Cinacalcet

Cinacalcet

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Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	EU EMA: by INN US FDA: Cinacalcet
Pregnancy category	AU: B3 US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	H05BX01 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	20 to 25% Increases if taken with food
Protein binding	93 to 97%
Metabolism	Hepatic (CYP3A4-, CYP2D6- and CYP1A2-mediated)
Elimination half-life	30 to 40 hours
Excretion	Renal (80%) and fecal (15%)
Identifiers
IUPAC name N-[(1R)-1-(1-naphthyl)ethyl]-3- [3-(trifluoromethyl)phenyl]propan-1-amine
CAS Number	226256-56-0
PubChem CID	156419
DrugBank	APRD00872
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C22H22F3N
Molar mass	357.412 g/mol

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List of terms related to Cinacalcet

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

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.

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

• Hypersensitivity

External links

• Sensipar website run by Amgen
• Prescribing information
• Cinacalcet - Medlineplus.org
• Cinacalcet - Drug Digest.

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