Calcitriol
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| Pronunciation | US: /ˌkælsɪˈtraɪɒl/;[1][2][3][4][5] UK: /kælˈsɪtriɒl/ |
| Trade names | Rocaltrol, Calcijex, Decostriol, others |
| Other names | 1,25-dihydroxycholecalciferol, 1alpha,25-dihydroxyvitamin D3, 1,25-dihydroxyvitamin D3, 1α,25-(OH)2D3, 1,25(OH)2D[6] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682335 |
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| Routes of administration | By mouth, intravenous[7] |
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| Protein binding | 99.9% |
| Metabolism | Kidney |
| Elimination half-life | 5–8 hours (adults), 27 hours (children) |
| Excretion | Faeces (50%), urine (16%) |
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| ECHA InfoCard | 100.046.315 |
| Chemical and physical data | |
| Formula | C27H44O3 |
| Molar mass | 416.646 g·mol−1 |
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Calcitriol is a hormone and the active form of vitamin D, normally made in the kidney.[8][9][10] It is also known as 1,25-dihydroxycholecalciferol. It 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 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]
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 2022, it was the 254th most commonly prescribed medication in the United States, with more than 1 million 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.
- ^ a b c d e f g "Calcitriol Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 9 April 2019.
- ^ Plum LA, DeLuca HF (December 2010). "Vitamin D, disease and therapeutic opportunities". Nature Reviews. Drug Discovery. 9 (12): 941–955. doi:10.1038/nrd3318. PMID 21119732. S2CID 8894111.
- ^ Encyclopedia of Endocrine Diseases. Academic Press. 2018. p. 344. ISBN 978-0-12-812200-6.
- ^ "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.
- ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 1050–1051. ISBN 978-0-85711-338-2.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Calcitriol Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
- ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.