What are the primary uses of cinacalcet. How does cinacalcet work in the body. What are the common side effects of cinacalcet. How should cinacalcet be taken for optimal effectiveness. What precautions should be considered when using cinacalcet. How does cinacalcet interact with other medications.

Understanding Cinacalcet: A Comprehensive Overview

Cinacalcet is a medication that plays a crucial role in managing certain hormonal imbalances in the body. It’s primarily used to address elevated levels of parathyroid hormone (PTH) in specific medical conditions. To fully grasp the significance of this drug, it’s essential to delve into its uses, mechanisms, and important considerations for patients and healthcare providers alike.

The Primary Uses of Cinacalcet in Medical Treatment

Cinacalcet serves several important purposes in medical treatment. Its primary applications include:

• Treating increased parathyroid hormone levels in patients with chronic kidney disease who are on dialysis
• Managing elevated calcium levels in individuals with overactive parathyroid glands
• Addressing high calcium levels in patients with parathyroid gland cancer

These uses highlight the drug’s importance in endocrine and renal medicine. But how exactly does cinacalcet achieve these therapeutic effects?

The Mechanism of Action: How Cinacalcet Works in the Body

Cinacalcet functions by reducing the levels of three key substances in the body:

1. Parathyroid hormone
2. Calcium
3. Phosphorus

By modulating these levels, cinacalcet helps maintain the delicate balance necessary for optimal bone health. This action is particularly crucial for patients with conditions that disrupt normal calcium and phosphorus metabolism.

Proper Administration: How to Take Cinacalcet Effectively

For cinacalcet to be most effective, it’s crucial to follow the proper administration guidelines. The medication should be taken orally with food or shortly after a meal, as directed by a healthcare provider. Typically, it’s recommended to take cinacalcet at the same time(s) each day to maintain consistent levels in the body.

Is it safe to split or crush cinacalcet tablets? The manufacturer advises against splitting, chewing, or crushing the tablets before ingestion. However, it’s worth noting that similar immediate-release tablets can often be split or crushed. Always consult your doctor for specific instructions on how to take cinacalcet.

Potential Side Effects: What to Watch For When Taking Cinacalcet

Like all medications, cinacalcet can cause side effects. Some common side effects include:

• Nausea
• Vomiting
• Unusual tiredness

While these effects are generally mild, it’s important to inform your healthcare provider if they persist or worsen. More serious side effects can occur, particularly related to low calcium levels in the blood.

Recognizing Symptoms of Low Calcium Levels

Cinacalcet can cause hypocalcemia (low blood calcium levels). Patients should be vigilant for symptoms such as:

• Numbness or tingling in the skin
• Severe muscle spasms
• Seizures
• Fast, irregular, or pounding heartbeat

If any of these symptoms occur, it’s crucial to seek medical attention promptly. Regular monitoring of calcium levels by a healthcare provider is an essential part of cinacalcet therapy.

Important Precautions and Considerations for Cinacalcet Use

Before starting cinacalcet treatment, it’s vital to disclose all relevant medical information to your healthcare provider. This includes:

• Any allergies to cinacalcet or its ingredients
• Complete medical history, especially concerning low blood calcium levels, seizures, or gastrointestinal problems
• All medications, including prescription, over-the-counter, and herbal products

Are there specific conditions that require extra caution when using cinacalcet? Yes, patients with heart rhythm problems or other cardiac issues should inform their doctor, as very low calcium levels can affect heart rhythm.

Cinacalcet Use During Pregnancy and Breastfeeding

The safety of cinacalcet during pregnancy and breastfeeding is not fully established. It should only be used during pregnancy when clearly necessary, and the risks and benefits should be thoroughly discussed with a healthcare provider. The passage of cinacalcet into breast milk is unknown, so consultation with a doctor is crucial before breastfeeding while on this medication.

Drug Interactions: Understanding How Cinacalcet Affects Other Medications

Cinacalcet can interact with various other medications, potentially altering their effectiveness or increasing the risk of side effects. Some important interactions to be aware of include:

• Thioridazine: This antipsychotic medication may interact with cinacalcet
• Etelcalcetide: If switching from cinacalcet to etelcalcetide, a 7-day gap is recommended to avoid increased risk of side effects

To ensure safe and effective treatment, it’s crucial to inform your healthcare provider about all medications you’re taking. They can help identify potential interactions and adjust your treatment plan accordingly.

The Importance of Medication Interaction Checks

Given the potential for drug interactions, it’s advisable to use medication interaction checkers regularly. These tools can help identify potential conflicts between cinacalcet and other drugs you may be taking, allowing for proactive management of your medication regimen.

