Alfacalcidol Canon (Capsules) Instructions for Use

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

Manufactured By

Novamedica Innotech, LLC (Russia)

ATC Code

A11CC03 (Alfacalcidol)

Active Substance

Alfacalcidol (Rec.INN registered by WHO)

Dosage Forms

	Alfacalcidol Canon	Capsules 0.25 mcg: 30 or 60 pcs.
		Capsules 1 mcg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Capsules gelatinous, transparent, oval, soft, reddish-brown in color; the contents of the capsules are a colorless or light yellow to yellow-brown oily liquid.

Excipients: peanut oil – 98.79975 mg, citric acid – 0.015 mg, propyl gallate – 0.02 mg, alpha-tocopherol – 0.02 mg, ethyl alcohol – 1.145 mg.

Soft gelatin capsule shell: anhydrous sorbitol – 12.45 mg, glycerol 85% – 18.38 mg, gelatin – 78.32 mg, iron oxide red dye – 0.85 mg.

10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
30 pcs. – jars – cardboard packs.
60 pcs. – jars – cardboard packs.

Capsules gelatinous, transparent, oval, soft, light yellow in color; the contents of the capsules are a colorless or light yellow to yellow-brown oily liquid.

Excipients: peanut oil – 98.8 mg, citric acid (anhydrous) – 0.015 mg, propyl gallate – 0.02 mg, alpha-tocopherol – 0.02 mg, ethyl alcohol (ethanol) – 1.144 mg.

Composition of the soft gelatin capsule shell: sorbitol partially dehydrated – 12.39 mg, glycerol – 18.67 mg, gelatin – 77.8 mg, iron oxide yellow dye – 0.08 mg, titanium dioxide – 1.06 mg.

10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
30 pcs. – jars – cardboard packs.
60 pcs. – jars – cardboard packs.

Clinical-Pharmacological Group

Drug regulating calcium and phosphorus metabolism

Pharmacotherapeutic Group

Vitamins; vitamin A and D, including their combinations; vitamin D and its analogues

Pharmacological Action

Regulator of calcium and phosphorus metabolism, 1α-hydroxyvitamin D₃. It causes an increase in the absorption of calcium and phosphorus in the intestine, an increase in their reabsorption in the kidneys; regulates bone tissue mineralization. It restores positive calcium balance in the treatment of calcium malabsorption syndrome and reduces the concentration of parathyroid hormone in the blood.

By affecting both parts of the bone remodeling process (resorption and synthesis), Alfacalcidol not only increases bone tissue mineralization but also increases its elasticity by stimulating the synthesis of bone matrix proteins, bone morphogenetic proteins, and bone growth factors, which contributes to a reduction in the incidence of fractures.

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

Alfacalcidol stimulates the regeneration of muscle fibers, which restores lost muscle tone.

Pharmacokinetics

After oral administration, Alfacalcidol is rapidly absorbed from the gastrointestinal tract. The T_max of the active substance in blood plasma ranges from 8 to 18 hours.

Alfacalcidol is metabolized in the liver to form the main active metabolite calcitriol (1α,25-dihydroxyvitamin D₃). A smaller part of the active substance is metabolized in bone tissue.

Indications

Osteodystrophy (including in chronic renal failure), hypoparathyroidism and pseudohypoparathyroidism, rickets and osteomalacia of various origins, osteoporosis (including postmenopausal, senile, steroid), renal acidosis, Fanconi syndrome (hereditary renal acidosis with nephrocalcinosis, late rickets, and adiposogenital dystrophy).

ICD codes

Dosage Regimen

Determine the dosage individually based on disease severity, biochemical parameters, and clinical response.

For adults, the typical daily dose ranges from 0.07 mcg to 20 mcg.

For children over 3 years, administer a daily dose of 0.01-0.08 mcg per kg of body weight.

Initiate therapy with a low dose, then titrate gradually.

Adjust the dose to maintain serum calcium within the normal range and to control symptoms of the underlying disease.

For renal osteodystrophy, start with 0.07-0.14 mcg daily. For hypoparathyroidism, initiate with 0.14-0.28 mcg daily.

In postmenopausal osteoporosis, a dose of 0.5-1.0 mcg daily is often used.

Administer the total daily dose orally in one or two divided doses.

Monitor serum calcium, phosphate, and creatinine levels regularly, especially after dose changes.

Reduce the dose or temporarily discontinue treatment if hypercalcemia or hypercalciuria occurs.

Resume therapy at a lower dose after calcium levels normalize.

Ensure adequate, unrestricted calcium intake from diet or supplements unless contraindicated.

In patients with renal impairment, dose adjustment is not typically required as alfacalcidol does not require renal hydroxylation.

Use with particular caution in patients with predisposition to hypercalcemia.

Adverse Reactions

From the digestive system: anorexia, nausea, vomiting, dry mouth, discomfort in the epigastric region, constipation; rarely – a slight increase in ALT, AST activity.

From the central nervous system: weakness, fatigue, dizziness, drowsiness.

From the cardiovascular system: tachycardia.

Allergic reactions: skin rash, itching.

From metabolism: rarely – an increase in HDL in plasma; with severe renal impairment – hyperphosphatemia.

Contraindications

Hypercalcemia, hyperphosphatemia (except for hyperphosphatemia in hyperparathyroidism), hypermagnesemia, hypervitaminosis D, lactation period (breastfeeding), children under 3 years of age, hypersensitivity to alfacalcidol.

Use in Pregnancy and Lactation

Use during pregnancy is possible only in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

Use during lactation (breastfeeding) is contraindicated.

Use in Renal Impairment

Use with caution in patients with an increased risk of developing hypercalcemia, especially with urolithiasis.

Pediatric Use

The daily dose for children is 0.01-0.08 mcg/kg.

Special Precautions

Use with caution in patients with nephrolithiasis, atherosclerosis, chronic heart failure, chronic renal failure, with sarcoidosis or other granulomatoses, pulmonary tuberculosis (active form), in patients with an increased risk of developing hypercalcemia, especially in the presence of urolithiasis, in children over 3 years of age.

During treatment, the level of calcium in blood plasma and urine should be regularly monitored, the development of the therapeutic effect should be observed, and the dose of alfacalcidol should be adjusted if necessary to avoid the development of hypercalcemia and hypercalciuria.

Unlike natural vitamin D, Alfacalcidol is not metabolized in the kidneys. There are reports of the effectiveness of alfacalcidol in secondary hyperparathyroidism caused by renal failure.

Drug Interactions

With simultaneous use with agents that cause induction of liver microsomal enzymes, the therapeutic effect of alfacalcidol decreases (a higher dose of alfacalcidol should be used).

With simultaneous use of alfacalcidol with digitalis preparations, the risk of arrhythmia increases; with calcium preparations, thiazide diuretics – the risk of hypercalcemia increases; with antacids or laxatives – the risk of hypermagnesemia increases.

Antiepileptic drugs, phenytoin, barbiturates, reduce the effectiveness of alfacalcidol; mineral oils, cholestyramine, colestipol, sucralfate, antacids, albumin reduce its absorption. Simultaneous laxative dialysis increases the risk of hypermagnesemia and hyperaluminemia.

Should not be used simultaneously with colecalciferol (vitamin D) and its derivatives.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.