| CINACALCET HYDROCHLORIDE
Classifications: hormone; parathyroid hormone agent; calcium receptor agonist; Therapeutic: parathyroid hormone agent
Pregnancy Category: C
30 mg, 60 mg, 90 mg tablets
Directly lowers parathyroid hormone (PTH) levels by increasing the sensitivity of calcium-sensing receptors on the parathyroid
gland to extracellular calcium. The reduction in PTH causes decreased calcium and phosphate adsorption from bone, and thus
decreased serum calcium and phosphate levels. The drug is a calcium receptor agonist, also known as a calcimimetic agent.
Lowers PTH production; this also decreases rate of bone turnover and bone fibrosis in chronic renal failure disease (CRFD).
Treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis; hypercalcemia in patients
with parathyroid cancer.
Hypersensitivity to cinacalcet; pregnancy (category C), lactation, children <18 y.
Moderate and severe hepatic impairment, hypocalcemia, history of seizures.
Route & Dosage
Adult: PO Start with 30 mg once daily; may increase q24wk until target iPTH of 150300 pg/mL (max: 300 mg/d)
Adult: PO 30 mg twice daily; titrate q24wk as 60 mg b.i.d., 90 mg b.i.d., then 90 mg 34 times daily as needed to normalize
- Give with food or shortly after a meal.
- Tablets should be swallowed whole and not divided, crushed, or chewed.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole:
Dizziness, asthenia, non-cardiac chest pain, dialysis access infection. CV:
Hypertension. GI: Nausea, vomiting, diarrhea,
Hypocalcemia. Musculoskeletal: Myalgia,
adynamic bone disease (renal osteodystrophy).
May increase amoxapine, atomoxetine, carvedilol, metoprolol, propranolol, timolol, encainide, flecainide, mexiletine, propafenone, clozapine,
codeine, cyclobenzaprine, fenfluramine, dexfenfluramine, dextromethorphan, donepezil, fluoxetine, haloperidol, hydrocodone,
maprotiline, meperidine, methadone, methamphetamine, morphine, oxycodone, paroxetine, perphenazine, risperidone, thioridazine
(use may be contraindicated with cinacalcet), tramadol, trazodone,
tricyclic antidepressants, venlafaxine, zolpidem
levels; cinacalcet levels may be increased by strong CYP3A4 inhibitors such as fluconazole, itraconazole, ketoconazole, miconazole, voriconazole, clarithromycin, erythromycin, dalfopristin; quinupristin,
troleandomycin, verapamil, diltiazem, amiodarone, aprepitant, fluvoxamine, nefazodone, zafirlukast, zileuton. Food: Grapefruit juice
may increase cinacalcet levels.
26 h. Distribution:
9397% protein bound. Metabolism:
In liver by CYP3A4. Elimination:
80% by kidneys, 15% in feces. Half-Life:
Assessment & Drug Effects
- Monitor for S&S of hypocalcemia (e.g., paresthesias, myalgias, cramping, tetany, convulsions).
- Withhold drug and notify physician for serum calcium <7.5 mg/dL or symptoms of hypocalcemia. Drug should not be resumed
until serum calcium levels reach 8.0 mg/dL, and/or symptoms of hypocalcemia resolve.
- Lab tests: Serum calcium and phosphorus within 1 wk after and iPTH 14 wk after initiation of drug or dose adjustment;
thereafter, monthly serum calcium and phosphorus (more often with a history of a seizure disorder), and iPTH every 13
- Closely monitor iPTH and serum calcium with concurrent administration of a strong CYP3A4 (e.g., ketoconazole, erythromycin,
Patient & Family Education
- Report promptly any of the following: seizure or convulsion; muscle spasms or cramping of the abdomen, back, legs, face;
burning, numbness, pricking, tickling, or tingling of the face, lips, tongue, hands, or feet; changes in mental status.