Loading…
PMS-CINACALCET is a brand name for Cinacalcet, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ..................................................................................... 3 CONTRAINDICATIONS ........................................................................................................... 4 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
pms-CINACALCET (cinacalcet hydrochloride) can be used alone or in combination with vitamin D sterols and/or phosphate binders. pms-CINACALCET (cinacalcet hydrochloride) is administered orally. Tablets should be taken whole and should not be chewed, crushed or divided.
Take pms-CINACALCET with food or shortly after a meal (see DRUG INTERACTIONS). Secondary Hyperparathyroidism in Patients with Chronic Kidney Disease (CKD) Receiving Dialysis The recommended starting oral dose of pms-CINACALCET is 30 mg once daily.
5 to 5 times the upper limit of normal. In CKD patients, PTH levels should be assessed at least 12 hours after dosing with pms-CINACALCET. Low serum calcium levels should be corrected before initiating therapy (see WARNINGS and PRECAUTIONS, Endocrine and Metabolism, Hypocalcemia).
During dose titration, serum calcium levels should be monitored frequently and if serum calcium levels decrease below the normal range, appropriate steps should be taken to increase serum calcium levels (see WARNINGS AND PRECAUTIONS).
Calcium levels should be corrected for albumin or ionized calcium levels should be measured. Parathyroid Carcinoma and Primary Hyperparathyroidism (HPT) The recommended starting dose of pms-CINACALCET for adults is 30 mg twice per day.
The dosage of pms-CINACALCET should be titrated sequentially every 2 to 4 weeks through dosages of 30 mg twice daily, 60 mg twice daily, and 90 mg twice daily to reduce serum calcium levels. For further information on higher dosages (90 mg 3 or 4 times daily) see CLINICAL TRIALS: Parathyroid Carcinoma and Primary HPT for Whom Parathyroidectomy is not a Treatment Option.
Special Populations Geriatric patients Age does not alter the pharmacokinetics of pms-CINACALCET; no dose adjustment is required for geriatric patients. pms-CINACALCET – Product Monograph Page 14 of 28 Patients with renal impairment Renal impairment does not alter the pharmacokinetics of pms-CINACALCET; no dosage adjustment is necessary for renal impairment.
Patients with hepatic impairment Moderate to severe hepatic impairment (Child-Pugh classification) increases pms-CINACALCET drug concentrations by approximately 2- to 4-fold. In patients with moderate-severe hepatic impairment, PTH and serum calcium concentrations should be closely monitored during dose titration of pms-CINACALCET.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Cinacalcet in Canada.
Know a brand we are missing in Canada? Suggest a brand →
Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
OVERDOSAGE Doses titrated up to 300 mg once daily have been safely administered to patients receiving dialysis. Overdosage of pms-CINACALCET (cinacalcet hydrochloride) may lead to hypocalcemia. In the event of overdosage, patients should be monitored for signs and symptoms of hypocalcemia and appropriate measures taken to correct serum calcium levels (see WARNINGS AND PRECAUTIONS).
Since pms-CINACALCET is highly protein bound, hemodialysis is not an effective treatment for overdosage of pms-CINACALCET. For management of a suspected drug overdose, contact your regional Poison Control Centre. ACTION AND CLINICAL PHARMACOLOGY Mechanism of Action Secondary hyperparathyroidism is a progressive disease, which occurs in patients with chronic kidney disease and manifests as increases in parathyroid hormone levels and derangements in calcium and phosphorous metabolism.
Increased PTH stimulates osteoclastic activity resulting in cortical bone resorption and marrow fibrosis. The calcium-sensing receptor on the surface of the chief cell of the parathyroid gland is the principal regulator of PTH secretion.
Cinacalcet hydrochloride directly lowers PTH levels by increasing the sensitivity of the calcium-sensing receptor to extracellular calcium. The reduction in PTH is associated with a concomitant decrease in serum calcium levels. Pharmacodynamics Reduction in iPTH levels is correlated with cinacalcet concentration.
The nadir in iPTH level occurs approximately 2 to 6 hours post dose, corresponding with the Cmax of cinacalcet. After steady state is reached, serum calcium concentrations remain constant over the dosing interval. pms-CINACALCET – Product Monograph Page 15 of 28 Pharmacokinetics Absorption and Distribution After oral administration of cinacalcet hydrochloride, maximum plasma concentration is achieved in approximately 2 to 6 hours.
The absolute bioavailability of cinacalcet is approximately 25%. Administration of cinacalcet hydrochloride with food results in an approximate 50 to 80% increase in bioavailability. Increases in plasma concentrations are similar regardless of the fat content of the meal.
After absorption, cinacalcet concentrations decline in a biphasic fashion with an initial half-life of approximately 6 hours and a terminal half-life of 30 to 40 hours. Steady state drug levels are achieved within 7 days with minimal accumulation.
The AUC and Cmax of cinacalcet increase linearly over the dose range of 30 to 180 mg once daily. The pharmacokinetics of cinacalcet does not change over time. The volume of distribution is high (approximately 1000 L), indicating extensive distribution.
Cinacalcet is approximately 97% bound to plasma proteins and distributes minimally into red blood cells. Metabolism and Excretion Cinacalcet is metabolized by multiple enzymes, primarily CYP3A4 and CYP1A2. The major circulating metabolites are inactive.
After administration of a 75 mg radio-labeled dose to healthy volunteers, cinacalcet was rapidly and extensively metabolized by oxidation followed by conjugation. Renal excretion of metabolites was the prevalent route of elimination of radioactivity.
Approximately 80% of the dose was recovered in the urine and 15% in the feces. Special Populations and Conditions Geriatric Patients The pharmacokinetics of cinacalcet hydrochloride are similar in patients greater than, or less than, 65 years of age.
No dosage adjustment based on age is necessary. Pediatric Patients The pharmacokinetics of cinacalcet hydrochloride have not been studied in […]