From WikiMD's Wellnesspedia

(Redirected from 1,25(OH)2D)

What is Calcitriol?[edit | edit source]

  • Calcitriol (Rocaltrol) is a synthetic vitamin D analog which is active in the regulation of the absorption of calcium from the gastrointestinal tract and its utilization in the body.

What are the uses of this medicine?[edit | edit source]

Calcitriol is used:

How does this medicine work?[edit | edit source]

  • Natural supply of vitamin D depends mainly on exposure to the ultraviolet rays of the sun for conversion of 7-dehydrocholesterol in the skin to vitamin D3 (cholecalciferol).
  • Vitamin D3 must be metabolically activated in the liver and the kidney before it is fully active as a regulator of calcium and phosphorus metabolism at target tissues.
  • The initial transformation of vitamin D3 is catalyzed by a vitamin D3-25-hydroxylase enzyme (25-OHase) present in the liver, and the product of this reaction is 25-hydroxyvitamin D3 [25-(OH)D3].
  • Hydroxylation of 25-(OH)D3 occurs in the mitochondria of kidney tissue, activated by the renal 25-hydroxyvitamin D3-1 alpha-hydroxylase (alpha-OHase), to produce 1,25-(OH)2D3 (calcitriol), the active form of vitamin D3.
  • Rocaltrol (calcitriol) is a synthetic vitamin D analog which is active in the regulation of the absorption of calcium from the gastrointestinal tract and its utilization in the body.

Who Should Not Use this medicine ?[edit | edit source]

This medicine cannot be used in patients with:

  • hypercalcemia or evidence of vitamin D toxicity
  • known hypersensitivity to Rocaltrol (or drugs of the same class) or any of the inactive ingredients

What drug interactions can this medicine cause?[edit | edit source]

  • Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

  • Tell your doctor or pharmacist if you are taking ergocalciferol (Deltalin, Drisdol) or have stopped taking it in the past few months.

Is this medicine FDA approved?[edit | edit source]

  • Calcitriol was identified as the active form of vitamin D in 1971 and the drug was approved for medical use in the United States in 1978.

How should this medicine be used?[edit | edit source]

  • The optimal daily dose of Rocaltrol must be carefully determined for each patient.
  • Rocaltrol therapy should always be started at the lowest possible dose and should not be increased without careful monitoring of serum calcium.
  • Rocaltrol can be administered orally either as a capsule (0.25 mcg or 0.50 mcg) or as an oral solution (1 mcg/mL).
  • Patients are advised to have a dietary intake of calcium at a minimum of 600 mg daily.

Recommended dosage: Dialysis Patients:

  • The recommended initial dose of Rocaltrol is 0.25 mcg/day.
  • If a satisfactory response in the biochemical parameters and clinical manifestations of the disease state is not observed, dosage may be increased by 0.25 mcg/day at 4- to 8-week intervals.


  • The recommended initial dosage of Rocaltrol is 0.25 mcg/day given in the morning.
  • If a satisfactory response in the biochemical parameters and clinical manifestations of the disease is not observed, the dose may be increased at 2- to 4-week intervals.
  • Most adult patients and pediatric patients age 6 years and older have responded to dosages in the range of 0.5 mcg to 2 mcg daily.
  • Pediatric patients in the 1- to 5-year age group with hypoparathyroidism have usually been given 0.25 mcg to 0.75 mcg daily.

Predialysis Patients:

  • The recommended initial dosage of Rocaltrol is 0.25 mcg/day in adults and pediatric patients 3 years of age and older.
  • This dosage may be increased if necessary to 0.5 mcg/day.
  • For pediatric patients less than 3 years of age, the recommended initial dosage of Rocaltrol is 10 to 15 ng/kg/day.


  • Calcitriol comes as a capsule and a solution (liquid) to take by mouth.
  • It usually is taken once a day or once every other day in the morning with or without food.
  • Your doctor will probably start you on a low dose of calcitriol and may gradually increase your dose depending on your body's response to calcitriol.

What are the dosage forms and brand names of this medicine?[edit | edit source]

This medicine is available in fallowing doasage form:

  • As capsules containing 0.25 mcg or 0.5 mcg calcitriol and as an oral solution containing 1 mcg/mL of calcitriol.

This medicine is available in fallowing brand namesː

  • Rocaltrol

What side effects can this medication cause?[edit | edit source]

The most common side effects of this medicine include:

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

What special precautions should I follow?[edit | edit source]

