Cinacalcet
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| Cinacalcet
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| Systematic (IUPAC) name | |
| N-[(1R)-1-(1-naphthyl)ethyl]-3- [3-(trifluoromethyl)phenyl]propan-1-amine | |
| Identifiers | |
| CAS number | |
| ATC code | H05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C22H22F3N |
| Mol. mass | 357.412 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 20 to 25% Increases if taken with food |
| Protein binding | 93 to 97% |
| Metabolism | Hepatic (CYP3A4-, CYP2D6- and CYP1A2-mediated) |
| Half life | 30 to 40 hours |
| Excretion | Renal (80%) and fecal (15%) |
| Therapeutic considerations | |
| Licence data |
, |
| Pregnancy cat. | |
| Legal status |
℞ Prescription only |
| Routes | Oral |
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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
External links
- Sensipar website run by Amgen
- Prescribing information
- Cinacalcet - Medlineplus.org
- Cinacalcet - Drug Digest.
Calcium homeostasis (H05) | |
|---|---|
| Parathyroid hormones and analogues | Teriparatide |
| Calcitonin preparations | Elcatonin - Cinacalcet |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
