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Identification
NameCalcitriol
Accession NumberDB00136  (NUTR00003, APRD00246)
TypeSmall Molecule
GroupsApproved, Nutraceutical
Description

Calcitriol or 1,25-dihydroxycholecalciferol (abbreviated 1,25-(OH)2-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 (PO43−) 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.

Structure
Thumb
Synonyms
(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
(5Z,7e)-(1S,3R)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol
1-alpha-25-Dihydroxyvitamin D3
1,25-DHCC
1,25-dihydroxycholecalciferol
1alpha,25-Dihydroxycholecalciferol
1alpha,25-Dihydroxyvitamin D3
1alpha,25(OH)2D3
1α,25-dihydroxycholecalciferol
1α,25-dihydroxyvitamin D3
1α,25(OH)2D3
5-{2-[1-(5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexane-1,3-diol
Calcijex
Calcitriol
Calcitriolum
Decostriol
Rocaltrol
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcijexinjection, solution1 ug/mLintravenousAbb Vie Inc.2010-06-012016-04-23Us
Calcijexsolution2 mcgintravenousAbbvie Corporation1990-12-31Not applicableCanada
Calcijexsolution1 mcgintravenousAbbvie Corporation1990-12-31Not applicableCanada
Calcitriolointment3 ug/gtopicalPerrigo New York Inc2012-03-082016-04-05Us
Calcitriolcapsule.25 ug/1oralCarilion Materials Management2009-08-262016-04-05Us
Calcitriolcapsule.25 ug/1oralDispensing Solutions, Inc.2009-08-262016-04-05Us
Calcitriolsolution1 ug/mLoralRanbaxy Pharmaceuticals Inc.2009-08-262016-04-05Us
Calcitriolcapsule.5 ug/1oralRanbaxy Pharmaceuticals Inc.2009-08-262016-04-05Us
Calcitriolcapsule.25 ug/1oralRanbaxy Pharmaceuticals Inc.2009-08-262016-04-05Us
Calcitriol Injectionsolution1 mcgintravenousFresenius Kabi Canada Ltd2003-07-07Not applicableCanada
Calcitriol Injection USPsolution2 mcgintravenousSterimax Inc2015-04-16Not applicableCanada
Calcitriol Injection USPsolution1 mcgintravenousSterimax Inc2015-03-27Not applicableCanada
Calcitriol-odancapsule0.5 mcgoralOdan Laboratories Ltd2014-10-10Not applicableCanada
Calcitriol-odancapsule0.25 mcgoralOdan Laboratories Ltd2014-10-10Not applicableCanada
Rocaltrolcapsule, gelatin coated.25 ug/1oralAphena Pharma Solutions Tennessee, Inc.2009-08-102016-04-05Us
Rocaltrolsolution1 ug/mLoralValidus Pharmaceuticals LLC2009-07-232016-04-05Us
Rocaltrolcapsule, gelatin coated.5 ug/1oralValidus Pharmaceuticals LLC2009-08-102016-04-05Us
Rocaltrolcapsule, gelatin coated.25 ug/1oralValidus Pharmaceuticals LLC2009-08-102016-04-05Us
Rocaltrolcapsule, gelatin coated.25 ug/1oralKAISER FOUNDATION HOSPITALS2010-08-092016-04-23Us
Rocaltrolcapsule, gelatin coated.5 ug/1oralKAISER FOUNDATION HOSPITALS2010-06-042016-04-23Us
Rocaltrol Cap 0.25mcgcapsule0.25 mcgoralHoffmann La Roche Limited1979-12-31Not applicableCanada
Rocaltrol Cap 0.5mcgcapsule0.5 mcgoralHoffmann La Roche Limited1979-12-31Not applicableCanada
Rocaltrol Oral Solution 1mcg/mlsolution1 mcgoralHoffmann La Roche Limited1992-12-312013-06-24Canada
Silkisointment3 mcgtopicalGalderma Canada Inc2010-04-09Not applicableCanada
Vecticalointment3 ug/gtopicalGalderma Laboratories, L.P.2009-02-012016-04-23Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcitriolcapsule, liquid filled.25 ug/1oralCardinal Health2009-10-292016-04-05Us
Calcitriolinjection, solution1 mg/mLintravenousPhysicians Total Care, Inc.2011-05-172016-04-05Us
