Cinacalcet

Generic name: cinacalcet
Brand name: Sensipar
Dosage form: oral tablet (30 mg; 60 mg; 90 mg)
Drug class: Calcimimetics

Medically reviewed by  A Ras MD.

Description

Cinacalcet tablets contain the hydrochloride salt of the active ingredient Cinacalcet, a positive modulator of the calcium sensing receptor. The empirical formula for Cinacalcet is C22H22F3N•HCl with a molecular weight of 393.9 g/mol (hydrochloride salt) and 357.4 g/mol (free base). It has one chiral center having an R-absolute configuration. The R-enantiomer is the more potent enantiomer and has been shown to be responsible for pharmacodynamics activity. The hydrochloride salt of Cinacalcet is a white to off-white, crystalline solid that is soluble in methanol or 95% ethanol and slightly soluble in water. The hydrochloride salt of Cinacalcet is described chemically as N-[1-(R)-(-)-(1-naphthyl)ethyl]-3[3-(tifluoromethyl)phenyl]-1-aminopropane hydrochloride and has the following structural formula:

The following structural formula for hydrochloride salt of cinacalcet is described chemically as N-[1-(R)-(-)-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]-1-aminopropane hydrochloride.

Cinacalcet Tablets are formulated as white to off-white, oval-shaped, biconvex film-coated tablets for oral administration in strengths of 30 mg, 60 mg, and 90 mg of cinacalcet as the free base equivalent (33 mg, 66 mg, and 99 mg as the hydrochloride salt, respectively).

Inactive Ingredients 

The following are the inactive ingredients in Cinacalcet Tablets: pre-gelatinized starch, microcrystalline cellulose, crospovidone, colloidal silicon dioxide and sodium stearyl fumarate.  Tablets are coated with Opadry II white (hypromellose, lactose monohydrate, titanium dioxide, triacetin), and Opadry clear (hypromellose, macrogol/PEG)

 Mechanism of Action

The calcium-sensing receptor on the surface of the chief cell of the parathyroid gland is the principal regulator of PTH synthesis and secretion.  Cinacalcet, the active ingredient in Cinacalcet Tablets, is a calcimimetic agent that directly lowers PTH levels by increasing the sensitivity of the calcium-sensing receptor to activation by extracellular calcium. The reduction in PTH is associated with a concomitant decrease in serum calcium levels.

What is cinacalcet used for?

  • Cinacalcet is used to treat high parathyroid hormone levels in certain patients.
  • It is used to treat high calcium levels in patients with parathyroid disease.

Before taking cinacalcet, tell your doctor:

  • If you are allergic to cinacalcet; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
  • If you have low calcium levels.
  • If you have taken etelcalcetide within the past 4 weeks.

This is not a list of all drugs or health problems that interact with cinacalcet.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take cinacalcet with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take cinacalcet?

  • Tell all of your health care providers that you take cinacalcet. This includes your doctors, nurses, pharmacists, and dentists.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • This medicine lowers blood calcium levels. Life-threatening and fatal events linked to low blood calcium levels have happened in people taking cinacalcet.
  • This medicine is not approved for use in children. A death has happened in a child with severe low blood calcium levels. Talk with the doctor.
  • Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is cinacalcet best taken?

Use cinacalcet as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take with or right after a meal.
  • Swallow whole. Do not chew, break, or crush.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it, with food.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

What are the side effects of cinacalcet that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of low calcium levels like muscle cramps or spasms, numbness and tingling, or seizures.
  • Signs of high or low blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
  • Signs of dehydration like dry skin, mouth, or eyes; thirst; fast heartbeat; dizziness; fast breathing; or confusion.
  • Signs of electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, seizures, not hungry, or very bad upset stomach or throwing up.
  • Chest pain or pressure.
  • Low mood (depression).
  • Joint pain.
  • Bone pain.
  • Stomach or bowel bleeding has happened with cinacalcet. Call your doctor or get medical help right away if you have black, tarry, or bloody stools; throwing up blood or throw up that looks like coffee grounds; very bad stomach pain; or very upset stomach or throwing up.
  • Heart failure has gotten worse in some people taking cinacalcet. If you have heart failure, talk with your doctor. Call your doctor right away if you have shortness of breath, a big weight gain, or swelling in the arms or legs.

What are some other side effects of cinacalcet?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Feeling dizzy, tired, or weak.
  • Headache.
  • Constipation, diarrhea, stomach pain, upset stomach, throwing up, or feeling less hungry.
  • Cough.
  • Signs of a common cold.
  • Back pain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out cinacalcet?

  • Store at room temperature in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

 

Label

PRINCIPAL DISPLAY PANEL

  • NDC 71093-152-01
  • Cinacalcet Tablets
  • Rx Only
  • 30 tablets
  • 30 mg
  • Each film-coated tablet contains:
  • Cinacalcet 30 mg (equivalent to 33 mg of Cinacalcet Hydrochloride).
  • Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
  • See USP controlled room temperature.
  • Dispense in tight, light-resistant container per USP.
  • Distributed by
  • ACI Healthcare USA, Inc.
  • 10100 W. Sample Road,
  • Suite 406Coral Springs, FL 33065
30 mg

Imprint CL 410 - cinacalcet 30 mg

PRINCIPAL DISPLAY PANEL

  • NDC 71093-153-01
  • Cinacalcet Tablets
  • Rx Only
  • 30 tablets
  • 60 mg
  • Each film-coated tablet contains:
  • Cinacalcet 60 mg (equivalent to 66 mg of Cinacalcet Hydrochloride).
  • Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
  • See USP controlled room temperature.
  • Dispense in tight, light-resistant container per USP.
  • Distributed by
  • ACI Healthcare USA, Inc.
  • 10100 W. Sample Road,
  • Suite 406Coral Springs, FL 33065
60 mg

Imprint CL 411 - cinacalcet 60 mg

PRINCIPAL DISPLAY PANEL

  • NDC 71093-154-01
  • Cinacalcet Tablets
  • Rx Only
  • 30 tablets
  • 90 mg
  • Each film-coated tablet contains:
  • Cinacalcet 90 mg (equivalent to 99 mg of Cinacalcet Hydrochloride).
  • Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
  • See USP controlled room temperature.
  • Dispense in tight, light-resistant container per USP.
  • Distributed by
  • ACI Healthcare USA, Inc.
  • 10100 W. Sample Road,
  • Suite 406Coral Springs, FL 33065
90 mg

SRC: NLM .