Active substanceAlfacalcidolAlfacalcidol
Dosage form: & nbspcapsules
Composition:

1 capsule contains: active substance: alfacalcidol 0.25 / 1.0 μg;

Excipients: citric acid 0.015 / 0.015 mg, propyl gallate 0.020 / 0.020 mg, alpha-tocopherol 0.020 / 0.020 mg, ethanol 1.145 / 1.144 mg, peanut oil 98.79975 / 98.800 mg; sheath (soft gelatin capsule): gelatin 48.55 / 48.27 mg, glycerol 85% 11.70 / 11.88 mg, anhydrizor 85/70 (sorbitol 25-40%, sorbitan 20-30%, mannitol 0-6%, higher polyols 12.5 -19%, water 15-17%) 7.92 / 7.88 mg, iron dye red oxide (E172) 0.54 / - mg, iron oxide pigment oxide yellow (E172) - / 0.05 mg, titanium dioxide E171) - /0.68 mg, black ink S-1-27794 (shellac 59.420%, iron stain oxide black (E172) 24.650%, butanol * 9.750%, water * 3.250%, propylene glycol (E1520) 1.300%, ethanol denatured [methylated 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%, ammonia water * (E527) 1,000%) traces / tracks.

* Butanol, water, ethanol denatured [methylated alcohol], isopropanol, aqueous ammonia - volatile compounds that evaporate completely during the process of applying the inscriptions on the capsules and do not remain on the surface of the capsules.

Description:

Dosage 0.25 μg: oval, reddish-brown, soft gelatin capsules with a printed "0.25" black paint, containing a pale yellow oil solution.

Dosage 1 mcg: oval, from cream color to ivory, soft gelatin capsules with a printed "1.0" black paint containing a pale yellow oil solution.

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

A.11.C.C.03   Alfacalcidol

Pharmacodynamics:Alfacalcidol (1α-hydroxyvitamin D3) is rapidly converted into a liver in 1,25-dihydroxybamidine 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 a 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, thereby reducing 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 the total muscle mass (sarcopenia) and the appearance of a syndrome of muscle weakness (due to disruption of the normal functioning of the neuromuscular apparatus), which is accompanied by an increased 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 the lost muscle tone.
Pharmacokinetics:

Alfacalcidol is fat-soluble and its bioavailability when taken orally - about 100%. After suction alfacalcidol is metabolized in the liver to form an active metabolite of 1,25-dihydroxyvitamin D3. The concentration of 1,25-dihydroxyvitamin D3 in blood plasma reaches a maximum in 8-12 hours after a single dose of alfacalcidol; the elimination half-life of 1,25-dihydroxyvitamin D3 . about 35 hours. It is excreted by the kidneys and with bile in approximately the same amount.

Indications:

Diseases caused by a violation of calcium and phosphorus metabolism due to insufficient endogenous synthesis of 1,25-dihydroxyvitamin D3:

- Osteoporosis (including postmenopausal, senile, steroid, etc.);

- osteodystrophy in chronic renal failure (CRF);

- hypoparathyroidism and pseudohypoparathyroidism;

- vitamin D-resistant rickets and osteomalacia.

Contraindications:

- Hypersensitivity to the components of the drug, including peanuts.

- Hypercalcemia.

- Hyperphosphatemia.

- Hypermagnesia.

- Hypervitaminosis D.

- The period of pregnancy and breastfeeding.

- Children under 12 years.

- Long-term immobilization.

- Tuberculosis of the lungs (active form).

Carefully:Assign the drug for organic heart lesions; atherosclerosis; acute and chronic diseases of the liver and kidneys; with nephrourolythiasis in the anamnesis; diseases of the gastrointestinal tract (including gastric ulcer and duodenal ulcer); hypothyroidism; sarcoidosis; tuberculosis or other granulomatosis, as these conditions have a predisposition to increase the sensitivity to vitamin D.
Pregnancy and lactation:

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 pregnancy and during breastfeeding.

Dosing and Administration:

The drug is taken inside regardless of food intake, without chewing, squeezed with enough liquid, once a day. The duration of treatment is determined by the doctor individually in each case and depends on the nature of the disease and the effectiveness of therapy.

Adults and children weighing more than 20 kg

The initial dose is 1 μg per day.

The maintenance dose is 0.25-2 μg per day.

With rickets and osteomalacia: from 1 to 3 mcg per day; when hypoparathyroidism: 1-4 μg per day; in osteodystrophy in chronic renal failure: 0.5-2 μg per day; with osteoporosis (including postmenopausal, senile, steroid, etc.): 0.5-1 mcg per day.

