Rotpcalcet

Uses

Rotpcalcet is used for-

• For the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis
• For the treatment of hypercalcemia in patients with parathyroid carcinoma
• For the treatment of hypercalcaemia in patients with primary hyperparathyroidism who still have high calcium level after removal of the parathyroid gland

Rotpcalcet is also used to associated treatment for these conditions: Hypercalcemia

How Rotpcalcet works

Rotpcalcet directly lowers parathyroid hormone levels by increasing the sensitivity of the calcium sensing receptors to activation by extracellular calcium, resulting in the inhibition of PTH secretion. The reduction in PTH is associated with a concomitant decrease in serum calcium levels.

Dosage

Rotpcalcet dosage

Hypercalcaemia associated with parathyroid carcinoma or primary hyperparathyroidism:≥18 yr, initial: 30 mg bid. Titrate dose every 2-4 wk in sequential doses of 60 mg bid, 90 mg bid, and 90 mg 3-4 times daily as needed until serum calcium levels normalised. Max: 90 mg 4 times/day.

Secondary hyperparathyroisim in patients with chronic kidney disease on dialysis: ≥18 yr, initial: 30 mg once daily. Titrate dose every 2-4 wk in steps of 30 mg as necessary to achieve intact parathyroid hormone (iPTH) levels of 150-300 pg/mL. Max: 180 mg once daily. May be used alone or in combination with vitamin D sterols and/or phosphate binders.

Side Effects

The common side effects of Rotpcalcet are nausea, vomiting, anorexia; dizziness, paraesthesia, asthenia; reduced testosterone concentrations; myalgia; rash; less commonly dyspepsia, diarrhoea, and seizures; hypotension and heart failure also reported.

Toxicity

Doses titrated up to 300 mg once daily have been safely administered to patients on dialysis. Overdosage of cinacalcet may lead to hypocalcemia.

Precaution

Rotpcalcet treatment should not be initiated if serum calcium is less than the lower limit of the normal range (8.4 mg/dL). Serum-calcium concentration should be measured before initiation of treatment and within 1 week after starting treatment or adjusting dose, then monthly for secondary hyperparathyroidism and every 2–3 months for primary hyperparathyroidism and parathyroid carcinoma; treatment should not be initiated in patients with hypocalcaemia; in secondary hyperparathyroidism PTH concentration should be measured 1–4 weeks after starting treatment or adjusting dose, then every 1–3 months; dose adjustment may be necessary if smoking started or stopped during treatment; hepatic impairment; pregnancy.

Interaction

Rotpcalcet is a strong CYP2D6 inhibitor and may increase serum concentrations of amitriptyline, nortriptyline and desipramine. Rotpcalcet may decrease serum concentrations of tacrolimus. CYP3A4 inhibitors such as ketoconazole, erythromycin may increase plasma concentrations of Rotpcalcet.

Food Interaction

• Take with food. Food markedly increases product bioavailability.

[Moderate] ADJUST DOSING INTERVAL: Food enhances the oral absorption and bioavailability of cinacalcet.

According to the product labeling for cinacalcet, administration with a high-fat meal increased the peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of cinacalcet by 82% and 68%, respectively, compared to administration in the fasting state.

The Cmax and AUC were increased 65% and 50%, respectively, when cinacalcet was administered with a low-fat meal compared to fasting.

MANAGEMENT: To ensure maximal oral absorption, cinacalcet should be administered with or immediately after a meal.

The tablets should be taken whole and not divided or crushed.

Rotpcalcet Drug Interaction

Moderate: metoprolol, metoprolol, metoprolol, metoprololUnknown: aspirin, aspirin, apixaban, apixaban, insulin glargine, insulin glargine, atorvastatin, atorvastatin, clopidogrel, clopidogrel, multivitamin, multivitamin, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol

Rotpcalcet Disease Interaction

Moderate: hypocalcemia, hypotension, seizures

Volume of Distribution

• 1000 L

Elimination Route

Rapidly absorbed following oral administration.

Half Life

Terminal half-life is 30 to 40 hours. The mean half-life of cinacalcet is prolonged by 33% and 70% in patients with moderate and severe hepatic impairment, respectively.

Elimination Route

Rotpcalcet is metabolized by multiple enzymes, primarily CYP3A4, CYP2D6 and CYP1A2. Renal excretion of metabolites was the primary route of elimination of radioactivity.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies in pregnant women. Rotpcalcet should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It Only for the use of Medical Professionals is not known whether this drug is excreted in human milk. Considering the potential for clinically significant adverse reactions in infants from Rotpcalcet; it is recommended that breast-feeding be discontinued during treatment with Rotpcalcet.

Contraindication

Rotpcalcet is contraindicated in patients with hypersensitivity to any components of this product.

Special Warning

Pediatric use: The safety and efficacy of Rotpcalcet in pediatric patients have not been established.

Geriatric Use: No dosage adjustment is required for geriatric patients over 65 years of age.

Patients with renal impairment: No dosage adjustment is necessary for renal impaired patients.

Patients with hepatic impairment: In patients with moderate and severe hepatic impairment, PTH and serum calcium concentrations should be closely monitored throughout treatment with Rotpcalcet.

Acute Overdose

Overdosage may lead to hypocalcaemia. Provide treatment to correct serum calcium levels. Haemodialysis are unlikely to be useful.

Storage Condition

Store in a cool dry place below 30ºC. Protect from light.

Innovators Monograph

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