Calcidiol

Calcidiol Uses, Dosage, Side Effects, Food Interaction and all others data.

The major circulating metabolite of vitamin D3 (cholecalciferol). It is produced in the liver and is the best indicator of the body's vitamin D stores. It is effective in the treatment of rickets and osteomalacia, both in azotemic and non-azotemic patients. Calcidiol also has mineralizing properties.

Calcidiol is the precursor of vitamin D3. Vitamin D3 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 manifestations of vitamin D deficiency is rickets, which is seen in children and results in bony deformaties including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix, and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease, and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium and phosphorus mobilization from bone to plasma.

Trade Name Calcidiol
Availability Prescription only
Generic Calcifediol
Calcifediol Other Names 25-hydroxycholecalciferol, 25-Hydroxyvitamin D3, Calcidiol, Calcifediol, Calcifédiol, Calcifediolum
Related Drugs calcitriol, ergocalciferol, calcium carbonate, Caltrate, Drisdol, Rocaltrol, Rayaldee, Parsabiv, etelcalcetide
Type
Formula C27H44O2
Weight Average: 400.6371
Monoisotopic: 400.334130652
Groups Approved, Nutraceutical
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Calcidiol
Calcidiol

Uses

Calcidiol is an active metabolite of vitamin D used to treat hyperparathyroidism as well as to combat hypocalcemia in dialysis patients.

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.

Calcidiol is also used to associated treatment for these conditions: Secondary Hyperparathyroidism (SHPT)

How Calcidiol works

Calcidiol is transformed in the kidney by 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to calcitriol, the active form of vitamin D3. Calcitriol binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. 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.

Toxicity

Bone pain, constipation (especially in children or adolescents), diarrhea, drowsiness, dryness of mouth; headache (continuing), increased thirst, increase in frequency of urination, especially at night, or in amount of urine, irregular heartbeat, itching skin, loss of appetite, metallic taste, muscle pain, nausea or vomiting (especially in children or adolescents), unusual tiredness or weakness.

Food Interaction

  • Take with or without food. A high-fat, high-calorie meal may increase the AUC and Cmax of calcifediol by up to 3.5 and 5 fold, respectively.

Elimination Route

Readily absorbed.

Half Life

288 hours

Innovators Monograph

You find simplified version here Calcidiol

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000012
http://classyfire.wishartlab.com/tax_nodes/C0000258
http://classyfire.wishartlab.com/tax_nodes/C0001460
http://classyfire.wishartlab.com/tax_nodes/C0001460
http://classyfire.wishartlab.com/tax_nodes/C0001553
http://classyfire.wishartlab.com/tax_nodes/C0001670
http://classyfire.wishartlab.com/tax_nodes/C0001661
http://classyfire.wishartlab.com/tax_nodes/C0001292
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:17933
http://www.genome.jp/dbget-bin/www_bget?cpd:C01561
http://www.lipidmaps.org/data/LMSDRecord.php?LMID=LMST03020246
http://www.hmdb.ca/metabolites/HMDB0003550
http://www.genome.jp/dbget-bin/www_bget?cpd:C01561
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5283731
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505690
https://www.chemspider.com/Chemical-Structure.4446820.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50521013
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=1855064
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=17933
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1040
https://zinc.docking.org/substances/ZINC000004474414
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000290
http://www.pharmgkb.org/drug/PA164745614
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/VDY
http://www.pdrhealth.com/drug_info/nmdrugprofiles/nutsupdrugs/vit_0265.shtml
https://en.wikipedia.org/wiki/Calcifediol
*** Taking medicines without doctor's advice can cause long-term problems.
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