Begin treatment is recommended with minimal doses, controlling once a week the concentration of calcium and phosphorus in the blood plasma. The dose of the drug can be increased by 0.25 or 0.5 mcg / day until the biochemical parameters stabilize. When the minimum effective dose is reached, it is recommended to monitor the concentration of calcium in the blood plasma every 3-5 weeks.

Side effects:

The most common undesirable effects of the drug Alpha DZ-Teva * are: hypercalcemia, hypercalciuria and vitamin D-dependent toxicity.

The following are data on adverse adverse reactions, depending on the frequency of their occurrence. Adverse adverse reactions other than signs of hypercalcemia, obtained as separate reports, are also included.

The frequency is defined as: very often - ≥1 / 10;often - ≥1 / 100 and <1/10; infrequently - ≥1 / 1000 and <1/100; rarely - ≥1 / 10000 and <1/1000; very rarely - <1/10000 (including individual messages); frequency is unknown (can not be estimated from available data).

From the side of metabolism

Often: hypercalcemia; infrequently: metastatic calcifications, hyperphosphataemia, high content of calcium-phosphate compounds, anorexia; frequency is unknown: hypermagnesia, decreased appetite, weight loss, dehydration, cessation of growth, albuminuria, hypercholesterolemia, increased levels ACT and ALT in serum.

Allergic reactions

Frequency unknown: hypersensitivity reactions with symptoms such as: fever, chills, urticaria, and tongue edema.

From the nervous system

Infrequently: headache, dysesthesia, dysgeusia; rarely: mental disorders, hallucinations, coma, apathy; frequency is unknown: hyperthermia.

From the side of the cardiovascular system

Rarely: tachycardia, increased blood pressure.

From the digestive system

Infrequently: nausea, vomiting, abdominal pain, constipation, diarrhea, indigestion; rarely: acute pancreatitis; frequency is unknown: ulceration of the tongue, ulceration of the gums, polydipsia.

From the skin

Often: itching; rarely: erythema multiforme, psoriasis; frequency is unknown: rash (erythematous, maculopapular, pustular), exfoliative dermatitis.

From the sense organs

Rarely: calcification of the conjunctiva and sclera.

From the respiratory system

Frequency unknown: rhinitis.

From the urinary system

Often: hypercalciuria, increased serum creatinine and urea levels; frequency is unknown: renal failure, nephrocalcinosis, infection urinary tract.

From the side of the reproductive system

Frequency unknown: decreased libido.

Other

Rarely: calcification, asthenia and fatigue.

Overdose:

Early symptoms of vitamin hypervitaminosis D (caused by hypercalcemia): constipation or diarrhea, dryness of the oral mucosa, headache, thirst, pollakiuria, nocturia, polyuria, anorexia, metallic taste in the mouth, nausea, vomiting, general weakness, hypercalciuria.

Late symptoms of vitamin hypervitaminosis D: pain in the bones, clouding of urine (the appearance of hyaline cylinders in the urine), increased blood pressure, skin itching, photophobia, congestion hyperemia, arrhythmia, drowsiness, myalgia, nausea, vomiting, weight loss, rarely changes in the mind and mood, confusion.

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

The level of calcium in the blood serum is normalized 2-7 days after discontinuation of the drug.

Hypercalcemia is treated with a temporary discontinuation of alfacalcidol. the introduction of a diet with a low calcium content and stopping the intake of calcium supplements.

In severe cases of acute accidental overdose and persistent hypercalcemia, general supportive measures should be taken.

In case of an overdose, the drug should be discontinued. In the early periods of acute overdosage, gastric lavage and / or ingestion of mineral oil (vaseline), which reduces suction and increases the excretion of the drug through the intestine, is indicated.In severe cases (serum calcium level> 3mM / L), it may be necessary to carry out maintenance treatments - hydration with the introduction of infusion saline solutions (for the purpose of forced diuresis), in some cases - the appointment of glucocorticosteroid drugs, loop diuretics, bisphosphonates, calcitonin, peritoneal dialysis or hemodialysis using a dialysate that does not contain calcium. It is mandatory to monitor the content of electrolytes in the blood serum (especially calcium), kidney function and heart condition (according to the electrocardiogram), especially in patients taking digoxin (or other digitalis preparations).

