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Drug

D0832 | calcitriol

Molecular Formula C27H44O3
Molecular Weight 416.6
Structure
State solid
Clearance The metabolic clearance rate was 23.5±4.34 ml/min in healthy male volunteers and 10.1±1.35 ml/min in male patients with uraemia [A175726]. In the pediatric patients undergoing peritoneal dialysis receiving dose of 10.2 ng/kg (SD 5.5 ng/kg) for 2 months, the clearance rate was 15.3 mL/hr/kg [FDA Label].
Volume of distribution Upon intravenous administration, the volume of distribution of calcitriol was 0.49±0.14 L/kg in healthy male volunteers and 0.27±0.06 l/kg in uraemic male patients participating in a pharmacokinetic study [A175726]. There is some evidence that calcitriol is transferred into human milk at low levels (ie, 2.2±0.1 pg/mL) in mothers [FDA Label]. Calcitriol from maternal circulation may also enter the fetal circulation [FDA Label].
Route of elimination In normal subjects, approximately 27% and 7% of the radioactivity appeared in the feces and urine, respectively, within 24 hours [FDA Label]. Calcitriol undergoes enterohepatic recycling and biliary excretion. 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 [FDA Label].
Protein binding Calcitriol is approximately 99.9% bound in blood, mostly by an alpha-globulin vitamin D binding protein [FDA Label].
Half life After administration of single oral doses, the elimination half life was 5-8 hours [FDA Label].
Absorption Upon administration, calcitriol is rapidly absorbed from the intestines. When a single oral dose of 0.5 mcg of calcitriol was administered, the mean serum concentrations of calcitriol rose from a baseline value of 40.0±4.4 (SD) pg/mL to 60.0±4.4 pg/mL at 2 hours, and declined to 53.0±6.9 at 4 hours, 50±7.0 at 8 hours, 44±4.6 at 12 hours and 41.5±5.1 at 24 hours [FDA Label]. Following administration of single doses of 0.25 to 1.0 mcg of calcitriol, the peak plasma concentrations were reached within 3 to 6 hours [FDA Label]. In a pharmacokinetic study, the oral bioavailability was 70.6±5.8% in healthy male volunteers and 72.2±4.8% in male patients with uraemia [A175726].

D

A

D05AX03 Calcitriol


[D05AX] Other antipsoriatics for topical use


[D05A] ANTIPSORIATICS FOR TOPICAL USE


[D05] ANTIPSORIATICS


[D] Dermatological drugs

A11CC04 Calcitriol


[A11CC] Vitamin D and analogues


[A11C] VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO


[A11] VITAMINS


[A] Alimentary tract and metabolism

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 14.06±4.15 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 15.45 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 22.41±7.17 rat hepatocytes MMP assay decrease IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 89 companies from 10 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H300 (100%): Fatal if swallowed [Danger Acute toxicity, oral]


H310 (96.63%): Fatal in contact with skin [Danger Acute toxicity, dermal]


H330 (49.44%): Fatal if inhaled [Danger Acute toxicity, inhalation]


H361 (98.88%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P201, P202, P260, P262, P264, P270, P271, P280, P281, P284, P301+P310, P302+P350, P304+P340, P308+P313, P310, P320, P321, P322, P330, P361, P363, P403+P233, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 intraperitoneal 1900ug/kg (1.9mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 11, Pg. 4175, 1983.
rat LD50 intravenous 105ug/kg (0.105mg/kg) Japanese Kokai Tokyo Koho Patents. Vol. #94-247858,
rat LD50 intraperitoneal > 5mg/kg (5mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 11, Pg. 4175, 1983.
rat LD50 subcutaneous 66ug/kg (0.066mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 11, Pg. 4175, 1983.
mouse LD50 oral 1350ug/kg (1.35mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 11, Pg. 4175, 1983.
mouse LD50 subcutaneous 145ug/kg (0.145mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 11, Pg. 4175, 1983.
rat LD50 oral 620ug/kg (0.62mg/kg) Japanese Kokai Tokyo Koho Patents. Vol. #94-247858,


