Paricalcitol 5mcg/ml Inj, 2ml
It is used to treat or prevent high parathyroid hormone levels in certain patients.
Drug Class
Agents for hyperparathyroidism; Vitamin D analogs
Pharmacologic Class
Selective vitamin D receptor (VDR) activator
Pregnancy Category
C
FDA Approved
Dec 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Paricalcitol is a man-made form of vitamin D that helps control the levels of a hormone called parathyroid hormone (PTH) in people with kidney disease. When kidneys don't work well, PTH levels can get too high, which can cause problems with bones and other parts of the body. This medicine helps bring PTH levels down to a healthier range.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Adhere to the dosage instructions provided by your healthcare team. This medication is administered via intravenous injection.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor promptly to receive guidance on the next steps to take.
Lifestyle & Tips
- Follow your doctor's instructions regarding diet, especially limiting calcium and phosphorus intake.
- Do not take any calcium supplements, vitamin D supplements, or antacids containing calcium without consulting your doctor.
- Attend all scheduled blood tests to monitor your calcium, phosphorus, and PTH levels.
- Report any new or worsening symptoms to your healthcare provider promptly.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose based on baseline intact parathyroid hormone (iPTH) levels. Administered intravenously (IV) three times a week, no more frequently than every other day.
Dose Range:
0.04 - 0.24 mg
Condition-Specific Dosing:
Chronic Kidney Disease (CKD) Stage 3/4 (Pre-dialysis):
Initial dose 0.04 mcg/kg or 0.08 mcg/kg IV three times a week. Dosing adjusted based on iPTH, serum calcium, and phosphorus levels to maintain iPTH in target range (150-300 pg/mL) without hypercalcemia or hyperphosphatemia.
Chronic Kidney Disease (CKD) Stage 5 (Dialysis):
Initial dose 0.04 mcg/kg or 0.08 mcg/kg IV three times a week. Dosing adjusted based on iPTH, serum calcium, and phosphorus levels to maintain iPTH in target range (150-300 pg/mL) without hypercalcemia or hyperphosphatemia. Maximum dose typically 0.24 mcg/kg three times a week.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed beyond standard dosing for CKD stages 3/4.
Moderate:
No specific adjustment needed beyond standard dosing for CKD stages 3/4.
Severe:
No specific adjustment needed beyond standard dosing for CKD stage 5 (dialysis).
Dialysis:
Paricalcitol is indicated for patients on dialysis. Dosing is adjusted based on iPTH, calcium, and phosphorus levels.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended.
Pharmacology
Mechanism of Action
Paricalcitol is a synthetic analog of calcitriol, the active form of vitamin D. It selectively activates the vitamin D receptor (VDR) in the parathyroid glands, leading to a reduction in parathyroid hormone (PTH) synthesis and secretion. It also has effects on bone and mineral metabolism, but its selective action on the parathyroid VDRs minimizes the calcemic and phosphatemic effects seen with non-selective vitamin D analogs at therapeutic doses.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV administration)
Tmax:
Within minutes (IV administration)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
Approximately 0.6 L/kg
ProteinBinding:
Greater than 99%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 4-7 hours (terminal half-life)
Clearance:
Not readily quantifiable due to complex elimination pathways; primarily biliary/fecal.
ExcretionRoute:
Primarily biliary/fecal (approximately 70%), with a smaller portion excreted renally (approximately 30%).
Unchanged:
Less than 2% of the administered dose is excreted unchanged in urine or feces.
