How should this medicine be used?
Calcio 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. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take Calcio exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor will probably start you on a low dose of Calcio and may gradually increase your dose depending on your body's response to Calcio.
Rocaltrol (Calcio) is indicated in the management of secondary hyperparathyroidism and resultant metabolic bone disease in patients with moderate to severe chronic renal failure (Ccr 15 to 55 mL/min) not yet on dialysis. In children, the creatinine clearance value must be corrected for a surface area of 1.73 square meters. A serum iPTH level of ≥ 100 pg/mL is strongly suggestive of secondary hyperparathyroidism.
Treatment of Hypercalcemia and Overdosage in Predialysis Patients
If hypercalcemia ensues (greater than 1 mg/dL above the upper limit of the normal range), adjust dosage to achieve normocalcemia by reducing Rocaltrol (Calcio) therapy from 0.5 mcg to 0.25 mcg daily. If the patient is receiving a therapy of 0.25 mcg daily, discontinue Rocaltrol (Calcio) until patient becomes normocalcemic. Calcium supplements should also be reduced or discontinued. Serum calcium levels should be determined 1 week after withdrawal of calcium supplements. If serum calcium levels have returned to normal, Rocaltrol (Calcio) therapy may be reinstituted at a dosage of 0.25 mcg/day if previous therapy was at a dosage of 0.5 mcg/day. If Rocaltrol (Calcio) therapy was previously administered at a dosage of 0.25 mcg/day, Rocaltrol (Calcio) therapy may be reinstituted at a dosage of 0.25 mcg every other day. If hypercalcemia is persistent at the reduced dosage, serum PTH should be measured. If serum PTH is normal, discontinue Rocaltrol (Calcio) therapy and monitor patient in 3 months' time.
What Other Drugs Interact with Calcio?
If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.
Calcio has no known severe interactions with other drugs.
Serious interactions of Calcio include:
Moderate interactions of Calcio include:
- dienogest/estradiol valerate
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
Calcio has no known mild interactions with other drugs.
This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.
Tell your doctor about all prescription, nonprescription, illegal, recreational, herbal, nutritional, or dietary drugs you're taking, especially:
- Calcium supplements
- Questran (cholestyramine)
- Colestid (colestipol hydrochloride)
- Lanoxin (digoxin)
- Diuretics (water pills)
- Nizoral (ketoconazole)
- Fosrenol (lanthanum carbonate)
- Oral steroids, such as Decadron or Dexone (dexamethasone), Medrol (methylprednisolone), or Deltasone (prednisone)
- Other forms of vitamin D
- Luminal or Solfoton (phenobarbital)
- Dilantin (phenytoin)
- Renagel (sevelamer hydrochloride)
- Drisdol or Calciferol (ergocalciferol)
Calcio - Clinical Pharmacology
Man's 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 . 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 (Calcio), the active form of vitamin D3. Endogenous synthesis and catabolism of Calcio, as well as physiological control mechanisms affecting these processes, play a critical role regulating the serum level of Calcio. Physiological daily production is normally 0.5 to 1.0 mcg and is somewhat higher during periods of increased bone synthesis (eg, growth or pregnancy).
Before taking Calcio, tell your doctor if you have, or have ever had:
- Heart disease
- Blood vessel problems
- Kidney disease or kidney stones
- Liver disease
- High levels of phosphate, vitamin D, or calcium in your blood
- Allergies to medications or vitamins
Also, let your doctor know if you've recently been dehydrated or had surgery, or are unable to move around.
Your healthcare provider will probably recommend a very specific diet while you're taking Calcio. Follow your doctor's instructions carefully.
This medicine won't work well if you don't get the right amount of calcium in the foods you eat.
Be sure to drink plenty of fluids while taking Calcio. But if you have kidney disease, talk to your doctor about how much you should drink each day.
Let your doctor know that you're taking this medicine before you have any type of surgery, including a dental procedure.
Your doctor will probably order frequent tests to check your body's response to this medicine. Keep all appointments with your healthcare provider and laboratory.
Calcio dosage must be determined with care in patients undergoing treatment with digitalis, as hypercalcemia in such patients may precipitate cardiac arrhythmias (see PRECAUTIONS: General).
