Fortedetrim capsules 10000ME, No. 30

Treatment and prevention of vitamin D deficiency and deficiency and conditions caused by vitamin D deficiency in adults.

The capsules should be taken orally, swallowed whole and washed down with water, preferably during the main meal.

Capsules 2000 ME and 4000 ME

• Treatment of vitamin D deficiency (25 (OH) D level? 20 ng / ml) in adults - 8000 ME (4 capsules 2000 ME or 2 capsules 4000 ME) per day for 8 weeks,

• Treatment of vitamin D deficiency (25 (OH) D level - 20-29 ng / ml) in adults - 8000 ME (4 capsules 2000 ME or 2 capsules 4000 ME) per day for 4 weeks,

• Maintaining a normal level of vitamin D (level 25 (OH) D? 30 ng / ml) in adults - 2000 ME (1 capsule) per day.

Capsules 10000 ME

• Treatment of vitamin D deficiency (25 (OH) D level? 20 ng / ml) in adults - 50,000 ME (5 capsules 10,000 ME) once a week for 8 weeks,

• Treatment of vitamin D deficiency (25 (OH) D level - 20-29 ng / ml) in adults - 50,000 ME (5 capsules 10,000 ME) once a week for 4 weeks,

• Maintaining a normal level of vitamin D (25 (OH) D level? 30 ng / ml) in an adult - 10,000 ME (1 capsule) once a week.

With long-term treatment, you should regularly determine the concentration of calcium in the blood and urine, as well as determine the function of the kidneys by measuring the serum creatinine concentration. If necessary, the dose should be adjusted based on the serum calcium concentration.

Liver disease

No dose adjustment is required.

Impaired renal function

The drug should not be administered to patients with severe renal impairment.

Active ingredient: colecalciferol 10000 ME (0.25 mg);
Excipients: refined safflower oil;
capsule: gelatin, glycerol, purified water.

• Hypersensitivity to the active substance or any of the excipients listed in the 'Composition' section;

• Hypercalcemia and / or hypercalciuria;

• Urolithiasis (the formation of calcium oxalate stones);

• Hypervitaminosis D;

• Pseudohypoparathyroidism;

• Sarcoidosis

• Active form of pulmonary tuberculosis;

• Severe renal failure;

• Pregnancy and the period of breastfeeding (at these dosages);

• Children under the age of 18.

Carefully

Taking additional amounts of colecalciferol and calcium (for example, as part of other drugs), in case of violations of calcium and phosphate excretion in the urine, in the treatment of immobilized patients, while taking thiazides, cardiac glycosides (especially digitalis glycosides), benzothiadiazine derivatives, in patients with atherosclerosis.

Trade name of the drug:

Fortedetrim

International non-proprietary name:

colecalciferol

Dosage form:

capsules

Composition

1 capsule (2000 ME) contains:
active substance: colecalciferol 2000 ME (0.05 mg);
excipients: refined safflower oil;
capsule: gelatin, glycerol, purified water.

1 capsule (4000 ME) contains:
active substance: colecalciferol 4000 ME (0.10 mg);
excipients: refined safflower oil;
capsule: gelatin, glycerol, purified water.

1 capsule (10,000 ME) contains:
active ingredient: colecalciferol 10,000 ME (0.25 mg);
excipients: refined safflower oil;
capsule: gelatin, glycerol, purified water.

Description

Oval soft gelatin capsules of light yellow color with a seam, filled with a transparent light yellow liquid.

Pharmacotherapeutic group:

Calcium-phosphorus metabolism regulator.

ATX code:

A11CC05

Pharmacological properties

Pharmacodynamics

Vitamin D3 is a natural form of vitamin D that is produced in human skin by exposure to sunlight. Compared to vitamin D2, it is characterized by 25% higher activity.

Vitamin D binds to a specific vitamin D receptor (VDR), which regulates the expression of many genes, including the TRPV6 ion channel genes (provides for the absorption of calcium in the intestine), CALB1 (calbindin; provides calcium transport into the bloodstream), BGLAP (osteocalcin; provides bone mineralization tissue and calcium homeostasis), SPP1 (osteopontin; regulates the migration of osteoclasts), REN (renin; regulates blood pressure, being a key element of the renin-angiotensin-aldosterone regulation system), IGFBP (binding protein insulin-like growth factor; enhances the action of insulin-like growth factor) , FGF23 and FGFR23 (fibroblast growth factor 23; regulate calcium, phosphate anion levels, fibroblast cell division), TGFB1 (transforming growth factor beta-1;regulates the processes of cell division and differentiation of osteocytes, chondrocytes, fibroblasts and keratinocytes), LRP2 (LDL-receptor-associated protein 2; mediates endocytosis of low-density lipoproteins), INSR (insulin receptor; ensures the effects of insulin on all types of cells).

