Dosing and uses of Zemplar (paricalcitol)
Adult dosage forms and strengths
injectable solution
- 2mcg/mL
- 5mcg/mL
capsule
- 1mcg
- 2mcg
- 4mcg
Prevention & Treatment of Secondary Hyperparathyroidism
Associated with Chronic Kidney Disease (Stage 5)
- Initial 0.04-0.1 mcg/kg IV (no more frequent than every other day)
- Titrate up or down by 2-4 mcg q2-4Weeks
- Up to 0.24 mcg/kg PO have been administered
Associated with Chronic Kidney Disease (Stage 3 & 4)
- PTH ≤500 pg/mL: 1 mcg PO qDay OR 2 mcg PO 3 times/week
- PTH >500 pg/mL: 2 mcg PO qDay OR 4 mcg PO 3 times/week
- Do not administer 3 times/week dosing no more frequently than every other day
- Titrate dose based on response
Monitoring
Serum PTH, calcium & phosphorus
Monitoring parameters (Stage 5)
- PTH same or increased: Increase dose
- PTH level decreased by <30%: Increased dose
- PTH level decreased by >30% & <60%: Maintain dose
- PTH level decreased by >60%: Decrease dose
- PTH level 1.5-3 times upper limit of normal: Maintain dose
Monitoring parameters (Stage 3 & 4)
- Serum PTH at 2-4 week intervals
- PTH same or increased: Increase by 1 mcg/day OR 2 mcg three times/week
- PTH decreased <30%: Increase by 1 mcg/day OR 2 mcg three times/week
- PTH decreased >30% or <60%: Maintain current dose
- PTH decreased >60%: Decrease 1 mcg/day OR 2 mcg three times/week
- PTH <60 pg/mL: Decrease 1 mcg/day OR 2 mcg three times/week
Pediatric dosage forms and strengths
injectable solution
- 2mcg/mL
- 5mcg/mL
capsule
- 1mcg
- 2mcg
- 4mcg
Prevention & Treament of Secondary Hyperparathyroidism
Associated with Chronic Kidney Disease
- >5 Years old with Stage 5
- Initial 0.04-0.1 mcg/kg IV injection during dialysis (no more frequent than every other day)
- Titrate up or down 2-4 mcg q2-4Weeks
Monitoring
Serum PTH, calcium & phosphorus
Monitoring paremeter (Stage 5)
- Same or Increasing PTH level: Increase dose
- PTH level decreased <30%: Increase dose
- PTH level decreased > 30% & < 60%: Maintain current dose
- PTH level decreased > 60%: Decrease dose
- PTH level 1.5-3 times upper limit of normal: Maintain current dose
Zemplar (paricalcitol) adverse (side) effects
>10%
Nausea (13%)
1-10%
Vomiting
Edema
Palpitation
Chills
Pneumonia
Lightheadedness
GI bleeding
Flu
Sepsis
Hypokalemia
Hypercalcemia
Increase in blood creatinine
Warnings
Contraindications
Hypersensitivity
Hypercalcemia, hypervitaminosis d
Cautions
Monitor serum calcium, serum phosphorus, and serum or plasma iPTH during initial dosing or following any dose adjustment; in pre-dialysis patients, paricalcitol capsules may increase serum creatinine and therefore decrease the estimated GFR (eGFR)
Monitor serum calcium and phosphorus frequently; reduce dose or stop the drug if calcium (in mg/dL) times phosphorus (in mg/dL) product >75
Excessive administration of paricalcitol Capsules can cause over suppression of PTH, hypercalcemia, hypercalciuria, hyperphosphatemia, and adynamic bone disease; prescription-based doses of vitamin D and its derivatives should be withheld during pericalcitol therapy
Avoid excessive use of aluminum containing compounds
Patients receiving digitalis; digitalis toxicity is potentiated by hypercalcemia
Strong CYP3A4 inhibitors may increase paricalcitol AUC
Injection solution doesn't contain preservatives; discard unused portions
Hepatic impairment
Pregnancy and lactation
Pregnancy category: C
Lactation: not known if distributed into breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Zemplar (paricalcitol)
Mechanism of action
Synthetic vitamin D analog, reduces parathyroid hormone (PTH)
Absorption
Bioavailability (PO): 72%
Distribution
Protein Bound: 99.8%
Vd: 44-46 L in CRF; healthy patients 34 L
Metabolism
Extensively metabolized in liver
At least 5 unknown metabolites
Elimination
Half-Life: 14-20 hr in ESRd
Total Body Clearance: 2.5-4 L/hr
Excretion: Feces 74%; urine 16%
Hemodialysis: Not dialyzable
