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Calcitriol
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DRUG INFO
Calcitriol
Drug Name:
Calcitriol
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.
Pharmacology: Calcitriol, a pharmaceutical form of vitamin D, has anti-osteoporotic, immunomodulatory, anticarcinogenic, antipsoriatic, antioxidant, and mood-modulatory activities. Calcitriol has been found to be effective in the treatment of psoriasis when applied topically. Calcitriol has been found to induce differentiation and/or inhibit cell proliferation in a number of malignant cell lines including human prostate cancer cells. Vitamin D deficiency has long been suspected to increase the susceptibility to tuberculosis. The active form of Calcitriol, 1,25 (OH)2 D, has been found to enhance the ability of mononuclear phagocytes to suppress the intracellular growth of Mycobacterium tuberculosis. 1,25(OH)2D has demonstrated beneficial effects in animal models of such autoimmune diseases as rheumatoid arthritis. It has also been found to induce monocyte differentiation and to inhibit lymphocyte proliferation and production of cytokines, including interleukin IL-1 and IL-2, as well as to suppress immunoglobulin secretion by B lymphocytes. Vitamin D appears to demonstrate both immune-enhancing and immunosuppressive effects.
Mechanism Of Action: The mechanism of action of Calcitriol in the treatment of psoriasis is accounted for by their antiproliferative activity for keratinocytes and their stimulation of epidermal cell differentiation. The anticarcinogenic activity of the active form of Calcitriol appears to be correlated with cellular vitamin D receptor (VDR) levels. Vitamin D receptors belong to the superfamily of steroid-hormone zinc-finger receptors. VDRs selectively bind 1,25(OH)2D and retinoic acid X receptor (RXR) to form a heterodimeric complex that interacts with specific DNA sequences known as vitamin D-responsive elements. VDRs are ligand-activated transcription factors. The receptors activate or repress the transcription of target genes upon binding their respective ligands. It is thought that the anticarcinogenic effect of Calcitriol is mediated via VDRs in cancer cells. The immunomodulatory activity of Calcitriol is thought to be mediated by vitamin D receptors (VDRs) which are expressed constitutively in monocytes but induced upon activation of T and B lymphocytes. 1,25(OH)2D has also been found to enhance the activity of some vitamin D-receptor positive immune cells and to enhance the sensitivity of certain target cells to various cytokines secreted by immune cells.
Drug Category: ATC:A11CC04; ATC:D05AX03; Antihypocalcemic Agents; Antihypoparathyroid Agents; Essential Vitamin; Vitamins (Vitamin D)
Brand Names/Synonyms: Calcijex; Calcitriol; Rocaltrol
Dosage Forms: Capsule, solution
Absorption: Rapidly absorbed from the intestine.
Interactions: [an error occurred while processing this directive]
Chemical IUPAC Name: 5-[2-[1-(6-hydroxy-6-methyl-heptan-2-yl)-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidene-cyclohexane-1,3-diol
Chemical Formula: C27H44O3
Half Life: 5-8 hours
Drug Type: Approved Drug
# Accession No: APRD00246
CAS Registry Number: 32222-06-3
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Calcitriol News
(When available)
Teva and Ivax Cleared to Complete Merger Jan 27, 2006
...generic distribution relationships that Ivax had with respect to certain amoxicillin, amoxicillin and clavulanate, leuprolide, and calcitriol products have ... - International News Service,
FTC gives Ivax and Teva final go-ahead for merger Jan 23, 2006
...the companies said generic distribution relationships Ivax had for certain amoxicillin, amoxicillin and clavulanate, leuprolide, and calcitriol products have ... - South Florida Business Journal,
Sapphire Therapeutics, Inc. Appoints New Director and Scientific ... Jan 17, 2006
The second drug, RC-8800, is a small molecule that acts on the vitamin D (calcitriol) metabolic pathway, being developed as a treatment for various cancers ... - Genetic Engineering News,
Preserving Competition, FTC Requires Divestitures Before Allowing ... Jan 23, 2006
...tablets from Teva, to be divested to Barr; 13) glipizide and metformin hydrochloride tablets from IVAX, to be divested to Barr; 14) calcitriol injectables from ... - PharmaLive.com (press release),
Sapphire Therapeutics, Inc. Builds Drug Development Team Through ... Jan 9, 2006
The second drug, RC-8800, a small molecule that acts on the vitamin D (calcitriol) metabolic pathway, is being developed as a treatment for various cancers ... - dBusinessNews Newark (press release),
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