Complivit Aqua D3

GENERAL INFORMATION

Registration number:

Trade name of the drug:

Complivit® Aqua D3

International nonproprietary name:

Colecalciferol

Dosage form:

drops for oral administration

Description:

Colorless, transparent or slightly opalescent liquid with a characteristic odor.

Pharmacotherapeutic group:

Calcium-phosphorus metabolism regulator.

ATX Code:

A11СС05

Compound

for 1 ml:

Active substance:

colecalciferol (vitamin D3) - 0.375* mg (15,000 IU)

Excipients:

macrogol glyceryl ricinoleate - 75,000 mg; sucrose (white sugar) - 250,000 mg; sodium hydrogen phosphate dodecahydrate - 7,000 mg; citric acid (citric acid monohydrate) - 0.430 mg; anethole - 0.825 mg; benzyl alcohol - 15,000 mg; purified water to 1 ml.

* 1 mg of Colecalciferol corresponds to 40,000 IU of vitamin D3 activity.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics

Vitamin D3 is an active antirachitic factor. The most important function of vitamin D3 is to regulate calcium and phosphate metabolism, which promotes proper mineralization and skeletal growth. Vitamin D3 is a natural form of vitamin D that is formed in humans in the skin under the influence of sunlight. Compared to vitamin D2, it is characterized by 25% higher activity. Colecalciferol plays a significant role in the absorption of calcium and phosphates from the intestine, in the transport of mineral salts and in the process of bone calcification, and also regulates the excretion of calcium and phosphates by the kidneys. The concentration of calcium ions in the blood determines the maintenance of muscle tone of skeletal muscles, myocardial function, promotes nervous stimulation, and regulates the process of blood clotting. Vitamin D is necessary for the normal function of the parathyroid glands and is also involved in the functioning of the immune system, influencing the production of lymphokines. Lack of vitamin D in food, impaired absorption, calcium deficiency, as well as insufficient exposure to sunlight leads to: in children during a period of intensive growth - to rickets, in adults - to osteomalacia, in pregnant women symptoms of tetany may occur, in newborns - a disorder processes of bone tissue calcification. An increased need for vitamin D occurs in women during menopause due to the development of hormonal disorders leading to osteoporosis.

Pharmacokinetics.

An aqueous solution of vitamin D3 is absorbed better than an oil solution. In premature babies, there is insufficient formation and flow of bile into the intestines, which interferes with the absorption of vitamins in the form of oil solutions. After oral administration, colecalciferol is absorbed in the small intestine. Metabolized in the liver and kidneys. The half-life of colecalciferol from the blood is several days and may be prolonged in cases of renal failure. The drug penetrates the placental barrier and into mother's milk. Vitamin D3 has the property of cumulation. It is excreted from the body by the kidneys in small quantities, most of it is excreted in bile.

INDICATIONS FOR USE

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

Treatment of rickets.

Complex therapy of osteoporosis of various origins.

CONTRAINDICATIONS

Hypersensitivity to the components of the drug, especially benzyl alcohol. Sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption. Hypervitaminosis of vitamin D. Increased level of calcium in the blood (hypercalcemia), increased excretion of calcium in the urine (hypercalciuria), urolithiasis (formation of calcium oxalate stones), incl. history of renal osteodystrophy with hyperphosphatemia, pseudohypoparathyroidism. Sarcoidosis. Acute and chronic diseases of the liver and kidneys, renal failure. Active form of pulmonary tuberculosis. Children up to 4 weeks of age.

CAREFULLY

In patients in a state of immobilization. In patients taking thiazide diuretics, as well as in patients with cardiovascular diseases taking cardiac glycosides (see section "Interaction with other drugs"). During pregnancy and breastfeeding (see section “Use during pregnancy and breastfeeding”) In infants with a predisposition to early overgrowth of the fontanelles (when the small size of the anterior crown is established from birth). When taking additional amounts of vitamin D and calcium (for example, as part of other drugs), in case of impaired excretion of calcium and phosphate in the urine, during treatment with benzothiadiazine derivatives and in immobilized patients (risk of developing hypercalcemia and hypercalciuria) (see section Special instructions). In patients with the following concomitant diseases: atherosclerosis, heart failure, organic heart disease, granulomatosis, hyperphosphatemia, phosphate nephrolithiasis, gastrointestinal diseases, gastric and duodenal ulcers, hypothyroidism. If you have one or more of the listed diseases and conditions, you should consult your doctor before taking the drug.

