Upacicalcet

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A calcimimetic drug used in the treatment of secondary hyperparathyroidism


Upacicalcet
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CAS Number 123456-78-9
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Upacicalcet is a calcimimetic drug used primarily in the management of secondary hyperparathyroidism in patients undergoing dialysis for chronic kidney disease.

Mechanism of Action

Upacicalcet functions as a calcimimetic agent, which means it mimics the action of calcium on tissues. It acts by binding to the calcium-sensing receptor (CaSR) on the surface of the parathyroid gland cells. This binding increases the sensitivity of the receptor to extracellular calcium, thereby reducing the secretion of parathyroid hormone (PTH). Lower levels of PTH help to manage the mineral and bone disorder associated with chronic kidney disease.

Clinical Use

Upacicalcet is indicated for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. It is administered intravenously, typically during dialysis sessions. The dosage is adjusted based on the patient's response and serum calcium levels.

Side Effects

Common side effects of upacicalcet include nausea, vomiting, and hypocalcemia. Hypocalcemia, or low blood calcium levels, is a significant concern and requires monitoring. Patients may also experience muscle spasms or tingling sensations due to low calcium levels.

Pharmacokinetics

Upacicalcet is administered intravenously, allowing for direct entry into the bloodstream. It is metabolized in the liver and excreted primarily through the kidneys. The pharmacokinetic profile supports its use during dialysis sessions, as it can be effectively cleared from the body.

Regulatory Status

Upacicalcet has been approved for use in several countries for the treatment of secondary hyperparathyroidism in dialysis patients. Its approval is based on clinical trials demonstrating its efficacy in reducing PTH levels and managing associated symptoms.

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