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| http://linked.open...gbank/description
| - Calcitriol or 1,25-dihydroxycholecalciferol (abbreviated 1,25-(OH)<sub>2</sub>-D3) is the active form of vitamin D found in the body (vitamin D3). Calcitriol is marketed under various trade names including Rocaltrol (Roche), Calcijex (Abbott) and Decostriol (Mibe, Jesalis). It is produced in the kidneys via 25-hydroxyvitamin D-1 α-hydroxylase by conversion from 25-hydroxycholecalciferol (calcidiol). This is stimulated by a decrease in serum calcium, phosphate (PO<sub>4</sub><sup>3−</sup>) and parathyroid hormone (PTH) levels. It regulates calcium levels by increasing the absorption of calcium and phosphate from the gastrointestinal tract, increasing calcium and phosphate reabsorption in the kidneys and inhibiting the release of PTH. Calcitriol is also commonly used as a medication in the treatment of hypocalcemia and osteoporosis. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...gy/drugbank/group
| - approved (en)
- nutraceutical (en)
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| http://linked.open...drugbank/halfLife
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| http://linked.open...ugbank/indication
| - 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. (en)
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| http://linked.open...bank/manufacturer
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| Title
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| http://linked.open...mechanismOfAction
| - The mechanism of action of calcitriol in the treatment of psoriasis is accounted for by their antiproliferative activity for keratinocytes and their stimulation of epidermal cell differentiation. The anticarcinogenic activity of the active form of Calcitriol appears to be correlated with cellular vitamin D receptor (VDR) levels. Vitamin D receptors belong to the superfamily of steroid-hormone zinc-finger receptors. VDRs selectively bind 1,25-(OH)<sub>2</sub>-D3 and retinoic acid X receptor (RXR) to form a heterodimeric complex that interacts with specific DNA sequences known as vitamin D-responsive elements. VDRs are ligand-activated transcription factors. The receptors activate or repress the transcription of target genes upon binding their respective ligands. It is thought that the anticarcinogenic effect of Calcitriol is mediated via VDRs in cancer cells. The immunomodulatory activity of calcitriol is thought to be mediated by vitamin D receptors (VDRs) which are expressed constitutively in monocytes but induced upon activation of T and B lymphocytes. 1,25-(OH)<sub>2</sub>-D3 has also been found to enhance the activity of some vitamin D-receptor positive immune cells and to enhance the sensitivity of certain target cells to various cytokines secreted by immune cells. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Enterohepatic recycling and biliary excretion of calcitriol occur. The metabolites of calcitriol are excreted primarily in feces. Cumulative excretion of radioactivity on the sixth day following intravenous administration of radiolabeled calcitriol averaged 16% in urine and 49% in feces. (en)
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| http://linked.open.../drugbank/synonym
| - Calcitriol (en)
- Calcijex (en)
- Decostriol (en)
- Rocaltrol (en)
- 1,25-dihydroxycholecalciferol (en)
- (1S,3R,5Z,7e)-9,10-Secocholesta-5,7,10-triene-1,3,25-triol (en)
- 1,25-DHCC (en)
- 1-alpha-25-Dihydroxyvitamin D3 (en)
- 1alpha,25(OH)2D3 (en)
- 1alpha,25-Dihydroxycholecalciferol (en)
- 1alpha,25-Dihydroxyvitamin D3 (en)
- 1α,25(OH)2D3 (en)
- 1α,25-dihydroxycholecalciferol (en)
- 1α,25-dihydroxyvitamin D3 (en)
- Calcitriolum (en)
- 5-{2-[1-(5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexane-1,3-diol (en)
- (1alpha,3beta,5Z,7e)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol (en)
- (5Z,7e)-(1S,3R)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol (en)
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| http://linked.open...drugbank/toxicity
| - LD<sub>50</sub> (oral, rat) = 620 μg/kg; LD<sub>50</sub> (intraperitoneal, rat) > 5 mg/kg; Overdose evident in elevated blood calcium levels causing symptoms of anorexia, nausea and vomiting, polyuria, polydipsia, weakness, pruritus, and nervousness, potentially with irreversible calcification of soft tissue in the kidney and liver. (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...nk/proteinBinding
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| http://linked.open...ynthesisReference
| - Raymond E. Conrow, "Process for preparation of calcitriol lactone and related intermediates." U.S. Patent US5457245, issued April, 1994. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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