Calcelar 25

Calcelar 25

Manufacturer:

Unison

Distributor:

Medline

Marketer:

Medline
Full Prescribing Info
Contents
Cinacalcet hydrochloride.
Description
Each film coated tablet contains Cinacalcet hydrochloride 27.55 mg eq. to Cinacalcet 25 mg.
Action
Pharmacology: Pharmacodynamics: Increased the sensitivity of the calcium-sensing receptor on the parathyroid gland thereby, concomitantly lowering parathyroid hormone (PTH), serum calcium, and serum phosphorus levels, preventing progressive bone disease and adverse events associated with mineral metabolism disorders.
Pharmacokinetics: Distribution: Vd: ~ 1,000 L.
Protein binding: ~ 93% to 97%.
Metabolism: Hepatic (extensive) via CYP3A4, 2D6, 1A2; forms inactive metabolites.
Half-life elimination: Terminal: 30 to 40 hours; moderate hepatic impairment: 65 hours; severe hepatic impairment: 84 hours.
Time to peak, Plasma: ~ 2 to 6 hours; increased with food.
Excretion: Urine ~ 80% (as metabolites); feces~ 15%.
Indications/Uses
Secondary hyperparathyroidism in patients undergoing maintenance dialysis.
Dosage/Direction for Use
Administer with a food or shortly after a meal.
Do not break or divide tablet; should be taken whole.
Do not titrate dose more frequently than every 2 to 4 weeks.
May be used alone or in combination with vitamin D and/or phosphate binders.
Dosage adjustment may be required in patients on concurrent CYP3A4 inhibitors.
Secondary hyperparathyroidism: The starting dosage for adult is 25 mg of cinacalcet once daily, to be orally administered. With careful management of the patient's serum parathyroid hormone (PTH) and calcium levels, the dose may then be adjusted with a range of 25-75 mg once daily. If no improvement is found in PTH, the dose may be increased up to 100 mg once daily. If dose increase is required, dose should be increased by 25 mg at a time, at intervals of at least 3 weeks.
Dosage adjustment for hypocalcemia: Hypocalcemia (serum calcium 7.5 to 8.4 mg/dL or hypocalcemia symptoms): Raise calcium levels with calcium-containing phosphate binders and vitamin D sterols.
Hypocalcemia (serum calcium less than 7.5 mg/dL or persistent symptoms and unable to increase vitamin D dose): Stop cinacalcet therapy and reinitiate with the next lowest dose when serum calcium reaches 8 mg/dL or symptoms resolve.
If iPTH <150 pg/dL: Reduce dose or discontinue cinacalcet and/or vitamin D.
Dosage adjustment for renal impairment: No dosage adjustment necessary.
Dosage adjustment for hepatic impairment: Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate to severe impairment (Child-Pugh class B or C): May have an increased exposure to cinacalcet and increased half-life. Dosage adjustment may be necessary based on serum calcium, serum phosphorus and/or iPTH.
Overdosage
Overdose data are limited. Doses up to 300 mg daily in dialysis patients have been well-tolerated. Overdose effects are anticipated to be an extension of adverse effect following therapeutic administration.
Management of mild to moderate toxicity: Treatment is symptomatic and supportive. Correct any significant fluid and/or electrolyte abnormalities in patients with severe diarrhea and/or vomiting.
Management of severe toxicity: Treatment is symptomatic and supportive. Intravenous administration of calcium gluconate or calcium chloride may be required for significant hypocalcemia. Institute continuous cardiac monitoring and monitor ECG for evidence of QT prolongation or dysrhythmias. Treat seizures with IV benzodiazepines; barbiturates or propofol may be needed if seizures persist or reoccur.
Contraindications
Hypersensitivity to cinacalcet or to any of the excipients.
Serum calcium lower than lower limit of normal range.
Special Precautions
Cardiovascular: QT interval prolongation and ventricular arrhythmia secondary to hypocalcemia have been reported.
Arrhythmia, hypotension, and worsening of heart failure have been reported in patients with impaired cardiac function.
Endocrine and metabolic: Hypocalcemia can occur and may result in life-threatening or fatal events; monitor recommended.
Not indicated for use in patients not undergoing dialysis due to an increased risk of hypocalcemia.
Hepatic: Monitoring recommended in patients with hepatic impairment.
Musculoskeletal: Adynamic bone disease may occur with intact parathyroid hormone (iPTH) levels less than 100 pg/mL.
Neurologic: Seizures have been reported and may be due to hypocalcemia; monitoring recommended.
Use In Pregnancy & Lactation
Pregnancy risk factor C.
There are no adequate and well controlled studies in pregnant women. Weigh the potential benefits of treatment against potential risks before prescribing cinacalcet.
It is not known if cinacalcet is excreted in breast milk. Due to potential for clinically significant adverse reaction in the nursing infant, a decision should be made whether to discontinue nursing or the drug.
Adverse Reactions
Cardiovascular: Hypertension, hypotension.
Central nervous system: Depression, dizziness, fatigue, headache, noncardiac chest pain, paresthesia, seizure.
Endocrine & metabolic: Dehydration, hypercalcemia, hyperkalemia, hypocalcemia, hypoparathyroidism (intact parathyroid hormone).
Gastrointestinal: Abdominal pain, anorexia, constipation, decreased appetite, diarrhea, dyspepsia, nausea, vomiting, upper abdominal pain.
Hematologic: Anemia.
Neuromuscular & skeletal: Arthralgia, back pain, bone fracture, limb pain, muscle spasm, myalgia, weakness.
Respiratory: Cough, dypsnea, upper respiratory tract infection.
Hypersensitivity: Hypersensitivity reaction.
Infection: Localized infection (dialysis access site).
Rare but important or life-threatening: Adynamic bone disease, cardiac arrhythmia, cardiac failure, hypotension (idiosyncratic), prolonged QT interval on ECG (secondary to hypocalcemia), ventricular arrhythmia (secondary to hypocalcemia).
Drug Interactions
Concurrent use of clozapine and CYP1A2, CYP2D6 or CYP3A4 inhibitors may result in increased clozapine exposure and increased risk of adverse effects.
Concurrent use of nebivolol, donepezil, brexpiprazole, doxorubicin, amitriptyline, tamsulosin, oxycodone, propranolol and CYP2D6 inhibitors may result in increased exposure to those medicines.
Concurrent use of eliglustat, fluoxetine and selected strong or moderate CYP2D6 inhibitors may result in increased those medicines exposure and subsequent prolongation of the QT interval.
Concurrent use of cinacalcet and desipramine, flecainide, doxepin, clomipramine, imipramine, vinblastine, protriptyline, amoxapine, nortriptyline, thioridazine, carvedilol, or trimipramine may result in increased those medicine exposure and plasma concentrations.
Concurrent use of ketoconazole and cinacalcet may result in increased bioavailability of cinacalcet and risk of hypocalcemia.
Concurrent use of indinavir, erythromycin, ritonavir, clarithromycin, nelfinavir, nefazodone, atazanavir, telithromycin, voriconazole, saquinavir, fosamprenavir, or delavirdine and cinacalcet may result in increased cinacalcet exposure and plasma concentrations.
Concurrent use of tamoxifen and cinacalcet may result in increased plasma levels of tamoxifen and decreased plasma levels of the active metabolite.
Storage
Store below 30°C.
ATC Classification
H05BX01 - cinacalcet ; Belongs to the class of other anti-parathyroid agents. Used in the management of calcium homeostasis.
Presentation/Packing
FC tab 25 mg (light green, round, biconvex, beveled on both sides with engraved CC 25 on one side and plain on the other) x 1 x 10's, 10 x 10's.
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