Dosing and uses of Sensipar (cinacalcet)
Adult dosage forms and strengths
tablet
- 30mg
- 60mg
- 90mg
Secondary Hyperparathyroidism (HPT)
Indicated for secondary HPT in patients with chronic kidney disease on dialysis
Initial dose: 30 mg PO qDay
May increase if needed by titrating at 2-4 week intervals through sequential doses of 60, 90, 120, or 180 mg qDay
Hypercalcemia in Patients with Parathyroid Carcinoma
Initial dose: 30 mg PO q12hr
May increase if needed at 2-4 week intervals through sequential doses 60 mg q12hr, 90 mg q12hr, or 90 mg q6-8hr as necessary to normalize serum calcium levels
Hypercalcemia With Primary Hyperparathyroidism (HPT)
Indicated for severe hypercalcemia in patients with primary HPT who are unable to undergo parathyroidectomy
Initial dose: 30 mg PO q12hr
May increase if needed at 2-4 week intervals through sequential doses 60 mg q12hr, 90 mg q12hr, or 90 mg q6-8hr as necessary to normalize serum calcium levels
Renal Impairment
Dose adjustment not necessary
Monitor
Secondary parathyroidism: Serum calcium (Ca), serum phosphorus and parathyroid hormone (PTH)
Parathyroid Cancer: Serum Ca
Monitoring of PTH and serum Ca particularly important for patients with hepatic impairment
Pediatric dosage forms and strengths
Safety and efficacy not established
Secondary Hyperparathyroidism (Orphan)
Orphan designation for treatment of secondary hyperparathyroidism (HPT) in pediatric patients with chronic kidney disease receiving dialysis
Sponsor
- Amgen, Inc; One Amgen Center Drive; Bldg 17, 1A-4-4, Mail Stop 17-1-B; Thousand Oaks, California 91320
Sensipar (cinacalcet) adverse (side) effects
>10%
Secondary Parathyroidism
- Diarrhea (20%)
- Nausea (19%)
- Vomiting (15%)
- Myalgia (14%)
1-10%
Secondary Parathyroidism
- Dizziness (8%)
- Hypertension (5%)
- Access infection (4%)
- Anorexia (4%)
- Asthenia (4%)
- Noncardiac chest pain (4%)
- Seizures 1.4%
Frequency not defined
Parathyroid CA
- Nausea/vomiting
- Hypocalcemia
Warnings
Contraindications
Hypersensitivity
Should not be initiated in severe hypocalcemia (serum Ca <lower limit of normal)
Cautions
History of seizure; seizures (primarily generalized or tonic-clonic) were observed in clinical trials (1.4% compared with 0.7% in placebo)
Not for therapy of patients with chronic kidney disease not on dialysis due to increased risk for hypokalemia
Cinacalcet exposure is increased in patients with moderate and severe hepatic impairment; monitor serum calcium, serum phosphorus, and intact parathyroid hormone closely
Adynamic bone disease may develop if PTH levels <100 pg/mL
Parathyroid carcinoma or primary hyperparathyroidism: Monitor serum calcium every 2 months
Monitoring serum calcium for secondary hyperparathyroidism in patients with CKD on dialysis
- Monitor serum calcium monthly
- If calcium levels fall to 7.5-8.4 mg/dL or hypocalcemia symptoms occur, give calcium-containing phosphate binders and/or vitamin D sterols to raise serum calcium
- If calcium levels <7.5 mg/dL or hypocalcemia symptoms persist and the dose of vitamin D cannot be increased, withhold cinaclacet until calcium levels reach 8 mg/dL and/or hypocalcemia symptom resolve, then reinitiate using next lowest dose
Pregnancy and lactation
Pregnancy category: C
Lactation: excretion in milk unknown/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Sensipar (cinacalcet)
Mechanism of action
Increases sensitivity of Ca-sensing receptor in parathyroid cells to activation by extracellular Ca, thereby downregulating PTH levels and consequently lowering serum Ca & phosphorus
Absorption
Bioavailability: High fat meal increases both peak plasma concentration and AUC vis-a-vis fasting
Peak Plasma Time: 2-6 hr
Distribution
Protein Bound: 93-97%
Vd: 1000 L
Metabolism
Metabolism: metabolized by CYP3A4, CYP2D6 & CYP1A2
Metabolites: hydrocinnamic and hydroxy-hydrocinnamic acid, naphthalene-ring-containing molecules, dihydrodiols
Enzyme Inhibited: CYP2D6
Elimination
Half-Life: 30-40 hr
Excretion: Urine (80%); feces (15%)
Administration
Oral Administration
Take with food or shortly after meaL
Swallow tablet whole, do not chew, crush, or divide
