Each 1 mL amp contains the following non-active ingredients: Polysorbate (NF) 4 mg, sodium chloride (USP) 1.5 mg, sodium ascorbate (USP) 10 mg, disodium edetate (USP) 1.11 mg, anhydrous dibasic sodium phosphate (USP) 7.6 mg, monobasic sodium phosphate monohydrate (USP) 1.84 mg and water for injection (USP) 1 mL.
Calcitriol is the active form of vitamin D3 (cholecalciferol). The natural endogenous supply of vitamin D in man mainly depends on ultraviolet light for conversion of 7-dehydrocholesterol to vitamin D3 in the skin. Vitamin D3 must be metabolically activated in the liver and the kidney before it is fully active on its target tissues. The initial transformation is catalyzed by a vitamin D3-25-hydroxylase enzyme present in liver, and the product of this reaction is 25-(OH)D3 (calcifediol). The latter undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-α-hydroxylase to product 1,25-(OH)2D3 (calcitriol), the active form of vitamin D3.
The known sites of action of calcitriol are intestine, bone, kidney and parathyroid gland. Calcitriol is the most active known form of vitamin D3 in stimulating intestinal calcium transport. In acutely uremic rats, calcitriol has been shown to stimulate intestinal calcium absorption. In bone, calcitriol, in conjunction with parathyroid hormone, stimulates resorption of calcium. And in the kidney, calcitriol increases the tubular reabsorption of calcium. In vitro and in vivo studies have shown that calcitriol directly suppresses secretion and synthesis of parathyroid hormone (PTH). A vitamin D-resistant state may exist in uremic patients because of the failure of the kidney to adequately convert precursors to the active compound, calcitriol.
Calcitriol when administered by bolus injection is rapidly available in the blood stream. Vitamin D metabolites are known to be transported in blood, bound to specific plasma proteins. The pharmacologic activity of an administered dose of calcitriol is about 3-5 days. Two (2) metabolic pathways for calcitriol have been identified, conversion to 1,24,25-(OH)3D3 and to calcitroic acid.
Softcap: Established postmenopausal osteoporosis; renal osteodystrophy in patients with chronic renal failure, particularly those undergoing hemodialysis; postsurgical hypoparathyroidism; idiopathic hypoparathyroidism; pseudohypoparathyroidism; vitamin D-dependent rickets; hypophosphatemic vitamin D-resistant rickets.
Inj: Management of hypocalcemia in patients undergoing chronic renal dialysis. It has been shown to significantly reduce elevated parathyroid hormone levels. Reduction of PTH has been shown to result in an improvement in renal osteodystrophy.
Softcap: The dose of calcitriol should be carefully adjusted for each patient on the basis of the serum calcium level. Calcitriol therapy should always be started at the lowest possible dose and serum calcium levels should be checked every month.
Renal Osteodystrophy: Initial Dose: 0.25 mcg daily. If no satisfactory response in the biochemical parameters and clinical manifestations of the disease is observed within 2-4 weeks, the dosage may be increased by 0.25 mcg daily at 2-4 week intervals.
Postmenopausal Osteoporosis: Recommended Dose: 0.25 mcg twice daily.
Hypoparathyroidism and Rickets: Recommended Initial Dose: 0.25 mcg/day in the morning.
Injection: The optimal dose must be carefully determined for each patient.
The effectiveness is predicated on the assumption that each patient is receiving an adequate and appropriate daily intake of calcium. The recommended dietary allowance (RDA) for calcium in adults is 800 mg. To ensure that each patient receives an adequate daily intake of calcium, the physician should either prescribe calcium supplement or instruct the patient in proper dietary measures.
The recommended initial dose is 0.5 mcg (0.01 mcg/kg) administered 3 times weekly, approximately every other day. Calomin Inj can be administered as a bolus dose IV through the catheter at the end of hemodialysis. If a satisfactory response in the biochemical parameters and clinical manifestations of the disease state is not observed, the dose may be increased by 0.25-0.5 mcg at 2-4 week intervals. During this titration period, serum calcium and phosphorus levels should be obtained at least twice weekly and if hypercalcemia is noted, it should be immediately discontinued until normocalcemia ensues. Most patients undergoing hemodialysis respond to doses between 0.5 and 3 mcg (0.01-0.05 mcg/kg) 3 times per week.
