Trade Names:Sensipar- Tablets 30 mg- Tablets 60 mg- Tablets 90 mg
Lowers parathyroid hormone (PTH) levels by increasing sensitivity of calcium-sensing receptor to extracellular calcium.
C max is approximately 2 to 6 h. Steady state achieved within 7 days.
C max increases proportionally over the dose range of 30 to 180 mg.
Vd is approximately 1,000 L. Protein binding is 93% to 97%.
Metabolized by CYP3A4, CYP2D6, and CYP1A2.
Terminal half-life 30 to 40 h. Approximately 80% of a dose is recovered in the urine and 15% in the feces.
Pharmacokinetics in patients with mild, moderate, or severe renal function impairment and those on hemodialysis or peritoneal dialysis are comparable with healthy volunteers.Hepatic Function Impairment
In patients with moderate or severe hepatic function impairment, the AUCs were 2.4 and 4.2 times higher, respectively, than in healthy subjects; the half-life is prolonged 33% and 70%, respectively.Elderly
Pharmacokinetics are similar in patients 65 yr of age and older compared with patients younger than 65 yr of age.
Treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis; hypercalcemia in patients with parathyroid carcinoma.
PO Start with 30 mg twice daily. Titrate every 2 to 4 wk through sequential doses of 30, 60, and 90 mg twice daily, and 90 mg 3 or 4 times daily as needed to normalize serum calcium levels.Secondary Hyperparathyroidism in Patients with Chronic Kidney Disease on DialysisAdults
PO Start with 30 mg daily. Titrate dose every 2 to 4 wk through sequential doses of 60, 90, 120, and 180 mg daily based on target intact PTH.
Store tablets at 59° to 86°F.
Plasma concentrations of these agents may be elevated, increasing the pharmacologic effects and adverse reactions. Dosage adjustments may be needed, especially in agents with a narrow therapeutic index.Strong inhibitors of CYP3A4 (eg, erythromycin, itraconazole, ketoconazole)
Cinacalcet concentrations may be elevated, increasing the pharmacologic effects and adverse reactions. Closely monitor patients and adjust the cinacalcet dose as needed.
None well documented.
Hypertension (7%); idiosyncratic hypotension and worsening heart failure (postmarketing).
Nausea (31%); vomiting (27%); diarrhea (21%); anorexia (6%).
Asthenia (7%); noncardiac chest pain (6%); access infection (5%).
Measure serum calcium and serum phosphorus within 1 wk and measure PTH 1 to 4 wk after initiating or adjusting the dose of cinacalcet. Once a maintenance dose is established, measure serum calcium and serum phosphorus monthly, and PTH every 1 to 3 months. Closely monitor PTH and serum calcium concentrations throughout treatment in patients with moderate or severe hepatic function impairment.Hypocalcemia
Carefully monitor patient for signs and symptoms of hypocalcemia (eg, convulsions, cramping, myalgia, paresthesias, tetany).Parathyroid carcinoma patients
Measure serum calcium within 1 wk after cinacalcet initiation or dose adjustment. Once the maintenance dose level has been established, measure serum calcium every 2 months. Ensure that therapy is not started in patients whose baseline serum calcium is less than 8.4 mg/dL.PTH
Ensure that intact PTH is measured 1 to 4 wk after initiating therapy or dose adjustment and then every 1 to 3 mo once maintenance dose has been established.
Category C .
Safety and efficacy not established.
Closely monitor PTH and serum calcium concentrations throughout therapy in patients with moderate or severe hepatic function impairment.
May occur if intact PTH levels are suppressed below 100 pg/mL.
Be prepared to administer calcium-containing phosphate binders and/or vitamin D to patient who develops symptoms of hypocalcemia, or whose serum calcium level falls below 8.4 mg/dL but is above 7.5 mg/dL.
May occur; closely monitor. Ensure that cinacalcet is temporarily discontinued in patient whose serum calcium falls below 7.5 mg/dL or if symptoms of hypocalcemia persist and the dose of vitamin D cannot be increased. Therapy can be reinstituted using next lowest dose when serum calcium level reaches 8 mg/dL and/or symptoms of hypocalcemia have resolved.
During postmarketing experience, idiosyncratic cases of hypotension and/or worsening of heart failure have been reported in patients with impaired cardiac function.
Ensure that dose of cinacalcet and/or vitamin D is reduced if intact PTH levels decrease to less than 150 pg/mL.
Seizures may occur. Closely monitor serum calcium levels, particularly in patients with a history of seizures.
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