Managing Cinacalcet Overdose: Recognizing and Responding to Emergencies

While following prescribed dosages is crucial, it’s also important to be aware of the signs of a potential cinacalcet overdose. Symptoms of overdose may include:

• Severe nausea or vomiting
• Extreme dizziness
• Unusual weakness
• Severe muscle spasms or seizures

If an overdose is suspected, immediate medical attention is necessary. Contact emergency services or a poison control center right away for guidance.

The Role of Emergency Services in Cinacalcet Overdose

In cases of suspected cinacalcet overdose, emergency medical professionals play a crucial role. They can provide immediate care and monitoring, potentially administering treatments to counteract the effects of the overdose and stabilize the patient’s condition.

Long-Term Management: Monitoring and Adjusting Cinacalcet Treatment

Effective use of cinacalcet often requires ongoing monitoring and potential adjustments to the treatment plan. This typically involves:

• Regular blood tests to check calcium, phosphorus, and parathyroid hormone levels
• Periodic evaluations of kidney function in patients with chronic kidney disease
• Assessments of bone health and density

Based on these monitoring results, healthcare providers may adjust the cinacalcet dosage or recommend additional treatments to optimize patient outcomes.

The Importance of Patient Compliance in Cinacalcet Therapy

For cinacalcet treatment to be most effective, patient compliance is crucial. This includes:

• Taking the medication as prescribed, at the same time(s) each day
• Attending all scheduled follow-up appointments and laboratory tests
• Promptly reporting any side effects or concerns to the healthcare provider
• Maintaining open communication about any changes in health status or other medications

By adhering to these guidelines, patients can help ensure the best possible outcomes from their cinacalcet therapy.

Alternative Treatments: Options Beyond Cinacalcet

While cinacalcet is an effective treatment for many patients with parathyroid hormone imbalances, it’s not the only option available. Depending on the specific condition and individual patient factors, healthcare providers might consider alternative treatments such as:

• Vitamin D supplements
• Calcium supplements
• Phosphate binders
• Parathyroidectomy (surgical removal of parathyroid glands)
• Other calcimimetic medications

The choice of treatment depends on various factors, including the underlying condition, severity of symptoms, overall health status, and patient preferences.

Comparing Cinacalcet to Other Treatment Options

How does cinacalcet compare to other treatments for parathyroid hormone imbalances? Each treatment option has its own set of benefits and potential drawbacks:

• Cinacalcet: Effective for lowering PTH levels without increasing calcium, but may cause gastrointestinal side effects
• Vitamin D supplements: Can help manage calcium levels, but may not be sufficient for severe cases
• Parathyroidectomy: Provides a permanent solution for some conditions, but carries surgical risks
• Other calcimimetics: May offer similar benefits to cinacalcet with different side effect profiles

The optimal treatment approach often involves a combination of these options, tailored to each patient’s specific needs and circumstances.

Future Directions: Ongoing Research and Developments in Parathyroid Hormone Management

The field of parathyroid hormone management continues to evolve, with ongoing research aimed at improving treatment options and patient outcomes. Some areas of current interest include:

• Development of new calcimimetic agents with improved efficacy or reduced side effects
• Exploration of combination therapies to optimize treatment of secondary hyperparathyroidism
• Investigation of novel drug delivery methods for more consistent hormone control
• Research into personalized medicine approaches for individualized treatment planning

These ongoing efforts hold promise for enhancing the management of parathyroid hormone imbalances and related conditions in the future.

The Role of Genetic Research in Parathyroid Disorders

Genetic research is playing an increasingly important role in understanding and treating parathyroid disorders. Studies are exploring:

• Genetic factors that contribute to the development of hyperparathyroidism
• Potential genetic markers for predicting treatment response to medications like cinacalcet
• Gene therapies that could offer new treatment approaches for parathyroid disorders

As this research progresses, it may lead to more targeted and effective treatments for patients with parathyroid hormone imbalances.

Patient Education: Empowering Individuals on Cinacalcet Therapy

Effective management of conditions treated with cinacalcet often requires active patient involvement. Patient education plays a crucial role in ensuring optimal outcomes. Key areas of focus for patient education include:

• Understanding the importance of medication adherence
• Recognizing and reporting potential side effects
• Maintaining a balanced diet to support calcium and phosphorus management
• The significance of regular follow-up appointments and laboratory tests
• Lifestyle modifications that can complement medical treatment

By empowering patients with knowledge about their condition and treatment, healthcare providers can help improve treatment adherence and overall outcomes.

