DeTriFerol banana flavored drops 15000 me/ml 15 ml

Vitamin D and its analogues.

ATX code: A11CC05 Pharmacological properties

Pharmacodynamics

Vitamin D3 is a natural form of vitamin D, which is formed in human skin under the action of sunlight. Compared to vitamin D2, it has 25% higher activity.

Vitamin D3 is an active anti-rachitis factor. The most important function of vitamin D3 is to regulate calcium and phosphate metabolism, which promotes proper mineralization and skeletal growth.

Calciferol plays an essential role in the absorption of calcium and phosphate in the intestine, in the transport of mineral salts and in the calcification of bones, and also regulates the excretion of calcium and phosphate by the kidneys.

The concentration of calcium ions in blood determines the muscle tone of skeletal muscles, myocardial function, contributes to nerve stimulation and regulates the process of blood clotting.

Deficiency of vitamin D in food, disorders of its absorption, calcium deficiency, as well as lack of exposure to the sun during rapid growth of children leads to rickets, osteomalacia in adults, pregnant women may show symptoms of tetany, disruption of bone calcification in newborns.

The 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 extracellular 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.

It is shown that vitamin D is an important link in homeostasis of the immune system: it prevents autoimmune diseases (diabetes mellitus type 1, multiple sclerosis, rheumatoid arthritis, inflammatory bowel diseases, etc.).

Vitamin D has antiproliferative and pro-differentiation effects, which determine the oncoprotective effect of vitamin D. It is noted that the incidence of some tumors (breast cancer, colon cancer) is increased with low levels of vitamin D in the blood.

Vitamin D is involved in the regulation of carbohydrate and fat metabolism by affecting the synthesis of IRS1 (insulin receptor substrate 1; involved in intracellular pathways of insulin receptor signaling), IGF (insulin-like growth factor; regulates the balance of adipose and muscle tissue), PPAR-σ (Peroxisome proliferator activated receptor type σ; promotes recycling of excess cholesterol).

According to epidemiological studies, vitamin D deficiency is associated with the risk of metabolic disorders (metabolic syndrome and type 2 diabetes). Vitamin D receptors and metabolizing enzymes are expressed in arterial vessels, the heart and virtually all cells and tissues relevant to the pathogenesis of cardiovascular disease. Antiatherosclerotic effects, renin suppression and prevention of myocardial damage, etc., have been shown in animal models. Low levels of vitamin D in humans are associated with adverse cardiovascular risk factors such as diabetes, dyslipidemia, arterial hypertension, and are associated with the risk of cardiovascular accidents, including strokes.

In studies in experimental models of Alzheimer’s disease, vitamin D3 has been shown to reduce amyloid accumulation in the brain and improve cognitive function. In non-interventional studies in humans, the incidence of dementia and Alzheimer’s disease has been shown to increase with low vitamin D levels and low dietary intake of vitamin D. There has been a worsening of cognitive function and the incidence of Alzheimer’s disease at low levels of vitamin D.

Pharmacokinetics

Intake.

The aqueous solution of colecalciferol is absorbed better than the oil solution (this is important when used in premature infants, since this category of patients has insufficient production and intestinal intake of bile, which impairs absorption of vitamins in the form of oil solutions).

After oral administration colocalciferol is quickly absorbed from the distal small intestine, enters the lymphatic system, enters the liver and the general bloodstream.

Distribution.

In the blood it binds with α2-globulins and partially with albumin. Colecalciferol accumulates in the liver, bones, skeletal muscles, kidneys, adrenal glands, myocardium, adipose tissue. The maximum concentration in tissues is reached after 4-5 hours, after that it decreases slightly, remaining at a constant level for a long time. Cumulative. It penetrates through the placental barrier and into the breast milk.

Metabolism.

Biotransformation occurs in the liver and kidneys: In the liver, colecalciferol is converted to the inactive metabolite calcifediol (25-dihydrocolecalciferol); in the kidneys, it is converted from calcifediol to the active metabolite calcitriol (1,25-dihydroxycolecalciferol) and the inactive metabolite 24,25-dihydroxycolecalciferol. It is subject to intestinal-hepatic recirculation.

Elimination.

The drug is excreted mainly with the bile and a small amount with the kidneys.

Indications

Prevention of rickets Preventing vitamin D deficiency and diseases associated with its insufficiency (rickets, osteomalacia).

Treatment of rickets.

Complex therapy for osteoporosis of different genesis.

