Calcitriol is the active form of vitamin D, normally made in the kidney.[8][9][10] It is also known as 1,25-dihydroxycholecalciferol. It is a hormone which binds to and activates the vitamin D receptor in the nucleus of the cell, which then increases the expression of many genes.[11] Calcitriol increases blood calcium (Ca2+) mainly by increasing the uptake of calcium from the intestines.[7]
It can be given as a medication for the treatment of low blood calcium and hyperparathyroidism due to kidney disease, low blood calcium due to hypoparathyroidism, osteoporosis, osteomalacia, and familial hypophosphatemia,[7][12] and can be taken by mouth or by injection into a vein.[7] Excessive amounts or intake can result in weakness, headache, nausea, constipation, urinary tract infections, and abdominal pain.[7][12] Serious side effects may include high blood calcium and anaphylaxis.[7] Regular blood tests are recommended after the medication is started and when the dose is changed.[12]
Calcitriol was identified as the active form of vitamin D in 1971 and the drug was approved for medical use in the United States in 1978.[7] It is available as a generic medication.[12] In 2021, it was the 258th most commonly prescribed medication in the United States, with more than 1million prescriptions.[13][14] It is on the World Health Organization's List of Essential Medicines.[15]
^Elsevier, Dorland's Illustrated Medical Dictionary, Elsevier.
^Wolters Kluwer, Stedman's Medical Dictionary, Wolters Kluwer.
^Merriam-Webster, Merriam-Webster's Medical Dictionary, Merriam-Webster.
^Houghton Mifflin Harcourt, The American Heritage Dictionary of the English Language, Houghton Mifflin Harcourt, archived from the original on 25 September 2015, retrieved 25 September 2015.
^Merriam-Webster, Merriam-Webster's Unabridged Dictionary, Merriam-Webster, archived from the original on 25 May 2020, retrieved 25 September 2015.
^"IUPAC-IUB Joint Commission on Biochemical Nomenclature (JCBN): Nomenclature of vitamin D. Recommendations 1981". European Journal of Biochemistry. 124 (2): 223–227. May 1982. doi:10.1111/j.1432-1033.1982.tb06581.x. PMID 7094913.
^ abcdefg"Calcitriol Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 9 April 2019.
^Encyclopedia of Endocrine Diseases. Academic Press. 2018. p. 344. ISBN 9780128122006.
^"Office of Dietary Supplements - Vitamin D". ods.od.nih.gov. 9 October 2020. Retrieved 31 October 2020.
^Norman AW (August 2008). "From vitamin D to hormone D: fundamentals of the vitamin D endocrine system essential for good health". The American Journal of Clinical Nutrition. 88 (2): 491S–499S. doi:10.1093/ajcn/88.2.491S. PMID 18689389.
^ abcdBritish national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 1050–1051. ISBN 9780857113382.
^"The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
^"Calcitriol - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
^World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02. Archived (PDF) from the original on 23 January 2024.
Calcitriol is the active form of vitamin D, normally made in the kidney. It is also known as 1,25-dihydroxycholecalciferol. It is a hormone which binds...
immune system cells to form calcitriol (1,25-dihydroxycholecalciferol), the biologically active form of vitamin D. Calcitriol circulates as a hormone in...
calcifediol (25-hydroxyvitamin D) which is then converted in the kidney to calcitriol (1,25-dihydroxyvitamin D). One of its actions is to increase calcium uptake...
regulated by the calcitriol (or 1,25 dihydroxycholecalciferol, or 1,25 dihydroxyvitamin D3) concentration in the blood. Calcitriol is a cholesterol derivative...
Vitamin D5 (sitocalciferol) is a form of vitamin D. Analogs of calcitriol, a form of vitamin D3, have been proposed for use as antitumor agents. Studies...
by the enzyme 25(OH)D-1α-hydroxylase, primarily in the kidney, to form calcitriol (1,25-(OH)2D3), which is the active hormonal form of vitamin D. Calcifediol...
For example, they convert a precursor of vitamin D to its active form, calcitriol; and synthesize the hormones erythropoietin and renin. Chronic kidney...
receptor (VDR also known as the calcitriol receptor) is a member of the nuclear receptor family of transcription factors. Calcitriol (the active form of vitamin...
weaker impact on calcium metabolism and parathyroid hormone levels than calcitriol; but significant effects on the immune system, including regulatory T...
27-tetranorvitamin D3) is a major metabolite of 1α,25-dihydroxyvitamin D3 (calcitriol). Around 1980, scientists first reported the isolation of calcitroic acid...
Calcipotriol, also known as calcipotriene, is a synthetic derivative of calcitriol, a form of vitamin D. It is used in the treatment of psoriasis. It is...
the conversion of 25-hydroxy vitamin D into 1,25-dihydroxy vitamin D (calcitriol), which is released into the circulation. This latter form of vitamin...
to elevated levels of plasma calcium, and thus lower bone resorption. Calcitriol (1,25-dihydroxycholecalciferol) is the active form of vitamin D3. It has...
calcium-phosphate product, medications such as warfarin, vitamin D derivatives (e.g. calcitriol, calcium-based binders, or systemic steroids), protein C or S deficiency...
calcitriol activated VDR, in turn, upregulates PLC-γ1 expression. Hence the activation of naive T cells is crucially dependent on adequate calcitriol...
Long-term treatment of hypoparathyroidism is with vitamin D analogs (such as calcitriol or alfacalcidol), vitamin D supplementation and calcium supplementation...
into circulation, and increases in the activation of vitamin D3 to calcitriol. Calcitriol, the active form of vitamin D3, promotes absorption of calcium from...
modifications. They aim to reduce the classical renal and intestinal effects of calcitriol on calcium and phosphate homeostasis, from its effects on other biologic...
thyroid hormone (T3) (thyroid hormone receptors), calcitriol (the active form of vitamin D) (calcitriol receptors), and the retinoids (vitamin A) (retinoid...
The kidneys secrete a variety of hormones, including erythropoietin, calcitriol, and renin. Erythropoietin is released in response to hypoxia (low levels...
to the production of red blood cells by the kidney. Helps synthesize calcitriol (the active form of Vitamin D). Stores waste products (mainly urea and...
antidote, acetylcysteine. Calcitriol, the active metabolite of vitamin D3, appears to be a catalyst for glutathione production. Calcitriol was found to increase...
concentration of ≈750 nmol/L) propose that: Intake of vitamin D raises calcitriol concentrations in the plasma and cell Intake of vitamin D raises plasma...
(also referred to as calcitriol) improves the ability of macrophages to kill bacteria; however, higher levels of calcitriol lead to higher calcium levels...
elevated parathyroid hormone (hyperparathyroidism) Suppressed calcitriol levels Calcium and Calcitriol supplements, the latter with a larger dose than for treatment...