Alpha D3-Teva® (Alpha D3-Teva®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAlfacalcidolAlfacalcidol
Dosage form: & nbspcapsules
Composition:

1 capsule contains: active substance alfacalcidol - 0.5 mcg; Excipients: citric acid anhydrous 0.015 mg, propyl gallate 0.020 mg, alpha-tocopherol 0.020 mg, ethanol 1.145 mg, peanut oil up to 100 mg; soft gelatin capsule: gelatin 48.35 mg, glycerol 11.81 mg, anhydrisorb 85/70 7.89 mg (sorbitol 25-40%, sorbitan 20-30%, mannitol 0-6%, higher polyols 12.5-19%, water 15-17%), iron dye red oxide (E172) 0.043 mg, titanium dioxide (E171) 0.65 mg, black ink S-1-27794 (shellac 59.420%, iron dye oxide black (E172) 24.650%, butanol 9.750 %, water 3.250%, propylene glycol (E1520) 1,300%, ethanol denatured [methyl alcohol] 1.080%, isopropanol 0.550%) or S-1-17823 (shellac 44.467%, isopropanol 26.882%, iron dye oxide black (E172) 23.409 %, butanol 2.242%, propylene glycol (E1520) 2,000%, aqueous ammonia (E527) 1,000%) traces / tracks.

* Butanol, water, ethanol denatured [methyl alcohol], isopropanol, ammonia water - volatile compounds. which completely evaporate during the application of the inscriptions on the capsules and on the surface of the capsules do not remain.

Description:

Soft gelatin capsules oval-shaped pale pink color with a printed "0.5" black paint.

The contents of the capsules are an oily solution of pale yellow color.

Pharmacotherapeutic group:Vitamin - calcium-phosphorus exchange regulator
ATX: & nbsp

A.11.C.C.03   Alfacalcidol

Pharmacodynamics:

Alfacalcidol (1α-hydroxyvitamin D3) quickly converted into a liver in 1,25-dihydroxyvitamin D3, active metabolite of the vitamin D (calcitriol), which acts as a regulator of calcium and phosphorus metabolism. Increases the absorption of calcium and phosphorus in the intestines, increases their reabsorption in the kidneys, restores the positive calcium balance in the treatment of calcium malabsorption syndrome and reduces the concentration of parathyroid hormone in the blood. Influencing both parts of the bone remodeling process (resorption and synthesis), alfacalcidol not only increases the mineralization of bone tissue, but also increases its elasticity by stimulating the synthesis of bone matrix proteins, bone morphogenetic proteins, bone growth factors, which helps to reduce the incidence of fractures.

In elderly patients against the background of endocrine-immune dysfunction, including a deficit of products Dhormone (calcitriol), there is a decrease in total muscle mass (sarcopenia) and the appearance of a syndrome of muscle weakness (due to disruption of the normal functioning of the neuromuscular system), which is accompanied by an increase risk of falls and the resulting injuries and fractures. A number of studies have shown a significant reduction in the incidence of falls in elderly patients with the use of alfacalcidol. Alfacalcidol stimulates the regeneration of muscle fibers, which restores lost muscle tone.
Pharmacokinetics:

Suction

After oral administration alfacalcidol quickly absorbed from the gastrointestinal tract (GIT). Maximum concentration (Cmax) is achieved 8-12 hours after a single intake of alfacalcidol.

Metabolism

The conversion of alfacalcidol into calcitriol (1,25-dihydroxycolecalciferol) occurs in the liver by hydroxylation at the 25th carbon atom, the hydroxylation process taking place very quickly (it has a substrate-dependent character). Unlike native vitamin D alfacalcidol does not require hydroxylation in the kidneys, therefore it is effective even in patients with decreased renal 1-alpha hydroxylase activity (kidney pathology, elderly age).

Excretion

It is excreted by the kidneys and through the intestine with bile approximately in equal parts. The half-life period is 19 days.

Indications:

Osteoporosis (including postmenopausal, senile, steroid); osteodystrophy in chronic renal failure; hypoparathyroidism and pseudohypoparathyroidism; rickets and osteomalacia associated with malnutrition or absorption; hypophosphatemic vitamin-D-resistant rickets and osteomalacia; pseudo-deficient (vitamin-D-dependent) rickets and osteomalacia; Fanconi syndrome (hereditary renal acidosis with nephrocalcinosis, late rickets and adiposogenital dystrophy); renal acidosis.

Contraindications:

Hypersensitivity to alfacalcidol and other components of the drug hypercalcemia; hyperphosphataemia (with the exception of hyperphosphatemia in hypoparathyroidism); hypermagnesia; hypervitaminosis D; pregnancy (I trimester); the period of breastfeeding; Children's age is less than 3 years.

