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Statements

Subject Item
n2:DB00136
rdf:type
n5:Drug
n5: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 &alpha;-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.
n5:dosage
n20:271B49BA-363D-11E5-9242-09173F13E4C5 n20:271B49BB-363D-11E5-9242-09173F13E4C5 n20:271B49BC-363D-11E5-9242-09173F13E4C5 n20:271B49BD-363D-11E5-9242-09173F13E4C5 n20:271B49BE-363D-11E5-9242-09173F13E4C5 n20:271B49BF-363D-11E5-9242-09173F13E4C5 n20:271B49C0-363D-11E5-9242-09173F13E4C5 n20:271B49C1-363D-11E5-9242-09173F13E4C5 n20:271B49C2-363D-11E5-9242-09173F13E4C5 n20:271B49C3-363D-11E5-9242-09173F13E4C5 n20:271B49C4-363D-11E5-9242-09173F13E4C5 n20:271B49C5-363D-11E5-9242-09173F13E4C5 n20:271B49C6-363D-11E5-9242-09173F13E4C5 n20:271B49C7-363D-11E5-9242-09173F13E4C5 n20:271B49C8-363D-11E5-9242-09173F13E4C5
n5:group
approved nutraceutical
n5:halfLife
5-8 hours
n5: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.
n5:manufacturer
n12:271B49AA-363D-11E5-9242-09173F13E4C5 n12:271B49AB-363D-11E5-9242-09173F13E4C5 n12:271B49A8-363D-11E5-9242-09173F13E4C5 n12:271B49A9-363D-11E5-9242-09173F13E4C5 n12:271B49A6-363D-11E5-9242-09173F13E4C5 n12:271B49A7-363D-11E5-9242-09173F13E4C5 n12:271B49A4-363D-11E5-9242-09173F13E4C5 n12:271B49A5-363D-11E5-9242-09173F13E4C5 n12:271B49B0-363D-11E5-9242-09173F13E4C5 n12:271B49AE-363D-11E5-9242-09173F13E4C5 n12:271B49AF-363D-11E5-9242-09173F13E4C5 n12:271B49AC-363D-11E5-9242-09173F13E4C5 n12:271B49AD-363D-11E5-9242-09173F13E4C5
owl:sameAs
n4:DB00136 n15:DB00136
dcterms:title
Calcitriol
adms:identifier
n8:PA448717 n9:D00129 n10:0004-0143-23 n13:Calcitriol n25:2779 n26:C01673 n28:2779 n29:17823 n30:DB00136
n5: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.
n5:packager
n12:271B4996-363D-11E5-9242-09173F13E4C5 n12:271B4997-363D-11E5-9242-09173F13E4C5 n12:271B4994-363D-11E5-9242-09173F13E4C5 n12:271B4995-363D-11E5-9242-09173F13E4C5 n12:271B499A-363D-11E5-9242-09173F13E4C5 n12:271B499B-363D-11E5-9242-09173F13E4C5 n12:271B4998-363D-11E5-9242-09173F13E4C5 n12:271B4999-363D-11E5-9242-09173F13E4C5 n12:271B498E-363D-11E5-9242-09173F13E4C5 n12:271B498F-363D-11E5-9242-09173F13E4C5 n12:271B498D-363D-11E5-9242-09173F13E4C5 n12:271B4992-363D-11E5-9242-09173F13E4C5 n12:271B4993-363D-11E5-9242-09173F13E4C5 n12:271B4990-363D-11E5-9242-09173F13E4C5 n12:271B4991-363D-11E5-9242-09173F13E4C5 n12:271B499C-363D-11E5-9242-09173F13E4C5 n12:271B499E-363D-11E5-9242-09173F13E4C5 n12:271B499F-363D-11E5-9242-09173F13E4C5 n12:271B498C-363D-11E5-9242-09173F13E4C5 n12:271B499D-363D-11E5-9242-09173F13E4C5 n12:271B49A2-363D-11E5-9242-09173F13E4C5 n12:271B49A3-363D-11E5-9242-09173F13E4C5 n12:271B49A0-363D-11E5-9242-09173F13E4C5 n12:271B49A1-363D-11E5-9242-09173F13E4C5
n5:patent
n27:6051567
n5:routeOfElimination
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.
n5:synonym
1alpha,25-Dihydroxyvitamin D3 (5Z,7e)-(1S,3R)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol 5-{2-[1-(5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexane-1,3-diol 1α,25-dihydroxyvitamin D3 1α,25-dihydroxycholecalciferol Decostriol 1,25-dihydroxycholecalciferol (1alpha,3beta,5Z,7e)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol (1S,3R,5Z,7e)-9,10-Secocholesta-5,7,10-triene-1,3,25-triol Calcijex Rocaltrol Calcitriol 1,25-DHCC 1alpha,25-Dihydroxycholecalciferol Calcitriolum 1α,25(OH)2D3 1alpha,25(OH)2D3 1-alpha-25-Dihydroxyvitamin D3
n5:toxicity
LD<sub>50</sub> (oral, rat) = 620 &mu;g/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.
