Alpha D3, 0.25 mcg capsules 30 pcs

Pharmgroup:

Vitamin – calcium-phosphorus metabolism regulator.

Pharmic action:

Alpha D3-Teva is a vitamin, regulator of calcium-phosphorus metabolism. It is a precursor of the active metabolite of vitamin D3 – calcitriol. It increases absorption of calcium and phosphorus in intestine, increases their reabsorption in kidneys, restores positive calcium balance in treatment of calcium malabsorption syndrome, reduces parathyroid hormone in blood.

Concerning both parts of bone remodeling process (resorption and synthesis) alfacalcidol not only increases mineralization of bone tissue, but also increases its elasticity by stimulating synthesis of bone matrix proteins, bone morphogenetic proteins and bone growth factors which promotes reduction of fracture frequency.

In elderly patients with endocrine-immune dysfunction, including deficiency of D-hormone production (calcitriol), a decrease of total muscle mass (sarcopenia) and the appearance of muscle weakness syndrome (due to the disturbance of normal neuromuscular system functioning) occur, 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 alfacalcidol.

Pharmacokinetics:

Intake

After oral administration alfacalcidol is rapidly absorbed from the GI tract. Cmax in plasma is reached 8-12 hours after a single dose of alfacalcidol.

Alfacalcidol is converted into calcitriol (1.25-dihydroxycalciferol) in liver by hydroxylation on carbon atom 25, and process of hydroxylation is very fast (substrate-dependent character). Unlike native vitamin D alfacalcidol does not require hydroxylation in kidneys, therefore it is effective even in patients with decreased activity of renal 1-alpha-hydroxylase (kidney pathology, old age).

Elimination

The T1/2 is 35 h. It is excreted by the kidneys and through the intestine with the bile in approximately equal proportions.

Indications

Osteoporosis, including postmenopausal, senile, steroid.

Osteodystrophy in chronic renal failure.

Hypoparathyroidism and pseudohypoparathyroidism.

Rachitis and osteomalacia associated with nutritional or absorption deficiencies.

Hypophosphatemic vitamin-D-resistant rickets and osteomalacia.

Pseudodeficient (vitamin-D-dependent) rickets and osteomalacia.

Fanconi syndrome (hereditary renal acidosis with nephrocalcinosis, tardive rickets and adiposogenital dystrophy).

Renal acidosis.

Active ingredient

Composition

Active ingredients:

Alfacalcidol – 0.25 mcg.

Excipients:

citric acid anhydrous – 0.015 mg,

propyl gallate – 0.02 mg,

D,L-α-tocopherol (vit. E) – 0.02 mg,

ethanol absolute – 1.145 mg,

peanut butter – up to 100 mg.

Composition of the soft gelatin capsule:

Gelatin – 48.55 mg,

Glycerol 85% – 11.7 mg,

Anidrisorb 85/70 – 7.92 mg (sorbitol – 24-40%, sorbitan – 20-30%, mannitol – 0-6%, higher polyols – 12.5-19%, water – 15-17%),

iron oxide red (E172) – 0.54 mg.

The composition of black food ink A10379:

shellac – 54%,

iron oxide black (E172) – 46%.

How to take, the dosage

Ingestion. Recommended daily dose of the drug Alpha D 3 -Teva can be taken all at once, or the dose can be divided into 2 doses. Therapy may last from 2-3 months to 1 year or more.

The duration of treatment is determined by the doctor for each patient individually.

From 1 to 3 mcg/d for at least 2 to 3 months.

From 2 to 4 mcg/d.

From 1 to 2 mcg/d for 2-3 months 2-3 times a year.

From 2 to 6 mcg/d.

Therapy starts with a dose of 4 mcg/day. The maximum daily dose can reach 20 mcg.

If high doses are prescribed, consider switching to a higher dosage of Alpha D3-Teva capsules (Alpha D3-Teva capsules. 1 mcg disp. 30 Teva Pharmaceutical Enterprises Ltd) or other dosage forms of alphacalcidol.

From 0.5 to 1 mcg/day. It is recommended to start treatment with the lowest of these doses, controlling the calcium and phosphorus levels in blood plasma once a week. The drug dose can be increased by 0.5 mcg/day until the biochemical parameters are stabilized.

From 1 to 3 mcg/day for at least 2-3 months.