USE IN PREGNANCY AND BREASTFEEDING

During pregnancy, the drug should not be used in doses exceeding those recommended for the prevention of vitamin D deficiency (see section “Method of administration and dosage”), due to the possibility of teratogenic effects in case of overdose. Vitamin D3 should be prescribed with caution in women who are breastfeeding, because a drug taken in high doses by the mother may cause overdose symptoms in the child. When using the drug during pregnancy and breastfeeding, 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 IU.

METHOD OF APPLICATION AND DOSES

Orally. The drug Complivit® Aqua D3 is taken orally in a spoonful of liquid. 1 drop contains about 500 IU of vitamin D3.

Prevention of rickets:

- full-term newborns from 4 weeks of life - 1 drop (500 IU) per day; - premature babies from 4 weeks of life - 2 drops (1000 IU) per day during the first year of life, then 1 drop (500 IU) per day. The drug should be used during the first two years of a child’s life, during periods of reduced insolation (especially in winter).

Treatment of rickets:

In the absence of visible deformations of the skeletal system (mild rickets) - 2-3 drops (1000-1500 IU) per day, continue treatment for 30 days. In the presence of deformations of the skeletal system, characteristic of moderate and severe rickets - 4-8 drops (2000-4000 IU) per day, continue treatment for 30-45 days, the dose of the drug and duration of therapy depend on the severity of the changes and are determined by the doctor ( see Special instructions).

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

1 drop (500 IU) per day during the entire period accompanied by a deficiency of vitamin D. The minimum duration of the course of prophylaxis is 1 month.

In complex treatment of osteoporosis:

1-2 drops (500-1000 IU) per day for 3 months. Repeated courses of therapy are possible on the recommendation of a doctor, depending on the results of assessing markers of bone metabolism and calcium metabolism (see Special instructions).

SIDE EFFECT

The frequency of adverse reactions has not been determined.

Metabolic and nutritional disorders: hypercalcemia and hypercalciuria.

Nervous system disorders: headache.

Cardiovascular system disorders: increased blood pressure, arrhythmias.

Disorders of the respiratory system, chest and mediastinal organs: exacerbation of the tuberculosis process in the lungs.

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

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

Musculoskeletal and connective tissue disorders: arthralgia, myalgia.

Renal and urinary tract disorders: renal dysfunction, polyuria.

If side effects occur, you should consult a doctor.

OVERDOSE

Symptoms of acute overdose of vitamin D3:
early manifestations
(due to hypercalcemia) - constipation or diarrhea, dry oral mucosa, headache, thirst, pollakiuria, nocturia, polyuria, anorexia, metallic taste in the mouth, nausea, vomiting, general weakness and fatigue, hypercalcemia, hypercalciuria, dehydration;
late manifestations
- bone pain, cloudiness of urine (appearance of hyaline casts in the urine, proteinuria, leukocyturia), increased blood pressure, skin itching, photosensitivity of the eyes, conjunctival hyperemia, arrhythmia, drowsiness, myalgia, nausea, vomiting, pancreatitis, gastralgia, weight loss, rarely - psychosis (mental changes) and mood changes.
Symptoms of chronic overdose of vitamin D3
(when taken for several weeks or months for adults in doses of 20000-60000 IU / day, children - 2000-4000 IU / day): calcification of soft tissues, kidneys, lungs, blood vessels, arterial hypertension, renal and chronic heart failure (these effects most often occur when hyperphosphatemia is added to hypercalcemia), growth impairment in children (long-term use at a dose of 1800 IU/day).
Treatment:
If the above symptoms appear, you should stop using the drug and consult a doctor. A diet low in calcium (for several weeks), consumption of large amounts of fluid, forced diuresis using furosemide, electrolytes, as well as the administration of glucocorticosteroids and calcitonin are indicated. If the kidneys are functioning properly, calcium levels can be significantly reduced by infusion of isotonic sodium chloride solution (3-6 liters over 24 hours) with the addition of furosemide and, in some cases, also sodium edetate at a dose of 15 mg/kg/hour, while constantly monitoring calcium levels and electrocardiogram data. With oligoanuria, on the contrary, hemodialysis (dialysate without calcium) is necessary. A specific antidote is unknown.