The Role of Support Groups in Cinacalcet Therapy

Support groups can play a valuable role for patients undergoing cinacalcet therapy. These groups offer benefits such as:

• Emotional support from others with similar experiences
• Practical tips for managing side effects and treatment challenges
• Information about new research and treatment options
• A platform for sharing concerns and asking questions

Participating in support groups can help patients feel more empowered and better equipped to manage their condition and treatment.

Cinacalcet in Special Populations: Considerations for Specific Patient Groups

While cinacalcet is effective for many patients, its use may require special considerations in certain populations. These include:

• Elderly patients: May be more susceptible to side effects and require closer monitoring
• Patients with liver impairment: May metabolize the drug differently, potentially requiring dosage adjustments
• Pediatric patients: Limited data on safety and efficacy in children
• Patients with multiple comorbidities: May have an increased risk of drug interactions or complications

Healthcare providers must carefully weigh the benefits and risks of cinacalcet therapy in these special populations, often requiring more frequent monitoring and potential dosage adjustments.

Cinacalcet Use in Patients with Chronic Kidney Disease

Chronic kidney disease (CKD) patients represent a significant population treated with cinacalcet. Special considerations for this group include:

• Potential for altered drug metabolism due to impaired kidney function
• Increased risk of mineral and bone disorders requiring careful management
• Need for coordinated care between nephrologists and other specialists
• Importance of monitoring for complications related to both CKD and cinacalcet therapy

Effective management of cinacalcet therapy in CKD patients often requires a multidisciplinary approach to ensure optimal outcomes and minimize potential complications.

Cinacalcet Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

Cinacalcet is used to treat increased amounts of a certain hormone (parathyroid) in people with long-term kidney disease who are on dialysis. It is also used to treat increased amounts of calcium in people with an overactive parathyroid gland or in people with cancer of the parathyroid gland. Cinacalcet works by decreasing the amount of parathyroid hormone, calcium, and phosphorus in your body. Having the right amount of these substances in your body helps to prevent bone disease.

How to use Cinacalcet HCL

Take this medication by mouth with food or shortly after a meal, as directed by your doctor.

The manufacturer directs not to split, chew, or crush the tablet before taking it. However, many similar drugs (immediate-release tablets) can be split, chewed, or crushed. Follow your doctor’s directions on how to take this medication.

The dosage is based on your medical condition, response to treatment, and laboratory tests.

Take this medication regularly in order to get the most benefit from it. Remember to take it at the same time(s) each day.

Side Effects

Nausea, vomiting, or unusual tiredness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Cinacalcet can cause low calcium blood levels. Your doctor will check your calcium blood levels while you are taking this medication. Tell your doctor right away if you have any of the following symptoms of low calcium levels: numb/tingling skin, severe muscle spasms, seizures, fast/irregular/pounding heartbeat.

Tell your doctor right away if you have any serious side effects, including: black/bloody stools, stomach/abdominal pain, vomit that contains blood or looks like coffee grounds.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking cinacalcet, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: low levels of calcium in the blood (hypocalcemia), seizures, stomach/intestinal problems (such as ulcers, gastritis, heartburn).

Very low levels of calcium can affect the heart rhythm (QT prolongation, ventricular arrhythmias). This risk may be increased if you have certain conditions or are taking drugs that can affect the heart rhythm. Before taking cinacalcet, tell your doctor of all the drugs you take and if you have heart rhythm problems or other heart problems (such as heart failure, low blood pressure).

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

A product that may interact with this drug is: thioridazine.

If your doctor tells you to switch from using this medication to etelcalcetide, this medication should be stopped at least 7 days before starting etelcalcetide. Using both medications together may increase the risk of side effects (especially low calcium levels).

Does Cinacalcet HCL interact with other drugs you are taking?

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Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe muscle spasms, seizures.

Do not share this medication with others.

Lab and/or medical tests (such as calcium, phosphorus, parathyroid hormone levels) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: A33 30

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 90 mg tablet

Color: light greenShape: ovalImprint: CL 412

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: CL 410

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 90 mg tablet

Color: light greenShape: ovalImprint: 90 CN

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: 60 CN

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: 30 CN

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: A 34 60

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 90 mg tablet

Color: light greenShape: ovalImprint: A35 90

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 90 mg tablet

Color: light greenShape: ovalImprint: HB 3

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: C 30

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: CL 411

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: H C6

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: H C7

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: HB2

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 30 mg tablet

Color: light greenShape: ovalImprint: HB1

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 90 mg tablet

Color: light greenShape: ovalImprint: H C8

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

cinacalcet 60 mg tablet

Color: light greenShape: ovalImprint: C 60

This medicine is a light green, oval, film-coated, tablet imprinted with “A33” and “30”.

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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Cinacalcet – StatPearls – NCBI Bookshelf

Syeda Zeenat S. Junaid; Jayesh B. Patel.

