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Drugs reference index «Cinacalcet Hydrochloride»

Cinacalcet Hydrochloride

Pronunciation: (sin-a-KAL-set HYE-droe-KLOR-ide)Class: Calcimimetic

Trade Names:Sensipar- Tablets 30 mg- Tablets 60 mg- Tablets 90 mg

Pharmacology

Lowers parathyroid hormone (PTH) levels by increasing sensitivity of calcium-sensing receptor to extracellular calcium.

Pharmacokinetics

Absorption

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.

Distribution

Vd is approximately 1,000 L. Protein binding is 93% to 97%.

Metabolism

Metabolized by CYP3A4, CYP2D6, and CYP1A2.

Elimination

Terminal half-life 30 to 40 h. Approximately 80% of a dose is recovered in the urine and 15% in the feces.

Special Populations

Renal Function Impairment

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.

Indications and Usage

Treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis; hypercalcemia in patients with parathyroid carcinoma.

Contraindications

Standard considerations.

Dosage and Administration

Parathyroid CarcinomaAdults

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.

General Advice

  • Can be used alone or in combination with vitamin D and/or phosphate binders.
  • Administer prescribed dose with food or shortly after a meal. Instruct patient to swallow tablets whole and not to crush, chew, or divide.

Storage/Stability

Store tablets at 59° to 86°F.

Drug Interactions

Drugs metabolized by CYP2D6 (eg, dextromethorphan, flecainide, most tricyclic antidepressants [eg, amitriptyline, desipramine], thioridazine, vinblastine)

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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (7%); idiosyncratic hypotension and worsening heart failure (postmarketing).

CNS

Dizziness (10%).

Dermatologic

Rash (postmarketing).

GI

Nausea (31%); vomiting (27%); diarrhea (21%); anorexia (6%).

Hypersensitivity

Hypersensitivity (postmarketing).

Musculoskeletal

Myalgia (15%).

Miscellaneous

Asthenia (7%); noncardiac chest pain (6%); access infection (5%).

Precautions

Monitor

Calcium/Phosphorus

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.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic Function

Closely monitor PTH and serum calcium concentrations throughout therapy in patients with moderate or severe hepatic function impairment.

Adynamic bone disease

May occur if intact PTH levels are suppressed below 100 pg/mL.

Calcium-containing phosphate binders

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.

Hypocalcemia

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.

Hypotension and/or worsening heart failure

During postmarketing experience, idiosyncratic cases of hypotension and/or worsening of heart failure have been reported in patients with impaired cardiac function.

Parathyroid carcinoma patients

See monitoring.

PTH levels

Ensure that dose of cinacalcet and/or vitamin D is reduced if intact PTH levels decrease to less than 150 pg/mL.

Seizures

Seizures may occur. Closely monitor serum calcium levels, particularly in patients with a history of seizures.

Overdosage

Symptoms

Hypocalcemia.

Patient Information

  • Advise patient to take prescribed dose with food or shortly after a meal. Caution patient to swallow tablets whole and not to chew, divide, or crush.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient to continue taking other medications (eg, vitamin D and/or phosphate binders) as prescribed by health care provider for controlling calcium levels.
  • Instruct patient to immediately inform health care provider if the following signs or symptoms of hypocalcemia develop: abnormal skin sensations, muscle aches, muscle cramping or spasm, seizure activity.

Copyright © 2009 Wolters Kluwer Health.

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