To prevent overdose, in some cases it is recommended to monitor the concentration of calcium in the blood.

INTERACTION WITH OTHER MEDICINES

Antiepileptic drugs (especially phenytoin and phenobarbital, primidone), rifampicin, cholestyramine reduce the reabsorption of vitamin D3. Use simultaneously with thiazide diuretics increases the risk of developing hypercalcemia. In such cases, it is necessary to constantly monitor the concentration of calcium in the blood. With hypervitaminosis D3, it is possible to enhance the effect of cardiac glycosides and increase the risk of arrhythmia due to the development of hypercalcemia (monitoring the concentration of calcium in the blood, an electrocardiogram, as well as adjusting the dose of cardiac glycoside are advisable). Concomitant therapy with glucocorticosteroids may reduce the effectiveness of vitamin D3. Long-term use of antacids containing aluminum and magnesium in combination with vitamin D3 may contribute to an increase in the concentration of aluminum and magnesium in the blood and, as a result, to the toxic effect of aluminum on bone tissue and hypermagnesemia in patients with renal failure. Cholestyramine, colestipol and mineral oils reduce the absorption of fat-soluble vitamins in the gastrointestinal tract and require an increase in their dose. Concomitant use of benzodiazepines increases the risk of hypercalcemia. Drugs containing high concentrations of calcium and phosphorus increase the risk of developing hyperphosphatemia. When used simultaneously 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 vitamin D analogues increases the risk of developing vitamin D hypervitaminosis. Ketoconazole can inhibit both the biosynthesis and catabolism of 1,25(OH)2-colecalciferol. Vitamin D is an antagonist of drugs used for hypercalcemia: calcitonin, etidronate, pamidronate, plicamycin, gallium nitrate. Isoniazid and rifampicin can reduce the effect of the drug due to an increase in the rate of biotransformation. Vitamin D3 does not interact with food.

SPECIAL INSTRUCTIONS

Avoid overdose. When taking the drug, the amount of vitamin D and calcium obtained from food and other medications should be taken into account. Too high doses of vitamin D3, used over a long period of time, or shock doses can cause chronic hypervitaminosis D3. High doses of calcium should not be taken at the same time as vitamin D3. The drug should be used with caution in patients with impaired urinary excretion of calcium and phosphate, during treatment with benzothiadiazine derivatives and in immobilized patients (risk of developing hypercalcemia and hypercalciuria). In such patients, calcium levels in the blood plasma and urine should be monitored. Vitamin D3 should not be taken if you have pseudohypoparathyroidism, as in this disease the need for vitamin D may be reduced, which may lead to a risk of long-term overdose. The main clinical manifestations of mild rickets include nervous excitability, anxiety, flinching at a sharp sound, a flash of light, sleep rhythm disturbances, superficial “anxious” sleep, sweating, itchy skin, baldness of the back of the head, pliability of the edges of the large fontanel. The presence of visible deformations of bone tissue is characteristic of moderate and severe rickets, which, as a rule, require hospitalization and complex therapy prescribed by a doctor based on the results of the examination. Repeated courses of therapy for osteoporosis are possible on the recommendation of a doctor, depending on the results of assessing markers of bone metabolism and calcium metabolism. If the doctor has prescribed a longer treatment than recommended in the instructions, then you should regularly (every three months of therapy) determine the level of calcium in the blood serum and urine, and also assess kidney function by measuring the level of creatinine in the blood serum. If necessary, the dose can be adjusted by the doctor according to the level of calcium in the blood serum. In case of hypercalcemia or signs of renal impairment, the dose of the drug should be reduced or treatment should be suspended. If the level of calcium in the urine exceeds 7.5 mmol/24 hours (300 mg/24 hours), it is recommended to reduce the dose of the drug or suspend treatment.

INFLUENCE ON THE ABILITY TO DRIVE VEHICLES AND MECHANISMS

There are no data on the possible effect of the drug on the ability to drive vehicles and machines.

RELEASE FORM

Drops for oral administration, 15000 IU/ml.

10 ml and 20 ml in dropper bottles made of dark (amber) glass, sealed with polyethylene dropper stoppers and plastic caps with first opening control.

