Does Rocaltrol (calcitriol) cause side effects?

Rocaltrol (calcitriol) is a synthetic active form of vitamin D3 (cholecalciferol) used to treat and prevent low levels of calcium in the blood of patients who have kidney disease or problems with their parathyroid gland, the gland that controls the amount of calcium in blood through its secretion of parathyroid hormone. 

Calcium plays an important role in maintaining bone health, and low levels of calcium may cause bone disease. Rocaltrol increases blood levels of calcium by increasing the absorption of calcium in the kidneys, increasing the absorption of calcium and phosphorus from the intestine, and increasing the release of calcium and phosphorus from the bones. Rocaltrol helps the body to use calcium found in foods and supplements.

Common side effects of Rocaltrol include

  • hypercalcemia (abnormally high levels of calcium in the blood),
  • hypercalciuria (elevated levels of calcium in the urine), and
  • hyperphosphatemia (high levels of phosphate in the blood).

Serious side effects of Rocaltrol include

  • bone disease.

Drug interactions of Rocaltrol include other vitamin D products because of the increased risk of additive side effects and toxicity. Cholestyramine, colestipol, mineral oil, and orlistat may decrease the intestinal absorption of Rocaltrol.

  • Phenytoin and phenobarbital may reduce blood concentrations of Rocaltrol, decreasing treatment effectiveness.
  • Higher doses of Rocaltrol may be necessary if these drugs are used together with calcitriol.
  • Thiazide diuretics may increase the blood levels of calcium.
  • Since Rocaltrol also increases calcium levels, taking these two types of medications together may cause hypercalcemia (abnormally high levels of calcium).
  • Rocaltrol should be used cautiously in patients taking digoxin.
  • High levels of calcium may cause symptoms of digoxin toxicity such as irregular heartbeats. Ketoconazole may decrease the activity of enzymes responsible for metabolizing or breaking down Rocaltrol and lead to the side effects of excessive vitamin D.
  • Magnesium containing medications (for example, antacids) should be avoided in patients undergoing chronic renal dialysis who are taking Rocaltrol.
  • These patients are at high risk of experiencing hypermagnesemia (high blood levels of magnesium) as their kidneys are unable to remove adequate amounts of magnesium from the blood.

There are no adequate and well-controlled studies of calcitriol treatment in pregnant women. Rocaltrol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. 

Rocaltrol may be excreted in breast milk. Mothers should not breastfeed while taking Rocaltrol.

What are the important side effects of Rocaltrol (calcitriol)?

WARNING

Excessive vitamin D may lead to hypercalcemia (abnormally high levels of calcium in the blood), hypercalciuria (elevated levels of calcium in the urine), hyperphosphatemia (high levels of phosphate in the blood), and bone disease. To avoid complications, vitamin D and its derivatives should be avoided during calcitriol therapy.

Hypercalcemia has been reported in patients treated with calcitriol. Patients should avoid making any sudden changes in their dietary calcium intake and maintain adequate intake of fluid (hydration) during treatment.

Rocaltrol (calcitriol) side effects list for healthcare professionals

Since Rocaltrol is believed to be the active hormone which exerts vitamin D activity in the body, adverse effects are, in general, similar to those encountered with excessive vitamin D intake, i.e., hypercalcemia syndrome or calcium intoxication, depending on the severity and duration of hypercalcemia.

Because of the short biological half-life of calcitriol, pharmacokinetic investigations have shown normalization of elevated serum calcium within a few days of treatment withdrawal, i.e., much faster than in treatment with vitamin D3 preparations.

The early and late signs and symptoms of vitamin D intoxication associated with hypercalcemia include:

In clinical studies on hypoparathyroidism and pseudohypoparathyroidism, hypercalcemia was noted on at least one occasion in about 1 in 3 patients and hypercalciuria in about 1 in 7 patients. Elevated serum creatinine levels were observed in about 1 in 6 patients (approximately one half of whom had normal levels at baseline). In concurrent hypercalcemia and hyperphosphatemia, soft-tissue calcification may occur; this can be seen radiographically.

In patients with normal renal function, chronic hypercalcemia may be associated with an increase in serum creatinine.

Hypersensitivity reactions (pruritus, rash, urticaria, and very rarely severe erythematous skin disorders) may occur in susceptible individuals. One case of erythema multiforme and one case of allergic reaction (swelling of lips and hives all over the body) were confirmed by rechallenge.

To report SUSPECTED ADVERSE REACTIONS, contact Validus Pharmaceuticals LLC at 1-866-982-5438 (1- 866-9VALIDUS) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

What drugs interact with Rocaltrol (calcitriol)?

Cholestyramine

  • Cholestyramine has been reported to reduce intestinal absorption of fat-soluble vitamins; as such it may impair intestinal absorption of Rocaltrol.

Phenytoin/Phenobarbital

  • The coadministration of phenytoin or phenobarbital will not affect plasma concentrations of calcitriol, but may reduce endogenous plasma levels of 25(OH)D3 by accelerating metabolism.
  • Since blood level of calcitriol will be reduced, higher doses of Rocaltrol may be necessary if these drugs are administered simultaneously.

Thiazides

  • Thiazides are known to induce hypercalcemia by the reduction of calcium excretion in urine.
  • Some reports have shown that the concomitant administration of thiazides with Rocaltrol causes hypercalcemia.
  • Therefore, precaution should be taken when coadministration is necessary.

Digitalis

  • Calcitriol dosage must be determined with care in patients undergoing treatment with digitalis, as hypercalcemia in such patients may precipitate cardiac arrhythmias.

Ketoconazole

  • Ketoconazole may inhibit both synthetic and catabolic enzymes of calcitriol.
  • Reductions in serum endogenous calcitriol concentrations have been observed following the administration of 300 mg/day to 1200 mg/day ketoconazole for a week to healthy men.
  • However, in vivo drug interaction studies of ketoconazole with Rocaltrol have not been investigated.

Corticosteroids

  • A relationship of functional antagonism exists between vitamin D analogues, which promote calcium absorption, and corticosteroids, which inhibit calcium absorption.

Phosphate-Binding Agents

  • Since Rocaltrol also has an effect on phosphate transport in the intestine, kidneys and bones, the dosage of phosphate-binding agents must be adjusted in accordance with the serum phosphate concentration.

Vitamin D

  • Since calcitriol is the most potent active metabolite of vitamin D3, pharmacological doses of vitamin D and its derivatives should be withheld during treatment with Rocaltrol to avoid possible additive effects and hypercalcemia.

Calcium Supplements

  • Uncontrolled intake of additional calcium-containing preparations should be avoided.

Magnesium

  • Magnesium-containing preparations (e.g., antacids) may cause hypermagnesemia and should therefore not be taken during therapy with Rocaltrol by patients on chronic renal dialysis.

Summary

Rocaltrol (calcitriol) is a synthetic active form of vitamin D3 (cholecalciferol) used to treat and prevent low levels of calcium in the blood of patients who have kidney disease or problems with their parathyroid gland, the gland that controls the amount of calcium in blood through its secretion of parathyroid hormone. Common side effects of Rocaltrol include hypercalcemia (abnormally high levels of calcium in the blood), hypercalciuria (elevated levels of calcium in the urine), and hyperphosphatemia (high levels of phosphate in the blood). There are no adequate and well-controlled studies of calcitriol treatment in pregnant women. Rocaltrol may be excreted in breast milk. Mothers should not breastfeed while taking Rocaltrol.

Treatment & Diagnosis

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Medically Reviewed on 1/21/2021
References
FDA Prescribing Information

Professional side effects and drug interactions sections courtesy of the U.S. Food and Drug Administration.