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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.
Calcitriol (1,25-dihydroxycholecalciferol) is the active form of vitamin D 3. [10] It has numerous functions involved in blood calcium levels. Recent research indicates that calcitriol leads to a reduction in osteoclast formation, and bone resorption.
Eldecalcitol is an analog of calcitriol, the active form of vitamin D. [1]Commonly used in Japan for the treatment of osteoporosis. [2] Osteoporosis is a common bone disease among the older generation, with an estimated prevalence of over 200 million people. [2]
Calcitriol plays a key role in regulating vitamin D levels through a negative feedback mechanism. [203] It strongly upregulates the expression of the enzyme CYP24A1 , which inactivates vitamin D. This activation happens through binding of the activated vitamin D receptor (VDR) to two vitamin D response elements (VDREs) in the in the CYP24A1 gene.
Mapping of several bone diseases onto levels of vitamin D (calcidiol) in the blood [6] Normal bone vs. osteoporosis. Vitamin D deficiency is typically diagnosed by measuring the concentration of the 25-hydroxyvitamin D in the blood, which is the most accurate measure of stores of vitamin D in the body.
Because of the high prevalence of vitamin D deficiency alongside the ageing of Australia's population, conditions such as osteoporosis have become widespread among Australians over 60. Osteoporosis can be defined as very fragile and brittle bones, in which serious fractures can occur with just the slightest bump or fall. [ 7 ]
Rickets in children is similar to osteoporosis in the elderly, with brittle bones. Pre-natal care includes checking vitamin levels and ensuring that any deficiencies are supplemented. [23] Exclusively breast-fed infants may require rickets prevention by vitamin D supplementation or an increased exposure to sunlight. [24]
The vitamin D receptor (VDR also known as the calcitriol receptor) is a member of the nuclear receptor family of transcription factors. [5] Calcitriol (the active form of vitamin D , 1,25-(OH) 2 vitamin D 3 ) binds to VDR, which then forms a heterodimer with the retinoid-X receptor .