Administration to patients in excess of their requirements can cause hypercalcemia, hypercalciuria and hyperphosphatemia. High intake of calcium and phosphate concomitant with Calomin may lead to similar abnormalities.
Treatment of Hypercalcemia and Overdosage in Patients on Dialysis: General treatment of hypercalcemia (>1 mg/dL above the upper limit of normal range) consists of immediate discontinuation of therapy, institution of a low calcium diet and withdrawal of calcium supplements. Serum calcium levels should be determined daily until normocalcemia ensues.
Hypercalcemia usually resolves in 2-7 days. When serum calcium levels have returned to within normal limits. Calomin Inj therapy may be reinstituted at a dose 0.5 mcg less than prior therapy serum calcium levels should be obtained at least twice weekly after all dosage changes.
Persistent or markedly elevated serum calcium levels may be corrected by dialysis against a calcium-free dialysate.
Treatment of Accidental Overdosage of Calcitriol Injection: The treatment acute accidental overdosage should consist of general supportive measures. Serial serum electrolyte determinations (especially calcium), rate of urinary calcium excretion and assessment of electrocardiographic abnormalities due to hypercalcemia should be obtained. Such monitoring is critical in patients receiving digitalis. Discontinuation of supplemental calcium and 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. Should, however, persistent and markedly elevated serum calcium levels occur, there are a variety of therapeutic alternatives which may be considered, depending on the patients' underlying condition. An appropriate forced diuresis, peritoneal dialysis against a calcium-free dialysate, the use of drugs eg, bisphosphonate, miramycin, calcitonin, glucocorticosteroids, nitrates and kalium have been reported.
Patients with known hypersensitivity to calcitriol (or drugs of the same class) or to any of the constituents of Calomin. All diseases associated with hypercalcemia. Evidence of vitamin D toxicity.
Since calcitriol is the most potent metabolite of vitamin D available, vitamin D and its derivatives should be withheld during treatment. A non-aluminum phosphate-binding compound should be used to control serum phosphorus levels in patients undergoing dialysis.
Overdosage of any form of vitamin D is dangerous (see Overdosage). Progressive hypercalcemia due to overdosage of vitamin D and its metabolites may be so severe as to require emergency attention. Chronic hypercalcemia can lead to generalized vascular calcification, nephrocalcinosis and other soft tissue calcification. The serum calcium times phosphate (Ca X P) product should not be allowed to exceed 70. Radiographic evaluation of suspect anatomical regions may be useful in the elderly detection of this condition.
Softcap: There is a close correlation between treatment with calcitriol and the development of hypercalcemia. In patients with normal renal function, chronic hypercalcemia may be associated with an increase in serum creatinine. Calcitriol increases inorganic phosphate levels in serum. Immobilized patients are particularly exposed to the risk of hypercalcemia.
Since calcitriol is the most effective vitamin D metabolite available, no other vitamin D preparation should be prescribed during treatment with calcitriol thereby ensuring that the development of hypervitaminosis D is avoided.
Injection: Excessive dosage induces hypercalcemia and in some instances hypercalciuria therefore, early in treatment during dosage adjustment, serum calcium and phosphorus should be determined at least twice weekly. Should hypercalcemia develop, Calomin should be discontinued immediately. Calomin Inj should be given cautiously to patients on digitalis, because hypercalcemia in such patients may precipitate cardiac arrhythmias.
Information for the Patient: The patient and his or her parents should be informed about adherence to instructions about diet and calcium supplementation and avoidance of the use of unapproved non-prescription drugs, including magnesium-containing antacids. Patients should also be carefully informed about the symptoms of hypercalcemia (see Adverse Reactions).
