A drug in a class of orally active, small molecules that
decrease the secretion of parathyroid hormone (PTH) by activating calcium receptors.
The secretion of PTH is normally regulated by the calcium-sensing receptor. Calcimimetic
agents increase the sensitivity of this receptor to calcium, which inhibits the
release of parathyroid hormone and lowers parathyroid hormone levels within a few
hours.
C alcimetics are used to treat hyperparathyroidism, a condition characterized
by the over-secretion of PTH that results when calcium receptors on parathyroid
glands fail to respond properly to calcium in the bloodstream. In March, 2004 the
US Food and Drug Administration (FDA) approved the drug cinacalcet (Sensipar), the
first calcimimetic, to treat to treat secondary hyperparathyroidism in patients
with chronic kidney disease on dialysis, and hypercalcemia in patients with parathyroid
cancer.
Elevated levels of PTH, the hallmark of secondary hyperparathyroidism, are associated
with altered metabolism of calcium and phosphorus, bone pain, fractures, and an
increased risk for cardiovascular death. Treatment with cinacalcet lowers serum
levels of PTH as well as the calcium x phosphorus ion product. The calcium x phosphorus
ion product is a measure of the amount of calcium and phosphorus in the blood, and
when elevated, causes harmful deposition of calcium in various parts of the body.
Hypercalcemia is associated with parathyroid carcinoma, a rare cancer that causes
significant elevations in serum calcium levels. Elevated levels of serum calcium
can cause mental confusion, lethargy, dehydration, nausea, vomiting, constipation,
and kidney damage.
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