Vitamin D analogs: Actions and role in the treatment of secondary hyperparathyroidism
Section snippets
Paricalcitol
This vitamin D analog, also known as 19-nor-1,25-dihydroxyvitamin D2, was studied extensively and shown to be effective in suppressing PTH, with markedly lesser effects on increasing the levels of serum calcium or phosphorus.13 In experimental animals, paricalcitol effectively decreased the levels of PTH and was found to be 10 times less active than calcitriol in mobilizing calcium or phosphate from bone.14 Thus, this vitamin D analog could achieve a dissociation of the PTH suppressive effect
22-oxacalcitriol
22-oxacalcitriol is a vitamin D analog based on the vitamin D3 structure. The structural modification of insertion of an oxygen in the 22 position results in a decreased binding affinity of 22-oxacalcitriol for the vitamin D receptor, as well as for vitamin D–binding protein.22, 23, 24 The decreased binding to vitamin D–binding protein results in a very rapid clearance from the circulation. This phenomenon potentially may account for the apparent lesser toxicities of this vitamin D analog in
Falecalcitriol
Falecalcitriol is a vitamin D analog that has the substitution of hydrogen with fluorine at carbons 26 and 27. This modification results in prolonged biological activity owing to decreased metabolism of the vitamin D analog.30 In limited clinical studies, this analog also has been shown to effectively suppress hyperparathyroidism and is currently in clinical use.31
Vitamin D prohormones
The vitamin D prohormones, 1-α-hydroxyvitamin D3 (alfacalcidol) and 1-α-hydroxyvitamin D3 (doxercalciferol) are also in clinical use for the therapy of hyperparathyroidism. 1-α-hydroxyvitamin D2 has been in clinical use for a number of years and is used widely outside the United States.32, 33, 34, 35, 36 This vitamin D sterol becomes 25-hydroxylated in the liver after entry into the circulation and, therefore, becomes 1, 25-dihydroxyvitamin D3. This sterol has been shown to have similar
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2012, Journal of Steroid Biochemistry and Molecular BiologyCitation Excerpt :The in vitro beneficial effects of these vitamin D analogs on the inflammatory process support the clinical findings reported in the literature [23,35,36]. Calcitriol suppresses PTH synthesis and secretion via VDR [22]. In addition, calcitriol was found to play an important role in renal, endothelial, and cardiovascular protection and to have antitumor activity [19,18].
Cardiorenal syndrome and vitamin D receptor activation in chronic kidney disease
2012, Kidney Research and Clinical PracticeCitation Excerpt :Some guidelines suggest correcting reduced 25-(OH)-D concentrations in CKD patients with an estimated GFR<60 mL/min/1.73 m2. Calcitriol and its analogs including vitamin D mimetics that activate VDR directly are commonly used to manage hyperparathyroidism secondary to CKD [94]. It has been shown that vitamin D3 supplementation reduces BP in patients with essential hypertension [95,96].
FGF23/Klotho new regulators of vitamin D metabolism
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