Doxercalciferol
- Atc Codes:H05BX03
- CAS Codes:54573-75-0
- PHARMGKB ID:54573-75-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Hectorol.
Drug combinations
Chemistry
Doxercalciferol: C~28~H~44~O~2~. Mw: 412.65. (5Z,7E,22E)-9,10-Secoergosta-5,7,10(19),22-tetraene-1α,3β-diol. CAS-54573-75-0.
Pharmacologic Category
Vitamins; Vitamin D. (ATC-Code: H05BX03).
Mechanism of action
Doxercalciferol (1-α-hydroxyvitamin D~2~, 1-hydroxyvitamin D~2~), the 1-hydroxylated form of ergocalciferol, is a synthetic vitamin D analog. In the body, doxercalciferol is hydroxylated to the active moiety, 1,25-dihydroxyvitamin D~2~ (1,25-dihydroxyergocalciferol), via the hepatic CYP27 isoenzyme. This active form increases the intestinal absorption of dietary calcium and the renal tubular reabsorption of urinary calcium, and also modulates bone formation and resorption, in conjunction with parathyroid hormone.
Therapeutic use
Used for the treatment of secondary hyperparathyroidism in chronic kidney disease undergoing dialysis. Oral doxercalciferol is also used for the treatment of secondary hyperparathyroidism in patients with chronic renal disease (stage 3 and 4) who do not yet require maintenance dialysis (predialysis patients).
Pregnancy and lactiation implications
Reproduction studies in animals do not reveal teratogenic or fetotoxic effects. Not recommended during lactation (potential risk (e.g. hypercalcemia) in nursing infants).
Unlabeled use
Contraindications
Hypersensitivity to any component of the formulation. Risk or history of hypercalcemia or hyperphosphatemia. Evidence of vitamin D toxicity.
Warnings and precautions
Hypercalcemia may occur with vitamin D analog toxicity. Acute hypercalcemia may increase the risk of cardiac arrhythmias and seizures, as well as having synergistic inotropic and toxic effects in the presence of cardiac glycosides. Chronic hypercalcemia increases the risk of soft-tissue calcification, including in the vasculature. Vitamin D and its analogs should not be used during doxercalciferol therapy (possible additive effects). Hyperphosphatemia may occur with vitamin D analog toxicity. Hyperphosphatemia exacerbates secondary hyperparathyroidism and diminishes efficacy of doxercalciferol in iPTH suppression. Excessive suppression of iPTH may result in adynamic bone syndrome. Magnesium-containing antacids should not be used concomitantly with doxercalciferol. Doxercalciferol should not be used for the treatment of nutritional vitamin D deficiency. Hypercalciuria can accelerate the onset of renal failure through nephrocalcinosis. Use with caution in hepatic impairment since doxercalciferol may not be metabolized appropriately.