Paricalcitol 2mcg Capsules
It is used to treat or prevent high parathyroid hormone levels in certain patients.
Drug Class
Vitamin D Analog
Pharmacologic Class
Selective Vitamin D Receptor Activator
Pregnancy Category
Not available
FDA Approved
Dec 2005
DEA Schedule
Not Controlled
Overview
What is this medicine?
Paricalcitol is a type of vitamin D that helps control the levels of parathyroid hormone (PTH) in your body. High PTH levels are common in people with kidney disease and can cause bone problems. This medicine helps lower PTH to protect your bones and overall health.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a safe place, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you take this medication three times a week and miss a dose, contact your doctor for guidance on what to do next.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a safe place, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you take this medication three times a week and miss a dose, contact your doctor for guidance on what to do next.
Lifestyle & Tips
- Follow your doctor's instructions regarding diet, especially limiting foods high in phosphorus.
- Do not take any other vitamin D supplements, calcium supplements, or antacids containing magnesium or calcium without consulting your doctor.
- Attend all scheduled blood tests to monitor your calcium, phosphorus, and PTH levels.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose based on baseline intact parathyroid hormone (iPTH) levels. For iPTH > 500 pg/mL, initial dose is 2 mcg daily or 4 mcg three times a week (e.g., Monday, Wednesday, Friday). For iPTH ≤ 500 pg/mL, initial dose is 1 mcg daily or 2 mcg three times a week. Doses are adjusted based on iPTH, serum calcium, and phosphorus levels.
Dose Range:
1 - 10 mg
Condition-Specific Dosing:
Secondary Hyperparathyroidism in CKD Stage 3/4:
Initial dose based on iPTH: If iPTH > 500 pg/mL, 2 mcg daily or 4 mcg three times a week. If iPTH ≤ 500 pg/mL, 1 mcg daily or 2 mcg three times a week. Doses adjusted every 2-4 weeks to maintain iPTH in target range (35-70 pg/mL for CKD Stage 3/4) while minimizing hypercalcemia and hyperphosphatemia.
Secondary Hyperparathyroidism in CKD Stage 5 (Dialysis):
Initial dose based on iPTH: If iPTH > 500 pg/mL, 2 mcg daily or 4 mcg three times a week. If iPTH ≤ 500 pg/mL, 1 mcg daily or 2 mcg three times a week. Doses adjusted every 2-4 weeks to maintain iPTH in target range (150-300 pg/mL) while minimizing hypercalcemia and hyperphosphatemia.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific initial dose adjustment; dose titration based on iPTH, calcium, and phosphorus levels.
Moderate:
No specific initial dose adjustment; dose titration based on iPTH, calcium, and phosphorus levels.
Severe:
No specific initial dose adjustment; dose titration based on iPTH, calcium, and phosphorus levels.
Dialysis:
Used in patients on dialysis for secondary hyperparathyroidism. Dosing as per adult guidelines, with careful monitoring of calcium, phosphorus, and iPTH.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended, but monitor closely.
Moderate:
No specific dose adjustment recommended, but monitor closely.
Severe:
No specific dose adjustment recommended, but monitor closely.
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 target tissues, including the parathyroid glands. By activating VDRs in the parathyroid glands, paricalcitol directly inhibits parathyroid hormone (PTH) synthesis and secretion without significantly increasing intestinal calcium and phosphorus absorption at therapeutic doses, thereby reducing the risk of hypercalcemia and hyperphosphatemia compared to non-selective vitamin D analogs.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 72% (capsules)
Tmax:
2-4 hours
FoodEffect:
High-fat meal increases AUC and Cmax by 20-30% but does not significantly alter Tmax. Can be taken with or without food.
Distribution:
Vd:
Approximately 0.6 L/kg
ProteinBinding:
>99%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 13-18 hours (terminal half-life)
Clearance:
Not available
ExcretionRoute:
Primarily biliary/fecal (approximately 70%), with renal excretion accounting for approximately 30%.
