Etafa - instructions for use, doses, side effects, contraindications

Alfacalcidol (1α-hydroxyvitamin D3) quickly turns into a liver in 1,25-dihydroxycholecalciferol - a metabolite of the vitamin D, which acts as a regulator of calcium and phosphorus metabolism. Inadequate endogenous synthesis in the kidneys 1,25-dihydroxycholecalciferol leads to disturbances in the metabolism of mineral salts. The drug increases the absorption of calcium and phosphorus in the intestine, increases their reabsorption in the kidneys, increases the mineralization of bone tissue, reduces the concentration of blood in the blood, parathyroid hormone. The main advantages of alfacalcidol in comparison with vitamin D - fast action and the possibility of a more accurate dose adjustment, which reduces the risk of hypercalcemia.

Pharmacokinetics:Alfacalcidol is metabolized mainly in the liver to form the active metabolite of 1,25-dihydroxycholecalciferol by hydroxylation with isoenzymes CYP27A1 and CYP3A4. Studies have shown that neither alfacalcidol, nor 1,25-dihydroxycholecalciferol does not inhibit the cytochrome P450 system.

Indications:Prophylaxis and treatment - renal osteodystrophy, treatment of secondary hyperparathyroidism in patients on hemodialysis with chronic renal failure 5 (terminal) stage.

Contraindications:

Hypersensitivity to the drug components

Hypercalcemia

Hyperphosphatemia

Hypermagnia

Hypervitaminosis D

The period of pregnancy and breastfeeding

Children under 12 years old

Long-term immobilization

Tuberculosis of the lungs (active form)

Carefully:

Carefully prescribe the drug for organic heart lesions; atherosclerosis; acute and chronic diseases of the liver and kidneys; nephrolithiasis in the anamnesis; diseases of the gastrointestinal tract (including gastric ulcer and 12the rectum); hypothyroidism; sarcoidosis, inactive forms of tuberculosis or other granulomatosis, as these conditions have a predisposition to increase the sensitivity to vitamin D.

Dosing and Administration:

Ampoules before use is necessary shake for 5 seconds.

The drug should be used immediately after dissection.

The drug Etalpha® is administered intravenously 3 times a week at the end of each hemodialysis session, bolus, for about 30 seconds in the return line of the device at the most approximate distance from the patient, Because of the absorption of alfacalcidol by plastic, an undesirable dose reduction may occur.

Patients on hemodialysis or peritoneal dialysis are advised to begin treatment when the concentration of intact parathyroid hormone in the blood serum more 300 ng / ml (33,0 nmol / l) to reduce it in the serum to a value of 150-300 ng / ml (16.5-33.0 nmol / l).

The dose of Ethal® should be determined for each individual patient under controlling the concentration of parathyroid hormone, concentration calcium, phosphate, calcium-phosphate compounds, activity of alkaline phosphatase in blood serum.

Adults

The recommended initial dose is 1 μg per 1 dialysis session. The dose may be increased with an interval of not less than 1 a week ₍until the controlled levels of laboratory indicators are within the limits of normal values.

The maximum recommended dose - 6 μg for 1 dialysis session, but no more than 12 mcg for a week.

In clinical practice, for children on hemodialysis or continuous ambulatory peritoneal dialysis, alfacalcidol in dosage forms for oral administration.

Elderly

When using the drug in elderly people on hemodialysis, at the age of 65 or more years, dose adjustment is not required^.

Patients with hepatic insufficiency

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

If the dose was missed - do not take a double dose of the drug. Continue to adhere to the proposed dosing regimen.

Side effects:

The most common undesirable effects of Ethal® are hypercalcemia; hypercalciuria and vitamin D-dependent toxicity.

The following are data on adverse adverse reactions, depending on their frequency occurrence. Unfavorable adverse reactions, other than signs of hypercalcemia, received as separate messages are also included.