Carefully:

In nephrolithiasis, atherosclerosis, chronic heart failure, chronic renal failure (CRF), sarcoidosis or other granulomatosis, pulmonary tuberculosis (active form), pregnancy (II-III trimester), in patients with an increased risk of hypercalcemia, especially in the presence of nephrolithiasis; children age over 3 years.

Pregnancy and lactation:

During pregnancy (II-III trimester) alfacalcidol appoint only if the expected benefit to the mother exceeds the possible risk to the fetus.

In animal experiments it was shown that calcitriol in doses 4-15 times higher than the recommended dose for humans, has a teratogenic effect. Hypercalcemia in the mother during pregnancy, associated with a prolonged overdose of the vitamin D, can cause the fetus to increase the sensitivity to vitamin D, suppression of parathyroid function, syndrome of specific elf-like appearance, mental retardation, aortic stenosis.

The drug is contraindicated for use during breastfeeding.

Dosing and Administration:

Inside. The recommended daily dose of the drug is Alpha D3-Tev® can be taken in one go, you can divide the dose into 2 doses. Therapy can last from 2-3 months to 1 year or more. The duration of treatment is determined by the doctor for each patient individually.

Adults

When osteomalacia associated with malnutrition or absorption: 1 to 3 mcg / day for a minimum of 2-3 months.

When hypoparathyroidism: from 2 to 4 mcg / day.

In osteodystrophy in chronic renal failure: from 1 to 2 mcg / day courses for 2-3 months 2-3 times a year.

With Fanconi syndrome and renal acidosis: from 2 to 6 mcg / day.

When hypophosphatemic osteomalacia: Therapy is started with a dose of 4 μg / day. The maximum daily dose can reach 20 mcg.

When administering high doses, consideration should be given to switching to a higher dosage of Alpha D3-Teva® capsules or other dosage forms of alfacalcidol.

With osteoporosis (including postmenopausal, senile, steroid): from 0.5 to 1 mcg / day. It is recommended to start treatment with the minimum of these doses, controlling once a week the level of calcium and phosphorus in the blood plasma. The dose of the drug can be increased by 0.5 mcg / day until the biochemical parameters stabilize.

Children over 3 years old

When rickets and osteomalacies associated with malnutrition or absorption: 1 to 3 mcg / day for a minimum of 2-3 months.

In osteodystrophy in chronic renal failure: from 0,5 to 1 mcg / day by courses for 2-3 months 2-3 times a year.

With Fanconi syndrome and renal acidosis: from 2 to 6 mcg / day.

With hypophosphatemic rickets and osteomalacia: therapy begins with a dose of 1 mcg / day.
Side effects:

On the part of the digestive system: anorexia, vomiting, heartburn, abdominal pain, nausea, dry mouth, discomfort in the epigastric region, constipation, diarrhea; rarely - a slight increase in "liver" enzymes.

From the nervous system: general weakness, fatigue, headache, dizziness, drowsiness.

From the cardiovascular system: tachycardia.

Allergic reactions: skin rash, itching.

From the musculoskeletal system: moderate pain in muscles, bones, joints.

Laboratory indicators: hypercalcemia, slight increase high-density lipoproteins. In patients with severe renal dysfunction, hyperphosphataemia may develop.

Overdose:

Early symptoms of hypervitaminosis D (caused by hypercalcemia): diarrhea, constipation, nausea, vomiting, dry mouth, anorexia, metallic taste in the mouth, hypercalciuria, polyuria, polydipsia, pollakiuria / nocturia, headache, fatigue, general weakness, myalgia, bone pain.

Late symptoms of hypervitaminosis D: dizziness, confusion, drowsiness, clouding of urine, heart rhythm disturbance, skin itching, increased blood pressure, conjunctival hyperemia, nephrolithiasis, weight loss, photophobia, pancreatitis, gastralgia, rarely - psychosis (change of mentality and mood).

Symptoms of chronic vitamin intoxication D: calcification of soft tissues, blood vessels and internal organs (kidneys, lungs), renal and cardiovascular insufficiency up to a lethal outcome, impaired growth in children.

Treatment: the drug should be discarded. In the early periods of acute overdosage - gastric lavage, the appointment of mineral oil (vaseline), which helps to reduce absorption and increase excretion through the intestine. In severe cases, it may be necessary to carry out supportive medical measures - hydration with the introduction of infusion saline solutions (forced diuresis),in some cases - the appointment of glucocorticosteroids, loop diuretics, bisphosphonates, calcitonin and hemodialysis with the use of solutions with a low content of calcium. It is recommended to control the content of electrolytes in the blood, the function of the kidneys and the state of the heart by data of the electrocardiogram especially in patients receiving digoxin.