Unchanged:
Less than 2% (renal)
Pharmacodynamics
OnsetOfAction:
Within days to weeks (reduction in PTH levels)
PeakEffect:
Weeks to months (stable PTH reduction)
DurationOfAction:
Dependent on dose and patient response; effects on PTH persist as long as therapy continues.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
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 or seek medical help right away:
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
+ Upset stomach and vomiting
+ Constipation
+ Bone pain
Signs of high or low blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
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 guidance:
Diarrhea
Upset stomach or vomiting
Dizziness or headache
Nose or throat irritation
Sleep disturbances
Joint pain
Eye redness
Reporting Side Effects
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 or seek medical help right away:
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
+ Upset stomach and vomiting
+ Constipation
+ Bone pain
Signs of high or low blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
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 guidance:
Diarrhea
Upset stomach or vomiting
Dizziness or headache
Nose or throat irritation
Sleep disturbances
Joint pain
Eye redness
Reporting Side Effects
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, feeling very tired or weak, headache, confusion, increased thirst, or urinating more often.
- Signs of too much phosphorus (hyperphosphatemia): Itching, bone pain, red eyes.
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.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine whether it is safe for you to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine whether it is safe for you to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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 antacids or other products that contain aluminum, inform your doctor, as this may interact with your medication.
Consuming grapefruit juice or eating grapefruit regularly may also interact with this medication, so it is crucial to discuss this with your doctor. To maximize the effectiveness of your treatment, follow the dietary plan recommended by your doctor.
If you are pregnant or planning to become pregnant, notify your doctor immediately. You will need to discuss the potential benefits and risks of using this medication during pregnancy to make an informed decision.
When taking this medication, be aware of potential interactions with other substances. If you are also taking cholestyramine or mineral oil, take this medication at least 1 hour before or 4 to 6 hours after taking cholestyramine or mineral oil to minimize interactions.
If you are currently taking other supplements that contain vitamin D, consult with your doctor to avoid excessive intake. Additionally, if you are using antacids or other products that contain aluminum, inform your doctor, as this may interact with your medication.
Consuming grapefruit juice or eating grapefruit regularly may also interact with this medication, so it is crucial to discuss this with your doctor. To maximize the effectiveness of your treatment, follow the dietary plan recommended by your doctor.
If you are pregnant or planning to become pregnant, notify your doctor immediately. You will need to discuss the potential benefits and risks of using this medication during pregnancy to make an informed decision.
When taking this medication, be aware of potential interactions with other substances. If you are also taking cholestyramine or mineral oil, take this medication at least 1 hour before or 4 to 6 hours after taking cholestyramine or mineral oil to minimize interactions.
Overdose Information
Overdose Symptoms:
- Hypercalcemia (severe): Nausea, vomiting, anorexia, constipation, weakness, fatigue, headache, confusion, polyuria, polydipsia, bone pain, metallic taste, muscle pain, abdominal pain, kidney stones, cardiac arrhythmias, coma.
- Hyperphosphatemia.
What to Do:
Discontinue paricalcitol immediately. Initiate measures to lower serum calcium (e.g., low-calcium diet, hydration, loop diuretics, corticosteroids, bisphosphonates, calcitonin, or dialysis in severe cases). Monitor serum calcium and phosphorus levels frequently. Call 1-800-222-1222 (Poison Control Center) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir): May significantly increase paricalcitol exposure, increasing risk of hypercalcemia and hyperphosphatemia. Co-administration should be avoided or paricalcitol dose significantly reduced and monitored closely.
- Digitalis glycosides: Hypercalcemia, a potential adverse effect of paricalcitol, can potentiate the toxic effects of digitalis.
Moderate Interactions
- Phosphate binders (especially calcium-containing): Increased risk of hypercalcemia and hyperphosphatemia. Monitor serum calcium and phosphorus closely.
- Magnesium-containing antacids or laxatives: Increased risk of hypermagnesemia, especially in patients with renal impairment. Avoid concomitant use.
- Other vitamin D analogs or derivatives: Increased risk of hypercalcemia and hyperphosphatemia. Avoid concomitant use.
Monitoring
Baseline Monitoring
Serum Calcium
Rationale: To establish baseline and identify pre-existing hypercalcemia, which is a contraindication.
Timing: Prior to initiation of therapy.
Serum Phosphorus
Rationale: To establish baseline and identify pre-existing hyperphosphatemia.