Clinical studies of Rocaltrol (Calcio) did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Rocaltrol (Calcio) should not be given to patients with hypercalcemia or evidence of vitamin D toxicity. Use of Rocaltrol (Calcio) in patients with known hypersensitivity to Rocaltrol (Calcio) (or drugs of the same class) or any of the inactive ingredients is contraindicated.
C 1,25-Dihydroxyvitamin D3 (Calcio)
Calcio is the active form of vitamin D, and it is essential for calcium absorption and bone mineralization. Vitamin D 3 is a steroid that is ingested in the diet or synthesized in the skin in the presence of ultraviolet light. It is converted in the liver into 25-hydroxyvitamin D3 and then hydroxylated again in the proximal tubular epithelial cells of the kidney by the enzyme 1-α hydroxylase into the active metabolite 1,25-dihydroxyvitamin D3 (Calcio). Parathyroid hormone stimulates Calcio production in the kidney by increasing the synthesis of 1-α hydroxylase.
Calcio has several important functions in the body. It maintains serum calcium levels by increasing calcium absorption in the gastrointestinal tract. It promotes healthy bone formation by the calcification of osteoid tissue. It also directly inhibits parathyroid gland activity by decreasing parathyroid hormone synthesis and release. In patients with chronic kidney disease, a lack of Calcio can result in metabolic bone disease. Calcio and several synthetic vitamin D analogs are now available for patients with kidney disease.
Man's natural 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 . 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 (Calcio), the active form of vitamin D3. Endogenous synthesis and catabolism of Calcio, as well as physiological control mechanisms affecting these processes, play a critical role regulating the serum level of Calcio. Physiological daily production is normally 0.5 to 1.0 mcg and is somewhat higher during periods of increased bone synthesis (eg, growth or pregnancy).
What Are Side Effects Associated with Using Calcio?
Common side effects of Calcio include:
- Abdominal or stomachpain
- Bone pain
- BUN and creatinine increased
- Changes in behavior
- Decreased sex drive (libido)
- Dry mouth
- Excessive nighttime urination
- Eye pain or redness
- Eye sensitivity to light
- Growth suppression
- Heart rate changes (fast, slow, or uneven)
- High blood calcium (hypercalcemia)
- High blood magnesium (hypermagnesemia)
- High blood phosphates (hyperphosphatemia)
- High blood pressure (hypertension)
- High cholesterol (hypercholesteremia)
- High core body temperature (hyperthermia)
- Increased thirst
- Loss of appetite
- Loss of height
- Lower back pain
- Metallic taste
- Muscle or bone pain
- Muscle pain or weakness
- Severe pain in your upper stomach spreading to your back
- Slow growth (in children)
- Urinating more than usual or changes in the amount of urine
- Weight loss
This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.
Calcio is commonly prescribed and relatively well-studied in the setting of CKD. It does not require renal activation for potent binding to the vitamin D receptor. As a result, it is an established therapy for the treatment of secondary hyperparathyroidism in all stages of CKD and is known to effectively lower serum PTH concentration (see Chapter 8 ). In addition, Calcio has been associated with improved survival in observational studies of CKD and ESRD (see Consequences ). Calcio can be administered intravenously with hemodialysis or orally at any stage of CKD.
Because Calcio potently activates the vitamin D receptor, one potential adverse effect is adynamic bone disease due to oversuppression of PTH (see Chapter 8 ). In addition, Calcio carries a risk of hypercalcemia and, less frequently, hyperphosphatemia. Regular monitoring is therefore required.
Enterohepatic recycling and biliary excretion of Calcio occur. The metabolites of Calcio are excreted primarily in feces. Following intravenous administration of radiolabeled Calcio in normal subjects, approximately 27% and 7% of the radioactivity appeared in the feces and urine, respectively, within 24 hours. When a 1-mcg oral dose of radiolabeled Calcio was administered to normal subjects, approximately 10% of the total radioactivity appeared in urine within 24 hours. Cumulative excretion of radioactivity on the sixth day following intravenous administration of radiolabeled Calcio averaged 16% in urine and 49% in feces. The elimination half-life of Calcio in serum after single oral doses is about 5 to 8 hours in normal subjects.