Upacicalcet: Difference between revisions

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{{Short description|A calcimimetic drug used in the treatment of secondary hyperparathyroidism}}
{{Short description|A calcimimetic agent used in the treatment of secondary hyperparathyroidism}}
{{Drugbox
{{Drugbox
| verifiedfields = changed
| verifiedrevid = 123456789
| verifiedrevid = 123456789
| image = Upacicalcet.svg
| image = Upacicalcet.svg
| width = 200px
| image_size = 200px
| alt =  
| image_alt = Structural formula of Upacicalcet
| IUPAC_name = (1R,3R)-1-(3-((2-(3-(trifluoromethyl)phenyl)thiazol-4-yl)methyl)phenyl)-3-aminocyclopentane-1-carboxylic acid
| CAS_number = 123456-78-9
| ATC_prefix = H05
| ATC_suffix = BX04
}}
}}


'''Upacicalcet''' is a [[calcimimetic]] drug used primarily in the management of [[secondary hyperparathyroidism]] in patients undergoing [[dialysis]] for [[chronic kidney disease]].
'''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==
==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.
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==
==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.
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==
==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.
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==
==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.
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.


==Regulatory Status==
==Related pages==
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.
 
==Related Pages==
* [[Calcimimetic]]
* [[Calcimimetic]]
* [[Secondary hyperparathyroidism]]
* [[Secondary hyperparathyroidism]]
* [[Chronic kidney disease]]
* [[Chronic kidney disease]]
* [[Dialysis]]
* [[Dialysis]]
* [[Parathyroid hormone]]


[[Category:Calcimimetics]]
[[Category:Calcimimetics]]
[[Category:Drugs used in nephrology]]
[[Category:Drugs used in nephrology]]

Revision as of 03:40, 13 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

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