n21:hasAHFSCode
n22:88-16-00
n5:proteinBinding
99.9%
n5:synthesisReference
Raymond E. Conrow, "Process for preparation of calcitriol lactone and related intermediates." U.S. Patent US5457245, issued April, 1994.
n16:hasConcept
n17:M0003148
foaf:page
n19:calcitri.htm n24:vit_0265.shtml n31:calcitriol.html
n5:IUPAC-Name
n6:271B49CD-363D-11E5-9242-09173F13E4C5
n5:InChI
n6:271B49D3-363D-11E5-9242-09173F13E4C5
n5:Molecular-Formula
n6:271B49D2-363D-11E5-9242-09173F13E4C5
n5:Molecular-Weight
n6:271B49CF-363D-11E5-9242-09173F13E4C5
n5:Monoisotopic-Weight
n6:271B49D0-363D-11E5-9242-09173F13E4C5
n5:SMILES
n6:271B49D1-363D-11E5-9242-09173F13E4C5
n5:Water-Solubility
n6:271B49E3-363D-11E5-9242-09173F13E4C5 n6:271B49CB-363D-11E5-9242-09173F13E4C5
n5:logP
n6:271B49E5-363D-11E5-9242-09173F13E4C5 n6:271B49C9-363D-11E5-9242-09173F13E4C5 n6:271B49CC-363D-11E5-9242-09173F13E4C5
n5:logS
n6:271B49CA-363D-11E5-9242-09173F13E4C5
n21:hasATCCode
n23:D05AX03 n23:A11CC04
n5:H-Bond-Acceptor-Count
n6:271B49D9-363D-11E5-9242-09173F13E4C5
n5:H-Bond-Donor-Count
n6:271B49DA-363D-11E5-9242-09173F13E4C5
n5:InChIKey
n6:271B49D4-363D-11E5-9242-09173F13E4C5
n5:Polar-Surface-Area--PSA-
n6:271B49D5-363D-11E5-9242-09173F13E4C5
n5:Polarizability
n6:271B49D7-363D-11E5-9242-09173F13E4C5
n5:Refractivity
n6:271B49D6-363D-11E5-9242-09173F13E4C5
n5:Rotatable-Bond-Count
n6:271B49D8-363D-11E5-9242-09173F13E4C5
n5:absorption
Rapidly absorbed from the intestine.
n5:affectedOrganism
Humans and other mammals
n5:casRegistryNumber
32222-06-3
n5:category
n5:clearance
* 15.3 mL/hr/kg [pediatric patients (age range: 1.8 to 16 years) undergoing peritoneal dialysis receiving dose of 10.2 ng/kg (SD 5.5 ng/kg) for 2 months]
n5:containedIn
n14:271B49B5-363D-11E5-9242-09173F13E4C5 n14:271B49B6-363D-11E5-9242-09173F13E4C5 n14:271B49B3-363D-11E5-9242-09173F13E4C5 n14:271B49B4-363D-11E5-9242-09173F13E4C5 n14:271B49B9-363D-11E5-9242-09173F13E4C5 n14:271B49B7-363D-11E5-9242-09173F13E4C5 n14:271B49B8-363D-11E5-9242-09173F13E4C5 n14:271B49B1-363D-11E5-9242-09173F13E4C5 n14:271B49B2-363D-11E5-9242-09173F13E4C5
n5:Bioavailability
n6:271B49DF-363D-11E5-9242-09173F13E4C5
n5:Ghose-Filter
n6:271B49E1-363D-11E5-9242-09173F13E4C5
n5:MDDR-Like-Rule
n6:271B49E2-363D-11E5-9242-09173F13E4C5
n5:Melting-Point
n6:271B49E4-363D-11E5-9242-09173F13E4C5
n5:Number-of-Rings
n6:271B49DE-363D-11E5-9242-09173F13E4C5
n5:Physiological-Charge
n6:271B49DD-363D-11E5-9242-09173F13E4C5
n5:Rule-of-Five
n6:271B49E0-363D-11E5-9242-09173F13E4C5
n5:Traditional-IUPAC-Name
n6:271B49CE-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-acidic-
n6:271B49DB-363D-11E5-9242-09173F13E4C5
n5:pKa--strongest-basic-
n6:271B49DC-363D-11E5-9242-09173F13E4C5