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

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

The concentration of calcium ions in the blood determines the maintenance of muscle tone in the skeletal muscles, myocardial function, promotes the conduction of nervous excitement, and regulates the blood coagulation process.

Lack of vitamin D in food, impaired absorption, calcium deficiency, as well as insufficient exposure to the sun during the period of rapid growth of the child leads to rickets, in adults - to osteomalacia, pregnant women may experience symptoms of tetany, impaired 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. non-skeletal effects.

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

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

Vitamin D has antiproliferative and differentiating effects, which determine the oncoprotective effect of vitamin D. It has been noted that the incidence of some tumors (breast cancer, colon cancer) increases with a low level 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 insulin receptor 1; participates in the intracellular pathways of insulin receptor signaling), IGF (insulin-like growth factor; regulates the balance of adipose and muscle tissue), PPAR-? (activated receptor of peroxisome proliferators, type?; 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, heart and practically all cells and tissues related to the pathogenesis of cardiovascular diseases. In animal models, anti-atherosclerotic action, renin suppression and prevention of myocardial damage have been shown. 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 catastrophes. , including strokes. Studies in experimental models of Alzheimer's disease have shownthat vitamin D3 reduced the accumulation of amyloid in the brain and improved cognitive function. Non-interventional studies in humans have shown that the incidence of dementia and Alzheimer's disease increases with low vitamin D levels and low dietary vitamin D intake. Cognitive function and Alzheimer's disease have been impaired with low vitamin D levels.

Pharmacokinetics

Suction

Colecalciferol (vitamin D3), when taken orally, is almost completely absorbed (80%) in the small intestine. The maximum concentration in the tissues is reached after 4-5 hours, after which the concentration decreases slightly, remaining at a constant level for a long time. After a single oral administration of cholecalciferol, the maximum serum concentration of the main form is reached after about 7 days.

Distribution

Colecalciferol accumulates in the liver, bones, skeletal muscles, kidneys, adrenal glands, myocardium, adipose tissue. The maximum concentration in the tissues is reached after 4-5 hours, after which the concentration decreases slightly, remaining at a constant level for a long time. Undergoes enterohepatic recirculation. The serum concentration of the inactive metabolite 25-hydroxycalciferol (25 (OH) D3, calcidiol) can be increased for several months after taking large doses of cholecalciferol. Overdose-induced hypercalcemia can persist for several weeks.

Metabolism

Colecalciferol in blood plasma binds to alpha-2-globulins and partially to albumin and is transported to the liver, where microsomal hydroxylation occurs with the formation of an inactive metabolite of 25-hydroxycalciferol (25 (OH) D3, calcidiol). The concentration of circulating calcidiol in the blood is an indicator of the level of vitamin D in the body. Calcidiol undergoes repeated hydroxylation in the kidneys to form the dominant active metabolite of 1,25-hydroxycolecalciferol (l, 25 (OH) 2D3, calcitriol).

Elimination

25 (OH) D3 is slowly excreted with an elimination half-life of about 50 days. The main way of excretion of colecalciferol, as well as its metabolites, is bile (feces), and at least 2% of these substances are excreted at night. Colecalciferol crosses the placental barrier and enters breast milk.

Indications for use

Treatment and prevention of vitamin D deficiency and deficiency and conditions caused by vitamin D deficiency in adults.

Contraindications

• Hypersensitivity to the active substance or any of the excipients listed in the 'Composition' section;

• Hypercalcemia and / or hypercalciuria;

• Urolithiasis (the formation of calcium oxalate stones);

• Hypervitaminosis D;

• Pseudohypoparathyroidism;

• Sarcoidosis

• Active form of pulmonary tuberculosis;

• Severe renal failure;

• Pregnancy and the period of breastfeeding (at these dosages);

• Children under the age of 18.

Carefully

Taking additional amounts of colecalciferol and calcium (for example, as part of other drugs), in case of violations of calcium and phosphate excretion in the urine, in the treatment of immobilized patients, while taking thiazides, cardiac glycosides (especially digitalis glycosides), benzothiadiazine derivatives, in patients with atherosclerosis.

Application during pregnancy and during breastfeeding

The use of the drug Fortedetrim during pregnancy and breastfeeding is not recommended at these dosages due to the excess of the recommended daily dose of 1000 IU. During pregnancy and during breastfeeding, the use of cholecalciferol preparations in lower doses is recommended, for example, Aquadetrim.

Method of administration and dosage:

The capsules should be taken orally, swallowed whole and washed down with water, preferably during the main meal.

