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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.
The level of serum 1,25(OH)D (calcitriol) is not usually used to determine vitamin D status because it often is regulated by other hormones in the body such as parathyroid hormone. [53] The levels of 1,25(OH)D can remain normal even when a person may be vitamin D deficient. [ 53 ]
The natural, active form of vitamin D is calcitriol (1,25-dihydroxycholecalciferol). This molecule and other naturally occurring forms of vitamin D, including its precursors and metabolites, have been modified to synthesize pharmaceuticals with potentially greater, or selective, therapeutic actions.
Calcitriol enters cells and binds to the VDR which forms a complex with its coreceptor RXR and the activated VDR/RXR complex is translocated into the nucleus. [203] The VDR/RXR complex subsequently binds to vitamin D response elements (VDRE) which are specific DNA sequences adjacent to genes, numbers estimated as being in the thousands.
In 2022, it was the 38th most commonly prescribed medication in the United States, with more than 15 million prescriptions. [10] [11] Certain foods such as breakfast cereal and margarine have ergocalciferol added to them in some countries. [12] [13] It is on the World Health Organization's List of Essential Medicines. [14]
Alfacalcidol (or 1-hydroxycholecalciferol) is an analogue of vitamin D used for supplementation in humans and as a poultry feed additive.. Alfacalcidol has a weaker impact on calcium metabolism [3] and parathyroid hormone levels [4] than calcitriol; but significant effects on the immune system, including regulatory T cells. [5]
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 .
Calcium/cholecalciferol is a combination of a calcium salt and vitamin D 3 (cholecalciferol). It is used to prevent and treat lack of calcium and vitamin D in the elderly, as well for osteoporosis in combination with other medications.