Essential Laboratory Tests: Serum calcium, phosphorus, magnesium and alkaline phosphatase and 24-hr urinary calcium and phosphorus should be determined periodically during the initial phase of the medication serum calcium and phosphorus should be determined more frequently (twice weekly).
Because the effect of calcitriol in the treatment of bone loss after implantation has not been established, Calomin should not be used.
Because the effect of calcitriol in patients with post menopausal osteoporosis cause by decrease of estrogen have not been established, Calomin should not be used.
Carcinogenesis, Mutagenesis & Impairment of Fertility: Long-term studies in animals have not been performed to evaluate the carcinogenic potential of Calomin Inj (calcitriol).
There was no evidence of mutagenicity as studies by the Ames method.
No significant effects of calcitriol on fertility were reported using oral calcitriol.
Use in pregnancy: Calcitriol given orally has been reported to be teratogenic in rabbits when given in doses 4 and 15 times the dose recommended for human use. All 15 fetuses in 3 L at these doses showed external and skeletal abnormalities however, none of the other 23 letters (156 fetuses) showed significant abnormalities compared with controls. Teratology studies in rats showed no evidence of teratogenic potential.
Safety and efficacy in pregnant women have not been established.
Calomin Inj should be used during pregnancy only if the potential benefit justifies potential risk to the fetus.
Use in lactation: It is not known whether Calomin Inj is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reaction in nursing infants from calcitriol, a decision should be made whether to discontinue nursing or to discontinue Calomin Inj, taking into account the importance of the drug to the mother.
Use in children: Safety and efficacy of Calomin Inj in children have not been established.
Use in pregnancy: Calcitriol given orally has been reported to be teratogenic in rabbits when given in doses 4 and 15 times the dose recommended for human use. All 15 fetuses in 3 L at these doses showed external and skeletal abnormalities however, none of the other 23 letters (156 fetuses) showed significant abnormalities compared with controls.
Teratology studies in rats showed no evidence of teratogenic potential.
Safety and efficacy in pregnant women have not been established.
Calomin Inj should be used during pregnancy only if the potential benefit justifies potential risk to the fetus.
Use in lactation: It is not known whether Calomin Inj is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reaction in nursing infants from calcitriol, a decision should be made whether to discontinue nursing or to discontinue Calomin Inj, taking into account the importance of the drug to the mother.
Hypersensitivity: Rarely, hypersensitivity reactions including anaphylaxis and local reddening at injection site have been reported.
Vitamin D Toxicity: Adverse effects of Calomin Inj (calcitriol inj) are, in general, similar to those encountered with excessive vitamin D intake. The early and late signs and symptoms of vitamin D intoxication associated with hypercalcemia include:
Early: Weakness, headache, somnolence, nausea, vomiting, dry mouth, constipation, muscle pain, bone pain and metallic taste.
Late: Polyuria, polydipsia, anorexia, weight loss, nocturia, conjunctivitis (calcific), pancreatitis, photophobia, rhinorrhea, pruritus, hyperthermia, decreased libido, elevated blood urea nitrogen (BUN), albuminuria, hypercholesterolemia, elevated aspartate aminotransferase (AST) and alanine transaminase (ALT), ectopic clarification, hypertension, cardiac arrhythmias and rarely, overt psychosis.
Occasional mild pain on injection have been observed.
Magnesium-containing antacids and Calomin Inj should not be used concomitantly because such use may lead to the development of hypermagnesemia.
When vitamin D derivatives and cardioglycosides have been administered concomitantly, cardiac arrhythmia may occur.
Efficacy of vitamin D may be reduced in patients with barbiturates or anticonvulsants.
Corticosteroids have been shown antagonization of vitamin D derivatives.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Discard unused portion.
Softcap: Store in well-tight container. Protect against heat and light.
Inj: Store in light-resistant and hermetic containers at controlled room temperature.
A11CC04 - calcitriol ; Belongs to the class of vitamin D and analogues. Used as dietary supplements.
Softcap 0.25 mcg (lemon-yellow colored, oval) x 100's. Inj (ampoule) 1 mcg/mL (colorless to pale yellow soln in transparent, amber glass amp) x 10's.
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