. Elevated serum calcium has been observed with excessive use of calcipotriene.
Chỉ Định : For the treatment of moderate plaque psoriasis in adults.
Tương Tác Thuốc :
  • Alfacalcidol Vitamin D Analogs may enhance the adverse/toxic effect of other Vitamin D Analogs. Avoid combined use of multiple vitamin D analogs (at pharmacologic doses). Prescribing information for calcitriol, doxercalciferol, paricalcitol, and alfacalcidol each specifically cautions against such combined use.
  • Aluminum hydroxide Vitamin D Analogs may increase the serum concentration of Aluminum Hydroxide. Specifically, the absorption of aluminum may be increased, leading to increased serum aluminum concentrations. Avoid chronic and/or excessive use of aluminum and aluminum-containing products in patients who are also taking vitamin D analogs. Any patients consuming such a combination should be monitored closely for aluminum status and signs/symptoms of aluminum-related toxicities.
  • Cholecalciferol Vitamin D Analogs may enhance the adverse/toxic effect of other Vitamin D Analogs. Avoid combined use of multiple vitamin D analogs (at pharmacologic doses). hough not specified in the prescribing information for calcipotriene, cholecalciferol, and ergocalciferol, each contains warnings regarding the potential for vitamin D toxicity.
  • Orlistat Orlistat may decrease the serum concentration of fat soluble vitamins like vitamin D. Hence, this applies to calcipotriol, a synthetic derivative of vitamin D. Administer oral fat soluble vitamins at least 2 hours before or after the administration of orlistat. Avoid concomitant administration due to the risk of impaired vitamin absorption. Similar precautions do not apply to parenterally administered fat soluble vitamins.
  • Sucralfate Vitamin D Analogs may increase the serum concentration of Sucralfate. Specifically, the absorption of aluminum from sucralfate may be increased, leading to an increase in the serum aluminum concentration. Avoid chronic and/or excessive use of aluminum and aluminum-containing products (such as sucralfate) in patients who are also taking vitamin D analogs. Any patients consuming such a combination should be monitored closely for aluminum status and signs/symptoms of aluminum-related toxicities.
Liều Lượng & Cách Dùng : Cream - Topical
Ointment - Topical
Shampoo - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Calcitrene
  • Công ty :
    Sản phẩm biệt dược : Daivonex
  • Công ty :
    Sản phẩm biệt dược : Dovonex
  • Công ty :
    Sản phẩm biệt dược : SORILUX
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB02300
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01125
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0168-0400-60
PharmGKB
http://www.pharmgkb.org/drug/PA448714
Wikipedia
http://en.wikipedia.org/wiki/Calcipotriol
RxList
http://www.rxlist.com/cgi/generic/calcipo.htm
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