Author Information and Affiliations

Last Update: August 12, 2022.

Continuing Education Activity

Cinacalcet is a medication used in the management and treatment of secondary hyperparathyroidism (on dialysis population), primary hyperparathyroidism for which the patient may not be a surgical candidate, and the treatment of calciphylaxis in patients with advanced kidney disease or on dialysis. It belongs to the calcimimetic class of medications. This activity reviews the indications, action, and contraindications for cinacalcet as a valuable agent in treating the conditions mentioned above. This activity will highlight the mechanism of action, adverse event profile, and other key factors (e.g., off-label uses, dosing, pharmacodynamics, pharmacokinetics, monitoring, relevant interactions) pertinent for members of the healthcare team in the care of patients with hyperparathyroidism and related conditions.

Objectives:

• Identify the mechanism of action of cinacalcet.

• Describe the possible adverse effects of cinacalcet

• Review the appropriate monitoring for patients receiving therapy with cinacalcet

• Outline some interprofessional team strategies for improving care coordination and communication to advance knowledge regarding the side effects of cinacalcet and improve outcomes.

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Indications

Cinacalcet hydrochloride classifies as a “calcimimetic.” Its primary indication is to reduce the parathyroid hormone level in patients with secondary hyperparathyroidism associated with end-stage kidney disease. In chronic kidney disease, patients often have high phosphorus levels, variable calcium levels, and increased parathyroid hormone levels (>300 pg/mL).[1] The role of the cinacalcet in this condition is to reduce the serum parathyroid hormone level and prevent bone destruction. This intervention reinstates the calcium levels within the target ranges defined by the Kidney Disease Outcomes Quality Initiative (K-DOQI) for disease management.[2] It reduces the chances of requiring a parathyroidectomy for secondary hyperparathyroidism. Clinicians often use this medication in combination therapy with an oral phosphorous binder (calcium acetate, sevelamer) as well as vitamin D analogs (calcitriol, paricalcitol).[1][3]

Cinacalcet can be used for the treatment of primary hyperparathyroidism in the individual who is not a surgical candidate or in whom surgery would be high risk. [4] Because cinacalcet lowers PTH and reduces serum calcium levels, it can be used along with bisphosphonates to reduce calcium resorption from bone. 

Cinacalcet is often a part of the treatment modality in individuals with calciphylaxis, which can present in the patient with end-stage kidney disease.[5] It is being used increasingly in pediatric populations with CKD and suffering from concomitant renal osteodystrophy, described as CKD–mineral and bone disorders (CKD–MBD). An important part of the management of this condition is lowering the parathyroid hormone level and treating hypercalcemia with cinacalcet, as well as treating hyperphosphatemia with a non-calcium-based phosphorus binder. Cinacalcet, when combined with other treatments for calciphylaxis, has shown improved efficacy in treating this condition.[5]  

Clinicians can also use this medication has also been used to treat hypercalcemia in patients with parathyroid carcinoma. While the treatment of parathyroid carcinoma is primarily surgical, therapy with cinacalcet does help reduce the serum calcium level. [6]  It may also be a therapeutic option in patients in whom surgical removal of the mass is deemed futile.[7]

Mechanism of Action

Cinacalcet is a “calcimimetic,” meaning that it acts on the calcium-sensing receptors (CaSR) located on the chief cells of the parathyroid gland.[8] CaSR detects a minor change in the extracellular calcium level and maintains the PTH level accordingly.[8] This process occurs through PTH gene transcription and parathyroid cell growth. The CaSR couples with a 7-transmembrane domain G-proteins. On the chief cells, the predominant forms are Gi and Gq. Once activated, cAMP accumulation becomes inhibited, and simultaneously the phosphoinositide-phospholipase C pathway gets stimulated. The ensuing increase in IP3 and DAG levels leads to intracellular calcium influx. The end result of this the Gq pathway is specifically dominant-negative, i.e., suppression of PTH secretion. Disruption of this cascade has also been present in various etiologies of hyperparathyroidism. [9] 

“Calcimimetic” medications, as the name suggests, may not be the real calcium ligands, but they activate these receptors and utilize the Gq/Gi pathways to establish the negative feedback loop to raise calcium levels. This feedback occurs through the suppression of both the production of PTH and its secretion and ultimately leads to the mitigation of calcium and phosphorus products in the blood.[10]

Administration

This medication is to be taken once daily with food. Most therapies directed at the endocrine axis should preferably be taken at the same time every day. Food has a positive effect on cinacalcet’s absorption, increasing its levels in the plasma by more than three-fold compared to when taking it without food.[11] It has a long half-life of approximately 1.5 days. It is highly bound to plasma proteins, metabolized primarily in the liver, and is dependent on the kidney for excretion.[11]

