Calciferol (colecalciferol)

Calciferol (colecalciferol) Medicine

Overdose

Symptoms: decreased appetite, nausea, vomiting, constipation, restlessness, thirst, polyuria, diarrhea, intestinal colic. Common symptoms are headache, muscle and joint pain, mental disorders, and t.tsch. depression, stupor, ataxia, and progressive weight loss. Developing impaired renal function with albinaria, the eritrotsituriey and polyuria, increased loss of potassium, hyposthenuria, nocturia and increased blood pressure. In severe cases, corneal opacity may occur, less often-edema of the papilla of the optic nerve, inflammation of the iris up to the development of cataracts. Kidney stones may form. There is a process of calcification of soft tissues, in t.tsch. blood vessels, heart, lungs, and skin. Rarely develops cholestatic jaundice

Treatment: discontinue use of the drug and consult a doctor. Take large amounts of liquid. If necessary, you may need to be hospitalized.

Contraindications

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hypersensitivity to the components of the drug, especially to benzyl alcohol,

hypervitaminosis D,

increased concentration of calcium in the blood (hypercalcemia),

increased excretion of calcium in the urine (hypercalciuria),

urolithiasis (formation of calcium oxalate stones),

sarcoidosis,

acute and chronic liver and kidney diseases,

kidney failure,

active form of pulmonary tuberculosis.

With caution: the state of immobilization, the intake of thiazides, cardiac glycosides (especially digitalis glycosides), the period of pregnancy and breastfeeding, infants with a predisposition to early overgrowth of the fontanelles (when the small size of the anterior crown is established from birth).

Hypersensitivity, hypercalcemia, hypercalciuria, presence of renal calcareous stones, sarcoidosis, immobilization.

Incompatibilities

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Antiepileptic drugs, rifampicin, colestyramine reduce the reabsorption of vitamin D3.

Concomitant use with thiazide diuretics increases the risk of hypercalcemia.

Concomitant use with cardiac glycosides may increase their toxic effect (increased risk of cardiac arrhythmias).

The risk of hypercalcemia is increased by thiazide diuretics.

Undesirable effects

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Hypersensitivity to the components of the drug, hypervitaminosis D (hypervitaminosis a symptoms: loss of appetite, nausea, vomiting, headache, muscle and joint pain, constipation, dry mouth, polyuria, weakness, mental disorders, including depression, weight loss, sleep disturbance, fever, urine protein, white blood cells, hyaline casts, increased levels of calcium in the blood and its excretion, possible calcification of the kidneys, blood vessels, and lungs).

If signs of hypervitaminosis D appear, it is necessary to cancel the drug, limit the intake of calcium, and prescribe vitamins A, C, and B.

Hypercalcemia, hypercalciuria, arrhythmia, nausea, vomiting, disorders of consciousness and psyche, weight loss, urolithiasis, calcium deposits in soft tissues, decreased appetite, thirst, polyuria.

Therapeutic indications

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prevention and treatment of vitamin D deficiency,

prevention and treatment of rickets, rickets-like diseases, hypocalcemic tetany, osteomalacia, and metabolic bone diseases (such as hypoparathyroidism and pseudohypoparathyroidism),

complex treatment of osteoporosis, including postmenopausal.

The rickets, spasmophilia, osteomalacia.

Pharmacotherapeutic group

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  • Calcium-phosphorus metabolism regulator [Vitamins and vitamin-like products]
  • Vitamins and vitamin-like products

Pharmacodynamic properties

Vitamin D3 It is a natural form of vitamin D, which is formed in humans in the skin under the influence of sunlight. Compared to vitamin D2 it is characterized by 25% higher activity.

Vitamin D3 it is an active anti-cancer factor. The most important function of Vitamin D3 - regulation of calcium and phosphate metabolism, which promotes proper mineralization and skeletal growth. Colecalciferol plays a significant role in the absorption of calcium and phosphates in the intestine, the transport of mineral salts and the process of bone calcification, as well as regulates the excretion of calcium and phosphates by the kidneys.

The concentration of calcium ions in the blood determines the maintenance of skeletal muscle tone, the function of the myocardium, promotes nervous excitation, regulates the process of blood clotting.

A lack of vitamin D in food, a violation of its absorption, a lack of calcium, as well as insufficient exposure to the sun during the rapid growth of the child leads to rickets, in adults — to osteomalacia, in pregnant women, symptoms of tetany may occur, a violation of the processes of calcification of the bones of newborns.

An increased need for vitamin D occurs in women during menopause, as they often develop osteoporosis due to hormonal disorders.

Vitamin D has a number of so-called extra-skeletal effects.

Vitamin D is involved in the functioning of the immune system by modulating cytokine levels and regulates the division of T-helper lymphocytes and the differentiation of B-lymphocytes. A number of studies have shown a decrease in the incidence of respiratory tract infections with vitamin D supplementation.

Vitamin D has been shown to be an important part of the immune system homeostasis: it prevents autoimmune diseases (including type 1 diabetes, multiple sclerosis, rheumatoid arthritis, inflammatory bowel diseases). Vitamin D has antiproliferative and differentiating effects, which determine the oncoprotective effect of vitamin D. It is noted that the frequency of some tumors (breast cancer, colon cancer) increases against the background of low levels of vitamin D in the blood.

Vitamin D is involved in the regulation of carbohydrate and fat metabolism by influencing the synthesis of IRS1 (substrate of the insulin receptor 1, participates in the intracellular pathways of the insulin receptor signal), IGF (IGF, regulates the balance of fat and muscle tissue), PPAR-δ (activated peroxisome proliferator receptor, type δ, promotes the processing of excess Cholesterol). According to epidemiological studies, vitamin D deficiency is associated with the risk of metabolic disorders (metabolic syndrome and type 2 diabetes mellitus). Vitamin D receptors and metabolizing enzymes are expressed in arterial vessels, the heart, and virtually all cells and tissues related to the pathogenesis of cardiovascular diseases

In animal models, anti-atherosclerotic effects, renin suppression, and prevention of myocardial damage are shown.