Pharmacodynamics
OnsetOfAction:
Within hours (PTH suppression)
PeakEffect:
Within days to weeks (PTH reduction, with stable levels achieved over time with dose titration)
DurationOfAction:
Dependent on dose and individual patient response; effects on PTH persist for several days after a single dose.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high calcium levels, including:
+ Weakness
+ Confusion
+ Fatigue
+ Headache
+ Nausea and vomiting
+ Constipation
+ Bone pain
Signs of high or low blood pressure, such as:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in vision
Abnormal heartbeat
Seizures
Frequent urination
Weight loss
Decreased appetite
Excessive thirst
Swelling
Vomiting blood or coffee ground-like material
Black, tarry, or bloody stools
Fever or chills
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Diarrhea
Nausea or vomiting
Dizziness or headache
Nasal or throat irritation
Sleep disturbances
Joint pain
Eye redness
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high calcium levels, including:
+ Weakness
+ Confusion
+ Fatigue
+ Headache
+ Nausea and vomiting
+ Constipation
+ Bone pain
Signs of high or low blood pressure, such as:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in vision
Abnormal heartbeat
Seizures
Frequent urination
Weight loss
Decreased appetite
Excessive thirst
Swelling
Vomiting blood or coffee ground-like material
Black, tarry, or bloody stools
Fever or chills
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Diarrhea
Nausea or vomiting
Dizziness or headache
Nasal or throat irritation
Sleep disturbances
Joint pain
Eye redness
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of too much calcium (hypercalcemia): feeling sick to your stomach (nausea), throwing up (vomiting), constipation, loss of appetite, feeling very tired or weak, confusion, increased thirst, or urinating more often.
- Signs of too much phosphorus (hyperphosphatemia): itching, red eyes, or skin rashes.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, such as high calcium levels or high vitamin D levels, as these may affect your ability to take this medication safely.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
Additionally, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This will help ensure that it is safe to take this medication in combination with your other medications and health conditions.
Remember, this is not an exhaustive list of potential interactions. To guarantee your safety, always consult with your doctor before starting, stopping, or changing the dose of any medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, such as high calcium levels or high vitamin D levels, as these may affect your ability to take this medication safely.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
Additionally, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This will help ensure that it is safe to take this medication in combination with your other medications and health conditions.
Remember, this is not an exhaustive list of potential interactions. To guarantee your safety, always consult with your doctor before starting, stopping, or changing the dose of any medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
If you are currently taking other supplements that contain vitamin D, consult with your doctor to avoid excessive intake.
Additionally, if you are using products that contain aluminum, such as certain antacids, inform your doctor to minimize potential interactions.
If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor, as it may affect the medication's efficacy.
Adhere to the dietary plan recommended by your doctor to ensure optimal treatment outcomes.
If you are pregnant or planning to become pregnant, notify your doctor immediately. You will need to have a discussion about the potential benefits and risks associated with using this medication during pregnancy.
Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
If you are currently taking other supplements that contain vitamin D, consult with your doctor to avoid excessive intake.
Additionally, if you are using products that contain aluminum, such as certain antacids, inform your doctor to minimize potential interactions.
If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor, as it may affect the medication's efficacy.
Adhere to the dietary plan recommended by your doctor to ensure optimal treatment outcomes.
If you are pregnant or planning to become pregnant, notify your doctor immediately. You will need to have a discussion about the potential benefits and risks associated with using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Hypercalcemia (severe nausea, vomiting, constipation, weakness, confusion, stupor, coma, cardiac arrhythmias)
- Hyperphosphatemia
- Hypercalciuria
What to Do:
Discontinue paricalcitol immediately. Initiate measures to lower serum calcium, such as hydration with intravenous saline, loop diuretics, and in severe cases, corticosteroids or bisphosphonates. Monitor serum calcium and phosphorus levels closely. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Ketoconazole (and other strong CYP3A4 inhibitors): Concomitant use can significantly increase paricalcitol exposure, increasing the risk of hypercalcemia and hyperphosphatemia. Dose adjustment of paricalcitol may be necessary.
- Calcium-containing phosphate binders: Increased risk of hypercalcemia.
- Digitalis glycosides: Hypercalcemia, a potential adverse effect of paricalcitol, can potentiate the toxicity of digitalis.
Moderate Interactions
- Thiazide diuretics: May increase the risk of hypercalcemia.
- Other vitamin D analogs: Concomitant use may lead to additive effects and increased risk of hypercalcemia and hyperphosphatemia.
Monitoring
Baseline Monitoring
Intact Parathyroid Hormone (iPTH)
Rationale: To establish baseline for dose titration and assess severity of secondary hyperparathyroidism.
Timing: Prior to initiation of therapy.
Serum Calcium (corrected for albumin)
Rationale: To establish baseline and monitor for hypercalcemia, a potential adverse effect.
Timing: Prior to initiation of therapy.