Active ingredient

Colecalciferol

Composition

1 ml of the drug contains:

Active ingredient:

Colocalciferol 15000 IU (0.375 mg)

Excipients:

Propylene glycol 100 mg

Macrogol glyceryl hydroxystearate 50 mg

Methyl parahydroxybenzoate 1.0 mg

Sodium saccharinate 0.7 mg

How to take, the dosage

Orally.

The drug is taken in a spoonful of liquid. 1 drop contains about 500 ME of vitamin D3.

Prophylaxis of rickets:

Infants from 4 weeks of life, 1 drop (500 ME) per day;

Infants from 4 weeks of life, 2 drops (1000 ME) per day for the first year of life, then 1 drop (500 ME) per day.

The drug should be used during the first two years of the child’s life, during periods of low insolation (especially in winter).

The treatment of rickets:

In the absence of visible deformities of the bones (mild rickets) – 2-3 drops (1000-1500 ME) a day, the treatment should be continued for 30 days.

In case of visible deformities of the bones system typical for moderate and severe rickets 4-8 drops (2000-4000 ME) a day, the treatment should be continued for 30-45 days; the dose of the preparation and the duration of therapy depend on the intensity of the changes and are determined by the doctor.

Prevention of vitamin D deficiency and diseases associated with its insufficiency (osteomalacia):

1 drop (500 ME) per day for the duration of the period accompanied by vitamin D intake deficiency. The minimum duration of prophylaxis is 1 month.

In the complex treatment of osteoporosis:

1 to 2 drops (500-1000 ME) per day for 3 months. Repeated courses of therapy are possible upon a physician’s recommendation, depending on the results of the evaluation of markers of bone metabolism and calcium metabolism.

Interaction

Antiepileptic drugs (especially phenytoin and phenobarbital, primidone), rifampicin, colestiramine reduce reabsorption of vitamin D3.

Simultaneous use with thiazide diuretics increases the risk of hypercalcemia. In these cases the calcium concentration in blood should be continuously monitored.

In hypervitaminosis of vitamin D3 the enhancement of cardiac glycosides action and the increase of risk of arrhythmia caused by hypercalcemia are possible (it is reasonable to monitor the calcium concentration in blood and electrocardiogram, and also to correct the cardiac glycoside dose.)

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

Prolonged use of antacids containing aluminum and magnesium in combination with vitamin D3 may increase the concentration of aluminum and magnesium in the blood and, consequently, the toxic effects of aluminum on bone tissue and hypermagnesemia in patients with renal insufficiency.

Colestiramine, colestipol and mineral oils reduce absorption in the gastrointestinal tract of fat-soluble vitamins and require increasing their dose.

Concomitant use of benzodiazepines increases the risk of hypercalcemia.

Drugs containing high concentrations of calcium and phosphorus increase the risk of hyperphosphatemia.

In concomitant use with sodium fluoride the interval between doses should be at least 2 hours; with oral forms of tetracyclines – at least 3 hours.

Concomitant use with other analogues of vitamin D increases the risk of vitamin D hypervitaminosis.

Ketoconazole may inhibit both biosynthesis and catabolism of 1,25(OH)2-calciferol.

Vitamin D is an antagonist of drugs used in hypercalcemia: calcitonin, etidronate, pamidronate, plikamycin, gallium nitrate.

Isoniazid and rifampicin can reduce the effect of the drug due to increased rate of biotransformation.

Vitamin D3 does not interact with food.

Special Instructions

Avoid overdose.

The amount of vitamin D and calcium taken with food and other medications must be taken into account when taking the drug.

High doses of vitamin D3 used for prolonged periods or shock doses can cause chronic hypervitaminosis of D3.
High doses of calcium should not be used at the same time as vitamin D3.

The drug should be used with caution in patients with impaired urinary calcium and phosphate excretion, during treatment with benzothiadiazine derivatives and in immobilized patients (risk of hypercalcemia and hypercalciuria). In these patients the calcium concentration in plasma and urine should be monitored.

Vitamin D3 should not be taken in pseudohypoparathyroidism because in this disease the vitamin D requirement may be reduced, which could lead to the risk of long-term overdose.

The main clinical manifestations of mild rickets include nervous excitability, restlessness, flinching at sudden sounds, flash of light, sleep disturbances, superficial “anxious” sleep, sweating, itchy skin, baldness of the back of the head, and suppleness of the edges of the great fontanelle.
The presence of visible bone deformities is characteristic of moderate and severe rickets which, as a rule, require hospitalization and complex therapy prescribed by a physician based on the results of the examination.