Interaction:

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

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

Absorption of alfacalcidol decreases with its joint application with colestyramine. colestipol, mineral oil, sucralfate, antacids.To reduce the probability of interaction alfacalcidol should be applied for 1 hour before or 4-6 hours after taking the above drugs.

Calcitonin, derivatives of etidronic and pamidronic acids, plikamycin, gallium nitrate and glucocorticosteroids reduce the effect of alfacalcidol.

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.

Combined therapy with magnesium-containing antacids and vitamin D can cause an increase in the magnesium content in the blood, and aluminum-containing antacids - aluminum in the blood, especially in chronic renal failure.

Simultaneous application of various vitamin analogues D is accompanied by an additive effect with the development of hypercalcemia. The drug Alpha D3-Teva® should not be administered concomitantly with other preparations of the vitamin D and its derivatives.

Special instructions:

Pay attention to patients taking cardiac glycosides, as hypercalcemia can lead to the development of arrhythmia in such patients.

Attention should be paid to patients taking thiazide diuretics, since such patients may increase the risk of developing hypercalcemia.

The effectiveness of alfacalcidol is generally maintained in patients with reduced liver function. In severe hepatic insufficiency, the concentration of the active metabolite of 1,25-dihydroxyvitamin D can be reduced by decreasing the hydroxylation process or by decreasing the enterohepatic circulation. In this case, it may be necessary to administer the drug at higher doses.

When applying the drug in the elderly, dose adjustments are not required.

The drug can promote the development of hypercalcemia, so patients should be informed about the clinical symptoms of this condition (see the section "Overdose"). During the use of the Alpha D3-Teva® preparation, the concentration of calcium, phosphate, calcium-phosphate compounds, alkaline phosphatase and the level of parathyroid hormone in the blood serum should be regularly monitored.

The concentration of calcium should be determined once a week or a month, depending on the clinical situation.More frequent measurement of calcium is required at the beginning of treatment, especially in conditions without significant bone damage, for example, hypoparathyroidism, and if the calcium content in the plasma is already increased, as well as at later stages of treatment with signs of bone structure restoration. The risk of developing hypercalcemia is determined by such factors as: degree demineralization of bone, the functional capacity of the kidneys and the dose of the drug Alpha D3-Teva®. The appearance of hypercalcemia can be due to the fact that the dose of the drug does not decrease in a timely and adequate manner in the presence of biochemical signs of the restoration of the structure of bone tissue (normalization of alkaline phosphatase in the blood). It is necessary to prevent the development of prolonged hypercalcemia, especially in chronic renal failure, focusing on such factors as concentration in the serum of calcium, alkaline phosphatase, parathyroid hormone, the amount of calcium excreted in the urine, radiological and biochemical data.

With the development of hypercalcemia or a persistent increase in the level of calcium phosphate compounds, which goes beyond the clinical norm, the drug should be immediately canceled, at least,until these parameters are normalized (usually within one week), then the drug can be resumed at a dose that is half that of the previous one.

Patients with severe bone damage (in contrast to patients with renal insufficiency) can tolerate higher doses of the drug without signs of hypercalcemia. The lack of a rapid increase in serum calcium in patients with osteomalacia does not necessarily mean that the dose of the drug should be increased, since calcium can penetrate into the demineralized bone due to its increased absorption in the intestine.

It is necessary to avoid excessive suppression of parathyroid hormone. For patients on dialysis, the level of parathyroid hormone in serum should be consistent with the current treatment guidelines.

To prevent the development of hyperphosphataemia in patients with bone lesions of renal genesis, alfacalcidol can be used together with phosphate binding agents.

In osteoporosis, the use of the Alpha D3-Teva® drug can be combined with estrogens and antiresorptive drugs.

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

Effect on the ability to drive transp. cf. and fur:Alpha D3-Teva® does not influence or influences insignificantly the ability to drive vehicles and mechanisms.
Form release / dosage:Capsules 0.25 μg, 1 μg.
Packaging:

10 capsules per blister of light-protective polyvinylchloride and aluminum foil.

Dosage 1.0 mcg: 10 or 30 capsules per bottle of high-pressure polypropylene with a polypropylene lid.

Dosage of 0.25 μg: for 30 or 60 capsules in a bottle of high-pressure polypropylene with a polypropylene lid.

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

Storage conditions:

Store at a temperature not exceeding 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:П N012070 / 01
Date of registration:29.12.2011 / 16.09.2016
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: & nbsp08.11.2017
Illustrated instructions
    Instructions
    Up