Active substanceKolekaltsiferolKolekaltsiferol
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  • Dosage form: & nbsporal solution
    Composition:

    1 ml of solution (40 drops) contains:

    Active ingredient: colcalciferol 0.500 mg (corresponding to 20,000 ME vitamin A D3);

    Excipients: medium chain triglycerides - 939,500 mg.

    Description:

    Transparent, slightly yellowish, viscous solution.

    Pharmacotherapeutic group:Vitamin - calcium-phosphorus exchange regulator
    ATX: & nbsp

    A.11.C.C.05   Kolekaltsiferol

    Pharmacodynamics:

    Kolekaltsiferol is an anti-cancer remedy replenishing vitamin D deficiency3. It is involved in the regulation of calcium-phosphorus metabolism, enhances calcium absorption in the intestine and the reabsorption of phosphates in the kidneys, promotes the mineralization of bones and is necessary for the normal functioning of the parathyroid glands.

    Deficiency of calcium and / or vitamin D3 hypersecretion of the parathyroid hormone. As a result of this secondary hyperparathyroidism, there is an increase in bone remodeling, which leads to brittleness and bone fractures. The use of calcium and vitamin D3 in the recommended dose range causes a decrease in the secretion of parathyroid hormone.

    Pharmacokinetics:

    Absorption

    Vitamin D3 (colcalciferol) with oral administration is almost completely absorbed (80%) in the small intestine. The maximum concentration in tissues is reached in 4-5 hours, after which the concentration decreases slightly, remaining for a long time at a constant level.

    Distribution

    Kolekaltsiferol in plasma binds to Kolekaltsiferol binding protein and transported to the liver, where the microsomal hydroxylated to form an inactive metabolite 25-gidroksikolekaltsiferola (kaltsifediol). The concentration of circulating in the blood of calcipediol is an indicator of the level of vitamin D3 in organism.

    Metabolism

    Then kaltsifediol enters the kidneys, where it undergoes hydroxylation repeated to form the active metabolite 1,25-digidroksikolekaltsiferola (calcitriol). Vitamin D3 and its metabolites can accumulate in the muscle and fatty tissues, where their concentration can persist for several months. After taking high doses of vitamin A D3 the concentration of calcipediol in the serum can be kept high for several months. Hypercalcemia due to an overdose of vitamin A D3 can persist for several weeks.

    Excretion

    Calcitriol undergoes further hydroxylation before excretion from the body. The main way to excrete vitamin D3, as well as its hydroxylated and sulfate derivatives is bile (feces), and at least 2% of these substances are excreted in the urine. Kolekaltsiferol penetrates the placental barrier and is excreted in breast milk.

    Indications:

    - Prevention of rickets and osteomalacia in children and adults;

    - prevention of diseases associated with vitamin deficiency (deficiency) D3 in healthy children and adults without infringement of absorption;

    - Supportive therapy of osteoporosis in adults;

    - prevention of rickets in term and preterm infants;

    - prevention of diseases associated with vitamin deficiency (deficiency) D3, in children and adults with malabsorption syndrome (chronic small bowel disease, biliary cirrhosis, conditions after resection of the stomach and / or small intestine);

    - treatment of rickets and osteomalacia in newborns, children and adults (against the background of violations of mineral metabolism in patients older than 45 years, prolonged immobilization in case of injuries, compliance with diets with refusal to accept milk and dairy products);

    - treatment of hypoparathyroidism in adults.

    Contraindications:

    Hypersensitivity to the components of the drug, hypercalcemia, hypercalciuria. calcium nefrourolithiasis (including in the anamnesis), pseudohypoparathyroidism (see "Special instructions").

    Carefully:Carefully should prescribe the drug in sarcoidosis (see "Special instructions"), when taking additional amounts of vitamin D3 and calcium (for example, in other drugs), with impaired excretion of calcium and phosphate in the urine, in the treatment of benzothiadiazine derivatives and in immobilized patients (risk of hypercalcaemia and hypercalciuria) (see Special instructions).

    In the course of long-term vitamin treatment D3 in a daily dose of more than 1000 ME, the serum calcium level should be controlled.

    Pregnancy and lactation:

    During pregnancy and during breastfeeding, adequate vitamin intake is required D3.

    During pregnancy, you should avoid exceeding the recommended dose of vitamin A D3, t. hypercalcemia can lead to a delay in mental and physical development of the fetus, special forms of aortic stenosis and retinopathy in children.

    Daily doses up to 500 IU / day

    Currently, the risk of using the drug in this range of doses is unknown.

    Daily doses in excess of 500 IU / day

    The drug should be used during pregnancy only in case of obvious need and only in the exact doses that are required to fill the vitamin deficiency D3.

    Vitamin D3 and its metabolites penetrate into breast milk. Overdose in newborns during breastfeeding was not noted.

    Dosing and Administration:

    The drug Vigantol® take inside, diluting it in a teaspoon of milk or other liquid.