The dosage schedules are adapted according to the PTH response individually in patients. The pediatric population may warrant reduced dosages because of their lower body surface area and the changed CYP profiles.[2]

Adverse Effects

The common side effects are nausea and vomiting.[7] It can occur in up to one-third of patients taking this medication. Dizziness, diarrhea, and decreased appetite are other side effects of this medication as well. Cinacalcet can cause hypocalcemia. The patients on this medication need to be closely followed for common symptoms associated with hypocalcemia include tingling, muscle twitching, cramps, changes in mood, or irritability. On the ECG, a prolonged QT interval may be present. Patients with a history of congenital long QT syndrome, family history of long QT syndrome, and other conditions that predispose patients to QT interval prolongation may be at increased risk.[11] Oversuppresion of PTH can cause adynamic bone disease. 

Contraindications

Calcium level below 8.4 milligrams per deciliter is a contraindication to initiating this medication. [11]

Monitoring

Calcium levels need to be followed closely for any patient on this medication. Patients require assessment for signs and symptoms of hypocalcemia. Individuals on this medication need monitoring for side effects, including nausea and vomiting.[11] Cinacalcet may interact with other medications such as anticholinesterase inhibitors in dementia patients. Patients with hepatic impairment and hepatic impairment should have close monitoring.[3]

Toxicity

There is no “toxic” level of cinacalcet. Dose-limiting effects include nausea and vomiting, which would limit or preclude its use.[11] If hypocalcemia is present, the clinician should discontinue the medication, and hypocalcemia should have treated with intravenous calcium. Other electrolyte abnormalities, including magnesium and phosphorous, also need to be monitored.[11] To date, there is not much evidence to validate cinacalcet’s use or its toxicity in pregnant women. 

Enhancing Healthcare Team Outcomes

With the rise in the burden of non-communicable diseases, i. e., cardiovascular and chronic kidney disease, healthcare providers must refine all their non-surgical options. Cinacalcet, a calcimimetic that counteracts the increase in PTH, is gaining center stage. When instituting a multi-modality approach for calciphylaxis, chronic kidney disease, and hyperparathyroidism, this medication is one of the ‘essentials’ in the medical armamentarium.

Cinacalcet therapy is best when provided through an interprofessional healthcare team, including clinicians, mid-level practitioners (NPs and PAs), specialists, nurses, and pharmacists, all working together and having access to all patient information so they can drive the best possible patient outcomes. [Level 5]

Nephrologists most commonly prescribe it for patients with secondary hyperparathyroidism on dialysis. Endocrinologists may prescribe it in patients with primary hyperparathyroidism in patients in whom surgical intervention is not an option or who would otherwise be too high risk for surgery. Patients need to be aware of side effects, including nausea and vomiting. They also should be educated about the symptoms of hypocalcemia. Calcium levels should be monitored closely in these patients. The interprofessional healthcare team should also engage the consult of a clinical pharmacist to optimize therapeutic results and minimize adverse events.

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References

1.

Sekercioglu N, Busse JW, Sekercioglu MF, Agarwal A, Shaikh S, Lopes LC, Mustafa RA, Guyatt GH, Thabane L. Cinacalcet versus standard treatment for chronic kidney disease: a systematic review and meta-analysis. Ren Fail. 2016 Jul;38(6):857-74. [PubMed: 27137817]

2.

Sohn WY, Portale AA, Salusky IB, Zhang H, Yan LL, Ertik B, Shahinfar S, Lee E, Dehmel B, Warady BA. An open-label, single-dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of cinacalcet in pediatric subjects aged 28 days to < 6 years with chronic kidney disease receiving dialysis. Pediatr Nephrol. 2019 Jan;34(1):145-154. [PMC free article: PMC6244811] [PubMed: 30141180]

3.

Junaid SZS, Patel JB. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Aug 12, 2022. Cinacalcet. [PubMed: 32491590]

4.

Cetani F, Saponaro F, Marcocci C. Non-surgical management of primary hyperparathyroidism. Best Pract Res Clin Endocrinol Metab. 2018 Dec;32(6):821-835. [PubMed: 30665549]

5.

Deen J, Schaider H. The use of cinacalcet for the treatment of calciphylaxis in patients with chronic kidney disease: A comprehensive review. Australas J Dermatol. 2019 Aug;60(3):e186-e194. [PubMed: 30666627]

6.

