cinacalcet


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cinacalcet

(sin-a-kal-set) ,

Sensipar

(trade name)

Classification

Therapeutic: hypocalcemics
Pharmacologic: calcimimetic agents
Pregnancy Category: C

Indications

Secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on dialysis.Hypercalcemia caused by parathyroid carcinoma.Severe hypercalcemia in patients with primary hyperparathyroidism in patients who are unable to undergo parathyroidectomy.

Action

Increases sensitivity of calcium-sensing receptors located on the surface of chief cells of parathyroid gland to levels of extracellular calcium. This decreases parathyroid hormone production with resultant decrease in serum calcium.

Therapeutic effects

Decreased bone turnover and fibrosis.
Decreased serum calcium.

Pharmacokinetics

Absorption: Well absorbed following oral administration, absorption is enhanced by food and further enhanced by a high fat meal.
Distribution: Unknown.
Protein Binding: 93–97%.
Metabolism and Excretion: Highly metabolized by CYP3A4, CYP2D6, and CYP1A2 enzyme systems; 80% excreted in urine as metabolites, 15% in feces.
Half-life: 30–40 hr.

Time/action profile (effect on PTH levels)

ROUTEONSETPEAKDURATION
POrapid2–6 hr6–12 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Hypocalcemia; Lactation: Discontinue drug or bottle-feed.
Use Cautiously in: History of seizure disorder (↑ risk of seizures with hypocalcemia);Chronic kidney disease patients who are not being dialyzed (↑ risk of hypocalcemia);Intact parathyroid hormone (iPTH) level <150 pg/mL (dose ↓ or discontinuation may be warranted);Moderate to severe hepatic impairment; Obstetric: Use only if benefits justify risks to fetus; Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • seizures

Gastrointestinal

  • nausea (most frequent)
  • vomiting (most frequent)

Fluid and Electrolyte

  • hypocalcemia

Metabolic

  • adynamic bone disease

Interactions

Drug-Drug interaction

Inhibits CYP2D6 and may ↑ levels of flecainide, vinblastine, thioridazine, metoprolol, carvedilol, and most tricyclic antidepressants ; dose adjustments may be necessary.Blood levels are ↑ by strong CYP3A4 inhibitors including ketoconazole, itraconazole, and erythromycin ; monitoring and dose adjustment may be necessary.

Route/Dosage

Oral (Adults) Secondary hyperparathyroidism in CKD patients on dialysis—30 mg once daily; may ↑ dose every 2–4 wk (dose range 30–180 mg once daily) based on iPTH levels; Parathyroid carcinoma or primary hyperparathyroidism—30 mg twice daily; may titrate every 2–4 wk up to 90 mg 3–4 times daily based on serum calcium levels.

Availability

Tablets: 30 mg, 60 mg, 90 mg

Nursing implications

Nursing assessment

  • Monitor for signs and symptoms of hypocalcemia (paresthesias, myalgias, cramping, tetany, convulsions) during therapy. If calcium levels decrease to below normal, serum calcium may be increased by adjusting dose (see Lab Test Considerations) and providing supplemental serum calcium, initiating or increasing dose of calcium-based phosphate binder or vitamin D.
  • Lab Test Considerations: Monitor serum calcium and phosphorous levels within 1 wk after initiation of therapy or dose adjustment and monthly for patients with hyperparathyroidism or every 2 mo for patients with parathyroid carcinoma once maintenance dose has been established, especially in patients with a history of seizure disorder. Therapy should not be initiated in patients with serum calcium less than the lower limit of normal (8.4 mg/dL).
    • If serum calcium ↓ below 8.4 mg/dL but remains above 7.5 mg/dL, or if symptoms of hypocalcemia occur, use calcium-containing phosphate binders and/or vitamin D sterols to ↑ serum calcium. If serum calcium ↓ below 7.5 mg/dL, or if symptoms of hypocalcemia persist and the dose of vitamin D cannot be ↑, withhold administration of cinacalcet until serum calcium levels reach 8.0 mg/dL, and/or symptoms of hypocalcemia resolve. Re-initiate therapy using next lowest dose of cinacalcet.
    • Monitor serum iPTH levels 1 to 4 wk after initiation of therapy or dose adjustment, and every 1 to 3 mo after maintenance dose has been established. If iPTH levels ↓ below 150–300 pg/mL, reduce dose or discontinue cinacalcet.
    • Monitor liver function tests in patients with moderate to severe hepatic impairment during therapy.

Potential Nursing Diagnoses

Deficient knowledge, related to medication regimen (Patient/Family Teaching)

Implementation

  • Cinacalcet may be used alone or in combination with vitamin D and/or phosphate binders.
  • Oral: Administer with food or shortly after a meal. Take tablets whole, do not crush, break or chew.

Patient/Family Teaching

  • Instruct patient to take cinacalcet as directed.
  • Advise patient to report signs and symptoms of hypocalcemia to health care professional promptly.
  • Emphasize the importance of follow-up lab tests to monitor safely and efficacy.

Evaluation/Desired Outcomes

  • Decreased serum calcium levels.
References in periodicals archive ?
In the secondary analysis of the Achieve trial [6], 91 hemodialysis patients were administered low-dose of calcitriol analogues calcimimetic agent cinacalcet and FGF-23 levels were observed to decrease by 9,7% in cinacalcet group.
Cinacalcet, a calcimimetic for control of hypercalcemia and secondary hyperparathyroidism, was also started.
She was initiated on cinacalcet (Sensipar[R]) for treatment of calciphylaxis presenting as painful subcutaneous nodules on her shins.
Our objective was to determine whether N-PTH is overproduced in parathyroid cancer, the severest form of primary hyperparathyroidism (PHPT) and, if so, whether this overproduction is affected by therapy with the calcimimetic cinacalcet.
Teva Pharmaceutical Industries Ltd., announced that it has resolved its ongoing dispute with Amgen over Tevas generic cinacalcet HCl product.
The company carried out two pooled placebo-controlled trials in over 1,000 patients and a head-to-head study to assess etelcalcetide compared with cinacalcet.
Como una medida alternativa no quirurgica, se ha utilizado el cinacalcet, la ablacion percutanea de la paratiriodes, con sustancias como medios de contraste, termoablacion con laser o alcohol puro, siendo un manejo seguro, poco invasivo y con menor riesgo, como fuera ya descrito en Colombia entre otros por el grupo de la Fundacion Santa Fe de Bogota (7).
On admission, J.D.'s medications included allopurinol (Zyloprim[R]) 100 mg daily, calcitriol (Rocaltrol[R]) 0.25 mcg twice daily, Os-Cal[R] D 500 mg by mouth (po) twice daily, cinacalcet (Sensipar[R]) 60 mg daily, warfarin (Coumadin[R]), digoxin 0.125 mg daily, furosemide (Lasix[R]) 80 mg po twice daily, metolazone (Zaroxolyn[R]) 10 mg daily, Novolin 70/30-60 units subcutaneous (SQ) in the morning and 40 units SQ each evening, Novolin R sliding scale, levothyroxine sodium (Synthroid[R]) 50 mcg daily, acetaminophen and oxycodone (Percocet[R]) 5-325 1 pill every 4 hours as needed (prn), and simvastatin (Zocor[R]) 40 mg at the hour of sleep.
Cinacalcet HCl is a new calcimimetic agent that has been used successfully for the treatment of primary and secondary hyperparathyroidism in adults (10-12), but its use in adolescents with persistent primary hyperparathyroidism has not been previously reported.
* Sensipar[R]/Mimpara[R] (cinacalcet) sales decreased 57 percent driven primarily by the impact of competition on unit demand and, to a lesser extent, changes in inventory.
M2 EQUITYBITES-February 27, 2015-Amgen meet endpoints in Phase III study comparing AMG 416 with cinacalcet