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Brand Name :
Sensipar
Synonyms :
cinacalcet
Class :
Calcimimetics
Brand Name :
Sensipar
Synonyms :
cinacalcet
Class :
Calcimimetics
Dosage Forms & StrengthsÂ
TabletÂ
30mgÂ
60mgÂ
90mgÂ
Indicated in individuals with severe hypercalcemia who are unable to have a parathyroidectomy:
Initial Dose:30mg orally every 12 hours. Increase the dose every 2 to 4 weeks
60 mg every 12 hours, 90 mg every 12 hours, or 90 mg every 6 to 8 hours as needed to bring serum calcium levels back to normal
Maintenance dose: 60 to 360mg orally per day
Maximum dose:90mg 4 times a day orally
Dose Adjustments
Dosing Consideration
Before beginning Sensipar, discontinue etelcalcetide for a minimum of 4 weeks.
Before beginning Sensipar medication, make sure corrected serum calcium is at or above the lower limit of normal; start Sensipar at a starting dosage of 30 mg once a day
Initial Dose:30mg orally every 12 hours. Increase the dose every 2 to 4 weeks
60 mg every 12 hours, 90 mg every 12 hours, or 90 mg every 6 to 8 hours as needed to bring serum calcium levels back to normal
Secondary HyperparathyroidismÂ
Indicated in individuals on dialysis with chronic kidney disease (CKD):
Initial Dose:30mg orally every day
May be increased if necessary by titrating daily dosages of 60, 90, 120, or 180 mg at 2 to 4-week intervals
Safety and efficacy not establishedÂ
Refer adult dosingÂ
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of calcimimetic agents
may diminish the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may increase the hypocalcemic effect of cinacalcet
may enhance the serum concentrations of CYP3A4 inhibitors
may enhance the serum concentrations of CYP3A4 substrates
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations
may enhance the serum concentrations
may enhance the serum concentrations
may enhance the serum concentrations
may enhance the serum concentrations
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may enhance the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
may increase the serum concentrations of CYP2D6 inhibitors
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
it may diminish the metabolism when combined with azelastine
when bromazepam and cinacalcet are used together, there is a potential reduction in the bromazepam's metabolism
When cinacalcet is used together with somatotropin, this leads to a rise in cinacalcet metabolism
When encainide is used together with cinacalcet, this leads to a reduction in the encainide’s metabolism
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
It may enhance the serum concentration when combined with CYP3A4 Substrates
When cinacalcet is used together with oliceridine, this leads to enhanced concentration serum of oliceridine
When cinacalcet is aided by hesperetin, it reduces hesperetin’s metabolism
Actions and Spectrum:Â
The mechanism of action of cinacalcet involves binding to and activating the calcium-sensing receptor (CaSR) in the parathyroid gland, which results in a decrease in parathyroid hormone (PTH) secretion. The CaSR is a G protein-coupled receptor expressed on the surface of parathyroid cells.
Activation of the receptor by extracellular calcium ions decreases PTH secretion, while inhibition of the receptor leads to increased PTH secretion. cinacalcet binds to a different site on the CaSR than calcium, resulting in a conformational change in the receptor, enhancing its sensitivity to calcium and decreasing PTH secretion.Â
In addition to its effects on PTH secretion, cinacalcet can reduce serum calcium levels by increasing urinary calcium excretion and inhibiting bone resorption. It can also reduce the size of parathyroid glands and improve bone mineral density in patients with hyperparathyroidism cinacalcet has a spectrum of activity specific to its role in regulating calcium homeostasis.
