Alfadol (Alphadol)

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

Each capsule contains:

Active substance: Alfacalcidol 0.25 μg.

Excipients: Butyl hydroxy anisole 0.009 mg, corn oil 89.99 mg, dehydrated ethanol (not detectable in the finished product):

Capsule shell composition: Gelatin 446.2 mg, glycerol 95.6 mg, sorbitol 70% solution 95.6 mg, methyl parahydroxybenzoate 2.4 mg, propyl parahydroxybenzoate 1.4 mg, water purified 358.6 mg, dye crimson [Ponso 4R] 0.2 mg, soybean oil (not found in the finished product).

Description:Transparent round soft gelatin capsules in red. Contents of capsules: light yellow transparent oily liquid.
Pharmacotherapeutic group:Vitamin - calcium-phosphorus exchange regulator
ATX: & nbsp

A.11.C.C.03   Alfacalcidol

Pharmacodynamics:

Remedy for vitamin deficiency D3. Regulator of phosphoric-calcium exchange. Alfacalcidol - the precursor of the active metabolite of the vitamin D3 - calcitriol. Affects the nuclei of target cells and stimulates the transcription of DNA and RNA in the intestinal epithelium of bone tissue, renal parenchyma and skeletal muscles. Increases the absorption of calcium and phosphate in the intestine and their reabsorption in the proximal tubules of the kidneys, increases bone mineralization due to stimulation, synthesis osteocalcin in the bone tissue, reduces the activity of alkaline phosphatase (APF) and the content of parathyroid hormone in the blood.

It restores a positive calcium balance in the treatment of calcium malabsorption syndrome, reduces the intensity of bone resorption and the frequency of fracture development. Duration of action - up to 48 hours.
Pharmacokinetics:

Alfacalcidol is fat-soluble, and its bioavailability when taken orally is 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 at the blood plasma reaches a maximum after 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;

- hypoparathyroidism and pseudohypoparathyroidism;

- vitamin D-resistant rickets and osteomalacia.

Contraindications:

Hypersensitivity to alfacalcidol and other components of the drug, intolerance to fructose, hypercalcemia, hyperphosphataemia (with the exception of hyperphosphatemia in hypoparathyroidism), hypermagnesia, hypervitaminosis D, pregnancy, the period of breastfeeding, children under 3 years of age, children under 12 years (for the treatment of osteoporosis, hypoparathyroidism and pseudohypoparathyroidism).

Carefully:With nephrolithiasis, atherosclerosis, chronic heart failure,chronic renal failure, sarcoidosis, or other granulomatosis; pulmonary tuberculosis (active form), pregnancy (II-III trimester), patients with an increased risk of hypercalcemia, especially in the presence of kidney stones, 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. 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 and children over 12 years of age:

The initial dose is 1 μg per day,

The maintenance dose is 0.25-2 μg per day.

In case of rickets and osteomalacia: from 1 to 3 mcg / day for a minimum of 2-3 months.

When hypoparathyroidism: from 1 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 osteoporosis (including postmenopausal, senile, steroid): from 0.5 to 1 mcg / day.

It is recommended to start treatment 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.

Children from 3 to 12 years:

In case of rickets and osteomalacia: from 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.

Side effects:

Clinically important adverse reactions: acute renal failure, impaired liver function.

From the digestive system: anorexia, vomiting ,. heartburn, abdominal pain, nausea, dry mouth, discomfort in the epigastric region, constipation, diarrhea, a slight increase in "hepatic" enzymes.

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

Co cardiovascular system: tachycardia, enhancement. Blood pressure (BP).

Allergic reactions: skin rash, itching.

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

Laboratory, indicators: hypercalcemia, a slight increase in the concentration of high density lipoproteins. In patients with severe renal dysfunction, the development of hyperphosphataemia is possible.

Overdose:

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

Late symptoms of hypervitaminosis D: dizziness, confusion, drowsiness, clouding of urine (the appearance in the urine of hyaline cylinders, proteinuria, leukocyturia), heart rhythm disturbance, cutaneous, itching, enhancement blood pressure; hyperemia conjunctiva, nephrolithiasis, weight loss, photophobia, pancreatitis, gastralgia, rarely - psychosis (changes in the psyche and mood).