Takeuchi Y, Takahashi S, Miura D, Katagiri M, Nakashima N, Ohishi H, Shimazaki R, Tominaga Y. Cinacalcet hydrochloride relieves hypercalcemia in Japanese patients with parathyroid cancer and intractable primary hyperparathyroidism. J Bone Miner Metab. 2017 Nov;35(6):616-622. [PubMed: 27873072]

7.

Silverberg SJ, Rubin MR, Faiman C, Peacock M, Shoback DM, Smallridge RC, Schwanauer LE, Olson KA, Klassen P, Bilezikian JP. Cinacalcet hydrochloride reduces the serum calcium concentration in inoperable parathyroid carcinoma. J Clin Endocrinol Metab. 2007 Oct;92(10):3803-8. [PubMed: 17666472]

8.

Nagano N. Pharmacological and clinical properties of calcimimetics: calcium receptor activators that afford an innovative approach to controlling hyperparathyroidism. Pharmacol Ther. 2006 Mar;109(3):339-65. [PubMed: 16102839]

9.

Pi M, Chen L, Huang M, Luo Q, Quarles LD. Parathyroid-specific interaction of the calcium-sensing receptor and G alpha q. Kidney Int. 2008 Dec;74(12):1548-56. [PMC free article: PMC2760404] [PubMed: 18813283]

10.

Conigrave AD. The Calcium-Sensing Receptor and the Parathyroid: Past, Present, Future. Front Physiol. 2016;7:563. [PMC free article: PMC5156698] [PubMed: 28018229]

11.

Poon G. Cinacalcet hydrochloride (Sensipar). Proc (Bayl Univ Med Cent). 2005 Apr;18(2):181-4. [PMC free article: PMC1200722] [PubMed: 16200170]

Disclosure: Syeda Zeenat Junaid declares no relevant financial relationships with ineligible companies.

Disclosure: Jayesh Patel declares no relevant financial relationships with ineligible companies.

Cinacalcet instructions for use: indications, contraindications, side effects – description Cinacalcet tab, cover. film coated, 30 mg: 10, 14, 20, 28, 30, 60 or 140 pcs. (57373)