Capsules 2000 ME and 4000 ME

• Treatment of vitamin D deficiency (25 (OH) D level? 20 ng / ml) in adults - 8000 ME (4 capsules 2000 ME or 2 capsules 4000 ME) per day for 8 weeks,

• Treatment of vitamin D deficiency (25 (OH) D level - 20-29 ng / ml) in adults - 8000 ME (4 capsules 2000 ME or 2 capsules 4000 ME) per day for 4 weeks,

• Maintaining a normal level of vitamin D (level 25 (OH) D? 30 ng / ml) in adults - 2000 ME (1 capsule) per day.

Capsules 10000 ME

• Treatment of vitamin D deficiency (25 (OH) D level? 20 ng / ml) in adults - 50,000 ME (5 capsules 10,000 ME) once a week for 8 weeks,

• Treatment of vitamin D deficiency (25 (OH) D level - 20-29 ng / ml) in adults - 50,000 ME (5 capsules 10,000 ME) once a week for 4 weeks,

• Maintaining a normal level of vitamin D (25 (OH) D level? 30 ng / ml) in an adult - 10,000 ME (1 capsule) once a week.

With long-term treatment, you should regularly determine the concentration of calcium in the blood and urine, as well as determine the function of the kidneys by measuring the serum creatinine concentration. If necessary, the dose should be adjusted based on the serum calcium concentration.

Liver disease

No dose adjustment is required.

Impaired renal function

The drug should not be administered to patients with severe renal impairment.

Overdose

Symptoms

The intoxication threshold for colecalciferol varies between 40,000 and 100,000 IU per day for 1-2 months in adults with normal parathyroid function. Newborns and young children may be sensitive to much lower concentrations.

Acute and chronic overdose can lead to increased serum and urine phosphorus levels and hypercalcemia, which can be persistent and potentially life-threatening.

Typical changes in biochemical parameters include hypercalcemia, hypercalciuria, and increased serum levels of 25-hydroxycalciferol (25 (OH) D3, calcidiol). Chronic overdose of cholecalciferol can lead to calcium deposition in tissues and parenchymal organs, primarily in the kidneys (urolithiasis, nephrocalcinosis) and blood vessels.

Symptoms are general and manifest as nausea, vomiting, also initially as diarrhea, later as constipation, loss of appetite, weakness, headache, muscle and joint pain, muscle weakness, azotemia, persistent drowsiness, polydipsia and polyuria, and , at the final stage, in the form of dehydration of the body. An overdose of cholecalciferol can cause ECG changes, cardiac arrhythmias, pancreatitis, and renal failure.

Overdose treatment

ѕрежде всего необходимо прекратить прием колекальциферола. ?л¤ устранени¤ гиперкальциемии, вызванной передозировкой колекальциферолом, требуетс¤ несколько недель. ¬ зависимости от степени гиперкальциемии, в качестве мер лечени¤ назначают диету с низким содержанием кальци¤ или полностью без кальци¤, потребление большого количества жидкости, форсированный диурез с применением фуросемида, а также глюкокортикостероиды и кальцитонин. ѕри сохранной функции почек концентраци¤ кальци¤ может быть значительно снижена путем инфузии изотонического раствора хлорида натри¤ (3-6 литров в течение 24 часов) с добавлением фуросемида и, в некоторых случа¤х, также натри¤ эдетата в дозе 15 мг/кг/ч, при одновременном мониторинге уровн¤ кальци¤ и данных Ё v. Ќе следует примен¤ть инфузию фосфатов дл¤ уменьшени¤ гиперкальциемии, вызванной передозировкой колекальциферола, в св¤зи с опасностью развити¤ метастатической кальцификации. ѕри олигоанурии следует провести гемодиализ (диализат без кальци¤).

—пецифического антидота не существует.

–екомендуетс¤ обращать внимание пациентов на симптомы возможной передозировки при длительном приеме высоких доз препарата (тошнота, рвота, первоначально Ц диаре¤, позже Ц запор, потер¤ аппетита, слабость, головна¤ боль, боль в мышцах и суставах, мышечна¤ слабость, посто¤нна¤ сонливость, полидипси¤ и полиури¤).

¬заимодействие с другими лекарственными средствами

ќдновременный прием противосудорожных лекарственных препаратов (таких как фенитоин) или барбитуратов (и, возможно, других лекарственных средств, индуцирующих ферменты печени) может снизить эффективность колекальциферола за счет увеличени¤ скорости биотрансформации колекальциферола в неактивные метаболиты.

—опутствующа¤ терапи¤ препаратами глюкокортикостероидов может снижать эффективность колекальциферола.

ѕероральный прием колекальциферола может усилить терапевтический эффект и токсический потенциал наперст¤нки и других сердечных гликозидов (риск развити¤ аритмии) за счет развити¤ гиперкальциемии. “ребуетс¤ тщательное медицинское наблюдение, контроль показателей Ё v и уровней кальци¤ в плазме крови и моче, и, при необходимости, корректировка дозы сердечных гликозидов.

