Calcidiol drug data and news

Calcidiol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Calcidiol
Brand Names/Synonyms Calcidiol; Calcifediol; Calcifediol Anhydrous; Calcifediolum [Inn-Latin]; Calcifidiol; Calderol; Delakmin
Indication 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.
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Description Not Available
Pharmacology Calcidiol is a form 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.
Mechanism Of Action 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.
Calcidiol News
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Dosage Forms CAPSULES
Drug_Category ATC:A11CC06; Antihypocalcemic Agents; Antihypoparathyroid Agents; Vitamins (Vitamin D)
Absorption Readily absorbed.
Interactions [an error occurred while processing this directive]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.
Organisms Affected Humans and other mammals
Chemical IUPAC Name 6-[4-[2-(5-hydroxy-2-methylidene-cyclohexylidene)ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]-2-methyl-heptan-2-ol
Chemical Formula C27H44O2
Molecular Weight 400.637 g/mol
Smiles String CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CCC3=C)O)C
Melting Point Not Available
Water Solubility Insoluble
State Solid
LogP/Hphobicity 5.785
Isoelectric Point Not Available
Biotransformation Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25-dihydroxycholecalciferol), the active form of vitamin D3.
Half Life 288 hours
Protein Binding [%] Not Available
RxList Link Not Available>RXlist
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Drug Reference http://www.drugs.com/cons/Calcifediol.html
http://www.pdrhealth.com/drug_info/nmdrugprofiles/nutsupdrugs/vit_0265.shtml
Drug Type Approved Drug
Accession No APRD00428
CAS Registry Number 19356-17-3
KEGG Compound ID C01561
PubChem ID SID:171856
PharmGKB ID PA452501
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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