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Composition: each of capsules contents 0, 25 microgram of alphacalcidol
Other ingredients: Corn oil.
Pharmaceutical Form:
Capsules.
Pharmacotherapeutic group:
Preparation of the Vitamin D and its analogues. Code ATC: А11С С03.
Pharmacological properties:
Pharmacodynamics
Alphacalcidol is the predecessor of active metabolite of the vitamin D3. It increases the absorption of the calcium and phosphorus in the bowels, increases reabsorption of them in kidneys, intensifies the mineralization of the bones and decreases the level of the parathyroid hormone in blood.
Alphacalcidol renews the positive balance of the calcium during the treatment of calcium malabsorption and in this way it decreases the intensity of bones resorption that is promoted to decreasing of the fractures’ frequency.
In course of treatment it is decreased the bones and muscular’ pain, which appears due to the disturbance of calcium and phosphorus metabolism and it improves the coordination of movements too.
Pharmacokinetics
After internal usage alphacalcidol is absorbed in gastrointestinal tract. The time, during of which the drug reaches maximal concentration in plasma is 8 – 18 hours. In the liver alphacalcidol is metabolized to the main active metabolite of the vitamin D3 – calcitriol (1,25- dihydroxivitamin D3). The less part of the drug is metabolized in bones. In contrast with natural vitamin D3 the biotransformation of the drug does not carried out in kidneys. It is allowed to use the drug in patients with kidneys diseases.
Indications:
-Basic types and forms of osteoporosis (including postmenopausal osteoporosis, senile osteoporosis, steroid osteoporosis);
-osteodystrophy due to of chronic renal insufficiency;
-hypoparathyreosis and pseudohypoparathyreosis;
-hyperparathyreosis (with bones’ lesions);
-rickets and osteomalacia due to of malnutrition or malabsorption;
-hypophosphatemic (vitamin D-resistant) rickets and osteomalacia;
-pseudodeficient (vitamin D-dependent) rickets and osteomalacia;
-Fanconi syndrome;
-renal acidosis;
-psoriasis.
Administration and Dosage:
The drug is used internally. The duration of the course of the treatment is determined by physician individually and it depends on the character of disease and the efficacy of the therapy (on average it is 2 – 4 weeks). In isolated cases the drug is used during whole life.
In patients with rickets and osteomalacia, caused by exogenous scarcity of the vitamin D, gastro-intestinal tract diseases or prolonged antispasmodic therapy the drug is prescribed in dosage of 1,0-3,0 microgram per day.
In a case of hypoparathyreosis the daily dosage for adults is 2,0-4,0 microgram.
In osteodystrophy and chronic renal insufficiency the daily dosage for adults is 0,07 - 2 microgram.
In Fanconi syndrome and renal acidosis the drug is prescribed for adults in the daily dosage
of 2,0-6,0 microgram.
In hypophosphatemic rickets and osteomalacia the daily dosage for adults is 4,0-20,0 microgram.
In postmenopausal osteoporosis, senile osteoporosis, steroid osteoporosis and other types of it the daily dosage for adults is 0,5-1,0 microgram.
It is recommended to start the treatment from the minimal indicated doses, and it is necessary to control the level of calcium and phosphorus in the plasma ones in the week. The dose of the drug could be increased for 0,25 or 0,5 microgram per day for the stabilization of biochemical indexes. On reaching of minimal effective dose it is recommended to control the level of calcium in plasma every 3 – 5 weeks.
In children after 7 years, with the weight more than 20 kg - 1,0 microgram per day.
Side effects:
Gastro-intestinal tract and liver: anorexia, vomiting, heartburn, stomach pain, nausea, dry mouth, discomfort in epigastria, constipation, diarrhoea, and in rare cases it could be increasing of alanine aminotransferase and aspartate aminotransferase in plasma.
Central nervous system: weakness, fatigability, headache, dizziness, drowse.
Cardiovascular system: tachycardia is in rare cases.
Allergic reactions: skin rash, itch.
Contraindications:
Hypersensitivity for some of drugs components; -
hypercalcinemia, hypermagnesemia; -
hyperphosphatemia (except hyperphosphatemia, caused by hypoparathyreosis);
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pregnancy and lactation; -
stomach and duodenal ulcer; -
liver diseases; -
children under 7 years.
Overdosage:
Possible symptoms: weakness, inertia, dizziness, headache, nausea, dry mouth, constipation, diarrhoea, heartburn, vomiting, epigastria pain, bones pain, itch, tachycardia.
Treatment: it is necessary to stop the usage of the drug. On the early stage of the overdosage it could be the positive effect from the gastric lavage and/or from the prescription of mineral oil (which promotes to absorption and increasing of the excretion of the drug with faeces).
In serious cases it can be used isotonic solution of sodium chloride intravenously, loop diuretics, glucocorticoides.
Special indications:
For patients who are inclined to hypercalcaemia, especially for patients with urolithiasis it is necessary to administer the drug carefully.
During the usage of the drug it is necessary to control the level of the calcium in the plasma and urine, to observe the development of the therapeutic effect and correct the dosage of alphacalcidol for the avoidance of hypercalcaemia and hypercalcuria.
In the presence of the biochemical data of the normalization of the bones structure (the normalization of the alkaline phosphatases contents in the plasma) it is necessary to decrease the dose of alphacalcidol that allows to avoid hypercalcaemia. Hypercalcaemia and hypercalcuria could be corrected by finishing of the drug usage and decreasing of calcium usage for the normalization of calcium level in the blood. As rule this period is 1 week. Than, the therapy could be continued, starting from the half of the last dose.
During the period of the pregnancy alphacalcidol is prescribed only by vital indications.
Drug interactions:
During the course of the treatment alphacalcidol could combine with estrogens and antiresorptive drugs of different groups.
In synchronous usage of alphacalcidol and derivations of digitalis the risk of the arrhythmia is increased. If alphacalcidol and anticonvulsant drugs or other drugs, which could activate enzymes of the microsomal oxidation in the liver, are used synchronously, the efficacy of alphacalcidol decreases. Absorption of alphacalcidol decreases in a case of its synchronous prolonged usage with the mineral oils, colestyramine, colestipol, sucralfate, antacids and albumin preparations.
In a case of the synchronous usage of alphacalcidol and antacids the risk of the hypermagnesemia increases. There is the increased risk of hypercalcaemia if the drug is used with calcium preparations or thiazide diuretics. During the course of the treatment by alphacalcidol it is not allowed to prescribe the vitamin D and its derivates because of the possibility of additive interaction and hypercalcaemia.
Storage and Shelf-life: Keep in dry, protected from light place; keep out of reach of children, at the temperature not more than 255oC. Shelf-life – 2 years.
Conditions of supply: On prescription.
Package: 10 capsules are in a blister, 3 blisters are in a carton box (No10x3).
Manufacturer.
Kusum Healthcare Pvt. Ltd, India
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