💊 Composition of Cinacalcet ✅ Use of Cinacalcet Keep for yourself Search for analogues Interaction Description of the active ingredients of the preparation cinacalcet (Cinacalcet) The scientific information provided is general and cannot be used to make decisions. decisions about the use of a particular drug. Update date: 2020.06.30 Marketing authorization holder: HETERO LABS Limited (India) Manufactured: MAKIZ-PHARMA, OOO (Russia) or HETERO LABS Limited (India) ATX code: H05BX01 (Cinacalcet) Active substance: cinacalcet (cinacalcet) Rec.INN registered by WHO Dosage forms cinacalcet Tab, coated film coated, 30 mg: 10, 14, 20, 28, 30, 60 or 140 pcs. reg. No.: LP-006222 from 26.05.20 – Active Tab, coated film coated, 60 mg: 10, 14, 20, 28, 30, 60 or 140 pcs. reg. No.: LP-006222 from 26.05.20 – Active Tab, coated film coated, 90 mg: 10, 14, 20, 28, 30, 60 or 140 pcs. reg. No.: LP-006222 from 26.05.20 – Active Release form, packaging and composition drug Cinacalcet Film-coated tablets light green, oval, biconvex, debossed with “H” on one side and “C6” on the other side. Excipients : microcrystalline cellulose type 102 – 86.156 mg, pregelatinized starch – 46.747 mg, crospovidone – 11.333 mg, magnesium stearate – 1.8 mg, talc – 0.9 mg. Shell composition: Opadry II green 32K510043 (hypromellose – 39%, lactose monohydrate – 28%, titanium dioxide – 20.7%, triacetin – 8%, dye “indigo carmine aluminum varnish” – 2.2%, dye iron oxide yellow – 2.1 %) – 5.4 mg; Aquarius BP 19008 ICE white (hypromellose – 85%, macrogol – 15%) – 1.854 mg. 10 pcs. – cellular contour packings (1) – packs of cardboard. 10 pcs. – cellular contour packings (2) – packs of cardboard. 14 pcs. – cellular contour packings (1) – packs of cardboard. 14 pcs. – cellular contour packings (2) – packs of cardboard. 14 pcs. – cellular contour packings (10) – packs of cardboard. 30 pcs. – cans – packs of cardboard. 60 pcs. – cans – packs of cardboard. Clinical and pharmacological group: Antiparathyroid drug Pharmacotherapeutic group: Antiparathyroid agent Pharmacological action Antiparathyroid agent. Calcium-sensitive receptors located on the surface of the main cells of the parathyroid glands are the main regulators of the secretion of parathyroid hormone (PTH). Cinacalcet has a calcium mimetic effect that directly reduces PTH levels by increasing the sensitivity of this receptor to extracellular calcium. A decrease in PTH is accompanied by a decrease in serum calcium. Decrease in PTH level correlates with cinacalcet concentration. Shortly after taking cinacalcet, the PTH level begins to decrease: the maximum decrease occurs approximately 2-6 hours after taking a single dose, which corresponds to C max cinacalcet. Thereafter, the concentration of cinacalcet begins to decrease, and the concentration of PTH increases within 12 hours after dosing, and then the suppression of PTH remains at approximately the same level until the end of the daily interval with a dosing regimen of 1 time / day. After reaching the equilibrium state, the serum calcium concentration remains at a constant level during the entire interval between doses of cinacalcet. In patients with secondary hyperparathyroidism taking cinacalcet, there was a significant decrease in the level of intact PTH (iPTH), Ca × P (calcium-phosphorus product), serum calcium and phosphorus. The decrease in the concentration of iPTH and Ca × P was maintained throughout 12 months of therapy. Cinacalcet reduced iPTH, Ca × P, calcium, and phosphorus levels regardless of baseline iPTH or Ca × P levels, dialysis regimen (peritoneal dialysis versus hemodialysis), dialysis duration, and whether or not vitamin D was used. A decrease in PTH levels was associated with a non-significant decrease in the levels of markers of bone metabolism (specific bone ALP, N-telopeptides, bone turnover and bone fibrosis). In clinical studies in patients with parathyroid carcinoma and primary hyperparathyroidism, cinacalcet at doses of 30 mg 2 times / day to 90 mg 4 times / day caused a decrease in serum calcium concentration of ≥1 mg / dL (≥ 0.25 mmol / L ). Pharmacokinetics After oral administration C max cinacalcet in plasma is reached after about 2-6 hours. The absolute bioavailability when taken on an empty stomach, based on a comparison of the results of various studies, was approximately 20-25%. The increase in AUC and C max cinacalcet occurs almost linearly in the dose range of 30-180 mg 1 time / day. At doses greater than 200 mg, saturation of absorption is observed, probably due to poor solubility. The pharmacokinetic parameters of cinacalcet do not change with time. C ss cinacalcet is achieved within 7 days with minimal cumulation. A large V d of approximately 1000 liters is noted, indicating a wide distribution. Plasma protein binding is about 97% distributed at a minimal level in erythrocytes. Cinacalcet is metabolized mainly with the participation of CYP3A4 and CYP1A2 isoenzymes (the role of CYP1A2 has not been confirmed by clinical methods). The main metabolites found in the blood are inactive. According to in vitro studies, cinacalcet is a potent inhibitor of CYP2D6. However, at concentrations achieved in the clinical setting, cinacalcet does not inhibit the activity of other isoenzymes (including CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP3A4) and is also not an inducer of CYP1A2, CYP2C19 and CYP3A4. Following administration of a 75 mg radiolabeled dose to healthy volunteers, cinacalcet underwent rapid and significant oxidative metabolism followed by conjugation. The decrease in the concentration of cinacalcet occurs in 2 stages: the initial T 1/2 is approximately 6 hours, the final T 1/2 – 30-40 hours Metabolites are mainly excreted by the kidneys: approximately 80% of the dose was found in the urine and 15% in feces. Compared with the group with normal liver function, the mean AUC of cinacalcet was about 2 times higher in the group with moderate hepatic impairment, and about 4 times higher in severe liver failure. Average T 1/2 cinacalcet in patients with moderate and severe hepatic insufficiency increases by 33% and 70%, respectively. Clearance of cinacalcet may be lower in women than in men. Clearance of cinacalcet is higher in smokers than in non-smokers. Apparently, this is due to the induction of metabolism mediated by CYP1A2. If the patient stops or starts smoking during therapy, the plasma concentration of cinacalcet may change and dose adjustment may be required. Indications of the active substances of the drug cinacalcet Secondary hyperparathyroidism in patients with end-stage renal disease on dialysis; hypercalcemia in patients (in order to reduce the severity) caused by the following diseases: parathyroid carcinoma and primary hyperparathyroidism, if, despite serum calcium concentrations, parathyroidectomy is clinically unacceptable or contraindicated. Open list of ICD-10 codes C75.0 Malignant neoplasm of the parathyroid [parathyroid] gland E21. 