Cinacalcet


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Chống chỉ định
Serum Ca below the lower limit of normal range.
Thận trọng
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.
Phản ứng phụ
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.
Quá liều
Symptoms: Hypocalcaemia manifested by paraesthesia, myalgia, cramping, tetany, and seizures. Management: Symptomatic and supportive treatment.
Tương tác
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.
Tác dụng
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.
Đặc tính

Chemical Structure Image
Cinacalcet

Source: National Center for Biotechnology Information. PubChem Database. Cinacalcet, CID=156419, https://pubchem.ncbi.nlm.nih.gov/compound/Cinacalcet (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-30°C.
Phân loại ATC
H05BX01 - cinacalcet ; Belongs to the class of other anti-parathyroid agents. Used in the management of calcium homeostasis.
References
Anon. Cinacalcet. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/03/2017.

Buckingham R (ed). Cinacalcet Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/03/2017.

Joint Formulary Committee. Cinacalcet. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/03/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Cinacalcet Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/03/2017.

Sensipar Tablet, Coated (Avera McKennan Hospital). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/03/2017.

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