Serum Phosphorus
Rationale: To establish baseline and monitor for hyperphosphatemia, a potential adverse effect.
Timing: Prior to initiation of therapy.
Alkaline Phosphatase
Rationale: To assess bone turnover and overall mineral metabolism.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum Calcium (corrected for albumin)
Frequency: At least twice weekly initially (for 4 weeks), then weekly for 4 weeks, then monthly once stable.
Target: Within normal limits (e.g., 8.4-10.2 mg/dL)
Action Threshold: If corrected serum calcium exceeds 10.5 mg/dL, reduce or interrupt paricalcitol dose. If persistent, investigate other causes.
Serum Phosphorus
Frequency: At least twice weekly initially (for 4 weeks), then weekly for 4 weeks, then monthly once stable.
Target: Within normal limits (e.g., 2.5-4.5 mg/dL)
Action Threshold: If serum phosphorus exceeds 5.5 mg/dL, reduce or interrupt paricalcitol dose and/or adjust phosphate binder therapy.
Intact Parathyroid Hormone (iPTH)
Frequency: Every 2-4 weeks initially, then every 1-3 months once stable.
Target: 150-300 pg/mL (KDOQI guidelines for CKD Stage 5)
Action Threshold: Adjust dose based on trends. If iPTH is persistently above target, increase dose. If persistently below target or decreasing too rapidly, decrease dose.
Alkaline Phosphatase
Frequency: Periodically (e.g., every 3-6 months)
Target: Within normal limits
Action Threshold: Significant changes may indicate issues with bone turnover or mineral metabolism.
Symptom Monitoring
- Symptoms of hypercalcemia (e.g., nausea, vomiting, constipation, anorexia, weakness, fatigue, confusion, polyuria, polydipsia, bone pain)
- Symptoms of hyperphosphatemia (e.g., pruritus, vascular calcification)
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Risk not well-established; animal studies showed adverse effects at high doses.
Second Trimester:
Risk not well-established; animal studies showed adverse effects at high doses.
Third Trimester:
Risk not well-established; animal studies showed adverse effects at high doses.
Lactation
It is not known whether paricalcitol is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from paricalcitol, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Unknown; potential for hypercalcemia in infant.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Use is not recommended.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients. However, due to the higher prevalence of decreased renal function in the elderly, dose selection should be cautious, generally starting at the low end of the dosing range.
Clinical Information
Clinical Pearls
- Paricalcitol is a selective VDR activator, which means it aims to suppress PTH with less impact on serum calcium and phosphorus compared to non-selective vitamin D analogs like calcitriol.
- Close and frequent monitoring of serum calcium, phosphorus, and iPTH is crucial, especially during dose initiation and titration, to prevent hypercalcemia and hyperphosphatemia.
- Dose adjustments should be made gradually, typically in increments of 0.04 mcg/kg, and no more frequently than every 2-4 weeks.
- Patients should be advised to avoid calcium-containing products (e.g., certain antacids, calcium supplements) and high-dose vitamin D supplements unless specifically instructed by their physician.
- If hypercalcemia or hyperphosphatemia occurs, the dose of paricalcitol should be reduced or temporarily withheld until levels normalize. Other medications (e.g., phosphate binders) may also need adjustment.
Alternative Therapies
- Calcitriol (Rocaltrol, Calcijex): Non-selective vitamin D analog.
- Doxercalciferol (Hectorol): Another synthetic vitamin D analog.
- Cinacalcet (Sensipar): A calcimimetic agent that directly increases the sensitivity of the calcium-sensing receptor on the parathyroid gland, leading to decreased PTH secretion.
- Etelcalcetide (Parsabiv): An intravenous calcimimetic agent.
Cost & Coverage
Average Cost:
Highly variable, typically several hundred to over a thousand USD per vial depending on strength and quantity. per 2ml vial (5mcg/ml)
Generic Available:
Yes
Insurance Coverage:
Typically covered by Medicare Part D and most commercial insurance plans, often as a Tier 3 or specialty drug, requiring prior authorization.
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional or pharmacist. If you are unsure about the proper disposal method, consult with your pharmacist, who can also inform you about potential drug take-back programs in your area. Additionally, some medications may come with a separate patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken to ensure prompt and effective treatment.