Cinacalcet

What is Cinacalcet?

• Cinacalcet (Sensipar), is a positive modulator of the calcium-sensing receptor.

Cinacalcet

Cinacalcet ball-and-stick

Cinacalcet Structural Formulae

What are the uses of this medicine?

Cinacalcet (Sensipar), is used for:

• for the treatment of secondary hyperparathyroidism (HPT) in adult patients with chronic kidney disease (CKD) on dialysis.
• for the treatment of hypercalcemia in adult patients with Parathyroid Carcinoma.
• of severe hypercalcemia in adult patients with primary HPT for whom parathyroidectomy would be indicated on the basis of serum calcium levels, but who are unable to undergo parathyroidectomy.

How does this medicine work?

• 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.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• serum calcium is less than the lower limit of the normal range.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• antidepressants (mood elevators) such as amitriptyline (Elavil), clomipramine (Anafranil), desipramine (Norpramin), fluoxetine (Prozac, Sarafem), imipramine (Tofranil), nefazodone, nortriptyline (Aventyl, Pamelor), paroxetine (Paxil), protriptyline (Vivactil) and trimipramine (Surmontil)
• antifungals such as fluconazole (Diflucan), itraconazole (Sporanox), and ketoconazole (Nizoral)
• cimetidine (Tagamet)
• cyclosporine (Neoral, Sandimmune)
• danazol (Danocrine)
• delavirdine (Rescriptor)
• diltiazem (Cardizem, Dilacor, Tiazac)
• erythromycin (E.E.S., E-Mycin, Erythrocin)
• flecainide (Tambocor)
• HIV protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir)
• isoniazid (INH, Nydrazid)
• metronidazole (Flagyl)
• oral contraceptives (birth control pills)
• thioridazine (Mellaril)
• troleandomycin (TAO)
• verapamil (Calan, Covera, Isoptin, Verelan)
• vinblastine (Velban)
• zafirlukast (Accolate)

Is this medicine FDA approved?

• Cinacalcet was approved in the United States in March 2004.

How should this medicine be used?

Recommended dosage: For Secondary hyperparathyroidism (HPT) in patients with chronic kidney disease (CKD) on dialysis:

• Starting dose is 30 mg once daily.
• Titrate dose no more frequently than every 2 to 4 weeks through sequential doses of 30, 60, 90, 120, and 180 mg once daily as necessary to achieve targeted intact parathyroid hormone (iPTH) levels.
• iPTH levels should be measured no earlier than 12 hours after most recent dose.

For Hypercalcemia in patients with Parathyroid Carcinoma or hypercalcemia in patients with primary Hyperparathyroidism:

• Starting dose is 30 mg twice daily.
• Titrate dose every 2 to 4 weeks through sequential doses of 30 mg twice daily, 60 mg twice daily, 90 mg twice daily, and 90 mg three or four times daily as necessary to normalize serum calcium levels.

• Once the maintenance dose has been established, monitor serum calcium approximately monthly for patients with secondary HPT and every 2 months for patients with PC or primary HPT.

Administration:

• Cinacalcet comes as a tablet to take by mouth.
• Cinacalcet tablets should be taken with food or shortly after a meal.
• Cinacalcet tablets are administered orally and should always be taken whole and not chewed, crushed, or divided.
• Your doctor will probably start you on a low dose of cinacalcet and gradually increase your dose, not more than once every 2-4 weeks.
• Cinacalcet may help control your condition but will not cure it. Continue to take cinacalcet even if you feel well. Do not stop taking cinacalcet without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 30 mg, 60 mg and 90 mg tablets

This medicine is available in fallowing brand namesː Sensipar

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea and vomiting
• diarrhea
• dizziness
• weakness
• chest pain

Less common,but serious side effects may include:

• Hypocalcemia
• Upper Gastrointestinal Bleeding
• Hypotension, Worsening Heart Failure and/or Arrhythmias
• Adynamic Bone Disease

What special precautions should I follow?

• Cinacalcet lowers serum calcium and can lead to hypocalcemia. Life threatening events and fatal outcomes were reported. Hypocalcemia can prolong QT interval, lower the threshold for seizures, and cause hypotension, worsening heart failure, and/or arrhythmia. Monitor serum calcium carefully for the occurrence of hypocalcemia during treatment.
• Cases of gastrointestinal bleeding, mostly upper gastrointestinal bleeding, have occurred in patients using calcimimetics, including cinacalcet. Patients with risk factors for upper GI bleeding may be at increased risk. Monitor patients and promptly evaluate and treat any suspected GI bleeding.
• In postmarketing safety surveillance, isolated, idiosyncratic cases of hypotension, worsening heart failure, and/or arrhythmia have been reported in patients with impaired cardiac function.
• Advise patients to report nausea and vomiting to their health care provider.
• Advise patients to take cinacalcet tablets with food or shortly after a meal and to take the tablets whole and not divide them.
• Inform patients of the importance of regular blood tests, in order to monitor the safety and efficacy of cinacalcet tablets therapy.
• There are no data regarding the presence of cinacalcet in human milk or effects on the breastfed infant or on milk production.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• hypocalcemia

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• In the event of overdosage, patients should be monitored for signs and symptoms of hypocalcemia and appropriate measures taken to correct serum calcium levels
• Since cinacalcet is highly protein bound, hemodialysis is not an effective treatment for overdosage of cinacalcet tablets.

Can this medicine be used in pregnancy?

• Limited case reports of cinacalcet use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes.

Can this medicine be used in children?

• The safety and efficacy of cinacalcet have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• cinacalcet hydrochloride

Inactive Ingredients:

• cellulose, microcrystalline
• crospovidone
• magnesium stearate
• hypromellose, unspecified
• titanium dioxide
• triacetin
• fd&c blue no. 2
• ferric oxide yellow

Who manufactures and distributes this medicine?

Manufactured For:

• Accord Healthcare, Inc.,
• Slater Road,
• Suite 210-B,
• Durham, NC,
• USA.

Manufactured By:

• Intas Pharmaceuticals Limited,
• Village – Matoda,
• Bavla Road, Ta.- Sanand,
• Dist.- Ahmedabad
• INDIA.

What should I know about storage and disposal of this medication?

• Store at 25ºC (77ºF); excursions permitted from 15°C to 30ºC (59°F to 86ºF).

• Dailymed label info on Cinacalcet
• FDA Cinacalcet