etelcalcetide

Action and Spectrum

Actions and Spectrum: 

The actions of etelcalcetide can be summarized as follows: 

• Reduces PTH secretion: Etelcalcetide activates calcium-sensing receptors in the parathyroid gland, which leads to a decrease in PTH secretion. This helps to normalize the levels of PTH in the blood. 
• Reduces serum calcium levels: By reducing PTH secretion, etelcalcetide also helps to reduce serum calcium levels in patients with hyperparathyroidism. 
• Improves bone health: Hyperparathyroidism can lead to bone loss and fractures. By reducing PTH secretion and serum calcium levels, etelcalcetide can help to improve bone health and reduce the risk of fractures. 

The spectrum of etelcalcetide refers to the range of conditions that the medication can be used to treat. Etelcalcetide is approved by the FDA for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease who are undergoing dialysis. It is not indicated for the treatment of primary hyperparathyroidism or for patients who are not receiving dialysis. 

Drug Interaction

Adverse Reaction

Frequency Defined  

>10%  

Muscle spasms (12%)  

Nausea (11%)  

Diarrhea (11%)  

1-10%  

Headache (8%)  

Paresthesia (6%)  

Hypocalcemia (7%)  

Vomiting (9%)  

Hypersensitivity (4.4%)  

Hospitalization for heart failure (2%)  

Hyperkalemia (4%)  

Myalgia (2%)  

Hypophosphatemia (1%)  

QTc prolongation secondary to hypocalcemia (1.2%)  

Black Box Warning

Black Box Warning: 

The black box warning for etelcalcetide is related to the risk of hypocalcemia, which is a condition where there is a low level of calcium in the blood. Hypocalcemia can lead to a number of serious health problems, including seizures, cardiac arrhythmias, and muscle spasms. 

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity: etelcalcetide should not be used in patients with a history of hypersensitivity to the medication or any of its components. 
• Severe hepatic impairment: etelcalcetide should be used with caution in patients with severe hepatic impairment. The dosage may need to be adjusted based on the patient’s condition. 
• Pregnancy and breastfeeding: The safety of etelcalcetide in pregnant and breastfeeding women has not been established. It should be used only if the potential benefits outweigh the potential risks. 
• Hypocalcemia: etelcalcetide can cause hypocalcemia (low levels of calcium in the blood). Therefore, patients with a history of hypocalcemia should be monitored closely. 
• QT prolongation: it can prolong the QT interval of the electrocardiogram, which can lead to arrhythmias. Therefore, patients with a history of arrhythmias or those taking medications that can prolong the QT interval should be closely monitored. 
• Adynamic bone disease: it should be used with caution in patients with adynamic bone disease as it can worsen the condition. 
• Seizures: it has been associated with seizures in some patients. Therefore, patients with a history of seizures or those at risk of seizures should be closely monitored. 
• Gastrointestinal side effects: etelcalcetide can cause gastrointestinal side effects, including nausea, vomiting, and diarrhea. Therefore, patients with a history of gastrointestinal disorders should be monitored closely. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category  

Pharmacology

Pharmacology:  

etelcalcetide is a calcimimetic agent that is used for the treatment of secondary hyperparathyroidism (HPT) in patients with chronic kidney disease who are undergoing hemodialysis. 

Pharmacodynamics: 

 It works by activating the calcium-sensing receptors (CaSR) on the parathyroid gland, which results in the reduction of parathyroid hormone (PTH) secretion.  

Pharmacokinetics: 

Absorption  

etelcalcetide is administered intravenously, and its bioavailability is not applicable.  

Distribution  

The distribution of etelcalcetide in humans has not been specifically studied. However, it is known that the drug binds to the calcium-sensing receptor (CaSR) on the parathyroid gland, thereby decreasing the secretion of parathyroid hormone (PTH).  

Metabolism  

The metabolism of etelcalcetide has not been specifically studied in humans. It is known that the drug is a peptide and can be hydrolyzed by proteolytic enzymes.  

Elimination and Excretion  

etelcalcetide is eliminated primarily via the kidneys, with a half-life of approximately 5 hours in patients with end-stage renal disease

Adminstartion

Administration:  

etelcalcetide is a medication that is used to treat hyperparathyroidism in patients with chronic kidney disease who are undergoing dialysis. It is typically administered as an injection by a healthcare provider. 

The injection is given into a vein, usually in the arm or hand. The dose and frequency of administration will depend on the patient’s individual condition and response to treatment 

Patient Information Leaflet

Patient information leaflet 

Generic Name: etelcalcetide 

Why do we use etelcalcetide? 

etelcalcetide is used to treat hyperparathyroidism in patients with chronic kidney disease who are undergoing dialysis. Hyperparathyroidism is a condition where the parathyroid glands produce too much parathyroid hormone (PTH), which can lead to high levels of calcium in the blood, bone disease, and other complications. 

etelcalcetide works by binding to and activating calcium-sensing receptors in the parathyroid gland, which reduces the secretion of PTH. This helps to lower the levels of calcium in the blood and prevent complications associated with hyperparathyroidism.