Symptoms of chronic intoxication, vitamin D: calcification of soft tissues, blood vessels and internal organs (kidneys, lungs), arterial hypertension, renal and cardiovascular insufficiency up to the lethal outcome (these effects occur most often with hypercalcemia of hyperphosphatemia), growth disorders in children.

Treatment: Abolition of the drug before the normalization of calcium in the blood plasma (usually for 1 week); then treatment can be resumed at half the last dose applied. In the early periods of acute overdose - gastric lavage, the appointment mineral oil (vaseline), which helps to reduce absorption and increase excretion with caloric masses. In severe cases, supportive care activities may be required - hydration with the introduction of infusion salt solutions (forced diuresis), in some cases - the appointment of glucocorticosteroids, loop diuretics, bisphosphonates, calcitonin and hemodialysis using solutions with low calcium content.It is recommended to monitor the electrolyte content in the blood, the kidney function and the state of the heart according to the electrocardiogram, especially in patients receiving cardiac glycosides.

Interaction:

In the treatment of osteoporosis alfacalcidol can be administered in combination with estrogen and other drugs that reduce bone resorption.

Inductors of microsomal liver enzymes (incl. phenytoin and phenobarbital) are reduced, and inhibitors increase the concentration of alfacalcidol in the plasma (possibly - a change in its effectiveness).

Alfacalcidol increases the risk of heart rhythm disorders on the background of cardiac glycosides.

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. The toxic effect of alfacalcidol weakens retinol, tocopherol, ascorbic acid, pantothenic acid, thiamine, riboflavin.

Calcitonin, bisphosphonates, 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.

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:

During treatment, it is necessary to regularly check the concentration of calcium and phosphate in the blood plasma (at the beginning of treatment - once a week, when reaching the maximum concentration (Cmah) and throughout the treatment period - the concentration of calcium in the plasma and urine every 3-5 weeks), as well as the activity of AP (in chronic renal failure, weekly monitoring). With CRF, a preliminary correction of hyperphosphataemia is required.

When normalizing the content of alkaline phosphatase in blood plasma, it is necessary to reduce the dose of the drug Alfadol in order to avoid - the development of hypercalcemia.Hypercalcemia and hypercalciuria are corrected abolition of the drug and decrease in calcium intake to normalizing the calcium concentration in blood plasma, as a rule, it is usually 1 / week. After normalization, therapy is continued, appointing ½ the last dose applied.

It should be borne in mind that the sensitivity to vitamin D in different patients individual, and in a number of patients the administration of even therapeutic doses can cause hypervitaminosis.

Children receiving vitamin D for a long period of time, the risk of growth retardation increases.

For the prevention of hypovitaminosis D most preferably a balanced diet.

Alfacalcidol should be used with caution in patients with hypercalciuria, and particularly patients having kidney stones.

When taking Alfadol, children should start with low doses and gradually increase the dose under the control of calcium concentrations in plasma, as well as the ratio of calcium and creatinine in the urine. The drug should be used with caution in order to avoid an overdose.

In the elderly, the need for a vitamin D may increase as a result of a decrease Absorption of Vitamin D, reduce the ability of the skin to synthesize provitamin D3, reduce the time of insolation, the increase in the incidence of renal failure.
Effect on the ability to drive transp. cf. and fur:

One should refrain from managing vehicles and mechanisms that require an increased concentration of attention and speed of psychomotor reactions, since the use of the drug Alfadol may develop dizziness and drowsiness.

Form release / dosage:Capsules 0.25 μg.
Packaging:Primary packaging:

10 capsules in PVC / Aluminum foil blisters.

Secondary packaging:

For 3, 6 or 10 blisters with instructions for medical use in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription
Registration number:LP-001787
Date of registration:01.08.2012 / 20.05.2016
Expiration Date:01.08.2017
The owner of the registration certificate:Panacea Biotech Co., Ltd.Panacea Biotech Co., Ltd. India
Manufacturer: & nbsp
Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC
Information update date: & nbsp17.07.2017
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