Alpha Д3-Тева®

General characteristics. Structure:

Active agent: альфакальцидол - 0,5 mkg.
Excipients: citric acid anhydrous, propyl gallate, alpha tocopherol, ethanol, peanut oil.
The soft gelatin capsule contains: gelatin, глицерол, анидрисорб 85/70 (sorbitol, sorbitan, Mannitolum, the highest polyols, water), ferrous oxide red (E172), titanium dioxide (E171), ink black (shellac, ferrous oxide black (E172)).

Description: Soft gelatin capsules of an oval form of light pink color with printed with "0,5" black paint.
Contents of capsules - Solutio oleosa of pale yellow color.

Pharmacological properties:

Pharmacodynamics. Alfakaltsidol is the predecessor of an active metabolite of D3 vitamin - calcitriol. Increases absorption of calcium and phosphorus in intestines, increases their reabsorption in kidneys, recovers positive calcic balance at treatment of a syndrome of calcic malyabsorbtsiit reduces concentration in blood of parathyroid hormone. Influencing both parts of process of bone remodeling (a resorption and synthesis), альфакальцидол not only increases a mineralization of a bone tissue, but increases its elasticity due to stimulation of protein synthesis of a matrix of a bone, bone morphogenetic proteins, bone growth factors that promotes reduction of frequency of development of changes.
Patients of advanced age against the background of endocrine and immune dysfunction, including deficit of products of D-hormone (calcitriol), have a decrease in the general muscle bulk (sarkopeniye) and emergence of a syndrome of muscular weakness (owing to disturbance of normal functioning of the neuromuscular device) that is followed by increase in risk of falling and the injuries and fractures caused by it. In a number of researches considerable decrease in frequency of falling of elderly patients when using an alfakaltsidol was shown.

Pharmacokinetics. Absorption
After intake альфакальцидол it is quickly soaked up from the digestive tract (DT). The maximum concentration (Cmax) is reached in 8-12 hours after a single dose of an alfakaltsidol.
Metabolism
Transformation of an alfakaltsidol into calcitriol (1.25-digidroksikolekaltsiferol) happens in a liver by a hydroxylation on the 25th carbon atom, and process of a hydroxylation happens very quickly (carries substrate - dependent character). Unlike native vitamin D альфакальцидол does not need a hydroxylation in kidneys therefore it is effective even at patients with reduced activity renal 1 - alpha hydroxylases (pathology of kidneys, advanced age).
Removal
It is removed by kidneys and through intestines with bile approximately in equal shares. The elimination half-life makes 19 days

Indications to use:

Osteoporosis (including post-menopausal, senile, steroid); an osteodystrophy at a chronic renal failure; hypoparathyrosis and pseudohypoparathyroidism; the rickets and osteomalacy connected with insufficiency of food or absorption; gipofosfatemichesky vitamin - D-resistant rickets and osteomalacy; pseudo-scarce (vitamin - D-dependent) rickets and osteomalacy; Fankoni's syndrome (hereditary renal acidosis with a nephrocalcinosis, late rickets and an adiposagenital syndrome); renal acidosis.

Route of administration and doses:

Inside. The recommended daily dose of drug Alpha Д3-Тева® can be accepted at once at one time, it is possible to divide a dose into 2 receptions. Therapy can continue from 2-3 months to 1 year and more. Duration of treatment is defined by the doctor for each patient individually.
Adults
At the osteomalacy connected with insufficiency of food or absorption:
from 1 to 3 mkg/days within at least 2-3 months.
At a hypoparathyrosis: from 2 to 4 mkg/days.
At an osteodystrophy at HPN:
from 1 to 2 mkg/days courses within 2-3 months 2-3 times a year.
At Fankoni's syndrome and renal acidosis: from 2 to 6 mkg/days.
At gipofosfatemichesky osteomalacy: therapy begin 4 mkg/days with a dose. The maximum daily dose can reach 20 mkg.
At purpose of high doses it is necessary to consider a question of transition to higher dosage of capsules Alpha Д3-Тева® or other dosage forms of an alfakaltsidol.
At osteoporosis (including post-menopausal, senile, steroid):
from 0,5 to 1 mkg/days. It is recommended to begin treatment with minimum of the specified doses, controlling the level of calcium and phosphorus in a blood plasma once a week. The dose of drug can be raised on 0,5 mkg/days to stabilization of biochemical indicators.
Children are more senior than 3 years
At rickets and osteomalacy, connected with insufficiency of food or absorption:
from 1 to 3 mkg/days within at least 2-3 months. At an osteodystrophy at HPN:
from 0,5 to 1 mkg/days courses within 2-3 months 2-3 times a year.
At Fankoni's syndrome and renal acidosis: from 2 to 6 mkg/days.
At gipofosfatemichesky rickets and osteomalacy: therapy begin 1 mkg/days with a dose.

Features of use:

Therapy needs to be carried out under constant control of concentration of calcium and phosphates to blood (in an initiation of treatment - once a week, at achievement of Cmax and during the entire period of treatment - concentration of calcium in plasma and urine each 3-5 weeks), and also activities of the alkaline phosphatase (AP) (at HPN - weekly control). At HPN preliminary correction of a hyperphosphatemia is required.
At normalization of maintenance of ShchF in a blood plasma it is necessary to lower a drug dose Alpha Д3-Тева® that will allow to avoid development of a hypercalcemia. The hypercalcemia or a hypercalcuria korrigirutsya by drug withdrawal and decrease in consumption of calcium to normalization of concentration of calcium in a blood plasma. As a rule, this period makes 1 week. After normalization therapy is continued, appointing a half of the last applied dose.
It must be kept in mind that sensitivity to vitamin D at different patients is individual, and, reception even of therapeutic doses can cause the hypervitaminosis phenomena in a number of patients.
At the children receiving vitamin D for a long time the risk of emergence of a growth inhibition increases.
For prevention of a hypovitaminosis D most preferably balanced food.
The need for vitamin D can increase in advanced age owing to reduction of absorption of vitamin D, declines in the ability of skin to synthesize D3 provitamin, reduction of time of insolation, increase of frequency of developing of a renal failure.

