Paricalcitol was launched as Zemplar in the US for the prevention and
treatment of secondary hyperthyroidism associated with chronic renal failure.
Paricalcitol is a synthetic vitamin D2, namely a novel 1-alpha-hydroxy-19-noranalogue
in which the ring A exocyclic methylene group, typical of all vitamin D
systems, has been replaced by two hydrogen atoms. Paricalcitol is the first
vitamin D analogue marketed for this indication. In patients with chronic renal
failure, Paricalcitol appreciably reduced levels of parathyroid hormone (PTH)
without a significant difference in the incidence rate for hypercalcemia or
hyperphosphatemia when compared with placebo.
Paricalcitol is a synthetic 1,25-dihydroxy vitamin D2 analog. As vitamin D deficiency, associated with chronic kidney disease, leads to an increase in parathyroid hormone (secondary hyperparathyroidism), paricalcitol is used in renal patients to block parathyroid hormone overproduction. Vitamin D deficiency is also a risk factor in cancer, cardiovascular disease, hypertension, and diabetes, and paricalcitol may have applications in those contexts as well.
1,25-Dihydroxy vitamin D2 is a potent agonist of the vitamin D receptor. Paricalcitol is a synthetic 1,25-dihydroxy vitamin D2 analog. As vitamin D deficiency, associated with chronic kidney disease, leads to an increase in parathyroid hormone (secondary hyperparathyroidism), paricalcitol is used in renal patients to block parathyroid hormone overproduction. Vitamin D deficiency is also a risk factor in cancer, cardiovascular disease, hypertension, and diabetes, and paricalcitol may have applications in those contexts as well.
Synthetic analog of vitamin D. Antihyperparathyroid.
ChEBI: Paricalcitol is a seco-cholestane and a hydroxy seco-steroid. It has a role as an antiparathyroid drug. It is functionally related to a vitamin D2.
Vitamin D analogue:
Treatment and prevention of secondary
hyperparathyroidism associated with chronic renal
failure
Extensively metabolised via hepatic and non-hepatic
pathways to form two relatively inactive metabolites.
After oral administration of 3
H-paricalcitol, only about
2% of the dose was eliminated unchanged in the faeces,
and no parent drug found in the urine.
Approximately
70% of the radioactivity was eliminated in the faeces and
18% was recovered in the urine. Most of the systemic
exposure was from the parent drug.