Calcitriolinjection1 ug/mLintravenousAkorn, Inc.2013-03-222016-04-05Us
Calcitriolcapsule.25 ug/1oralRoxane Laboratories, Inc.2006-03-272016-04-23Us
Calcitriolcapsule.25 ug/1oralAmerican Health Packaging2012-03-012016-11-30Us
Calcitriolcapsule, liquid filled.25 ug/1oralPhysicians Total Care, Inc.2005-12-022016-04-05Us
Calcitriolinjection, solution1 ug/mLintravenousAmerican Regent, Inc.2005-03-142016-04-23Us
Calcitriolcapsule, liquid filled.5 ug/1oralPhysicians Total Care, Inc.2010-03-012016-04-05Us
Calcitriolcapsule, liquid filled.5 ug/1oralKAISER FOUNDATION HOSPITALS2015-12-032016-04-23Us
Calcitriolcapsule.5 ug/1oralStrides Arcolab Limited2015-01-062016-04-05Us
Calcitriolcapsule.25 ug/1oralAphena Pharma Solutions Tennessee, Llc2006-03-272016-04-05Us
Calcitriolcapsule, liquid filled.25 ug/1oralKAISER FOUNDATION HOSPITALS2015-12-032016-04-23Us
Calcitriolcapsule.25 ug/1oralStrides Arcolab Limited2015-01-062016-04-05Us
Calcitriolcapsule, liquid filled.5 ug/1oralHeritage Pharmaceuticals Inc2013-05-292016-04-05Us
Calcitriolinjection1 ug/mLintravenousWest ward Pharmaceutical Corp2006-02-082016-04-23Us
Calcitriolinjection, solution1 ug/mLintravenousFresenius Kabi USA, LLC2003-05-292016-04-05Us
Calcitriolcapsule, liquid filled.25 ug/1oralHeritage Pharmaceuticals Inc2013-05-292016-04-05Us
Calcitriolcapsule, liquid filled.5 ug/1oralTeva Pharmaceuticals USA Inc2001-10-152016-04-23Us
Calcitriolcapsule, liquid filled.5 ug/1oralGolden State Medical Supply, Inc.2014-12-262016-04-05Us
Calcitriolinjection2 ug/mLintravenousAkorn, Inc.2011-10-142016-04-05Us
Calcitriolcapsule, liquid filled.25 ug/1oralTeva Pharmaceuticals USA Inc2001-10-152016-04-23Us
Calcitriolcapsule, liquid filled.25 ug/1oralGolden State Medical Supply, Inc.2014-12-262016-04-05Us
Calcitriolcapsule, liquid filled.5 ug/1oralCardinal Health2009-10-292016-04-05Us
Calcitriolinjection1 ug/mLintravenousAkorn, Inc.2011-10-142016-04-05Us
Calcitriolsolution1 ug/mLoralRoxane Laboratories, Inc2003-07-182016-04-23Us
Over the Counter ProductsNot Available
International Brands
NameCompany
Calcitriol Oral SolutionRoxane
DecostriolMibe Jena (Germany), Jesalis (Hong Kong, Thailand)
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIFXC9231JVH
CAS number32222-06-3
WeightAverage: 416.6365
Monoisotopic: 416.329045274
Chemical FormulaC27H44O3
InChI KeyInChIKey=GMRQFYUYWCNGIN-NKMMMXOESA-N
InChI
InChI=1S/C27H44O3/c1-18(8-6-14-26(3,4)30)23-12-13-24-20(9-7-15-27(23,24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11,18,22-25,28-30H,2,6-9,12-17H2,1,3-5H3/b20-10+,21-11-/t18-,22-,23-,24+,25+,27-/m1/s1
IUPAC Name
(1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol
SMILES
C[[email protected]](CCCC(C)(C)O)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)C[[email protected]](O)C1=C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as triterpenoids. These are terpene molecules containing 8 isoprene units.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassPrenol lipids
Sub ClassTriterpenoids
Direct ParentTriterpenoids
Alternative Parents
Substituents
  • Polycyclic triterpenoid
  • Triterpenoid
  • Steroid
  • Cyclohexanol
  • Tertiary alcohol
  • Cyclic alcohol
  • Secondary alcohol
  • Hydrocarbon derivative
  • Organooxygen compound
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed 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.