From 0.5 to 1 mcg/d for 2-3 months 2-3 times a year.

From 2 to 6 mcg/d.

In hypophosphatemic rickets and osteomalacia

Therapy starts with a dose of 1 mcg/day.

Interaction

In the treatment of osteoporosis may be prescribed in combination with estrogens and antiresorptive drugs of different groups.
With concomitant use of Alpha D3-Teva with foxglove drugs the risk of cardiac rhythm disturbances increases.
When concomitant administration with barbiturates, anticonvulsants and other drugs that activate enzymes of microsomal oxidation in the liver, a higher dose of Alfa D3-Teva should be used.

The absorption of alfacalcidol is reduced when co-administered with mineral oil (for a long time), colestyramine, colestipol, sucralfate, antacids, albumin-based drugs.

The risk of hypermagnesemia increases when used concomitantly with Alpha D3-Teva antacids or laxative dialysis.
Concomitant administration of calcium drugs, thiazide diuretics increases the risk of hypercalcemia.

Vitamin D and its derivatives should not be prescribed against the background of Alpha D3-Teva therapy because of possible additive interaction and increased risk of hypercalcemia.

Special Instructions

The therapy should be carried out under constant control of calcium and phosphate concentrations in blood (at the beginning of treatment – once a week, when reaching and during the whole period of treatment – calcium concentration in plasma and urine every 3-5 weeks), as well as alkaline phosphatase (ALP) activity (in CKD – weekly control). In CKD it is required preliminary correction of hyperphosphatemia.

When plasma ALP content is normalized, the dose of the drug Alpha D 3 -Teva should be decreased to avoid the development of hypercalcemia. Hypercalcemia or hypercalciuria are corrected by discontinuation of the drug and reduction of calcium intake until normalization of plasma calcium concentration.

As a rule, this period is 1 week. After normalization, therapy is continued by administering half of the last dose used. We must keep in mind that vitamin D sensitivity varies from patient to patient and even therapeutic doses may cause hypervitaminosis in some patients.

In children receiving vitamin D for a long time, there is an increased risk of growth retardation. To prevent hypovitaminosis D, a balanced diet is preferable.

In old age, the need for vitamin D may increase due to decreased absorption of vitamin D, decreased ability of the skin to synthesize provitamin D 3 , decreased insolation time, and increased frequency of renal failure.

Contraindications

With caution in:

Side effects

Anorexia, nausea, vomiting, heartburn, abdominal pain, dry mouth, feeling of discomfort in the epigastrium, constipation, diarrhea.

Rarely, a slight increase in “liver” enzymes.

General weakness, fatigue, headache, Dizziness, drowsiness.

Tachycardia.

Skin rash, itching.

Moderate pain in muscles, bones, joints.

Hypercalcemia, mild elevation of high-density lipoproteins . In patients with significant renal dysfunction, hyperphosphatemia is possible.

Overdose

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

Late symptoms of hypervitaminosis D: dizziness, confusion, somnolence, blurred urine, abnormal heart rhythm, skin itching, increased blood pressure, conjunctival hyperemia, nephrolithiasis, weight loss, photophobia, pancreatitis, gastralgia. Rarely – psychosis (change of mind and mood).

The symptoms of chronic vitamin D intoxication: calcification of soft tissues, blood vessels and internal organs (kidneys, lungs), renal and cardiovascular failure up to death, growth disorders in children.

Treatment: The drug should be discontinued. In the early days of acute overdose – gastric lavage, prescription of mineral oil (Vaseline), which helps to reduce absorption and increase excretion through the intestine. In severe cases it may be required supportive therapeutic measures – hydration with infusion of saline solutions (forced diuresis), in some cases – prescription of glucocorticosteroids, loop diuretics, bisphosphonates, calcitonin and hemodialysis with solutions of low calcium content.

The monitoring of blood electrolytes, renal function and cardiac status by electrocardiogram especially in patients receiving digoxin is recommended.

Pregnancy use

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

In experiments on animals it was shown that calcitriol in doses 4-15 times higher than the recommended doses for humans has teratogenic effect.

Hypercalcemia in the mother during pregnancy associated with prolonged overdose of vitamin D can cause fetal hypersensitivity to vitamin D, suppression of parathyroid function, specific elf-like appearance syndrome, mental retardation, aortic stenosis.

The drug is contraindicated for use during breastfeeding.

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