    - Prevention of rickets: adults and children take 1 drop (corresponding to 500 ME vitamin A D3) in a day. In newborns, the dosage of the drug should be determined individually by the doctor, the drug is prescribed from the second week of life. To the finished healthy children Vigantol it is recommended to take on 1 drop (corresponds 500 ME vitamin A D3) per day, premature infants - 2 drops (corresponding to 1000 ME vitamin A D3) in a day. The drug is prescribed during the first and second years of life, especially during the winter months. Drops of the drug are diluted in a teaspoon of water, milk or baby food. If the drops are added to a bottle or a spoon with a nutrient mixture, you need to make sure that you have a full meal, because otherwise, the whole dose can not be guaranteed. Drip drops should be added only to the prepared and properly cooled nutritional formula.

    - Prevention of the risk of diseases associated with vitamin deficiency D3 in healthy individuals without impaired absorption: 1 drop of the drug Vigantol® (corresponding to 500 ME vitamin A D3) in a day;

    - Prevention of the risk of diseases associated with vitamin deficiency D3 with malabsorption syndrome: dosage of the drug should be determined individually by a doctor, it is recommended to take 6-10 drops of the drug Vigantol® (corresponding to 3000-5000 ME vitamin A D3) in a day;

    - Supportive therapy of osteoporosis: 2 drops of the drug Vigantol® (corresponds to 1000 ME vitamin A D3) in a day;

    - Treatment of diseases associated with vitamin deficiency D3 (rickets and osteomalacia), in newborns, children and adults: dosage of the drug should be determined individually by the doctor. It is recommended to take 2-10 drops of the drug Vigantol® (corresponding to 1000-5000 ME vitamin A D3) in a day. Treatment should be continued for 1 of the year;

    - Treatment of hypoparathyroidism: the dosage of the drug should be 20-40 drops of the drug Vigantol® (corresponding to 10000 - 20000 ME vitamin A D3) in a day. The concentration of calcium in the blood should be determined within 4-6 weeks, then every 3-6 months, and adjust the dose in accordance with the calcium content in the blood.

    For prolonged treatment with Wigantol®, serum calcium and urine levels should be regularly monitored and renal function assessed by measuring serum creatinine. If necessary, the dose should be adjusted in accordance with the level of calcium in the blood serum (see "Special instructions").

    Side effects:

    The frequency of undesired reactions is not determined, since studies to assess the frequency of adverse reactions have not been conducted.

    Disorders of metabolism and nutrition:

    Hypercalcemia and hypercalciuria.

    Disorders from the gastrointestinal tract:

    Complaints from the gastrointestinal tract, such as constipation, flatulence, nausea, abdominal pain or diarrhea.

    Disturbances from the skin and subcutaneous tissues:

    Hypersensitivity reactions, such as pruritus, rash and hives.

    Overdose:

    Symptoms of a vitamin overdose D3

    Acute and chronic overdose of vitamin D3 can lead to hypercalcemia, which can be of a persistent nature and potentially life-threatening. Symptoms are general and may include cardiac arrhythmias, thirst, nausea, vomiting, constipation, polydipsia, polyuria, dehydration, hypercalciuria with the formation of kidney stones, nephrocalcinosis, muscle weakness, adynamia and confusion. Moreover, a chronic overdose can lead to the deposition of calcium in the vessels and tissues.

    Daily doses up to 500 IU / day

    Prolonged overdose of vitamin D3 can lead to hypercalcemia and hypercalciuria. Substantial overuse for a long period of time can lead to calcification of the parenchymal organs.

    Daily doses, exceeding 500 IU / day

    Ergocalciferol (vitamin D2) and colcalciferol (vitamin D3) have a relatively low therapeutic index. Intoxication threshold for vitamin D3 varies between 40,000 and 100,000 ME per day for 1-2 months in adults with normal parathyroid function. In newborns and small children, sensitivity to significantly lower concentrations may be noted. Therefore, patients should be warned that the vitamin D3 Do not take without medical supervision.

    Overdosing increases the phosphorus levels in serum and urine as well as hypercalcemic syndrome and subsequent deposition of calcium in tissues, especially kidney (urolithiasis, nephrocalcinosis) and vessels.

    The symptoms of intoxication are general in nature and are manifested in the form of nausea, vomiting, also initially in the form of diarrhea, and later - in the form of constipation, loss of appetite, weakness, headache, muscle aches, joint pain, muscle weakness, persistent drowsiness, azotemia, polydipsia and polyuria and, at the final stage, in the form of dehydration of the body. Typical biochemical data include hypercalcemia, hypercalciuria.as well as an increase in the serum concentration of 25-hydroxycolecalciferol.

    Treatment of overdose

    Daily doses up to 500 IU / day

    If there are symptoms of chronic overdose with vitamin D3 it may be necessary to use forced diuresis, as well as the appointment of glucocorticoids and calcitonin.

    Daily doses, exceeding 500 IU / day

    When an overdose is required, measures must be taken to correct hypercalcemia, which is often of a persistent nature and, under certain circumstances, may endanger life.

