Upacicalcet: Difference between revisions

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'''Upacicalcet''' is a novel [[pharmaceutical drug]] currently under development for the treatment of [[hyperparathyroidism]] and [[hypercalcemia]] associated with [[chronic kidney disease]] (CKD). It is a [[calcimimetic]] agent, designed to mimic the action of calcium on tissues, particularly the [[parathyroid gland]].
{{Short description|A calcimimetic agent used in the treatment of secondary hyperparathyroidism}}
{{Drugbox
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| image = Upacicalcet.svg
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| image_alt = Structural formula of Upacicalcet
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== Mechanism of Action ==
'''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).


Upacicalcet works by binding to and activating the [[calcium-sensing receptor]] (CaSR) on the parathyroid gland. This receptor is responsible for detecting the level of calcium in the blood. When activated by upacicalcet, the CaSR signals the parathyroid gland to reduce the production and release of [[parathyroid hormone]] (PTH), which in turn helps to lower blood calcium levels.
==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 Trials ==
==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.


Several [[clinical trial]]s have been conducted to assess the safety and efficacy of upacicalcet. These trials have shown promising results, with upacicalcet demonstrating a significant reduction in PTH and serum calcium levels in patients with secondary hyperparathyroidism due to CKD.
==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]].


== Potential Benefits ==
==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.


Upacicalcet may offer several potential benefits over existing treatments for hyperparathyroidism and hypercalcemia. These include a more targeted mechanism of action, the potential for fewer side effects, and the possibility of improved patient compliance due to its oral administration.
==Related pages==
* [[Calcimimetic]]
* [[Secondary hyperparathyroidism]]
* [[Chronic kidney disease]]
* [[Dialysis]]
* [[Parathyroid hormone]]


== Side Effects ==
[[Category:Calcimimetics]]
 
[[Category:Drugs used in nephrology]]
As with any medication, upacicalcet may cause side effects. These can include [[nausea]], [[vomiting]], [[diarrhea]], and [[hypocalcemia]] (low calcium levels). However, these side effects are generally mild and manageable.
<gallery>
 
File:Upacicalcet.svg|Upacicalcet
== Future Directions ==
</gallery>
 
Further research is needed to fully understand the potential benefits and risks of upacicalcet. This includes additional clinical trials and long-term studies to assess the drug's safety and efficacy over time.
 
[[Category:Pharmaceutical Drugs]]
[[Category:Endocrinology]]
[[Category:Nephrology]]
 
{{medicine-stub}}

Latest revision as of 01:35, 20 February 2025

A calcimimetic agent used in the treatment of secondary hyperparathyroidism


Upacicalcet
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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[edit]

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[edit]

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[edit]

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[edit]

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[edit]