  • Excessive dosage of Rocaltrol induces hypercalcemia and in some instances hypercalciuria; therefore, early in treatment during dosage adjustment, serum calcium should be determined twice weekly. If hypercalcemia develop, treatment with Rocaltrol should be stopped immediately.
  • During periods of hypercalcemia, serum calcium and phosphate levels must be determined daily. When normal levels have been attained, treatment with Rocaltrol can be continued, at a daily dose 0.25 mcg lower than that previously used.
  • Immobilized patients, e.g., those who have undergone surgery, are particularly exposed to the risk of hypercalcemia.
  • Patients with normal renal function taking Rocaltrol should avoid dehydration. Adequate fluid intake should be maintained.
  • The patient and his or her caregivers should be informed about compliance with dosage instructions, adherence to instructions about diet and calcium supplementation, and avoidance of the use of unapproved nonprescription drugs.
  • Patients and their caregivers should also be carefully informed about the symptoms of hypercalcemia.
  • Patients are advised to have a dietary intake of calcium at a minimum of 600 mg daily.
  • Magnesium-containing preparations (e.g., antacids) and Rocaltrol should not be used concomitantly in patients on chronic renal dialysis because such use may lead to the development of hypermagnesemia.
  • Tell your doctor if you have recently had surgery or are unable to move around for any reason and if you have or have ever had kidney or liver disease.
  • Rocaltrol is the most potent metabolite of vitamin D available. The administration of Rocaltrol to patients in excess of their daily requirements can cause hypercalcemia, hypercalciuria, and hyperphosphatemia. Therefore, pharmacologic doses of vitamin D and its derivatives should be withheld during Rocaltrol treatment to avoid possible additive effects and hypercalcemia.

What to do in case of emergency/overdose?[edit | edit source]

Symptoms of overdosage may include: hypercalcemia, hypercalciuria, and hyperphosphatemia

  • Since calcitriol is a derivative of vitamin D, the signs and symptoms of overdose are the same as for an overdose of vitamin D .

Management of overdosage:

  • In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

Treatment of Hypercalcemia:

  • General treatment of hypercalcemia (greater than 1 mg/dL above the upper limit of the normal range) consists of immediate discontinuation of Rocaltrol therapy, institution of a low-calcium diet and withdrawal of calcium supplements.
  • Serum calcium levels should be determined daily until normocalcemia ensues.
  • Hypercalcemia frequently resolves in 2 to 7 days.

Treatment of Hyperphosphatemia:

  • If serum phosphorus levels exceed 5.0 mg/dL to 5.5 mg/dL, a calcium-containing phosphate-binding agent (i.e., calcium carbonate or calcium acetate) should be taken with meals.
  • Serum phosphorus levels should be determined as described earlier.
  • Aluminum-containing gels should be used with caution as phosphate-binding agents because of the risk of slow aluminum accumulation.

Treatment of Accidental Overdosage of Rocaltrol:

  • The treatment of acute accidental overdosage of Rocaltrol should consist of general supportive measures.
  • If drug ingestion is discovered within a relatively short time, induction of emesis or gastric lavage may be of benefit in preventing further absorption.
  • If the drug has passed through the stomach, the administration of mineral oil may promote its fecal elimination.
  • Discontinuation of supplemental calcium and a low-calcium diet are also indicated in accidental overdosage.
  • Due to the relatively short duration of the pharmacological action of calcitriol, further measures are probably unnecessary.
  • If persistent and markedly elevated serum calcium levels occur, there are a variety of therapeutic alternatives which may be considered, depending on the patient's underlying condition.
  • These include the use of drugs such as phosphates and corticosteroids as well as measures to induce an appropriate forced diuresis.
  • The use of peritoneal dialysis against a calcium-free dialysate has also been reported.

Can this medicine be used in pregnancy?[edit | edit source]

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

Can this medicine be used in children?[edit | edit source]

  • Safety and effectiveness of Rocaltrol in pediatric patients undergoing dialysis have not been established.
  • The safety and effectiveness of Rocaltrol in pediatric predialysis patients have been established.
  • Dosing guidelines have not been established for pediatric patients under 1 year of age with hypoparathyroidism or for pediatric patients less than 6 years of age with pseudohypoparathyroidism.

What are the active and inactive ingredients in this medicine?[edit | edit source]

Active ingredient:

  • calcitriol

Inactive ingredients:

  • butylated hydroxyanisole
  • butylated hydroxytoluene
  • coconut oil
  • glycerin
  • sorbitol
  • fd&c yellow no. 6
  • titanium dioxide

Who manufactures and distributes this medicine?[edit | edit source]

Manufactured for and Distributed by:

What should I know about storage and disposal of this medication?[edit | edit source]

  • Store at 59° to 86°F (15° to 30°C).
  • Dispense in a tight, light-resistant container as defined in USP.

Calcitriol Resources

Find a healthcare provider anywhere in the world quickly and easily!

Translate to: East Asian 中文, 日本, 한국어, South Asian हिन्दी, Urdu, বাংলা, తెలుగు, தமிழ், ಕನ್ನಡ,
Southeast Asian Indonesian, Vietnamese, Thai, မြန်မာဘာသာ, European español, Deutsch, français, русский, português do Brasil, Italian, polski


WikiMD is the world's largest, free medical and wellness encyclopedia edited only by professionals. Advertise!


Navigation: Wellness - Encyclopedia - Health topics - Disease Index‏‎ - Drugs - World Directory - Gray's Anatomy - Keto diet - Recipes

Search WikiMD

Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro) available.
Advertise on WikiMD

WikiMD is not a substitute for professional medical advice. See full disclaimer.

Credits:Most images are courtesy of Wikimedia commons, and templates Wikipedia, licensed under CC BY SA or similar.