endolet

endolet Uses, Dosage, Side Effects, Food Interaction and all others data.

endolet is a calcimimetic agent. It lowers parathyroid hormone (PTH) secretion by increasing the sensitivity of the calcium-sensing receptor of the parathyroid gland to activation by extracellular calcium. PTH reduction leads to concomitant decrease in serum calcium and phosphorus concentrations.

endolet is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues). Secondary hyperparathyroidism (HPT) in patients with chronic kidney disease (CKD) is a progressive disease, associated with increases in parathyroid hormone (PTH) levels and derangements in calcium and phosphorus metabolism. Increased PTH stimulates osteoclastic activity resulting in cortical bone resorption and marrow fibrosis. The goals of treatment of secondary hyperparathyroidism are to lower levels of PTH, calcium, and phosphorus in the blood, in order to prevent progressive bone disease and the systemic consequences of disordered mineral metabolism. In CKD patients on dialysis with uncontrolled secondary HPT, reductions in PTH are associated with a favorable impact on bone-specific alkaline phosphatase (BALP), bone turnover and bone fibrosis. endolet reduces calcium levels by increasing the sensitivity of the calcium sensing receptor to extracellular calcium.

Trade Name endolet
Availability Prescription only
Generic Cinacalcet
Cinacalcet Other Names Cinacalcet
Related Drugs prednisone, dexamethasone, Decadron, denosumab, Reclast, Sensipar, paricalcitol, Zemplar, Hectorol, doxercalciferol
Weight 30mg, 60mg, 90mg
Type Tablet, Film Coated
Formula C22H22F3N
Weight Average: 357.412
Monoisotopic: 357.170434324
Protein binding

Approximately 93 to 97% bound to plasma proteins.

Groups Approved
Therapeutic Class Calcium Regulator
Manufacturer Tabuk Pharmaceutical Manufacturing Co,
Available Country Saudi Arabia
Last Updated: September 19, 2023 at 7:00 am
endolet
endolet

Uses

endolet 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

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

How endolet works

endolet 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

endolet 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 endolet 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

endolet 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

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

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.

endolet 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

endolet 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. endolet 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 endolet; it is recommended that breast-feeding be discontinued during treatment with endolet.

Contraindication

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

Special Warning

Pediatric use: The safety and efficacy of endolet 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 endolet.

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

You find simplified version here endolet

endolet contains Cinacalcet see full prescribing information from innovator endolet Monograph, endolet MSDS, endolet FDA label

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