Side effects:

From digestive organs: anorexia, vomiting, heartburn, an abdominal pain, nausea, dryness in a mouth, a sensation of discomfort in the field of an epigastrium, a lock, diarrhea; seldom - slight increase of "hepatic" enzymes.
From a nervous system: general weakness, fatigue, headache, dizziness, drowsiness.
From cardiovascular system: tachycardia.
Allergic reactions: skin rash, itch.
From a musculoskeletal system: moderate muscle, bones, joints pains.
Laboratory indicators: hypercalcemia, slight increase of lipoproteins of high density. At patients with the expressed renal failures development of a hyperphosphatemia is possible.

Interaction with other medicines:

At treatment of osteoporosis альфакальцидол it can be appointed in a combination with the estrogen and medicines reducing a bone resorption.
At simultaneous use of an alfakaltsidol with drugs of a foxglove the risk of development of arrhythmia increases.
Inductors of microsomal enzymes of a liver (including Phenytoinum and phenobarbital) reduce, and inhibitors - increase concentration of an alfakaltsidol in plasma (possibly change of its efficiency).
Absorption of an alfakaltsidol decreases at its combined use with mineral oil (for a long time), Colestyraminum, kolestipoly, sukralfaty, antacids, drugs on the basis of albumine.
Reception of antacids increases risk of development of a gipermagniyemiya and giperalyuminiyemiya. Toxic action is weakened by Retinolum, tocopherol, ascorbic acid, pantothenic acid, thiamin, Riboflavinum.
The calcitonin, derivatives of etidronovy and pamidronovy acids, пликамицин, gallium nitrate and glucocorticosteroids reduce effect.
Alfakaltsidol increases absorption of phosphorus drugs and risk of emergence of a hyperphosphatemia.
Simultaneous use of an alfakaltsidol with calcium drugs, thiazide diuretics can cause a hypercalcemia, due to increase in absorption of calcium in intestines, increases in its reabsorption in kidneys.
Against the background of therapy alfakaltsidoly it is not necessary to appoint other medicines of vitamin D and its derivatives because of possible additive interaction and increase in risk of development of a hypercalcemia.

Contraindications:

Hypersensitivity to an alfakaltsidol and other components of drug a hypercalcemia; a hyperphosphatemia (except for a hyperphosphatemia at a hypoparathyrosis); gipermagniyemiya; hypervitaminosis of D; pregnancy (I trimester); breastfeeding period; the children's age is younger than 3 years.

WITH CARE
At a nephrolithiasis, atherosclerosis, chronic heart failure, the chronic renal failure (CRF), a sarcoidosis or other granulomatoses, a pulmonary tuberculosis (an active form), pregnancies (the II-III trimester), patients with the increased risk have a development of a hypercalcemia, especially in the presence of a nephrolithiasis; the children's age is more senior than 3 years.

USE AT PREGNANCY AND DURING BREASTFEEDING
During pregnancy (the II-III trimester) альфакальцидол appoint only if the expected advantage for mother exceeds possible risk for a fruit.
In experiments on animals it is shown that calcitriol in doses, at 4-15 times exceeding the recommended doses for the person has teratogenic effect. The hypercalcemia at mother during pregnancy connected with long overdose of vitamin D can cause in a fruit increase in sensitivity to vitamin D, epithelial body function suppression, a syndrome of specific elfopodobny appearance, a delay of intellectual development, an aortal stenosis. Drug is contraindicated to use during breastfeeding.

Overdose:

The early symptoms of a hypervitaminosis of D (caused by a hypercalcemia): diarrhea, a lock, nausea, vomiting, dryness in a mouth, anorexia, metal taste in a mouth, a hypercalcuria, a polyuria, a polydipsia, a pollakiuria/nocturia, a headache, fatigue, the general weakness, a mialgiya, ostealgias.
Late symptoms of a hypervitaminosis of D: dizziness, confusion of consciousness, drowsiness, urine opacification, disturbance of a heart rhythm, a skin itch, increase in arterial pressure, a conjunctiva hyperemia, a nephrolithiasis, decrease in body weight, a photophobia, pancreatitis, a gastralgia, is rare - psychosis (change of mentality and mood).
Symptoms of chronic intoxication vitamin D: calcification of soft tissues, blood vessels and internals (kidneys, lungs), renal and cardiovascular failure up to a lethal outcome, a growth disorder at children.
Treatment: drug should be cancelled. In early terms of acute overdose - a gastric lavage, purpose of the mineral oil (vaseline) promoting reduction of absorption and increase in removal through intestines. In hard cases holding the supporting medical actions - hydrations with introduction of infusion saline solutions (artificial diuresis), in certain cases - purpose of glucocorticosteroids, loopback diuretics, bisfosfonat, a calcitonin and hemodialysis using solutions with the low content of calcium can be required. It is recommended to control the content of electrolytes in blood, function of kidneys and a condition of heart according to the electrocardiogram especially at the patients receiving digoxin

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Capsules of 0,5 mkg.
10 capsules in the blister aluminum/aluminium.
1 or 3 blisters together with the application instruction in a cardboard pack.
30 or 60 capsules in a bottle from polypropylene with a polypropylene cover. The bottle is supplied with a security tape of control of the first opening.
1 bottle together with the application instruction in a cardboard pack.