Interaction:

In the treatment of osteoporosis alfacalcidol can be assigned in combination with estrogens and drugs that reduce bone resorption.

With the simultaneous use of alfacalcidol with digitalis drugs, the risk of arrhythmia increases.

Inductors of microsomal enzymes of the liver (incl. phenytoin and phenobarbital) reduce, and inhibitors - increase the concentration of alfacalcidol in the plasma (it is possible to change its effectiveness).

Absorption of alfacalcidol decreases when it is used together with mineral oil (for a long time), colestyramine, colestipol, sucralfate, antacids, albumin-based preparations.

Admission of antacids increases the risk of hypermagnesemia and hyperaluminia. Toxic effect weakens retinol, tocopherol, ascorbic acid, pantothenic acid, thiamine, riboflavin.

Calcitonin, etidronic and pamidronic acid derivatives, plikamycin, gallium nitrate and glucocorticosteroids reduce the effect.

Alfacalcidol increases the absorption of phosphorus-containing drugs and the risk of hyperphosphataemia.

Simultaneous use of alfacalcidol with calcium preparations, thiazide diuretics can cause hypercalcemia, by increasing the absorption of calcium in the intestine, increasing its reabsorption in the kidneys.

Against the background of therapy with alfacalcidol, do not prescribe other medicines of the vitamin D and its derivatives because of the possible additive interaction and increased risk of hypercalcemia.

Special instructions:

In children, patients with chronic renal failure (CRF) should regularly monitor the calcium and phosphate levels in the blood plasma (at the beginning of treatment - once a week, when reaching Cmax and throughout the treatment period - every 3-5 weeks), as well as the activity of alkaline phosphatase (with CRF - weekly monitoring).

With CRF, a preliminary correction of hyperphosphataemia is required.When the activity of alkaline phosphatase in the blood plasma is normalized, the dose of Alfa D3-Teva® must be reduced, which will allow the development of hypercalcemia. At the beginning of Alpha D3-Teva® treatment, calcium measurement is recommended especially in conditions without significant bone damage, for example, in hypoparathyroidism and if the calcium content in the blood plasma is already elevated, and also at later stages of treatment - if there are signs of restoring the structure bone tissue. The risk of hypercalcemia is determined by such factors as the degree of bone demineralization, the functional ability of the kidneys and the dose of the drug.

Hypercalcemia or hypercalciuria is corrected by lowering the dose of Alfa-D3-Teva® and reducing calcium intake before normalizing the calcium content in the blood plasma. Typically, this period is 1 week. After normalization, the therapy is continued, applying half of the last applied dose. With the development of hypercalcemia or a persistent increase in the content of calcium phosphate compounds, which goes beyond the clinical norm, the drug should be immediately discontinued, at least,until these data are not normalized (usually within a week), then the drug can be resumed at a dose that is half the previous one.

Patients with severe bone disease (unlike patients with renal insufficiency) can tolerate higher doses of the drug without signs of hypercalcemia. The absence of a rapid increase in serum calcium in patients with osteomalacia does not always mean that the dose of the drug should be increased, since calcium can penetrate the demineralized bone due to its increased absorption in the intestine. It is necessary to prevent the development of prolonged hypercalcemia, especially in chronic renal failure, focusing on such factors as calcium and serum calcium, alkaline phosphatase activity, parathyroid hormone concentration, radiologic and histological data.

To prevent the development of hyperphosphataemia in patients with bone lesions of renal genesis, alfacalcidol can be used together with phosphate binders. It must be taken into account that the sensitivity to vitamin D in different patients is individual, and sometimes even the administration of therapeutic doses can cause hypervitaminosis.

In children receiving vitamin D for a long time, the risk of growth retardation increases.

For prevention of hypovitaminosis D, a balanced diet is most preferable. In the elderly, the need for vitamin D may increase due to a decrease in vitamin D absorption, a decrease in the ability of the skin to synthesize provitamin D3, a decrease in the time of insolation, an increase in the incidence of renal failure.

The composition of excipients of the drug includes peanut butter. Patients with an allergic reaction to peanut butter and soy bean is contraindicated.

Form release / dosage:

Capsules 0.5 mcg.

Packaging:

10 capsules in aluminum / aluminum blister.

1 or 3 blisters together with instructions for use in a cardboard bundle.

30 or 60 capsules in a polypropylene bottle with a polypropylene lid.

The bottle is equipped with a security tape control the first opening.

1 bottle with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription
Registration number:LSR-007813/10
Date of registration:10.08.2010 / 01.12.2016
Expiration Date:Unlimited
The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
Manufacturer: & nbsp
Representation: & nbspTeva Teva Israel
Information update date: & nbsp16.07.2017
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