Instructions for Decristol 1000 IU tablets No. 50
Composition
active ingredient: cholecalciferol;
1 tablet contains 25 mcg of cholecalciferol (in the form of a concentrate [powder form]), which corresponds to 1000 IU of vitamin D3;
excipients: all-rac-alpha-tocopherol, modified corn starch, medium chain triglycerides, crystalline sodium ascorbate, sucrose, silicon dioxide, lactose monohydrate, microcrystalline cellulose, corn starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: white, oblong tablets with a score on both sides. The tablet can be divided in half.
Pharmacotherapeutic group
Vitamins. Vitamin D and analogues. Cholecalciferol.
ATX code A11C C05.
Pharmacological properties
Pharmacodynamics.
Cholecalciferol (vitamin D3) is synthesized in the skin under the influence of UV rays from 7-dehydrocholesterol and converted to its biologically active form (1,25-dihydroxycholecalciferol) as a result of two stages of hydroxylation: first in the liver (position 25), and then in the kidney tissues (position 1). Together with parathyroid hormone (PTH) and calcitonin, 1,25-dihydroxycholecalciferol plays an important role in regulating the calcium-phosphate balance. In its biologically active form, vitamin D3 stimulates the absorption of calcium in the intestine, the incorporation of calcium into osteoid and the release of calcium from bone tissue. In case of vitamin D deficiency, skeletal calcification does not occur (rickets) or bone decalcification occurs (osteomalacia).
Calcium and/or vitamin D deficiency induces reversible increased secretion of PTH. This secondary hyperparathyroidism causes increased bone metabolism, which can lead to bone fragility and fractures.
From the point of view of its formation, physiological regulation, and mechanism of action, vitamin D3 can be considered as a precursor of a steroid hormone.
In addition to its physiological formation in the skin, cholecalciferol can be ingested with food or as a drug. In the latter case, overdose and intoxication are possible, since physiologically the drug does not inhibit the synthesis of vitamin D in the skin.
Ergocalciferol (vitamin D2) is produced in plants. In humans, it is metabolically activated in a similar way to cholecalciferol. Ergocalciferol exhibits the same effects as cholecalciferol both qualitatively and quantitatively.
Pharmacokinetics.
Absorption
Vitamin D is almost completely absorbed from food along with dietary lipids and bile acids. Higher doses are absorbed by about two-thirds.
Distribution and biotransformation
Cholecalciferol and its metabolites circulate in the blood, bound to proteins. In the liver, it is metabolized by microsomal hydroxylase to 25-hydroxycholecalciferol. It is then converted in the kidneys to 1,25-dihydroxycholecalciferol.
Vitamin D that is not metabolized is stored in muscle and adipose tissue and therefore has a long biological half-life. After taking high doses of vitamin D, serum 25-hydroxyvitamin D concentrations may be elevated for months. Hypercalcemia caused by overdose may persist for weeks (see section "Overdose").
Breeding
Vitamin D and its metabolites are excreted in the bile/feces.
Indication
− Prevention of rickets and osteomalacia in children and adults.
− Prevention of vitamin D deficiency in children and adults at risk of such deficiency.
− As an adjunct to specific osteoporosis therapy in adults.
Contraindication
- Hypersensitivity to the active substance or to any of the excipients listed in the "Composition" section.
- Hypercalcemia.
- Hypercalciuria.
- Hypervitaminosis D.
- Pseudohypoparathyroidism (the need for vitamin D may be lower than during the period of normal sensitivity to the vitamin, there is a risk of prolonged overdose).
- Nephrolithiasis (urinary stone disease).
- Renal failure.
- Sarcoidosis.
- Tuberculosis.
- Taking additional vitamin D can lead to an overdose.
Interaction with other medicinal products and other types of interactions
Phenytoin or barbiturates
In the case of simultaneous use of anticonvulsants such as phenobarbital, hydantoin derivatives, in particular phenytoin, and other barbiturates or primidone, as well as, possibly, other drugs that inhibit the activity of liver enzymes, a decrease in the effect of vitamin D3 may occur due to metabolic inactivation, for example, as a result of activation of the microsomal enzyme system.
Glucocorticoids
Due to increased metabolism of vitamin D, its effect may decrease.
Rifampicin
Rifampicin may reduce the effectiveness of cholecalciferol due to activation of liver enzymes.
Isoniazid
Isoniazid may reduce the effectiveness of cholecalciferol due to inhibition of the metabolic activation of cholecalciferol.
Ion exchangers, laxatives, orlistat
Concomitant treatment with ion exchangers such as cholestyramine or colestipol, laxatives such as liquid paraffin or fat-absorbing agents such as orlistat may reduce the absorption of vitamin D in the gastrointestinal tract.