0 Primary hyperparathyroidism N25.8 Other disorders due to renal tubular dysfunction (renal tubular acidosis, secondary renal hyperparathyroidism) Dosage regimen The method of administration and dosing regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed. For oral administration. The recommended starting dose is 30 mg once daily. Then the dose is increased by titration under the control of the content of PTH and calcium in the blood. The maximum dose, depending on the indications and the effectiveness of treatment, can be 180-360 mg / day. Side effects From the digestive system: very often – nausea, vomiting; often – anorexia; sometimes – dyspepsia, diarrhea. From the side of the nervous system: often – dizziness, paresthesia; sometimes convulsions. From the musculoskeletal system: often – myalgia. From the endocrine system: often – a decrease in testosterone levels. Dermatological reactions: often – rash. Allergic reactions: sometimes – hypersensitivity reactions. From the side of the cardiovascular system: in patients with heart failure, isolated idiosyncratic cases of a decrease in blood pressure and / or worsening of the course of heart failure were recorded. Other: often – asthenia, hypocalcemia. Contraindications for use Children and adolescents under 18 years of age; hypersensitivity to cinacalcet. Use in pregnancy and lactation There are no clinical data on the use of cinacalcet during pregnancy. Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. So far, the possibility of excretion of cinacalcet in human breast milk has not been studied. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding. In experimental studies preclinical studies of cinacalcet in rabbits have shown that cinacalcet crosses the placental barrier. There was no direct negative effect on the course of pregnancy, childbirth or postnatal development. Neither embryotoxic nor teratogenic effects were found in experiments on pregnant female rats and rabbits, with the exception of a decrease in fetal body weight in rats at doses that caused toxicity in pregnant females. Cinacalcet is excreted in breast milk in lactating rats, with a high milk/plasma concentration ratio. Precautions Cinacalcet should not be used when serum calcium levels (adjusted for albumin) are below the lower limit of the normal range. Since cinacalcet lowers serum calcium levels, patients should be carefully monitored for the development of hypocalcemia. In the case of hypocalcemia, calcium-containing phosphate binders, vitamin D, and/or correction of the calcium concentration in the dialysis solution can be used to increase serum calcium levels. With persistent hypocalcemia, dose reduction or discontinuation of cinacalcet should be considered. Potential signs of the development of hypocalcemia can be paresthesia, myalgia, convulsions, tetany. Cinacalcet is not indicated in patients with chronic kidney disease not on dialysis due to an increased risk of hypocalcemia (serum calcium <8.4 mg/dl or <2.1 mmol/l) compared to patients on dialysis, which may be due to lower initial calcium levels and/or the presence of residual kidney function. With caution and under close monitoring of liver function, cinacalcet should be used in patients with moderate to severe hepatic insufficiency (Child-Pugh scale), because. in such cases, the concentration of cinacalcet in plasma can be 2-4 times higher. Chronic suppression of PTH levels below approximately 1. 5% of ULN as measured by iPTH can lead to adynamic bone disease. If the PTH concentration falls below the recommended range, the dose of cinacalcet and/or vitamin D should be reduced or therapy discontinued. Influence on the ability to drive vehicles and mechanisms Some adverse reactions of cinacalcet may affect the ability to drive vehicles or work with mechanisms. Drug interactions Cinacalcet is partially metabolized by the CYP3A4 isoenzyme. Simultaneous administration of ketoconazole (a strong inhibitor of CYP3A4) at a dose of 200 mg 2 times / day led to an increase in the concentration of cinacalcet in plasma by about 2 times. If potent inhibitors (eg, ketoconazole, itraconazole, telithromycin, voriconazole, ritonavir) or CYP3A4 inducers (eg, rifampicin) are needed concomitantly, dose adjustment of cinacalcet may be required. Experimental in vitro studies have shown that cinacalcet is partially metabolized with the participation of the CYP1A2 isoenzyme. Smoking stimulates CYP1A2 activity. Clearance of cinacalcet is 36-38% higher in smokers than in non-smokers. The effect of CYP1A2 inhibitors (fluvoxamine, ciprofloxacin) on plasma concentrations of cinacalcet has not been studied. Dose adjustment may be required if the patient starts/stops smoking or starts/stops concomitant use of potent CYP1A2 inhibitors during drug therapy. Cinacalcet is a potent inhibitor of CYP2D6. The combined use of cinacalcet and drugs with a narrow therapeutic range and / or variable pharmacokinetics, metabolized by the CYP2D6 isoenzyme (for example, flecainide, propafenone, metoprolol, desipramine, nortriptyline, clomipramine), may require dose adjustment of these drugs. Co-administration of cinacalcet 90 mg once daily with desipramine (a tricyclic antidepressant metabolized by CYP2D6) at a dose of 50 mg increases desipramine exposure by 3.6 times in patients with active CYP2D6 metabolism. Keep If you want to place a link to the description of this drug – use this code Cinacalcet . Description of the drug in the reference book Vidal.

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