¬ случае сопутствующей терапии тиазидными диуретиками, которые уменьшают экскрецию кальци¤ с мочой, рекомендуетс¤ контролировать содержание кальци¤ в сыворотке крови и моче.

ќдновременное лечение ионообменными смолами (такими как колестирамин), препаратами орлистата или слабительными средствами (такими как парафиновое масло) может уменьшать всасывание колекальциферола в пищеварительном тракте. ќдновременный прием рифампицина и изониазида может снизить эффективность препарата из-за увеличени¤ скорости биотрансформации колекальциферола.

Ќа фоне одновременного приема антацидов, содержащих магний, и колекальциферола может повышатьс¤ концентраци¤ магни¤ в крови.

Ќа фоне одновременного приема антацидов, содержащих алюминий, и колекальциферола может повышатьс¤ концентраци¤ алюмини¤ в крови, что увеличивает риск токсического воздействи¤ алюмини¤.

ќсобые указани¤

?сли одновременно назначены другие препараты, содержащие колекальциферол, следует учитывать дозу колекальциферола, содержащегос¤ в препарате ‘ортедетрим. ?ополнительное применение колекальциферола или кальци¤ следует проводить только под наблюдением врача. ¬ этом случае необходимо контролировать концентрацию кальци¤ в сыворотке крови и моче. ” пациентов с почечной недостаточностью, получающих лечение препаратом ‘ортедетрим, следует контролировать показатели метаболизма кальци¤ и фосфатов. ѕрепарат не следует примен¤ть у пациентов с предрасположенностью к кальциевому нефроуролитиазу.

ѕрепарат следует примен¤ть с осторожностью у пациентов с нарушенной экскрецией кальци¤ и фосфатов с мочой, при лечении производными бензотиазидина и у иммобилизованных пациентов (риск развити¤ гиперкальциемии и гиперкальциурии). ” таких пациентов следует контролировать концентрацию кальци¤ в плазме крови и моче.

ѕрепарат не следует принимать при псевдогипопаратиреозе, поскольку в фазе нормальной чувствительности к колекальциферолу потребность в колекальцифероле может уменьшатьс¤, что приводит к риску развити¤ отсроченной передозировки. ¬ таких случа¤х лучше использовать активные метаболиты витамина D, позвол¤ющие более точно регулировать дозировку.

ѕри длительном лечении препаратом ‘ортедетрим следует контролировать концентрацию кальци¤ в плазме крови и моче, а также проводить оценку функции почек путем измерени¤ концентрации сывороточного креатинина. Ёто особенно важно дл¤ пациентов пожилого возраста и при сопутствующем лечении сердечными гликозидами или диуретиками.

¬ случае развити¤ гиперкальциемии на фоне лечени¤ препаратом ‘ортедетрим (концентраци¤ кальци¤ в крови превышает 7,5 ммоль/24 ч (300 мг/24 ч) или наличи¤ признаков нарушени¤ функции почек дозу препарата необходимо снизить или приостановить лечение.

¬ли¤ние на способность управл¤ть транспортными средствами, механизмами

»сследовани¤ по вли¤нию на способность управл¤ть транспортным средством и работу с механизмами не проводились.

‘орма выпуска

 апсулы 2000 ME, 4000 ME, 10000 ME.

ѕо 15 капсул в блистер из ѕ¬’/ѕ¬?’ и алюминиевой фольги.

?озировка 2000 ME, 4000 ME:
ѕо 2, 4 или 6 блистеров в пачку картонную вместе с инструкцией по применению.

?озировка 10000 ME:
ѕо 2 или 4 блистера в пачку картонную вместе с инструкцией по применению.

”слови¤ хранени¤

’ранить при температуре не выше 30 ?—, в оригинальной упаковке (блистер в пачке).

’ранить в недоступном дл¤ детей месте.

—рок годности

3 года.

Ќе примен¤ть по истечении срока годности.

”слови¤ отпуска

ќтпускают по рецепту.

¬ладелец регистрационного удостоверени¤

‘армацевтический завод ЂѕќЋ№‘ј–ћјї јќ
ул. ѕельплиньска 19, 83-200 —тарогард vданьски, ѕольша.

ѕроизводитель

ћедана ‘арма јкционерное ќбщество
98-200 —ерадз, ул. ѕольской ќрганизации ¬ойсковой 57, ѕольша.

ќрганизаци¤, принимающа¤ претензии потребителей

Joint Stock Company 'Chemical and Pharmaceutical Plant' AKRIKHIN '(JSC' AKRIKHIN '), Russia
142450, Moscow region, Noginsky district, Staraya Kupavna, st. Kirov, 29.