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SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › CALCIUM HOMEOSTASIS › ANTI-PARATHYROID AGENTS › Other anti-parathyroid agents
cinacalcet
H05BX01
Forms & Strengths
- Oral tablets: 30 mg
- Oral tablets: 60 mg
- Oral tablets: 90 mg
Adult Dosing
- Secondary hyperparathyroidism in CKD on dialysis: Initial 30 mg PO once daily; titrate every 2-4 weeks through 30, 60, 90, 120, and 180 mg daily to target intact PTH 150-300 pg/mL.
- Hypercalcemia in parathyroid carcinoma and primary PTH: Initial 30 mg PO twice daily; titrate every 2-4 weeks through 30 mg twice daily, 60 mg twice daily, 90 mg twice daily, and 90 mg 3-4 times daily as needed to normalize serum calcium.
- Severe hypercalcemia in primary hyperparathyroidism unable to undergo parathyroidectomy: Initial 30 mg PO twice daily.
Pediatric Dosing
- Secondary hyperparathyroidism in CKD on dialysis (age < 18 years): Safety and efficacy have not been established.
Indications
- Treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease on dialysis.
- Treatment of hypercalcemia in adult patients with parathyroid carcinoma.
- Treatment of severe hypercalcemia in adult patients with primary hyperparathyroidism who are unable to undergo parathyroidectomy.
Mechanism of Action
- Calcimimetic agent that increases the sensitivity of the calcium-sensing receptor (CaSR) on the parathyroid gland to extracellular calcium.
- Lowers parathyroid hormone (PTH) secretion, subsequently decreasing serum calcium and phosphorus levels.
Contraindications
- Hypersensitivity to cinacalcet or any component of the product.
- Serum calcium levels falling below the lower limit of normal.
Adverse Reactions
- Nausea and vomiting (frequently leading to treatment discontinuation)
- Hypocalcemia (can be severe and lead to QT prolongation and seizures)
- Diarrhea and myalgia
- Dizziness and asthenia
- Upper respiratory tract infection
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole): May significantly increase cinacalcet plasma concentrations.
- CYP3A4 inducers (e.g., rifampin): May decrease cinacalcet plasma concentrations.
- CYP2D6 substrates (e.g., desipramine, metoprolol, flecainide): Cinacalcet is a strong inhibitor of CYP2D6; may increase concentrations of co-administered drugs metabolized by CYP2D6.
- Other medications that lower serum calcium: Concomitant use increases the risk of hypocalcemia.
Curated Content: Needs Vetting Before Put to Clinical Use