Cinacalcet


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Secondary hyperparathyroidism in CKD patients on dialysis Initial: 30 mg once daily, titrated by 30 mg 2-4 wkly to achieve iPTH levels of 150-300 pg/mL. Max: 180 mg once daily. Hypercalcaemia associated w/ parathyroid carcinoma or primary hyperparathyroidism Initial: 30 mg bid, titrated through sequential doses of 30 mg bid, 60 mg bid, 90 mg bid, and 90 mg 3-4 times/day as necessary 2-4 wkly to normalise serum Ca levels. Max: 90 mg 4 times/day.
Dosage Details
Oral
Hypercalcaemia associated with parathyroid carcinoma or primary hyperparathyroidism
Adult: Initially, 30 mg bid, titrated through sequential doses of 30 mg bid, 60 mg bid, 90 mg bid, and 90 mg 3-4 times daily as necessary 2-4 wkly to normalise serum Ca levels. Max: 90 mg 4 times daily.

Oral
Secondary hyperparathyroisim in patients with chronic kidney disease on dialysis
Adult: Initially, 30 mg once daily, titrated in increments of 30 mg 2-4 wkly to achieve intact parathyroid hormone (iPTH) levels of 150-300 pg/mL. Max: 180 mg once daily.
Contraindications
Serum Ca below the lower limit of normal range.
Special Precautions
Patient w/ history of seizure disorders, known congenital long QT syndrome, impaired cardiac function. Smokers. Not indicated for use in CKD patients not on dialysis. Moderate to severe hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: QT prolongation, ventricular arrhythmia, hypotension, worsening of heart failure, seizures, adynamic bone disease.
Nervous: Dizziness, headache, paraesthesia, asthenia.
CV: HTN.
GI: Nausea, vomiting, anorexia, diarrhoea, constipation, abdominal pain, dyspepsia, decreased appetite.
Resp: Dyspnoea, cough, upper resp tract infection.
Endocrine: Decreased testosterone levels.
Musculoskeletal: Myalgia.
Dermatologic: Rash, angioedema, urticaria.
Others: Non-cardiac chest pain, dialysis access site infection.
Potentially Fatal: Hypocalcaemia.
MonitoringParameters
Monitor for signs and symptoms of hypocalcaemia. Secondary hyperparathyroidism: Monitor serum Ca and phosphorus levels prior to and w/in a wk of initiation, and regularly during dose titrations. Obtain serum Ca levels mthly after establishing maintenance dose. Measure iPTH 1-4 wk after initiation or dose titrations (wait at least 12 hr after dose). Hypercalcaemia: Monitor serum Ca levels prior to and w/in a wk of initiation or dose titrations. Obtain serum Ca levels 2 mthly after establishing maintenance dose.
Overdosage
Symptoms: Hypocalcaemia manifested by paraesthesia, myalgia, cramping, tetany, and seizures. Management: Symptomatic and supportive treatment.
Drug Interactions
Increased concentration by 2-fold w/ strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, telithromycin, ritonavir). May increase exposure of desipramine, amitriptyline, and nortriptyline. May increase AUC of dextromethorphan.
Food Interaction
Increased peak plasma concentration and bioavailability w/ food.
Action
Description: Cinacalcet is a calcimimetic agent that increases the sensitivity of the Ca-sensing receptors of the parathyroid gland to activation by extracellular Ca. This lowers parathyroid hormone (PTH) levels, and leads to concomitant decrease in serum Ca and phosphorus levels, thereby preventing complications w/ mineral metabolism disorders.
Pharmacokinetics:
Absorption: Increased bioavailability w/ food. Time to peak plasma concentration: Approx 2-6 hr.
Distribution: Volume of distribution: Approx 1,000 L. Plasma protein binding: Approx 93-97%.
Metabolism: Rapidly and extensively metabolised by CYP3A4, CYP2D6, and CYP1A2 enzymes via oxidative N-dealkylation to hydrocinnamic acid and hydroxy-hydrocinnamic acid (further metabolised via β-oxidation and glycine conjugation) and metabolites containing naphthalene ring; also via oxidation of the naphthalene ring on the parent drug to form dihydrodiols which are further conjugated w/ glucuronic acid.
Excretion: Via urine (approx 80%, as metabolites) and faeces (approx 15%). Terminal elimination half-life: Approx 30-40 hr.
Chemical Structure

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Storage
Store between 15-30°C.
ATC Classification
H05BX01 - cinacalcet ; Belongs to the class of other anti-parathyroid agents. Used in the management of calcium homeostasis.
Disclaimer: This information is independently developed by MIMS based on Cinacalcet from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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