Recurrent courses of therapy for osteoporosis may be possible on the recommendation of the doctor, depending on the results of the assessment of bone and calcium metabolism markers. If the physician prescribed longer treatment than recommended in the instructions, the calcium concentration in serum and urine should be determined regularly (every three months of therapy), and renal function should be evaluated by measuring serum creatinine concentration.

If necessary, the dose can be adjusted by the physician according to the serum calcium concentration.

In case of hypercalcemia or signs of renal dysfunction, the dose should be reduced or the treatment should be stopped. If urinary calcium concentration exceeds 7.5 mmol/24 h (300 mg/24 h), it is recommended to reduce the dose of the drug or suspend treatment.

Influence on driving and operating ability

There are no data on possible effect of the drug on driving and operating ability.

Contraindications

• Hypersensitivity to colocalciferol and/or to any of the excipients in the drug.
• Vitamin D hypervitaminosis.
• Acute and chronic liver and kidney disease, renal failure.
• Active form of pulmonary tuberculosis.
• Children under 4 weeks.

Cautious

• In immobilized patients.
• In patients taking thiazide diuretics, and in patients with cardiovascular disease taking cardiac glycosides.
• In pregnancy and breastfeeding.
• In patients with the following comorbidities: atherosclerosis, heart failure, organic heart disease, granulomatosis, hyperphosphatemia, phosphate nephrourolithiasis, gastrointestinal diseases, peptic ulcer, hypothyroidism.
• If one or more of the above diseases and conditions are present, consult a physician before taking the drug

.

Side effects

The frequency of adverse reactions has not been determined.

Metabolism and nutrition disorders: hypercalcemia and hypercalciuria, decreased appetite.

Nervous system disorders: headache.

Cardiac disorders: arrhythmias.

Vascular disorders: increase in blood pressure.

Respiratory system, chest and mediastinum disorders: exacerbation of tuberculosis in the lungs.

Gastrointestinal disorders: constipation, flatulence, nausea, abdominal pain or diarrhea.

Skin and subcutaneous tissue disorders: hypersensitivity reactions such as itching, skin rash and urticaria.

Muscular and connective tissue disorders: arthralgia, myalgia.

Renal and urinary tract disorders: renal dysfunction, polyuria.

In case of adverse reactions, a physician should be consulted.

Overdose

Symptoms of acute vitamin D3 overdose:

• .Early manifestations (due to hypercalcemia) – constipation or diarrhea, dry mouth, headache, thirst, Pollakiuria, nycturia, polyuria, anorexia, metallic taste in the mouth, nausea, vomiting, general weakness and fatigue, hypercalcemia, hypercalciuria, dehydration;
• Symptoms of chronic vitamin D3 overdose (when taken for several weeks or months for adults at doses of 20000-60000 IU/day, children 2000-4000 IU/day): Calcinosis of soft tissues, kidneys, lungs, blood vessels, arterial hypertension, renal and chronic heart failure (these effects most often occur when hypercalcemia is joined with hyperphosphatemia), growth disorder in children (long-term administration at a dose of 1800 IU/day).

Treatment: If the above symptoms occur, discontinue the drug and consult a physician. Low-calcium diet (for several weeks), large fluid intake, forced diuresis with furosemide, electrolytes, and administration of glucocorticosteroids, calcitonin are indicated.

With proper renal function, plasma calcium concentration can be significantly reduced by infusion of isotonic sodium chloride solution (3-6 liters for 24 hours) with furosemide and, in some cases, also sodium edetate at a dose of 15 mg/kg/h, while continuous monitoring of plasma calcium concentration and electrocardiogram data. In contrast, hemodialysis (dialysate without calcium) is necessary in oligoanuria. A specific antidote is not known.

To prevent overdose, blood calcium concentration control is recommended in some cases.

Pregnancy use

During pregnancy the drug should not be used in doses greater than those recommended for the prevention of vitamin D deficiency because of the possibility of teratogenic action in case of overdose.

Vitamin D3 should be administered with caution to women during breast-feeding as the drug taken in high doses by the mother may cause symptoms of overdose in the child.

In the case of the drug during pregnancy and lactation it is necessary to take into account the intake of vitamin D from other sources, the daily dose of vitamin D should not exceed 600 ME.

Similarities

Vigantol, Aquadetrim (Vitamin D3), Univit Energy, Fortedetrim