PharmacodynamicsCalcitriol, a pharmaceutical form of vitamin D, has anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Calcitriol has been found to be effective in the treatment of psoriasis when applied topically. Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in a number of malignant cell lines including human prostate cancer cells. Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of calcitriol, 1,25-(OH)2-D3, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25-(OH)2-D3 has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. It has also been found to induce monocyte differentiation and to inhibit lymphocyte proliferation and production of cytokines, including interleukin IL-1 and IL-2, as well as to suppress immunoglobulin secretion by B lymphocytes. Vitamin D appears to demonstrate both immune-enhancing and immunosuppressive effects.
Mechanism of actionThe 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)2-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)2-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.
Related Articles
AbsorptionRapidly absorbed from the intestine.
Volume of distributionNot Available
Protein binding99.9%
Metabolism

The first pathway involves 24-hydroxylase activity in the kidney; this enzyme is also present in many target tissues which possess the vitamin D receptor such as the intestine. The end product of this pathway is a side chain shortened metabolite, calcitroic acid. The second pathway involves the conversion of calcitriol via the stepwise hydroxylation of carbon-26 and carbon-23, and cyclization to yield ultimately 1a,25R(OH)2-26,23S-lactone D3. The lactone appears to be the major metabolite circulating in humans.

SubstrateEnzymesProduct
Calcitriol
Not Available
Calcitroic acidDetails
Route of eliminationEnterohepatic 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.
Half life5-8 hours
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]
ToxicityLD50 (oral, rat) = 620 μg/kg; LD50 (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.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9924
Blood Brain Barrier+0.8524
Caco-2 permeable+0.7812
P-glycoprotein substrateSubstrate0.7843
P-glycoprotein inhibitor INon-inhibitor0.6065
P-glycoprotein inhibitor IINon-inhibitor0.6073
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8367
CYP450 2D6 substrateNon-substrate0.9022
CYP450 3A4 substrateSubstrate0.7506
CYP450 1A2 substrateNon-inhibitor0.9033
CYP450 2C9 inhibitorNon-inhibitor0.8354
CYP450 2D6 inhibitorNon-inhibitor0.9495
CYP450 2C19 inhibitorNon-inhibitor0.7796
CYP450 3A4 inhibitorNon-inhibitor0.813
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6175
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9274
BiodegradationNot ready biodegradable0.9937
Rat acute toxicity5.1352 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8734
hERG inhibition (predictor II)Non-inhibitor0.8579
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Validus pharmaceuticals llc
  • Abbott laboratories hosp products div
  • Akorn inc
  • App pharmaceuticals llc
  • Fresenius medical care north america
  • Genix therapeutics inc
  • Hospira inc
  • Luitpold pharmaceuticals inc
  • Lyne laboratories inc
  • Teva parenteral medicines inc
  • Galderma laboratories lp
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous1 ug/mL
Solutionintravenous1 mcg
Solutionintravenous2 mcg
Capsuleoral.25 ug/1
Capsuleoral.5 ug/1
Capsule, liquid filledoral.25 ug/1
Capsule, liquid filledoral.5 ug/1
Injectionintravenous1 ug/mL
Injectionintravenous2 ug/mL
Injection, solutionintravenous1 mg/mL
Solutionoral1 ug/mL
Capsule, gelatin coatedoral.25 ug/1
Capsule, gelatin coatedoral.5 ug/1
Capsuleoral0.25 mcg
Capsuleoral0.5 mcg
Solutionoral1 mcg
Ointmenttopical3 mcg
Ointmenttopical3 ug/g
Prices
Unit descriptionCostUnit
Calcijex 2 mcg/ml19.38USD ml