    First of all, you need to stop taking a vitamin D3. To eliminate hypercalcemia caused by vitamin intoxication D3, it takes several weeks.

    Depending on the degree of hypercalcemia, as a measure of treatment, a diet with a low calcium content or completely without calcium is prescribed, consumption of large amounts of fluid, forced diuresis with furosemide, as well as glucocorticoids and calcitonin.

    With proper functioning of the kidneys, the calcium level can be significantly reduced by infusing an isotonic sodium chloride solution (3-6 liters within 24 hours) with the addition of furosemide and,in some cases, sodium edetate at a dose of 15 mg / kg / h, while simultaneously monitoring the level of calcium and ECG data. In oligoanuria, on the contrary, it is necessary to conduct hemodialysis (dialysate without calcium). There is a specific antidote.

    It is recommended that patients be alerted to the symptoms of a possible overdose with prolonged consumption of high doses of vitamin A D3 (nausea, vomiting, also initially diarrhea, later - constipation, anorexia, weakness, headache, muscle pain, joint pain, muscle weakness, drowsiness, azotemia, polydipsia and polyuria).

    Interaction:

    Phenytoin, primidon and drugs of the barbiturate group increase the need for a vitamin D3 because of an increase in the rate of biotransformation of colcalciferol in inactive metabolites, due to a decrease in the level of calcipediol in blood plasma.

    Concomitant therapy with glucocorticosteroids may decrease the effectiveness of the vitamin D3.

    Concomitant therapy with cardiac glycosides (foxglove) may increase their toxic potential due to the development of hypercalcemia (risk of cardiac arrhythmia). These patients need to monitor the ECG and calcium levels in blood and urine, and adjust the dose of cardiac glycosides.And also it is necessary to control the levels of digoxin and digitoxin in the blood plasma in the presence of indications.

    Vitamin D3 can be combined with metabolites or analogs of the vitamin D3 only in exceptional cases and under the control of the level of calcium in the blood serum.

    Thiazide diuretics can reduce the excretion of calcium in the urine and, accordingly, increase the risk of hypercalcemia. In such patients, it is necessary to continuously monitor calcium levels in the blood and urine with prolonged use of the drug.

    Rifampicin and isoniazid can reduce the effectiveness of the drug because of the increased rate of biotransformation of the vitamin D3.

    Does not interact with food.

    Special instructions:

    If other drugs containing vitamin D3, should take into account the dose of vitamin A D3, contained in the preparation Vigantol®. Additional vitamin supplementation D3 or calcium should be done only under medical supervision. In this case, it is necessary to monitor the level of calcium in the serum and urine.

    In patients with renal insufficiency treated with Wigantol®, it is necessary to control the effect on the metabolism of calcium and phosphate.

    The drug should not be used in patients with a predisposition to calcium nephrourolythiasis.

    The drug should be used with caution in patients with impaired excretion of calcium and phosphate in the urine, in the treatment of benzothiadiazine derivatives and in immobilized patients (risk of hypercalcemia and hypercalciuria). These patients should monitor the level of calcium in the blood and urine.

    It is advisable to use caution when using the drug Vigantol® in patients with sarcoidosis due to the risk of rapid conversion of vitamin® into its active metabolite. These patients should monitor the level of calcium in the blood and urine.

    The drug should not be taken with pseudohypoparathyroidism, because in the phase of normal sensitivity to vitamin D3 the need for a vitamin D3 may decrease, leading to a risk of delayed overdose. In such cases, it is better to use active metabolites of the vitamin D3, allowing more accurately adjust the dosage.

    With prolonged treatment with Wigantol® in a daily dose exceeding 500 IU / day, serum calcium and urine calcium levels should be monitored, and renal function assessed by measuring serum creatinine.This is especially important for elderly patients and with concomitant treatment with cardiac glycosides or diuretics. In the case of hypercalcemia or the presence of signs of impaired renal function, the dose of the drug should be reduced or suspended treatment. If the level of calcium in the urine exceeds 7.5 mmol / 24 h (300 mg / 24 h), it is recommended to reduce the dose of the drug or suspend treatment.

    With prolonged treatment with Wigantol® in a daily dose exceeding 1000 IU vitamin D3, you should monitor the level of calcium in the blood serum.

    Effect on the ability to drive transp. cf. and fur:

    Studies on the impact on the ability to drive a vehicle and work with mechanisms have not been carried out.

    Form release / dosage:

    Solution for oral ingestion, 0.5 mg / ml.

    Packaging:For 10 ml of the drug in a bottle of brown-orange light-protection glass (type III Eur.), Sealed with a stopper-dropper made of white polyethylene and a screw cap made of white polypropylene.
    One bottle together with the instruction for use is placed in a cardboard box.
    Storage conditions:

    In the dark place at a temperature of 15-25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011712 / 01
    Date of registration:27.09.2011 / 05.03.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:Merck KGaAMerck KGaA Germany
    Manufacturer: & nbsp
    Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.
    Information update date: & nbsp09.03.2017
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