Upacicalcet

A calcimimetic agent used in the treatment of secondary hyperparathyroidism

Upacicalcet
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Upacicalcet is a calcimimetic agent used primarily in the management of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) undergoing dialysis. It functions by modulating the activity of the calcium-sensing receptor (CaSR) on the parathyroid gland, thereby reducing the secretion of parathyroid hormone (PTH).

Mechanism of action

Upacicalcet acts as an allosteric modulator of the calcium-sensing receptor, which is a G-protein coupled receptor located on the surface of the parathyroid cells. By enhancing the sensitivity of the CaSR to extracellular calcium, upacicalcet effectively lowers PTH levels, which in turn helps to manage the mineral and bone disorder associated with CKD.

Clinical use

Upacicalcet is indicated for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease on dialysis. It is administered intravenously, typically during dialysis sessions, to ensure optimal control of PTH levels.

Side effects

Common side effects of upacicalcet include nausea, vomiting, and hypocalcemia. Patients receiving upacicalcet should be monitored for signs of low calcium levels, as severe hypocalcemia can lead to muscle cramps, seizures, and cardiac arrhythmias.

Pharmacokinetics

Upacicalcet is administered intravenously, allowing for rapid onset of action. It is metabolized primarily in the liver and excreted via the kidneys. The pharmacokinetic profile of upacicalcet supports its use in patients undergoing dialysis, as it is not significantly removed by the dialysis process.

Related pages

• Calcimimetic
• Secondary hyperparathyroidism
• Chronic kidney disease
• Dialysis
• Parathyroid hormone

• 
  Upacicalcet