Description

Simple

A medication found in many nutritional supplements and multivitamins that is used to treat conditions related to low vitamin D levels.

Clinical

A form of Vitamin D used in the treatment of specific medical conditions such as refractory rickets, hypoparathyroidism, and familial hypophosphatemia, as well as osteoporosis and chronic kidney disease.

Overview

Vitamin D, in general, is a secosteroid generated in the skin when 7-dehydrocholesterol located there interacts with ultraviolet irradiation - like that commonly found in sunlight [9]. Both the endogenous form of vitamin D (that results from 7-dehydrocholesterol transformation), vitamin D3 (cholecalciferol), and the plant-derived form, vitamin D2 (ergocalciferol), are considered the main forms of vitamin d and are found in various types of food for daily intake [9]. Structurally, ergocalciferol differs from cholecalciferol in that it possesses a double bond between C22 and C23 and has an additional methyl group at C24 [9]. Finally, ergocalciferol is pharmacologically less potent than cholecalciferol, which makes vitamin D3 the preferred agent for medical use [Read more

Pharmacology

Indication

Cholecalciferol use is indicated for the treatment of specific medical conditions like refractory rickets (or vitamin D resistant rickets), hypoparathyroidism, and familial hypophosphatemia [12 Read more

Pharmacodynamic

The in vivo synthesis of the predominant two biologically active metabolites of vitamin D occurs in two steps. The first hydroxylation of vitamin D3 cholecalciferol (or D2) occurs in the liver to yield 25-hydroxyvitamin D while the second hydroxylation happens in the kidneys to give 1, 25-dihydroxyv... Read more

Mechanism of action

Most individuals naturally generate adequate amounts of vitamin D through ordinary dietary intake of vitamin D (in some foods like eggs, fish, and cheese) and natural photochemical conversion of the vitamin D3 precursor 7-dehydrocholesterol in the skin via exposure to sunlight [ Read more

Absorption

Cholecalciferol is readily absorbed from the small intestine if fat absorption is normal [12, Read more

Protein binding

The protein binding documented for cholecalciferol is 50 to 80% [8]. Specifically, i... Read more

Volume of distribution

Studies have determined that the mean central volume of distribution of administered cholecalciferol supplementation in a group of 49 kidney transplant patients was approximately 237 L [ Read more

Clearance

Studies have determined that the mean clearance value of administered cholecalciferol supplementation in a group of 49 kidney transplant patients was approximately 2.5 L/day [ Read more

Half life

At this time, there have been resources that document the half-life of cholecalciferol as being about 50 days [ Read more

Route of elimination

It has been observed that administered cholecalciferol and its metabolites are excreted primarily in the bile and feces [ Read more

Toxicity

Chronic or acute administration of excessive doses of cholecalciferol may lead to hypervitaminosis D, manifested by hypercalcemia and its sequelae [12, Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • Vitamin D or any of its analogues and derivatives.
  • Sex Group: all
  • Regions: US
  • Sex Group: all
  • Regions: US
  • Patient Conditions:
      • Name: Hypervitaminosis D
      • Drugbank Id: DBCOND0015762
  • Sex Group: all
  • Regions: US
  • Patient Conditions:
      • Name: Abnormal sensitivity to the toxic effects of vitamin D
      • Drugbank Id: DBCOND0107478
  • Sex Group: all
  • Regions: US
  • Patient Conditions:
      • Name: Malabsorption Syndrome
      • Drugbank Id: DBCOND0038388
  • Sex Group: all
  • Regions: US
  • Patient Conditions:
      • Name: Hypercalcemia
      • Drugbank Id: DBCOND0003950

Food Interactions

  • Take on an empty stomach. Must be taken 30 minutes before the first food, beverage, or medication of the day.