Calcijex 1 mcg/ml ampul14.7USD ml
Calcijex 1 mcg/ml10.68USD ml
Calcitriol 1 mcg/ml ampul6.0USD ml
Vectical 3 mcg/g ointment4.68USD g
Rocaltrol 0.5 mcg capsule2.02USD capsule
Calcitriol 0.5 mcg capsule1.97USD capsule
Rocaltrol 0.25 mcg capsule1.46USD capsule
Calcitriol 0.25 mcg capsule1.45USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6051567 Yes2000-02-022020-02-02Us
US6265392 Yes2000-02-022020-02-02Us
US6274169 Yes2000-02-022020-02-02Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point113-114Uskokovic, M.R., Narwid, T.A., lacobelli, J.A. and Baggiolini, E.; U.S. Patent 3,993,675; November 23, 1976; assigned to Hoffmann-La Roche, Inc.
water solubilityInsolubleNot Available
logP5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00667 mg/mLALOGPS
logP5.51ALOGPS
logP4.35ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)14.39ChemAxon
pKa (Strongest Basic)-1.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area60.69 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity126.53 m3·mol-1ChemAxon
Polarizability51.02 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Raymond E. Conrow, “Process for preparation of calcitriol lactone and related intermediates.” U.S. Patent US5457245, issued April, 1994.

US5457245
General ReferencesNot Available
External Links
ATC CodesA11CC04D05AX03
AHFS Codes
  • 88:16.00
PDB EntriesNot Available
FDA labelDownload (39.2 KB)
MSDSDownload (74.7 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolCalcitriol may decrease the anticoagulant activities of Acenocoumarol.
Aluminum hydroxideThe serum concentration of Aluminum hydroxide can be increased when it is combined with Calcitriol.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Calcitriol.
AprepitantThe serum concentration of Calcitriol can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Calcitriol.
BetamethasoneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Betamethasone.
BexaroteneThe serum concentration of Calcitriol can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Calcitriol can be decreased when it is combined with Bosentan.
CeritinibThe serum concentration of Calcitriol can be increased when it is combined with Ceritinib.
ColesevelamThe serum concentration of Calcitriol can be decreased when it is combined with Colesevelam.
ConivaptanThe serum concentration of Calcitriol can be increased when it is combined with Conivaptan.
CorticotropinThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Cortisone acetate.
DabrafenibThe serum concentration of Calcitriol can be decreased when it is combined with Dabrafenib.
DanazolDanazol may increase the hypercalcemic activities of Calcitriol.
DasatinibThe serum concentration of Calcitriol can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Calcitriol can be decreased when it is combined with Deferasirox.
DexamethasoneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Dexamethasone.
DigoxinCalcitriol may increase the arrhythmogenic activities of Digoxin.
DihydrotachysterolThe risk or severity of adverse effects can be increased when Dihydrotachysterol is combined with Calcitriol.
FluconazoleThe metabolism of Calcitriol can be decreased when combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Fludrocortisone.
FosaprepitantThe serum concentration of Calcitriol can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Calcitriol can be increased when it is combined with Fusidic Acid.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Calcitriol.
HydrocortisoneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Hydrocortisone.
IdelalisibThe serum concentration of Calcitriol can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Calcitriol can be increased when it is combined with Ivacaftor.
LuliconazoleThe serum concentration of Calcitriol can be increased when it is combined with Luliconazole.