Low levels of vitamin D in humans are associated with adverse risk factors for cardiovascular disease, such as diabetes mellitus, dyslipidemia, and hypertension, and are associated with the risk of cardiovascular disasters, including strokes.

Studies in experimental models of Alzheimer's disease have shown that vitamin D3 reduced amyloid accumulation in the brain and improved cognitive function. Non-interventional studies in humans have shown that the incidence of dementia and Alzheimer's disease increases against the background of low vitamin D levels and low dietary intake of vitamin D.

There was a decrease in cognitive function and the incidence of Alzheimer's disease with low levels of vitamin D.

Pharmacokinetic properties

Water solution of vitamin D3 it is absorbed better than an oil solution. In premature infants, there is insufficient formation and flow of bile into the intestine, which disrupts the absorption of vitamins in the form of oil solutions.

After oral administration, colecalciferol is absorbed in the small intestine.

It is metabolized in the liver and kidneys. T1/2 the amount of calciferol from the blood is several days and can last in the case of renal failure.

The drug penetrates through the placental barrier and into the mother's milk.

It is excreted by the kidneys in small amounts, most of it is excreted with bile.

Vitamin D3 it has the property of cumulation.

Dosage (Posology) and method of administration

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Inside. The drug is taken in a spoonful of liquid.

1 drop contains about 500 ME of vitamin D3.

If the doctor does not prescribe otherwise, the drug is used in the following dosages.

Preventive doses

Full-term newborns from the 4th week of life, up to 2-3 years with proper care and sufficient exposure to the fresh air: 500 IU (1 drop) per day.

Premature infants with 4 weeks of life, twins, infants in poor living conditions: 1000-1500 ME (2-3 drops) per day. In the summer, you can limit the dose to 500 ME (1 drop) per day.

Adult healthy individuals without malabsorption: 500 ME (1 drop) per day.

Adult patients with malabsorption syndrome: 3000-5000 ME (6-10 drops) per day.

Pregnant women: daily dose of 500 ME (1 drop) of vitamin D3 during the entire period of pregnancy, or taking 1000 ME (2 drops) per day starting from 28 weeks of pregnancy.

In the postmenopausal period: 500-1000 ME (1-2 drops) per day.

Therapeutic doses

For rickets: daily 1000-5000 ME (2-10 drops), depending on the severity of rickets (I, II or III) and the course of the disease, for 4-6 weeks, under careful control of the clinical condition and biochemical parameters (calcium, phosphorus, alkaline phosphatase) of blood and urine. You should start with 1000 ME within 3-5 days. Then, with good tolerability, the dose is increased to an individual therapeutic dose (most often 3000 ME). The dose of 5000 ME is prescribed only for severe bone changes. If necessary, after a 1-week break, you can repeat the course of treatment.

Treatment is carried out until a clear therapeutic effect is obtained, followed by a transition to a preventive dose of 500-1500 ME/day.

Treatment of rickets-like diseases: 20000-30000 ME/day (40-60 drops), depending on the age, weight and severity of the disease, under the control of biochemical blood parameters and urine analysis. The course of treatment is 4-6 weeks. Treatment is carried out under the supervision of a doctor.

Complex treatment of postmenopausal osteoporosis: 500-1000 ME (1-2 drops) per day. The dosage is usually prescribed taking into account the amount of vitamin D that comes with food.

Inside, in a spoonful of milk or other liquid.

Prevention of rickets: full-term healthy children Calciferol (Colecalciferol) is prescribed from the second month of life for 1 drop (about 500 ME of vitamin D3) daily (take 5 days, then take a break of 2 days) during the first and second year of life, excluding the summer months. Preterm infants are prescribed 2 drops (about 1000 IU of vitamin D3) per day from the 10th day of life (take 5 days, then take a break for 2 days), excluding the summer months.

For the treatment of rickets from the 10th day of life, 2-8 drops of Calciferol (Colecalciferol)a (about 1000-5000 ME of vitamin D) are prescribed3) per day. During the first two months of life, as well as the 5th and 9th months of life, in the second year-1-2 courses during the winter-spring period.

Prevention of the risk of diseases associated with vitamin D deficiencyZ: 1-2 drops of Calciferol (Colecalciferol)a (about 500-1000 ME of vitamin D3) per day (take 5 days, then take a break for 2 days).

Prevention of vitamin D deficiency3 in malabsorption syndrome: 4-8 drops of Calciferol (Colecalciferol)a (about 3000-5000 IU of vitamin D3) per day.

Treatment of osteomalacia caused by vitamin D deficiencyZ: 2-8 drops of Calciferol (Colecalciferol)a (about 1000-5000 IU of vitamin D3) per day. Treatment should be continued for 1 year.

Supportive therapy for osteoporosis: 2-4 drops of Calciferol (Colecalciferol)A (about 1000-3000 IU of vitamin D3) per day.

Treatment of hypoparathyroidism and pseudohypoparathyroidism: depending on the concentration of calcium in the plasma, 15-30 drops of Calciferol (Colecalciferol)a (about 10000-20000 ME of vitamin D) are prescribed3) per day. If a higher dose is required, it is recommended to take drugs with a higher dosage. The level of calcium in the blood and urine should be checked for 4-6 weeks, then every 3-6 months and adjust the dose in accordance with the normal content of calcium in the blood.