It is not effective against other types of endocrine disorders or hormonal imbalances. It is primarily used to treat hyperparathyroidism associated with chronic kidney disease, primary hyperparathyroidism, and parathyroid carcinoma. It is generally well-tolerated, although side effects may include nausea, vomiting, diarrhoea, headache, and hypocalcaemiaÂ
Frequency defined Â
>10%Â
Secondary parathyroidismÂ
Nausea (19%)Â
Myalgia (14%)Â
Diarrhea (20%)Â
Vomiting (15%)Â
1-10%Â
Secondary parathyroidismÂ
Seizures (1.4%)Â
Hypertension (5%)Â
Anorexia (4%)Â
Access infection (4%)Â
Noncardiac chest pain (4%)Â
Asthenia (4%)Â
Dizziness (8%)Â
Frequency not definedÂ
Parathyroid CAÂ
HypocalcemiaÂ
Nausea/vomitingÂ
Post-marketing reportsÂ
HypotensionÂ
Adynamic bone diseaseÂ
Worsening heart failure and/or arrhythmiasÂ
Chondrocalcinosis pyrophosphateÂ
Gastrointestinal bleedingÂ
Contraindications/caution:Â
Contraindications:Â
Caution:Â
Pregnancy consideration: CÂ
Lactation: Excretion of the drug in human breast milk is unknownÂ
Pregnancy category:Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.  Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.Â
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.   Â
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.   Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   Â
Category N: There is no data available for the drug under this categoryÂ
Pharmacology:Â
cinacalcet is a calcimimetic agent that increases the sensitivity of the calcium-sensing receptor (CaSR) to extracellular calcium ions, decreasing parathyroid hormone (PTH) secretion. The CaSR is a G protein-coupled receptor expressed on the surface of parathyroid cells.
Activation of the receptor by extracellular calcium ions decreases PTH secretion, while inhibition of the receptor leads to an increase in PTH secretion. cinacalcet binds to a different site on the CaSR than calcium, resulting in a conformational change in the receptor that enhances its sensitivity to calcium, decreasing PTH secretionÂ
Pharmacodynamics:Â
The pharmacodynamics of cinacalcet involves its effects on the calcium-sensing receptor (CaSR) in the parathyroid gland and other tissues. cinacalcet is a calcimimetic agent that binds to a different site on the CaSR than calcium, resulting in a conformational change in the receptor, enhancing its sensitivity to calcium.
This leads to decreased parathyroid hormone (PTH) secretion by the parathyroid gland, as the CaSR mediates the inhibitory effect of extracellular calcium on PTH secretion. cinacalcet also directly affects other tissues that express the CaSR, such as the kidney and bone.
In the kidney, cinacalcet can increase urinary calcium excretion and inhibit calcium reabsorption from the renal tubules, reducing serum calcium levels. In bone, cinacalcet can inhibit bone resorption and promote bone formation, leading to improvements in bone mineral density in patients with hyperparathyroidismÂ
Pharmacokinetics:Â
AbsorptionÂ
cinacalcet has high bioavailability, and a high-fat meal can increase its peak plasma concentration and AUC compared to fasting. It is rapidly absorbed after oral administration, with peak plasma concentrations reached within 1-3 hours. The medication is highly lipophilic, and food enhances its absorption. It is not affected by pH changes in the gastrointestinal tract.Â
DistributionÂ
It is highly protein-bound (93-97%) and has a large volume of distribution (Vd) of 1000 L, indicating that it can enter tissues throughout the body. Â
MetabolismÂ
It is extensively metabolized by several cytochrome P450 enzymes, including CYP3A4, CYP2D6, and CYP1A2. The primary metabolites are hydrocinnamic and hydroxy-hydrocinnamic acid, naphthalene-ring-containing molecules, and dihydrodiols. Cinacalcet can also inhibit the activity of CYP2D6.Â
Elimination and ExcretionÂ
cinacalcet has a long elimination half-life of 30-40 hours, and it is primarily eliminated through the urine (80%) and feces (15%)Â
Administration:Â
cinacalcet should be taken with food or shortly after a meal. The tablet should be swallowed whole and not chewed, crushed, or dividedÂ
Patient information leafletÂ
Generic Name: cinacalcetÂ
Pronounced: [ sin-ah-CAL-set ]Â
Why do we use cinacalcet?Â
It is a medication primarily used to treat hypercalcemia in patients with primary or secondary hyperparathyroidism. Â
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