cinacalcet hydrochloride


Also found in: Wikipedia.

cinacalcet hydrochloride

Mimpara (UK), Sensipar

Pharmacologic class: Calcimimetic

Therapeutic class: Endocrine and metabolic agent

Pregnancy risk category C

Action

Directly lowers parathyroid hormone (PTH) levels by increasing sensitivity of calcium-sensing receptors to extracellular calcium

Availability

Tablets: 30 mg, 60 mg, 90 mg

Indications and dosages

Secondary hyperparathyroidism in patients with chronic renal disease who are on dialysis

Adults: Dosage individualized; recommended starting dosage is 30 mg P.O. daily. Measure serum calcium and phosphorus levels within 1 week and intact parathyroid hormone (iPTH) 1 to 4 weeks after initiation or dosage adjustment; titrate dosage no more often than every 2 to 4 weeks through sequential doses of 60 mg, 90 mg, 120 mg, and 180 mg P.O. once daily to recommended target iPTH for chronic renal disease patients on dialysis of 150 to 300 pg/ml.

Hypercalcemia in patients with parathyroid carcinoma

Adults: Recommended starting dosage is 30 mg P.O. twice daily, titrated every 2 to 4 weeks through sequential doses of 60 mg and 90 mg twice daily, and 90 mg three or four times daily as needed to normalize serum calcium level.

Dosage adjustment

• Decreased calcium or iPTH level
• Concurrent use or discontinuation of strong CYP3A4 inhibitors (such as erythromycin, itraconazole, or ketoconazole)

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• decreased serum calcium level, moderate or severe hepatic impairment
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Don't initiate therapy if serum calcium level is less than lower limit of normal range (8.4 mg/dl).
• Administer tablets whole with food or shortly after a meal.
• If iPTH level decreases below recommended target range (150 to 300 pg/ml), reduce dosage of cinacalcet and vitamin D sterols or discontinue therapy.
• During titration, monitor serum calcium level frequently; if level drops below normal, take appropriate measures to increase it, such as providing supplemental calcium, initiating or increasing dosage of calcium-based phosphate binder or vitamin D sterols, or withholding cinacalcet temporarily.
• Adjust dosage and closely monitor iPTH and calcium levels if patient is receiving or discontinuing a strong CYP3A4 inhibitor.

Adverse reactions

CNS: dizziness, asthenia

CV: hypertension

GI: nausea, vomiting, diarrhea, anorexia

Musculoskeletal: myalgia

Other: chest pain (noncardiac)

Interactions

Drug-drug.Amitriptyline: increased amitriptyline and nortriptyline (active metabolite) exposure

Drugs metabolized by CYP4502D6 (such as flecainide, thioridazine, most tricyclic antidepressants, vinblastine): increased blood levels of either drug

Ketoconazole and other strong CYP3A4 inhibitors: increased cinacalcet exposure

Drug-diagnostic tests.Calcium: decreased

Patient monitoring

• Closely monitor iPTH and serum calcium levels throughout therapy in patients with moderate to severe hepatic impairment and in those who start or discontinue therapy with strong CYP3A4 inhibitor.
• Monitor iPTH level carefully to ensure that it doesn't fall below 100 pg/ml because adynamic bone disease may develop.
• Measure serum calcium and phosphorus levels within 1 week and iPTH level 1 to 4 weeks after initiation or dosage adjustment. Once maintenance dosage is established, measure serum calcium and phosphorus levels approximately monthly and iPTH level every 1 to 3 months.
• Monitor serum calcium level closely in patient with history of seizure disorders.

Patient teaching

• Instruct patient to take tablets whole with food or shortly after a meal.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

Mentioned in ?
References in periodicals archive ?
The acquisition will further solidify 3SBio's leading position in nephrology and oncology as it also provides a platform for the company to proceed with the clinical development of over 12 small-molecule pipeline candidates in our core therapeutic areas using internal facilities and expertise, including HIF-PH inhibitor for anemia; cinacalcet hydrochloride for hyperparathyroidism; sevelamer carbonate for hyperphosphatemia; Colestilan for hyperphosphatemia and hypercholesteremia; DJ5 for autosomal dominant polycystic kidney disease (ADPKD); PEG-Irinotecanfor solid tumors; nadroparin calcium for blood clotting and thrombosis; and fondaparinux sodium for prophylaxis of deep vein thrombosis.
Contract award: cinacalcet hydrochloride package vii - the program of drugs for dialysis in the healthcare in debica.
Cinacalcet hydrochloride treatment significantly improves all-cause and cardiovascular survival in a large cohort of hemodyalisis patients.
Biovitrum will also have co-promotion rights in the Nordic region for all products developed under the agreement as well as for Amgen's cinacalcet hydrochloride, a treatment for some hyperparathyroid conditions, and palifermin, a therapy for treating chemotherapy-related inflammations of the mouth.
Improved Clinical Outcomes in Hemodialysis Patients Prescribed Cinacalcet Hydrochloride