One dropper bottle along with instructions for use is placed in a cardboard pack.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

BEST BEFORE DATE

2 years.

Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies

Over the counter.

MANUFACTURER INFORMATION

Manufacturer's name and address:

OJSC Pharmstandard-Leksredstva,

305022, Russia, Kursk, st. 2nd Aggregatnaya, 1a/18, tel./fax: (4712) 34-03-13

www.pharmstd.ru

Marketing authorization holder/organization receiving consumer complaints:

OTCPharm JSC, Russia, 123317, Moscow, st. Testovskaya, 10

Tel.

Fax

www.otcpharm.ru

Complivit Aqua D3 bottle-drops (drops for oral administration) 15000 IU/ml 20ml Pharmstandard-Leksredstva/Russia

Dosage form

Colorless, transparent or slightly opalescent liquid with a characteristic odor.
Composition
Composition per 1 ml: Active ingredient: colecalciferol (vitamin D3) - 0.375* mg (15000 IU); Excipients: macrogol glyceryl ricinoleate - 75,000 mg; sucrose (white sugar) - 250,000 mg; sodium hydrogen phosphate dodecahydrate - 7,000 mg; citric acid (citric acid monohydrate) - 0.430 mg; anethole - 0.825 mg; benzyl alcohol - 15,000 mg; purified water to 1 ml. * 1 mg of Colecalciferol corresponds to 40,000 IU of vitamin D3 activity.

Special conditions

Drug interactions

Pharmacodynamics

Vitamin D3 is a natural form of vitamin D that is formed in humans in the skin under the influence of sunlight. Compared to vitamin D2, it is characterized by 25% higher activity. Vitamin D binds to the specific vitamin D receptor (VDR), which regulates the expression of many genes, including the ion channel genes TRPV6 (ensures the absorption of calcium in the intestine), CALB1 (calbindin; ensures the transport of calcium into the bloodstream), BGLAP (osteo-calcine) ; ensures bone tissue mineralization and calcium homeostasis), SPP1 (osteopontin; regulates osteoclast migration), REN (renin; ensures regulation of blood pressure, being a key element of the renin-angiotensin-aldosterone regulatory system), IGFBP (insulin-like growth factor binding protein; enhances the effect insulin-like growth factor), FGF23 (fibroblast growth factor 23; regulates the levels of calcium, phosphate anion, processes of cell division of fibroblasts), TGFB1 (transforming growth factor beta-1; regulates the processes of cell division and differentiation of osteocytes, chondrocytes, fibroblasts and keratinocytes), LRP2 (LDL receptor-related protein 2; mediates the endocytosis of low-density lipoproteins), INSR (insulin receptor; ensures the effects of insulin on any cell type). Vitamin D3 is an active antirachitic factor. The most important function of vitamin D3 is to regulate calcium and phosphate metabolism, which promotes proper mineralization and skeletal growth. Colecalciferol plays a significant role in the absorption of calcium and phosphates from the intestine, in the transport of mineral salts and in the process of bone calcification, and also regulates the excretion of calcium and phosphates by the kidneys. The concentration of calcium ions in the blood determines the maintenance of muscle tone of skeletal muscles, myocardial function, promotes nervous stimulation, and regulates the process of blood clotting. Lack of vitamin D in food, impaired absorption, calcium deficiency, as well as insufficient exposure to the sun leads to: in children during periods of intensive growth - to rickets, in adults - to osteomalacia, in pregnant women, symptoms of tetany may occur - disruption of the processes calcification of newborn bones. An increased need for vitamin D occurs in women during menopause, as they often develop osteoporosis due to hormonal imbalances. Vitamin D has a number of so-called. extraskeletal effects. Vitamin D is involved in the functioning of the immune system by modulating cytokine levels and regulating the division of T-helper lymphocytes and the differentiation of B-lymphocytes. A number of studies have noted a decrease in the incidence of respiratory tract infections when taking vitamin D. It has been shown that vitamin D is an important part of the homeostasis of the immune system: it prevents autoimmune diseases (type 1 diabetes, multiple sclerosis, rheumatoid arthritis, inflammatory bowel diseases, etc.). Vitamin D has antiproliferative and prodifferentiating effects, which determine the oncoprotective effect of vitamin D. It has been noted that the incidence of certain 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 (insulin receptor substrate 1; participates in the intracellular pathways of the insulin receptor signal), IGF (insulin-like growth factor; regulates the balance of adipose and muscle tissue), PPAR-? (activated peroxisome proliferator receptor type ?; helps process 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 relevant to the pathogenesis of cardiovascular disease. Animal models show anti-atherosclerotic effects, renin suppression and prevention of myocardial damage, etc. Low levels of vitamin D in humans are associated with unfavorable risk factors for cardiovascular pathology, such as diabetes mellitus, dyslipidemia, arterial hypertension, and are associated with the risk of cardiovascular accidents , incl. strokes. Studies in experimental models of Alzheimer's disease showed that vitamin D3 reduced amyloid accumulation in the brain and improved cognitive function. Non-interventional human studies have shown that the incidence of dementia and Alzheimer's disease increases with low vitamin D levels and low dietary intake of vitamin D. Cognitive function and the incidence of Alzheimer's disease have been impaired with low vitamin D levels.

