Calcitriol
Active form of vitamin D / From Wikipedia, the free encyclopedia
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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]
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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 |
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Formula | C27H44O3 |
Molar mass | 416.646 g·mol−1 |
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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 1 million prescriptions.[13][14] It is on the World Health Organization's List of Essential Medicines.[15]