  • (1?,3?,5Z,7E)-9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol (1R,3S)-5-{2-[(1R,3aS,7aR)-1-((R)-5-Hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexane-1,3-diol (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R)-5-hydroxy-1,5-dimethyl-hexyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylene-cyclohexane-1,3-diol
    (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol (1R,3S,Z)-5-((E)-2-((1R,3aS,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methylhexahydro-1H-inden-4(2H)-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol (1R,3S,Z)-5-(2-((1R,3aS,7aR,E)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol;
    (1S,3R,5Z,7E)-9,10-seco-5,7,10(19)-cholestatriene-1,3,25-triol (1S,3R,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
    (1S,3R,5Z,7E,14beta,17alpha)-9,10-secocholesta-5,7,10-triene-1,3,25-triol (1alpha,3beta,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol (3b,5Z,7E)-9,10-Secocholesta-5,7,10(19)-trienetriol
    (5Z,10-secocholesta-5,7,10(19)-triene-1.alpha.,3.beta.,25-triol (5Z,7E)-(1S,3R)-9,10-seco-5,7,10(19)-cholestatriene-1,3,25-triol (5Z,7E)-(1S,3R)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
    (5Z,7E)-9,10-Secocholesta-5,7,10(19)-triene-1-alpha,3-beta,25-triol (5Z,7E)-9,10-Secocholesta-5,7,10(19)-triene-1alpha,3beta,25-triol 1 alpha,25-Dihydroxyvitamin D3
    1,25 (OH)2 D3 1,25 DIHYDROXY VITAMIN D3 1,25 Dihydroxycholecalciferol
    1,25(OH)2-20epi-D3 1,25(OH)2D3 & CD4 1,25(OH2)D3
    1,25-(OH)2-D3 1,25-(OH)2D3 1,25-DHCC
    1,25-DIHYDROXYCHOLECALCIFEROL 1,25-Dihydroxycholecaliferol 1,25-Dihydroxyvitamin D
    1,25-Dihydroxyvitamin D3 1,25-dihydroxy vitamin D3 1,25-dihydroxy-20-epi-Vitamin D3
    1,25D3 1-alpha,-1,25-Dihydroxyvitamin D3 1-alpha,25-Dihydroxycholecalciferol
    1-alpha,25-Dihydroxyvitamin D3 1-alpha-25-dihydroxyvitamin D3 1.Alpha.,25-Dihydroxy-26,27-hexadeuterovitamin D3
    1.alpha.,25-Dihydroxyvitamin D(sub 3) 1.alpha.,25-dihydroxycholecalciferol 1a,25-(OH)2D3
    1a,25-Dihydroxycholecalciferol 1a,25-Dihydroxyvitamin D3 1alpha 25-dihydroxycholecalciferol
    1alpha,25(OH)2-D3 1alpha,25(OH)2D3 1alpha,25-Dihydroxycholecalciferol
    1alpha,25-Dihydroxyvitamin D 1alpha,25-Dihydroxyvitamin D3 1alpha,25-Dihydroxyvitamin D3, >=97.0% (HPLC)
    1alpha,25-Dihydroxyvitamin D3, >=99% (HPLC) 1alpha,25-dihydroxyvitamin D3 / 1alpha,25-dihydroxycholecalciferol / calcitriol 1db1
    1|A,25-Dihydroxyvitamin D3 20-epi-1alpha,25-dihydroxycholecaliferol 222C063
    25-dihydroxycholecalciferol 32222-06-3 5-{2-[1-(5-HYDROXY-1,5-DIMETHYL-HEXYL)-7A-METHYL-OCTAHYDRO-INDEN-4-YLIDENE]-ETHYLIDENE}-4-METHYLENE-CYCLOHEXANE-1,3-DIOL
    62019-EP2292592A1 62019-EP2298772A1 62019-EP2308828A2
    62019-EP2308839A1 9,10-Seco(5Z,7E)-5,7,10(19)-cholestatriene-1alpha,3beta,25-triol 9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol, (1.alpha.,3.beta,.5Z,7E)-
    9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol, (1.alpha.,3.beta,.5Z,7E)- & CD4 9,10-Secocholesta-5,7,10(19)-triene-1,3,25-triol, (1alpha,3beta,5Z,7E)- 9,10-seco(5Z,7E)-5,7,10(19)-cholestatriene-1alpha, 3beta, 25-triol
    AB00639957-06 AB00639957_07 AC-1859
    ACT06832 AKOS015961898 Asentar
    BCBcMAP01_000160 BCP9000474 BCPP000304
    BDBM50200182 BML2-E03 BRD-K27316855-001-06-7
    BRD-K27316855-001-19-0 BSPBio_001287 C01673
    CAS-32222-06-3 CCG-101001 CCRIS 5522
    CD-2027 CHEBI:17823 CHEBI:93988
    CHEMBL846 CPD000466393 CS-0388
    Calcijex Calcitriol (JAN/USP/INN) Calcitriol (Rocaltrol)
    Calcitriol [USAN:INN:BAN:JAN] Calcitriol [USAN:USP:INN:BAN:JAN] Calcitriol, European Pharmacopoeia (EP) Reference Standard
    Calcitriol-(Rocaltrol) Calcitriolum Calcitriolum [INN-Latin]
    Cholecalciferol, 1-alpha,25-dihydroxy- D00129 DB00136
    DN 101 DN-101 DSSTox_CID_2722
    DSSTox_GSID_22722 DSSTox_RID_76700 DTXSID5022722
    Decostriol Dihydroxyvitamin D3 EINECS 250-963-8
    FXC9231JVH GMRQFYUYWCNGIN-NKMMMXOESA-N GTPL2779
    HMS1361A09 HMS1791A09 HMS1989A09
    HMS2051F06 HMS2089N03 HMS2232D18
    HMS3402A09 HSDB 3482 HY-10002
    IDI1_033757 LMST03020258 LS-53093
    MC-1288 MC1288 MFCD00867079
    MLS000759536 MLS001424122 NC00251
    NCGC00161327-01 NCGC00161327-04 NSC-749776
    NSC749776 Panbonis PubChem18818
    PubChem19327 Q139195 RO215535
    Ro 21-5535 Ro 215535 Ro-21-5535
    Ro-215535 Rocaltrol Rocaltrol (TN)
    SC-17020 SCHEMBL3245 SMR000466393
    SR-01000759361 SR-01000759361-4 SR-01000946978
    SR-01000946978-1 Silkis Soltriol
    Spectrum5_002061 Synthetic vitamin D analog Topitriol
    Toptriol Tox21_111988 U 49562
    UNII-FXC9231JVH Vectical Vitamin D3, 1alpha, 25-Dihydroxy-
    W-5161 ZINC100015048 ZX-AFC000310
    calcitriol dihydroxy-vitamin D3 s1466
    vit D

    DrugBank Name calcitriol
    DrugBank DB00136
    CAS Number 1000873-74-4, 32222-06-3, 491-70-3, 66772-14-3
    PubChem Compound 5280453
    KEGG Compound ID C01673
    KEGG Drug D00129
    ChEBI 17823
    PharmGKB PA448717