The cytostatic drug actinomycin and the antifungal drug imidazole interfere with the activity of vitamin D3 by inhibiting the conversion of 25-hydroxycholecalciferol to 1,25-dihydroxycholecalciferol by the renal enzyme 25-hydroxyvitamin D-1-hydrolase.
May reduce the conversion of vitamin D metabolites and therefore reduce its effectiveness.
Metabolites or analogues of vitamin D (e.g. calcitriol)
The combination of Decristol® 1000 IU with metabolites or analogues of vitamin D should be avoided. Simultaneous administration of vitamin D3 with metabolites or analogues of vitamin D is possible only as an exception and only under the condition of monitoring the level of calcium in the blood serum (increases the risk of toxic effects).
Thiazide diuretics
Thiazide diuretics may cause hypercalcemia due to decreased renal calcium excretion. In case of prolonged use of the drug, serum and urine calcium levels should be monitored.
Digitalis (cardiac glycosides)
Oral vitamin D may increase the efficacy and toxicity of cardiac glycosides due to increased calcium levels (risk of cardiac arrhythmias). Patients should be monitored with ECG, plasma and urine calcium levels, and, if necessary, digoxin or digitoxin levels.
Antacids containing aluminum or magnesium
Concomitant use of the drug with antacids containing aluminum or magnesium may provoke aluminum toxicity on bones and hypermagnesemia in patients with renal failure.
Ketoconazole
Ketoconazole may reduce the biosynthesis and catabolism of 1,25(OH)2-cholecalciferol.
Medicines containing high doses of calcium and phosphorus
Concomitant use with drugs containing high doses of calcium and phosphorus increases the risk of hyperphosphatemia.
Calcitonin, gallium nitrate, bisphosphonates, etidronate, pamidronate, plicamycin
Vitamin D may antagonize drugs prescribed for hypercalcemia, such as calcitonin, etidronate, and pamidronate.
Application features
When prescribing other drugs containing vitamin D, the dose of vitamin D in Decristol® 1000 IU should be taken into account. Additional vitamin D or calcium preparations should be used only under the supervision of a physician to prevent hypercalcemia. In such cases, it is necessary to monitor the level of calcium in the blood serum and urine.
In patients with renal insufficiency receiving Decristol® 1000 IU, the effect on calcium-phosphate balance should be monitored.
Recommended doses should not be exceeded due to the risk of hypervitaminosis.
In patients with severe renal impairment, cholecalciferol is not metabolized normally. Therefore, such patients may require other forms of vitamin D.
When using the drug in patients with mild to moderate renal impairment, it is recommended to monitor calcium and phosphate levels. The risk of soft tissue calcification should be taken into account.
Decristol® 1000 IU should not be prescribed if patients are prone to the formation of calcium-containing kidney stones.
Decristol® 1000 IU should be used with special caution in patients with impaired renal excretion of calcium and phosphate, in patients receiving treatment with benzothiadiazine derivatives and in immobilized patients (risk of hypercalcemia, hypercalciuria). In such patients, the level of calcium in the blood plasma and urine should be monitored.
Decristol® 1000 IU should be used with caution in patients with sarcoidosis, as there is a risk of increased conversion of vitamin D to its active metabolites. In such patients, plasma and urinary calcium levels should be monitored.
Decristol® 1000 IU should not be used in the presence of pseudohypoparathyroidism (the need for vitamin D may be reduced sometimes to normal sensitivity to vitamin D, there is a risk of prolonged overdose). In such cases, it is recommended to use vitamin D derivatives, the doses of which are easier to adjust.
In patients with hepatic insufficiency, the hepatic hydroxylation of cholecalciferol to 25 OHD may be impaired.
Infants and young children
Dekristol® 1000 IU should be used with particular caution in infants and young children, as they may not swallow the tablets and choke. For such patients, it is advisable to dissolve the tablets according to the instructions (see section "Method of administration and dosage") or use drops.
Daily doses exceeding 500 IU
During long-term treatment with Decristol® 1000 IU, serum and urine calcium levels should be monitored and renal function should be checked by measuring serum creatinine. This monitoring is particularly important in elderly patients and in patients receiving concomitant treatment with cardiac glycosides or diuretics (see section "Interaction with other medicinal products and other forms of interaction").
This also applies to patients who are particularly prone to the formation of calcium-containing kidney stones.
Treatment should be discontinued if symptoms of hypervitaminosis appear, such as fatigue, nausea, diarrhea, or polyuria. Since such symptoms are non-specific, a doctor should be consulted to determine whether they can be associated with excess vitamin D.
One tablet of the drug Decristol® 1000 IU contains 175 mg of sucrose.
Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
One tablet of the drug Decristol® 1000 IU contains 68.94 mg of lactose monohydrate.
