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, incl. postmenopausal, senile, steroid.

Osteodystrophy in chronic renal failure.

Hypoparathyroidism and pseudohypoparathyroidism.

Rickets and osteomalacia associated with malnutrition or malabsorption.

Hypophosphatemic vitamin D-resistant rickets and osteomalacia.

Pseudodeficiency (vitamin D-dependent) rickets and osteomalacia.

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

Renal acidosis.

Pharmacological effect

Pharmaceutical group:

vitamin – calcium-phosphorus metabolism regulator.

Pharmaceutical action:

Alpha D3-Teva – vitamin, regulator of calcium-phosphorus metabolism. It is a precursor to the active metabolite of vitamin D3 – calcitriol. 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 level of parathyroid hormone in the blood.

By 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, and bone growth factors, which helps reduce the incidence of fractures.

In elderly patients, against the background of endocrine-immune dysfunction, including deficiency of D-hormone (calcitriol) production, there is a decrease in total muscle mass (sarcopenia) and the appearance of muscle weakness syndrome (due to disruption of the normal functioning of the neuromuscular system), which is accompanied by an increased risk of falls and resulting injuries and fractures. A number of studies have shown a significant reduction in the incidence of falls in elderly patients when using alfacalcidol.

Pharmacokinetics:

Suction

After oral administration, alfacalcidol is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved 8-12 hours after a single dose of alfacalcidol.

Metabolism

The conversion of alfacalcidol to calcitriol (1.25-dihydroxycolecalciferol) occurs in the liver by hydroxylation at carbon 25, and the hydroxylation process occurs very quickly (it is substrate-dependent). Unlike native vitamin D, alfacalcidol does not require hydroxylation in the kidneys, therefore it is effective even in patients with reduced activity of renal 1-alpha-hydroxylase (kidney pathology, old age).

Removal

T1/2 is 35 hours. It is excreted by the kidneys and through the intestines with bile in approximately equal shares.

Special instructions

Therapy must be carried out under constant monitoring of the concentration of calcium and phosphate in the blood (at the beginning of treatment – once a week, upon reaching and throughout the entire period of treatment – the concentration of calcium in plasma and urine every 3-5 weeks), as well as the activity of alkaline phosphatase (ALP) (for chronic renal failure – weekly monitoring). In case of chronic renal failure, preliminary correction of hyperphosphatemia is required.

When normalizing the content of alkaline phosphatase in the blood plasma, it is necessary to reduce the dose of the drug Alpha D 3 -Teva, which will avoid the development of hypercalcemia. Hypercalcemia or hypercalciuria can be corrected by discontinuing the drug and reducing calcium intake until the concentration of calcium in the blood plasma is normalized.

Typically this period is 1 week. After normalization, therapy is continued, prescribing half the last dose used. It should be borne in mind that sensitivity to vitamin D varies from patient to patient, and in some patients taking even therapeutic doses can cause symptoms of hypervitaminosis.

Children who receive vitamin D for a long time are at increased risk of stunted growth. To prevent hypovitaminosis D, a balanced diet is most preferable.

In old age, the need for vitamin D may increase due to a decrease in the absorption of vitamin D, a decrease in the skin’s ability to synthesize provitamin D3, a decrease in sun exposure, and an increase in the incidence of renal failure.

Active ingredient

Alfacalcidol

Composition

Active ingredient:

alfacalcidol – 0.25 mcg.

Excipients:

anhydrous citric acid – 0.015 mg,

propyl gallate – 0.02 mg,

D,L-α-tocopherol (vit. E) – 0.02 mg,

absolute ethanol – 1.145 mg,

peanut oil – up to 100 mg.

Composition of 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.

Composition of black food ink A10379:

shellac – 54%,

iron oxide black (E172) – 46%.

Pregnancy

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

Animal experiments have shown that calcitriol in doses 4-15 times higher than recommended doses for humans has a teratogenic effect.

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

The drug is contraindicated for use during breastfeeding.

Contraindications

Hypersensitivity to alfacalcidol and other components of the drug.
Hypercalcemia.
Hyperphosphatemia (except for hyperphosphatemia in hypoparathyroidism).
Hypermagnesemia.
Hypervitaminosis D.
Pregnancy (1st trimester).
Breastfeeding period.
Children under 3 years of age.

With caution when:

Nephrolithiasis.
Atherosclerosis.
Chronic heart failure.
Chronic renal failure.
Sarcoidosis or other granulomatosis.
Pulmonary tuberculosis (active form).
Pregnancy (II-III trimester).
In patients with an increased risk of developing hypercalcemia, especially in the presence of kidney stones.
Children over 3 years of age.

Side Effects

Anorexia, nausea, vomiting, heartburn, abdominal pain, 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 in high-density lipoproteins. In patients with severe renal impairment, hyperphosphatemia may develop.

Interaction

In the treatment of osteoporosis, it can be prescribed in combination with estrogens and antiresorptive drugs of different groups.
When Alpha D3-Teva is used simultaneously with digitalis preparations, the risk of developing heart rhythm disturbances increases.
When prescribed simultaneously with barbiturates, anticonvulsants and other drugs that activate microsomal oxidation enzymes in the liver, it is necessary to use a higher dose of Alpha D3-Teva.

The absorption of alfacalcidol is reduced when it is used together with mineral oil (for a long time), cholestyramine, colestipol, sucralfate, antacids, and albumin-based drugs.

When used simultaneously with Alpha D3-Teva antacids or laxative dialysis, the risk of developing hypermagnesemia increases.
The simultaneous administration of calcium supplements and thiazide diuretics increases the risk of developing hypercalcemia.

Vitamin D and its derivatives should not be prescribed during Alpha D3-Teva therapy due to possible additive interactions and an increased risk of hypercalcemia.

Overdose

Symptoms: early symptoms of hypervitaminosis D (due to 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, cloudy urine, heart rhythm disturbances, skin itching, increased blood pressure, conjunctival hyperemia, nephrolithiasis, weight loss, photophobia, pancreatitis, gastralgia. Rarely – psychosis (changes in mentality and mood).

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

Treatment: the drug should be discontinued. In the early stages of acute overdose – gastric lavage, administration of mineral oil (vaseline), which helps reduce absorption and increase excretion through the intestines. In severe cases, it may be necessary to carry out supportive treatment measures – hydration with the introduction of infusion saline solutions (forced diuresis), in some cases – the prescription of glucocorticosteroids, loop diuretics, bisphosphonates, calcitonin and hemodialysis using solutions with low calcium content.

It is recommended to monitor blood electrolytes, renal function and cardiac status using electrocardiogram data, especially in patients receiving digoxin.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Manufacturer

Catalent Germani Eberbach GmbH, Germany