Tìm theo
Calcidiol
Các tên gọi khác (12 ) :
  • (3beta,5Z,7e)-9,10-Secocholesta-5,7,10(19)-triene-3,25-diol
  • (3S,5Z,7e)-9,10-Secocholesta-5,7,10-triene-3,25-diol
  • (3β,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-3,25-diol
  • (5Z,7e)-(3S)-9,10-Secocholesta-5,7,10(19)-triene-3,25-diol
  • 25-hydroxycholecalciferol
  • 25-Hydroxyvitamin D3
  • 25(OH)D3
  • 3-{2-[1-(5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexanol
  • Calcidiol
  • Calcifediol
  • Calcifediol Anhydrous
  • Calcifediolum
Vitamin
Thuốc Gốc
Small Molecule
CAS: 19356-17-3
ATC: A11CC06
ĐG : Organon Pharmaceuticals , http://www.organonshop.com
CTHH: C27H44O2
PTK: 400.6371
The major circulating metabolite of vitamin D3 (cholecalciferol). It is produced in the liver and is the best indicator of the body's vitamin D stores. It is effective in the treatment of rickets and osteomalacia, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H44O2
Phân tử khối
400.6371
Monoisotopic mass
400.334130652
InChI
InChI=1S/C27H44O2/c1-19-10-13-23(28)18-22(19)12-11-21-9-7-17-27(5)24(14-15-25(21)27)20(2)8-6-16-26(3,4)29/h11-12,20,23-25,28-29H,1,6-10,13-18H2,2-5H3/b21-11+,22-12-/t20-,23+,24-,25+,27-/m1/s1
InChI Key
InChIKey=JWUBBDSIWDLEOM-DTOXIADCSA-N
IUPAC Name
(1S,3Z)-3-{2-[(1R,3aS,4E,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexan-1-ol
Traditional IUPAC Name
25-hydroxycholecalciferol
SMILES
C[C@H](CCCC(C)(C)O)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)CCC1=C
Độ hòa tan
Insoluble
logP
6
logS
-5.3
pKa (strongest acidic)
18.38
pKa (Strongest Basic)
-0.98
PSA
40.46 Å2
Refractivity
125.06 m3·mol-1
Polarizability
50.32 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Calcidiol is the precursor of vitamin D3. Vitamin D3 is a steroid hormone that has long been known for its important role in regulating body levels of calcium and phosphorus, in mineralization of bone, and for the assimilation of vitamin A. The classical manifestations of vitamin D deficiency is rickets, which is seen in children and results in bony deformaties including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix, and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease, and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium and phosphorus mobilization from bone to plasma.
Cơ Chế Tác Dụng : The major circulating metabolite of vitamin D3 (cholecalciferol). It is produced in the liver and is the best indicator of the body's vitamin D stores. It is effective in the treatment of rickets and osteomalacia, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties. [PubChem] Calcidiol is transformed in the kidney by 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to calcitriol, the active form of vitamin D3. Calcitriol binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. Calcitriol increases the serum calcium concentrations by: increasing GI absorption of phosphorus and calcium, increasing osteoclastic resorption, and increasing distal renal tubular reabsorption of calcium. Calcitriol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein.
Dược Động Học :
▧ Absorption :
Readily absorbed.
▧ Metabolism :
Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25- dihydroxycholecalciferol), the active form of vitamin D3.
▧ Half Life :
288 hours
Độc Tính : Bone pain, constipation (especially in children or adolescents), diarrhea, drowsiness, dryness of mouth; headache (continuing), increased thirst, increase in frequency of urination, especially at night, or in amount of urine, irregular heartbeat, itching skin, loss of appetite, metallic taste, muscle pain, nausea or vomiting (especially in children or adolescents), unusual tiredness or weakness.
Chỉ Định : Used to treat vitamin D deficiency or insufficiency, refractory rickets (vitamin D resistant rickets), familial hypophosphatemia and hypoparathyroidism, and in the management of hypocalcemia and renal osteodystrophy in patients with chronic renal failure undergoing dialysis. Also used in conjunction with calcium in the management and prevention of primary or corticosteroid-induced osteoporosis.
Liều Lượng & Cách Dùng : Capsule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Upjohn
    Sản phẩm biệt dược : Calderol
  • Công ty : Medica
    Sản phẩm biệt dược : Caldiol
  • Công ty : China Otsuka
    Sản phẩm biệt dược : De Kai
  • Công ty : Desma
    Sản phẩm biệt dược : Dedrogyl
  • Công ty : DB
    Sản phẩm biệt dược : Dédrogyl
  • Công ty : Bruno Farm.
    Sản phẩm biệt dược : Didrogyl
  • Công ty : Faes
    Sản phẩm biệt dược : Hidroferol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00146
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C01561
PharmGKB
http://www.pharmgkb.org/drug/PA164745614
Wikipedia
http://en.wikipedia.org/wiki/Calcidiol
PDRhealth
http://www.pdrhealth.com/drug_info/nmdrugprofiles/nutsupdrugs/vit_0265.shtml
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