Magnesium chlorideThe serum concentration of Magnesium chloride can be increased when it is combined with Calcitriol.
Magnesium citrateThe serum concentration of Magnesium citrate can be increased when it is combined with Calcitriol.
Magnesium hydroxideThe serum concentration of Magnesium hydroxide can be increased when it is combined with Calcitriol.
Magnesium oxideThe serum concentration of Magnesium oxide can be increased when it is combined with Calcitriol.
Magnesium salicylateThe serum concentration of Magnesium salicylate can be increased when it is combined with Calcitriol.
Magnesium SulfateThe serum concentration of Magnesium Sulfate can be increased when it is combined with Calcitriol.
MethylprednisoloneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Methylprednisolone.
MifepristoneThe serum concentration of Calcitriol can be increased when it is combined with Mifepristone.
Mineral oilThe serum concentration of Calcitriol can be decreased when it is combined with Mineral oil.
MitotaneThe serum concentration of Calcitriol can be decreased when it is combined with Mitotane.
NelfinavirThe metabolism of Calcitriol can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Calcitriol can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Calcitriol.
OrlistatThe serum concentration of Calcitriol can be decreased when it is combined with Orlistat.
PalbociclibThe serum concentration of Calcitriol can be increased when it is combined with Palbociclib.
PhenytoinThe metabolism of Calcitriol can be increased when combined with Phenytoin.
PrednisoloneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Prednisone.
Repository corticotropinThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Repository corticotropin.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Calcitriol.
SevelamerThe serum concentration of Calcitriol can be decreased when it is combined with Sevelamer.
SiltuximabThe serum concentration of Calcitriol can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Calcitriol can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Calcitriol can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Calcitriol can be increased when it is combined with Stiripentol.
SucralfateThe serum concentration of Sucralfate can be increased when it is combined with Calcitriol.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Calcitriol.
TocilizumabThe serum concentration of Calcitriol can be decreased when it is combined with Tocilizumab.
TriamcinoloneThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Triamcinolone.
TrichlormethiazideTrichlormethiazide may increase the hypercalcemic activities of Calcitriol.
WarfarinCalcitriol may decrease the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B/WSTF which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.
Gene Name:
VDR
Uniprot ID:
P11473
Molecular Weight:
48288.64 Da
References
  1. Reinhart GA: Vitamin D analogs: novel therapeutic agents for cardiovascular disease? Curr Opin Investig Drugs. 2004 Sep;5(9):947-51. [PubMed:15503649 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Oxidoreductase activity
Specific Function:
Has a role in maintaining calcium homeostasis. Catalyzes the NADPH-dependent 24-hydroxylation of calcidiol (25-hydroxyvitamin D(3)) and calcitriol (1-alpha,25-dihydroxyvitamin D(3)). The enzyme can perform up to 6 rounds of hydroxylation of calcitriol leading to calcitroic acid. It also shows 23-hydroxylating activity leading to 1-alpha,25-dihydroxyvitamin D(3)-26,23-lactone as end product.
Gene Name:
CYP24A1
Uniprot ID:
Q07973
Molecular Weight:
58874.695 Da
References
  1. Schuster I: Cytochromes P450 are essential players in the vitamin D signaling system. Biochim Biophys Acta. 2011 Jan;1814(1):186-99. doi: 10.1016/j.bbapap.2010.06.022. Epub 2010 Jul 7. [PubMed:20619365 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Xu Y, Hashizume T, Shuhart MC, Davis CL, Nelson WL, Sakaki T, Kalhorn TF, Watkins PB, Schuetz EG, Thummel KE: Intestinal and hepatic CYP3A4 catalyze hydroxylation of 1alpha,25-dihydroxyvitamin D(3): implications for drug-induced osteomalacia. Mol Pharmacol. 2006 Jan;69(1):56-65. Epub 2005 Oct 5. [PubMed:16207822 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on April 29, 2016 03:10