Patients with rare hereditary conditions of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
One tablet of the drug Decristol® 1000 IU contains less than 1 mmol sodium (23 mg).
Caution should be exercised when used in patients on a controlled sodium diet.
Use during pregnancy or breastfeeding
Pregnancy
Daily use in a dose of up to 500 IU/day
To date, the risks of using the drug in the indicated dose range are unknown.
Vitamin D overdose should be avoided during pregnancy, as long-term hypercalcemia can lead to delayed physical and mental development of the fetus, aortic stenosis, and retinopathy in children.
Daily use in doses exceeding 500 IU/day
During pregnancy, Decristol® 1000 IU should be used only in cases of urgent need in doses that are truly necessary to correct vitamin D deficiency.
Long-term overdose of vitamin D should be avoided due to the possible development of hypercalcemia, which can lead to defects in the physical and mental development of the fetus, aortic stenosis, and retinopathy in the child.
Breast-feeding
Vitamin D and its metabolites are excreted in breast milk. Cases of overdose in infants have not been recorded. However, this should be kept in mind when prescribing additional vitamin D to a child.
Fertility
In fertility studies with cholecalciferol, no effects on reproductive performance were observed. The potential benefit/risk balance for humans is unknown.
Ability to influence reaction speed when driving vehicles or other mechanisms
Not detected.
Method of administration and doses
Dosage.
Prevention of rickets and osteomalacia in children and adults
1/2 tablet of Decristol® 1000 IU per day (equivalent to 0.0125 mg, or 500 IU, of vitamin D3) (see section “Special instructions”).
The dosage should be determined by a doctor. Usually, for the prevention of rickets in children (premature newborns):
- whose body weight at birth is > 1500 g, prescribe 1/2 tablet of Decristol® 1000 IU per day (equivalent to 0.0125 mg, or 500 IU, of vitamin D3);
- whose body weight at birth ® 1000 IU per day (equivalent to 0.025 mg, or 1000 IU, of vitamin D3)
(see section "Features of use").
Prevention of vitamin D deficiency in children and adults at risk of such deficiency
Children (infants) aged 0–12 months:
1/2 tablet of Decristol® 1000 IU per day (equivalent to 0.0125 mg, or 500 IU, of vitamin D3) (see section “Special instructions”).
Children, adolescents and adults
1/2–1 tablet of Decristol® 1000 IU per day (equivalent to 0.0125–0.025 mg, or 500–1000 IU, of vitamin D3) (see section “Special instructions”).
As an adjunct to specific osteoporosis therapy in adults
1 tablet of Decristol® 1000 IU per day (equivalent to 0.025 mg, or 1000 IU, of vitamin D3) (see section “Special instructions”).
During prolonged use of the drug Decristol® 1000 IU in daily doses exceeding 500 IU, serum and urine calcium levels should be regularly monitored and renal function should be checked by determining serum creatinine. If necessary, the dose should be adjusted depending on the serum calcium level (see section "Special instructions").
Alternatively, national dosage recommendations for the prevention and treatment of vitamin D deficiency can be followed.
Method of application
Infants and young children.
Prevention of rickets in infants
Infants receive Decristol® 1000 IU from the second week of life until the end of the first year of life. During the second year of life, continued use of Decristol® 1000 IU is recommended, especially in winter.
The tablet is dissolved in a teaspoon of water or milk and the dissolved tablet is administered directly into the child's mouth, preferably during a meal. The tablet dissolves in 1–2 minutes. To speed up the dissolution process, the spoon should be moved slightly.
It is not recommended to add the dissolved tablet to a baby's feeding bottle or soft puree as complete administration of the dose cannot be guaranteed. However, if the tablet is to be administered with food, it should be prepared first and then allowed to cool before adding the tablet.
When consuming foods enriched with vitamins, you should consider the amount of vitamin D they contain.
Adults
The tablets are taken with sufficient water, preferably during meals.
The duration of treatment depends on the course of the disease.
Special patient groups
In case of severe liver dysfunction, the dose should be adjusted by the attending physician (see also the section "Special instructions").
Patients with renal impairment/hypercalcemia
If hypercalcemia or signs of decreased renal function occur, the dose should be reduced or treatment discontinued. If hypercalciuria occurs (more than 7.5 mmol, corresponding to 300 mg of calcium per 24 hours), the dose should be reduced or treatment discontinued.
Elderly people
Elderly people with a history of falls should avoid doses exceeding 24,000 IU per month.
For elderly people aged > 70 years
When treating with vitamin D in a loading dose protocol, serum 25(OH)D3 levels should also be monitored regularly. Treatment should be discontinued at levels ≥ 50 ng/mL.
Children.
To prevent vitamin D deficiency, it is used in children from birth.
