Cinacalcet
Cinacalcet decreases levels of parathyroid hormone (PTH), calcium, and phosphorous in the body. Cinacalcet is used to treat hyperparathyroidism (overactive functioning of the parathyroid glands) in people who are on long-term dialysis for kidney disease. Cinacalcet is also used to treat hypercalcemia (high levels of calcium in the blood) in people with cancer of the parathyroid gland, and in people with overactive parathyroid glands that cannot be treated surgically.
Mechanism of effect
Increases 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.
Pharmacodynamic
Pharmacokinetics
Metabolism:Hepatic (extensive) Excretion:Urine ~80% (as metabolites); feces ~15% Time to Peak:~2 to 6 hours; increased with food Half-Life Elimination:Terminal: 30 to 40 hours Protein Binding:~93% to 97%
Drug indications
Hyperparathyroidism, primary , Hyperparathyroidism, secondary , Parathyroid carcinomaDosage
Dosing: Adult Hyperparathyroidism, primary: Oral: Initial: 30 mg twice daily; increase dose incrementally (to 60 mg twice daily, 90 mg twice daily, and 90 mg 3 or 4 times daily) as necessary to normalize serum calcium levels. Hyperparathyroidism, secondary: Oral: Initial: 30 mg once daily; increase dose incrementally (to 60 mg once daily, 90 mg once daily, 120 mg once daily, and 180 mg once daily) as necessary to maintain intact parathyroid hormone (iPTH) level between 150 to 300 pg/mL. Parathyroid carcinoma: Oral: Initial: 30 mg twice daily; increase dose incrementally (to 60 mg twice daily, 90 mg twice daily, and 90 mg 3 to 4 times daily) as necessary to normalize serum calcium levels
Drug contraindications
hypersensitivity to drug or its components. , hypocalcemia
Side effects
nausea , Headache , vomiting , fatigue , Depression , Dyspnea , hypotension , anemia , paresthesia , Cough , myalgia , dehydration , Arthralgia , Upper respiratory tract infection , Hypocalcemia
Interactions
Amitriptyline , Ipratropium bromide , Pimozide , Tamsulosin , Aripiprazole , Aprepitant , Expectorant codein , Doxorubicin , Metoprolol , Clozapine , Granisetron , Mexiletine , Venlafaxine , Rifabutin , Burosumab , Pitolisant , Lopinavir and Ritonavir , EliglustatAlerts
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. Not indicated for chronic kidney disease (CKD) patients not receiving dialysis
Points of recommendation
Administer with food or shortly after a meal. Do not break or divide tablet; should be taken whole. Monitor for signs/symptoms of hypocalcemia
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