Interactions

Type in a drug name to check for interaction with Cholecalciferol
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1alpha-Hydroxyvitamin D5
The risk or severity of adverse effects can be increased when Cholecalciferol is combined with 1alpha-Hydroxyvitamin D5.
1alpha,24S-Dihydroxyvitamin D2
The risk or severity of adverse effects can be increased when Cholecalciferol is combined with 1alpha,24S-Dihydroxyvitamin D2.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Cholecalciferol.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Cholecalciferol.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Cholecalciferol.
Acetaminophen
The metabolism of Cholecalciferol can be decreased when combined with Acetaminophen.
Acetyldigitoxin
The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Acetyldigitoxin.
Acetyldigoxin
The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Acetyldigoxin.
Aldosterone
The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Aldosterone.
Alfacalcidol
The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Alfacalcidol.
Almotriptan
The metabolism of Almotriptan can be decreased when combined with Cholecalciferol.
Alogliptin
The metabolism of Alogliptin can be decreased when combined with Cholecalciferol.
Alprenolol
The metabolism of Alprenolol can be decreased when combined with Cholecalciferol.
Aluminum hydroxide
The serum concentration of Aluminum hydroxide can be increased when it is combined with Cholecalciferol.
Aminophenazone
The metabolism of Aminophenazone can be decreased when combined with Cholecalciferol.
Amiodarone
The metabolism of Amiodarone can be decreased when combined with Cholecalciferol.
Amitriptyline
The metabolism of Amitriptyline can be decreased when combined with Cholecalciferol.
Amoxapine
The metabolism of Amoxapine can be decreased when combined with Cholecalciferol.
Amphetamine
The metabolism of Amphetamine can be decreased when combined with Cholecalciferol.
Amprenavir
The metabolism of Amprenavir can be decreased when combined with Cholecalciferol.
15 References
  1. 1 . Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91.PubMed: 15531486
  2. 2 . Jean G, Souberbielle JC, Chazot C: Vitamin D in Chronic Kidney Disease and Dialysis Patients. Nutrients. 2017 Mar 25;9(4). pii: nu9040328. doi: 10.3390/nu9040328.PubMed: 28346348
  3. 3 . Heaney RP: Alendronate plus cholecalciferol for the treatment of osteoporosis. Womens Health (Lond). 2006 Jan;2(1):23-7. doi: 10.2217/17455057.2.1.23.PubMed: 19803923
  4. 4 . DeLuca HF: Overview of general physiologic features and functions of vitamin D. Am J Clin Nutr. 2004 Dec;80(6 Suppl):1689S-96S.PubMed: 15585789
  5. 5 . Benaboud S, Urien S, Thervet E, Prie D, Legendre C, Souberbielle JC, Hirt D, Friedlander G, Treluyer JM, Courbebaisse M: Determination of optimal cholecalciferol treatment in renal transplant recipients using a population pharmacokinetic approach. Eur J Clin Pharmacol. 2013 Mar;69(3):499-506. doi: 10.1007/s00228-012-1378-3. Epub 2012 Aug 31.PubMed: 22936122
  6. 6 . Jones KS, Assar S, Harnpanich D, Bouillon R, Lambrechts D, Prentice A, Schoenmakers I: 25(OH)D2 half-life is shorter than 25(OH)D3 half-life and is influenced by DBP concentration and genotype. J Clin Endocrinol Metab. 2014 Sep;99(9):3373-81. doi: 10.1210/jc.2014-1714. Epub 2014 Jun 2.PubMed: 24885631
  7. 7 . Borel P, Caillaud D, Cano NJ: Vitamin D bioavailability: state of the art. Crit Rev Food Sci Nutr. 2015;55(9):1193-205. doi: 10.1080/10408398.2012.688897.PubMed: 24915331
  8. 8 . Caroline Ashley, Aileen Dunleavy (2018). The Renal Drug Handbook: The Ultimate Prescribing Guide for Renal Practitioners, 5th Edition (5th ed.). CRC Press.
  9. 9 . Cholecalciferol (Vitamin D3) – Pharmacological Properties, Therapeutic Utility and Potential New Fields of Clinical Application by Yulian Voynikov, Georgi Momekov, Plamen Peikov Link
  10. 10 . Vitamin D Supplementation: An Update Link
  11. 11 . NIH Vitamin D Fact Sheet for Health Professionals Link
  12. 12 . Cholecalciferol Canadian Prescribing Information File
  13. 13 . Decalcitrol (coated cholecalciferol tablet) US FDA Monograph File
  14. 14 . CLH Report for Cholecalciferol File
  15. 15 . Alendronate sodium and cholecalciferol Canadian Product Monograph File