For the prevention of rickets, it is used from the second week of life.
Overdose
Vitamin D3 regulates calcium and phosphate metabolism. In case of overdose, hypercalcemia, hypercalciuria, renal calcifications and bone lesions occur, as well as changes in the cardiovascular system. Hypercalcemia occurs after the use of 50,000–100,000 IU of vitamin D3 per day.
Symptoms of overdose
Acute and chronic overdose of vitamin D3 can lead to hypercalcemia, which can be persistent and possibly life-threatening. Symptoms are nonspecific and may include cardiac arrhythmias, thirst, dehydration, adynamia, and impaired consciousness. In addition, chronic overdose can lead to calcium deposits in blood vessels and tissues.
In addition to increased serum and urine phosphorus levels, overdose can also lead to hypercalcemia syndrome, which subsequently leads to calcium deposition in tissues, and especially in renal tissues (nephrolithiasis, nephrocalcinosis, renal failure) and blood vessels.
Symptoms of intoxication are not very characteristic and are manifested by nausea, vomiting, initial frequent diarrhea, progressing to constipation, anorexia, apathy, headache, myalgia, arthralgia, muscle weakness and constant drowsiness, arrhythmia, azotemia, polydipsia and polyuria, and in the preterminal stage - exsicosis. Symptoms of intoxication are also photosensitivity, pancreatitis, rhinorrhea, hyperthermia, decreased libido, conjunctivitis, hypercholesterolemia, increased transaminase activity, arterial hypertension, uremia. Common symptoms are pain in the muscles and joints.
Standard biochemical indicators are hypercalcemia, hypercalciuria, and elevated serum 25-hydroxycalciferol levels.
Treatment
Symptoms of chronic vitamin D overdose may require forced diuresis, as well as administration of glucocorticoids and calcitonin.
In the event of overdose, measures are necessary to treat the often chronic and potentially life-threatening hypercalcemia.
As an initial measure, vitamin D should be discontinued; it may take several weeks for hypercalcemia due to vitamin D intoxication to resolve.
Depending on the degree of hypercalcemia, a low-calcium or calcium-free diet may be used, and abundant hydration, forced diuresis with furosemide, and administration of glucocorticoids and calcitonin are recommended.
In the presence of normal renal function, infusions of isotonic NaCl solution (3–6 L per 24 hours) with furosemide and, in some cases, 15 mg/kg body weight/h of sodium edetate, administered under constant monitoring of calcium levels and ECG, demonstrate a highly reliable effect in lowering calcium levels.
However, in case of oligoanuria, hemodialysis (with dialysate that does not contain calcium) is indicated.
Specific antidote is unknown.
Patients on long-term treatment with higher doses of vitamin D are recommended to be informed about the symptoms of possible overdose (nausea, vomiting, initial diarrhea progressing to constipation, anorexia, apathy, headache, myalgia, arthralgia, muscular weakness, drowsiness, azotemia, polydipsia and polyuria).
Adverse reactions
The frequency of adverse reactions is unknown, as large-scale clinical studies that would allow for an estimate of the frequency have not been conducted.
Immune system disorders: hypersensitivity reactions, such as angioedema or laryngeal edema.
Visual disorders: conjunctivitis, photosensitivity.
Cardiovascular system disorders: arrhythmia, hypertension.
Metabolism and nutrition disorders: hypercholesterolemia, weight loss, polydipsia, increased sweating, pancreatitis, hypercalcemia and hypercalciuria.
Gastrointestinal disorders: gastrointestinal symptoms such as constipation, flatulence, nausea, abdominal pain or diarrhea, loss of appetite, colic (including exacerbation of colic), spasms, dyspepsia, dry mouth.
Urinary system disorders: increased calcium levels in the blood and/or urine, urolithiasis and tissue calcification, polyuria, uremia.
Musculoskeletal disorders: muscle and joint pain, muscle weakness.
Nervous system disorders: headache, drowsiness, mental disorders, depression.
Hepatobiliary system disorders: increased activity of aminotransferases.
Psychiatric disorders: decreased libido.
There have also been reports of rhinorrhea and hyperthermia.
Reporting of suspected adverse reactions
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product via the Automated Pharmacovigilance Information System at https//aisf.dec.gov.ua.
Expiration date
36 months.
Storage conditions
Store at a temperature not exceeding 25°C. Keep the blister in the package to protect from light. Keep out of the reach of children.
Packaging
10 tablets in a blister, 2 blisters in a pack. 25 tablets in a blister, 2, or 4, or 8 blisters in a pack.
Vacation category
Without a prescription.
Producer
mibe GmbH Arcnaymittel.
Location of the manufacturer and address of its place of business
Münchenerstrasse 15, Brena, Saxony-Anhalt, 06796, Germany.