Pharmakinetics

Indications

Prevention of vitamin D deficiency and diseases associated with its deficiency (rickets, osteomalacia). Treatment of rickets. Complex therapy of osteoporosis of various origins.

Contraindications

Carefully

Use during pregnancy and breastfeeding

Overdose

Symptoms of acute overdose of vitamin D3: early manifestations (due to hypercalcemia) - constipation or diarrhea, dry oral mucosa, headache, thirst, pollakiuria, nocturia, polyuria, anorexia, metallic taste in the mouth, nausea, vomiting, general weakness and fatigue, hypercalcemia, hypercalciuria, dehydration; late manifestations - bone pain, cloudiness of urine (appearance of hyaline casts in the urine, proteinuria, leukocyturia), increased blood pressure, skin itching, photosensitivity of the eyes, conjunctival hyperemia, arrhythmia, drowsiness, myalgia, nausea, vomiting, pancreatitis, gastralgia, weight loss, rarely - psychosis (mental changes) and mood changes. Symptoms of chronic overdose of vitamin D3 (when taken for several weeks or months for adults in doses of 20000-60000 IU / day, children - 2000-4000 IU / day): calcification of soft tissues, kidneys, lungs, blood vessels, arterial hypertension, renal and chronic heart failure (these effects most often occur when hyperphosphatemia is added to hypercalcemia), growth impairment in children (long-term use at a dose of 1800 IU/day). Treatment: If the above symptoms appear, you should stop using the drug and consult a doctor. A diet with a low calcium content (for several weeks), consumption of large amounts of fluid, formed diuresis using furosemide, electrolytes, as well as the administration of glucocorticosteroids and calcitonin are indicated. If the kidneys are functioning properly, calcium levels can be significantly reduced by infusion of isotonic sodium chloride solution (3-6 liters over 24 hours) with the addition of furosemide and, in some cases, also sodium edetate at a dose of 15 mg/kg/hour, while constantly monitoring calcium levels and electrocardiogram data. With oligoanuria, on the contrary, hemodialysis (dialysate without calcium) is necessary. A specific antidote is unknown. To prevent overdose, in some cases it is recommended to monitor the concentration of calcium in the blood.

Side effects

The frequency of adverse reactions has not been determined. Metabolic and nutritional disorders: hypercalcemia and hypercalciuria. Nervous system disorders: headache. Cardiovascular system disorders: increased blood pressure, arrhythmias. Disorders of the respiratory system, chest and mediastinal organs: exacerbation of the tuberculosis process in the lungs. Gastrointestinal disorders: decreased appetite, constipation, flatulence, nausea, abdominal pain or diarrhea. Skin and subcutaneous tissue disorders: hypersensitivity reactions such as itching, skin rash and urticaria. Musculoskeletal and connective tissue disorders: arthralgia, myalgia. Renal and urinary tract disorders: renal dysfunction, polyuria. If side effects occur, you should consult a doctor.

Dosage

Orally. The drug Complivit® Aqua D3 is taken orally in a spoonful of liquid. 1 drop contains about 500 IU of vitamin D3.

Prevention of rickets:

Treatment of rickets:

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

1 drop (500 IU) per day during the entire period accompanied by a deficiency of vitamin D. The minimum duration of the course of prophylaxis is 1 month.

In complex treatment of osteoporosis: