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.

cinacalcet

a calcium receptor agonist that directly lowers parathyroid hormone levels by increasing sensitivity of calcium-sensing receptors to extracellular calcium.
indications This drug is used to treat hypercalcemia in parathyroid carcinoma and secondary hyperparathyroidism in chronic kidney disease requiring dialysis.
contraindication Known hypersensitivity to this drug prohibits its use.
adverse effects Adverse effects of this drug include dizziness, hypertension, nausea, diarrhea, vomiting, anorexia, access infection, noncardiac chest pain, asthenia, and myalgia.
References in periodicals archive ?
Patient's Home Medications Albuterol (Ventolin[R]) as needed Aspirin 325 mg two tablets three times daily Carisoprodol (Soma[R]) 350 mg three times daily Cinacalcet (Sensipar[R]) 30 mg Monday, Wednesday, and Friday Dicyclomine (Bentyl[R]) 10 mg two capsules every 4 hours as needed Docusate (Colace[R]) 200 mg three times daily Folic acid 1 mg daily Fluticasone/salmeterol (Advair[R]) inhaler 250/50 one puff twice daily Magnesium 800 mg daily Multivitamin 1 tablet daily Oxycodone controlled release (Oxycontin[R]) 30 mg three times daily Oxycodone immediate release 5 mg three tablets every 3 hours as needed Senna 1 tablet three times daily as needed Valsartan (Diovan[R]) 160 mg daily Vitamin D 100 international units Monday to Friday Zoledronic acid (Reclast[R]) infusion yearly TABLE 2.
To correct the calcium-phosphate balance, several medications have been used, including sodium thiosulfate and cinacalcet.
Nine medicines incorporated received more than 250 responses (just one had more than 500): fingolimod for the 3rd line of treatment of multiple sclerosis (530 responses); cinacalcet and paricalcitol for therapy related to secondary hyperparathyroidism on chronic renal diseases requiring dialysis; antiviral dolutegravir sodium for HIV-related infections; palivizumab for the prevention of infections related to the respiratory syncytial virus, and sofosbuvir, daclatasvir and simeprevir indicated for chronic hepatitis C.
In an appraisal consultation document, the National Institute for Health and Care Excellence (NICE) has recommended Amgen's (NASDAQ: AMGN) Parsabiv (etelcalcetide) to treat secondary hyperparathyroidism (sHPT), if treatment with a calcimimetic is indicated but cinacalcet is not suitable, and as long as the company provides the drug with the discount agreed in the patient access scheme, Pharma Times reported on Tuesday.
1,5 Biphosphonates, phosphate binders, cinacalcet and sodium thiosulfate may be used.
Bone histomorphometry before and after long-term treatment with cinacalcet in dialysis patients with secondary hyperparathyroidism.
6) Elevated PTH levels in the dialysis population may be managed with activated vitamin D and/or cinacalcet.
For example, the co-administration of cinacalcet, a medication used to treat secondary hyperparathyroidism combined with metoprolol, a medication used to treat hypertension can cause cinacalcet to be less active in the body because both cinacalcet and metoprolol are inhibitors of the CYP26 pathway (Amgen, 2004).
La funcion renal permanecio estable durante el tratamiento, pero los niveles de calcio serico no disminuyeron en forma significativa a pesar de las dosis altas de cinacalcet, optandose por una dosis de mantenimiento de 90 mg.
Furthermore, results from the Evaluation of Cinacalcet Hydrochloride Therapy to Lower Cardiovascular Events (EVOLVE) trial (29) showed a reduction in plasma triglycerides, non-HDL cholesterol, VLDL cholesterol, remnant-like particle cholesterol, and apolipoprotein CIII for participants treated with [omega]-3 free fatty acids compared with placebo (olive oil); in addition, a recent metaanalysis (30) of 11 randomized controlled trials investigating the effect of high-dose ([greater than or equal to] 1 g/day) [omega]-3 fatty acid supplementation for patients with existing cardiovascular disease supplied evidence that long-term high dose [omega]-3 fatty acid supplementation may be beneficial for secondary prevention to reduce cardiovascular disease risk.
Impact of non-traditional phosphate binders and cinacalcet on haemodialysis patient biochemistry, pill burden and cost.
Patient was treated with cinacalcet for secondary hyperparathyroidism but became refractory to treatment after a period of time with persistently elevated calcium and PTH levels.