Cinacalcet

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Cinacalcet
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Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability20 to 25%
Increases if taken with food
Protein binding93 to 97%
MetabolismHepatic (CYP3A4-, CYP2D6- and CYP1A2-mediated)
Elimination half-life30 to 40 hours
ExcretionRenal (80%) and fecal (15%)
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
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Chemical and physical data
FormulaC22H22F3N
Molar mass357.412 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


For patient information click here

Overview

Cinacalcet (INN) is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues) by allosteric activation of the calcium-sensing receptor that is expressed in various human organ tissues. It is sold by Amgen under the trade name Sensipar® in North America and Australia and as Mimpara® in Europe. Cinacalcet is used to treat hyperparathyroidism (elevated parathyroid hormone levels), a consequence of parathyroid tumors and chronic renal failure.[1]

Clinical uses

Cinacalcet is indicated for the treatment of secondary hyperparathyroidism in patients with Chronic Kidney Disease on dialysis and hypercalcemia in patients with parathyroid carcinoma.

Dosage

Secondary Hyperparathyroidism in Patients with Chronic Kidney Disease on Dialysis

The recommended starting oral dose is 30 mg once daily. Serum calcium and serum phosphorus should be measured within 1 week and PTH should be measured 1 to 4 weeks after initiation or dose adjustment of cinacalcet. It should be titrated no more frequently than every 2 to 4 weeks through sequential doses of 60, 90, 120, and 180 mg once daily to target iPTH consistent with the NKF-K/DOQI recommendation for CKD patients on dialysis of 150-300 pg/mL. PTH levels should be assessed no earlier than 12 hours after dosing with cinacalcet.

Cinacalcet can be used alone or in combination with vitamin D sterols and/or phosphate binders.

During dose titration, serum calcium levels should be monitored frequently and if levels decrease below the normal range, appropriate steps should be taken to increase serum calcium levels, such as by providing supplemental calcium, initiating or increasing the dose of calcium-based phosphate binder, initiating or increasing the dose of vitamin D sterols, or temporarily withholding treatment with cinacalcet.

Parathyroid Carcinoma

The recommended starting oral dose is 30 mg twice daily.

The dosage of cinacalcet should be titrated every 2 to 4 weeks through sequential doses of 30 mg twice daily, 60 mg twice daily, 90 mg twice daily, and 90 mg three or four times daily as necessary to normalize serum calcium levels.

NOTE: Cinacalcet should be taken whole and should not be divided. It should be taken with food or shortly after a meal.

Contraindications

References

  1. Torres PU (2006). "Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease". Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation. 16 (3): 253–8. doi:10.1053/j.jrn.2006.04.010. PMID 16825031.

External links

Template:Calcium homeostasis

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