19-Nor-9,10-secoergosta-5,7,22-triene-1,3,25-triol,(1a,3b,7E,22E)- (9CI) 19-Nor-1,25-dihydroxyvitamin D2 1a,25-Dihydroxy-19-nor-vitamin D2
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.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.
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.
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.
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1-alpha-hydroxy-19-noranalogue in which the ring A exocyclic methylene group, typical of all vitamin D systems, has been replaced by two hydrogen atoms.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.
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