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Description
Curator's Comment:: description was created based on several sources, including http://www.drugbank.ca/drugs/DB00169

Cholecalciferol (/ˌkoʊləkælˈsɪfərɒl/) (vitamin D3) is one of the five forms of vitamin D. Cholecalciferol 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 manifestation of vitamin D deficiency is rickets, which is seen in children and results in bony deformities including bowed long bones. Most people meet at least some of their vitamin D needs through exposure to sunlight. Ultraviolet (UV) B radiation with a wavelength of 290–320 nanometers penetrates uncovered skin and converts cutaneous 7-dehydrocholesterol to previtamin D3, which in turn becomes vitamin D3. In supplements and fortified foods, vitamin D is available in two forms, D2 (ergocalciferol) and D3 (cholecalciferol) that differ chemically only in their side-chain structure. Vitamin D2 is manufactured by the UV irradiation of ergosterol in yeast, and vitamin D3 is manufactured by the irradiation of 7-dehydrocholesterol from lanolin and the chemical conversion of cholesterol. The two forms have traditionally been regarded as equivalent based on their ability to cure rickets and, indeed, most steps involved in the metabolism and actions of vitamin D2 and vitamin D3 are identical. Both forms (as well as vitamin D in foods and from cutaneous synthesis) effectively raise serum 25(OH) D levels. Firm conclusions about any different effects of these two forms of vitamin D cannot be drawn. However, it appears that at nutritional doses, vitamins D2 and D3 are equivalent, but at high doses, vitamin D2 is less potent. The American Academy of Pediatrics (AAP) recommends that exclusively and partially breastfed infants receive supplements of 400 IU/day of vitamin D shortly after birth and continue to receive these supplements until they are weaned and consume ≥1,000 mL/day of vitamin D-fortified formula or whole milk. Cholecalciferol is used in diet supplementary to treat Vitamin D Deficiency. Cholecalciferol is inactive: it is converted to its active form by two hydroxylations: the first in the liver, the second in the kidney, to form calcitriol, whose action is mediated by the vitamin D receptor, a nuclear receptor which regulates the synthesis of hundreds of enzymes and is present in virtually every cell in the body. 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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
42 ng/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CALCIDIOL serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
968.6 nM × day
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CALCIDIOL serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
15.5 day
2.5 mg single, oral
dose: 2.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CALCIDIOL serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100000 unit single, oral
Highest studied dose
Dose: 100000 unit
Route: oral
Route: single
Dose: 100000 unit
Sources:
healthy, 27-84 years
n = 30
Health Status: healthy
Age Group: 27-84 years
Sex: M+F
Population Size: 30
Sources:
200 ug 1 times / day multiple, oral
Highest studied dose
Dose: 200 ug, 1 times / day
Route: oral
Route: multiple
Dose: 200 ug, 1 times / day
Sources:
healthy, 33.4 ± 6.6 years
n = 25
Health Status: healthy
Age Group: 33.4 ± 6.6 years
Sex: M+F
Population Size: 25
Sources:
100000 unit single, intramuscular
Dose: 100000 unit
Route: intramuscular
Route: single
Dose: 100000 unit
Sources:
healthy, 34.9 ± 9.1 years
n = 12
Health Status: healthy
Age Group: 34.9 ± 9.1 years
Sex: M+F
Population Size: 12
Sources:
2000000 unit single, oral
Overdose
Dose: 2000000 unit
Route: oral
Route: single
Dose: 2000000 unit
Sources:
unhealthy, 90-95 years
n = 2
Health Status: unhealthy
Age Group: 90-95 years
Sex: M+F
Population Size: 2
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
strong
yes [Ki 10 uM]
yes
Drug as victim
PubMed

PubMed

TitleDatePubMed
Vitamin D and the Pathogenesis of Inflammatory Bowel Disease.
2016 Oct
Human cytomegalovirus infection downregulates vitamin-D receptor in mammalian cells.
2017 Jan
Patents

Patents

Sample Use Guides

200,000 IU injection within 12 weeks.
Route of Administration: Intramuscular
Purified T lymphocytes from 14 patients with systemic lupus erythematosus (SLE) and 13 healthy controls were cultured for 48 h in the presence and absence of 1 and 100 nM doses of vitamin D3.
Name Type Language
VITAMIN D
GREEN BOOK   VANDF  
Common Name English
VITAMIN D NOS [WHO-DD]
Common Name English
VITAMIN D [GREEN BOOK]
Common Name English
VITAMIN D NOS
WHO-DD  
Common Name English
VITAMIN D [VANDF]
Common Name English
CALCIFEROL
Common Name English
VITAMIN D2 AND/OR VITAMIN D3
Common Name English
VITAMIN D, UNSPECIFIED FORM
Common Name English
Classification Tree Code System Code
LOINC 35365-6
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
CFR 21 CFR 101.72
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LOINC 49543-2
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DSLD 3566 (Number of products:54)
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CFR 21 CFR 184.1950
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CFR 21 CFR 862.1825
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WHO-ATC A11CC20
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LOINC 60493-4
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DSLD 3120 (Number of products:1638)
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
LIVERTOX 1036
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LOINC 47094-8
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LOINC 2236-8
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
DSLD 1538 (Number of products:430)
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
Code System Code Type Description
MESH
D014807
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
CAS
1406-16-2
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
FDA UNII
9VU1KI44GP
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
DRUG BANK
DB11094
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
EVMPD
SUB129580
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
ECHA (EC/EINECS)
215-797-2
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
EPA CompTox
1406-16-2
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
RXCUI
11253
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY RxNorm
LACTMED
Vitamin D
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
EVMPD
SUB06596MIG
Created by admin on Sat Jun 26 18:19:17 UTC 2021 , Edited by admin on Sat Jun 26 18:19:17 UTC 2021
PRIMARY
Any of these components may be present:
Definition References