Timing: Prior to initiation of therapy.
Intact Parathyroid Hormone (iPTH)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation of therapy.
Alkaline Phosphatase
Rationale: To assess bone turnover status.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum Calcium
Frequency: At least weekly during dose titration, then monthly once stable.
Target: Within normal limits (e.g., 8.4-10.2 mg/dL), avoiding hypercalcemia.
Action Threshold: If corrected serum calcium > 10.5 mg/dL, reduce or interrupt paricalcitol dose.
Serum Phosphorus
Frequency: At least weekly during dose titration, then monthly once stable.
Target: Within normal limits (e.g., 2.5-4.5 mg/dL), avoiding hyperphosphatemia.
Action Threshold: If serum phosphorus > 5.5 mg/dL, reduce or interrupt paricalcitol dose and/or adjust phosphate binder regimen.
Intact Parathyroid Hormone (iPTH)
Frequency: Every 2-4 weeks during dose titration, then every 3 months once stable.
Target: CKD Stage 3/4: 35-70 pg/mL. CKD Stage 5: 150-300 pg/mL (KDIGO guidelines).
Action Threshold: Adjust dose to maintain iPTH within target range, avoiding over-suppression or inadequate suppression.
Calcium x Phosphorus Product
Frequency: Weekly during dose titration, then monthly once stable.
Target: < 55 mg²/dL²
Action Threshold: If product > 55 mg²/dL², reduce or interrupt paricalcitol dose and/or adjust phosphate binder regimen to reduce risk of vascular calcification.
Symptom Monitoring
- Symptoms of hypercalcemia: Nausea, vomiting, constipation, anorexia, muscle weakness, fatigue, headache, confusion, polyuria, polydipsia, bone pain.
- Symptoms of hyperphosphatemia: Pruritus, bone pain, red eye (conjunctival calcification).
Special Patient Groups
Pregnancy
Limited data on paricalcitol use in pregnant women are insufficient to inform a drug-associated risk for major birth defects or miscarriage. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
No specific data, but theoretical risk of hypercalcemia in mother affecting fetal development.
Second Trimester:
No specific data, but theoretical risk of hypercalcemia in mother affecting fetal development.
Third Trimester:
No specific data, but theoretical risk of hypercalcemia in mother affecting fetal development.
Lactation
There is no information on the presence of paricalcitol in human milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for paricalcitol and any potential adverse effects on the breastfed infant from paricalcitol or from the underlying maternal condition. Monitor breastfed infants for hypercalcemia.
Infant Risk:
Low to moderate; potential for hypercalcemia in infant. Monitor infant for signs of hypercalcemia.
Pediatric Use
Safety and efficacy have not been established in pediatric patients with chronic kidney disease (CKD) Stages 3-5. Use in pediatric patients is not recommended.
Geriatric Use
No overall differences in safety or effectiveness were observed between patients ≥65 years of age and younger patients. However, due to increased prevalence of comorbidities and polypharmacy, monitor elderly patients closely for adverse effects, particularly hypercalcemia.
Clinical Information
Clinical Pearls
- Paricalcitol is a selective VDR activator, which means it aims to suppress PTH with less impact on calcium and phosphorus levels compared to non-selective vitamin D analogs like calcitriol.
- Careful and frequent monitoring of serum calcium, phosphorus, and iPTH is crucial, especially during dose titration, to prevent hypercalcemia and hyperphosphatemia.
- Patients should be educated on the symptoms of hypercalcemia and instructed to report them immediately.
- Avoid concomitant use with magnesium-containing products due to the risk of hypermagnesemia in CKD patients.
- Dose adjustments should be made based on trends in iPTH, calcium, and phosphorus, not just single values.
Alternative Therapies
- Calcitriol (Rocaltrol, Calcijex)
- Doxercalciferol (Hectorol)
- Cinacalcet (Sensipar) - a calcimimetic, different mechanism but also used for secondary hyperparathyroidism.
- Etelcalcetide (Parsabiv) - another calcimimetic.
Cost & Coverage
Average Cost:
Varies widely by pharmacy and dosage; typically several hundred dollars per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Specialty/Non-preferred Brand, or Preferred Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.