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 based on available data)

Disorders from the metabolism and nutrition

Often:

Hypercalcemia

Infrequently:

Metastatic calcification, hyperphosphataemia, high content of calcium-phosphate compounds, anorexia

Frequency unknown:

Hypermagnesemia, decreased appetite

Immune system disorders:

Frequency unknown:

Hypersensitivity reactions with symptoms such as fever, chills, hives and swelling of the tongue.

Impaired nervous system:

Infrequently:

Headache, dysesthesia, dysgeusia

Disorders from the cardiovascular system:

Rarely:

Tachycardia, high blood pressure

Disorders from the gastrointestinal tract:

Infrequently:

Nausea, vomiting, abdominal pain, constipation, diarrhea, indigestion

Disturbances from the skin

Often:

Itchy skin

Frequency unknown:

Rash (erythematous, maculopapular, pustular), exfoliative dermatitis Disorders from the urinary system:

Often:

Hypercalciuria

Frequency unknown:

Renal failure, nephrocalcinosis

General disorders:

Rarely:

Calcification, asthenia and fatigue.

Overdose:

Early symptoms of 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 hypervitaminosis D: pain in the bones, clouding of urine (appearance of hyaline cylinders in the urine); increased blood pressure, itchy skin; photophobia; hyperemia of the conjunctiva, arrhythmia; drowsiness; myalgia; nausea; vomiting; decreased body weight; rarely - a change in the psyche and mood; confusion of consciousness.

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

The concentration 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 discontinuation of calcium supplements.

In severe cases of acute accidental overdose and persistent hypercalcemia, generalsupporting activities.

In case of an overdose, the drug should be discontinued. In severe cases (calcium concentration in the serum of blood more than 3 mmol / l) may be required carrying out supportive medical measures - 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. The content control is mandatory electrolytes in blood serum (especially calcium), kidney function and heart condition (according to the electrocardiogram) especially in patients taking digoxin (or other cardiac glycosides).

Interaction:

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

With the simultaneous use of alfacalcidol with cardiac glycosides, the risk of arrhythmia increases.

Absorption of alfacalcidol It 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, etidronic and pamidronic acid derivatives, plikamycin, gallium nitrate and glucocorticosteroids reduce the effect 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 concentration of magnesium in the blood, and aluminum-containing antacids - aluminum in the blood, especially in chronic kidney failure.

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

Special instructions:

The drug Ethal contains 10% by volume. ethanol, which corresponds to 240 mg of ethanol in a single dose of alfacalcidol. This should be taken into account in patients with alcoholism.

The drug contains less than 1 mmol sodium (23 mg) per 1 μg alfacalcidol.

One should pay attention to patients taking cardiac glycosides, since 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 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 application of the drug Etagol, it is necessary to regularly monitor the concentration calcium, phosphate, calcium-phosphate compounds, activity of alkaline phosphatase and concentration of parathyroid hormone in serum.

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 damage to the bones, for example, hypoparathyroidism and if the calcium content in the plasma is already increased, as well as in later stages of treatment in the presence of signs of restoration of the structure of bone tissue.The risk of developing hypercalcemia is determined by such factors as the degree of demineralization bone, the functional capacity of the kidneys, and the dose of Ethal's preparation. Appearance hypercalcemia may 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 restoring the structure of bone tissue (normalization of the activity of alkaline phosphatase in the blood)! It should be prevented the development of prolonged hypercalcemia, especially in chronic renal, insufficiency, focusing on such factors as the concentration in the blood serum of calcium, the activity of alkaline phosphatase, parathyroid hormone, the amount of calcium excreted in the urine, X-ray and biochemical data.

With the development of hypercalcemia or persistent increase in the concentration of calcium-phosphate compounds,the drug should be immediately canceled, at least until these parameters are normalized (usually within one week), then the drug can be prescribed again at a dose that is half of the previous one.

Patients with severe bone damage (unlike patients with renal insufficiency) can tolerate higher dose of the drug without signs of hypercalcemia. The absence of a rapid increase in the calcium content at serum 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 who are on dialysis, the concentration of parathyroid hormone in the serum should be no lower than 2-3 times the upper limit of the norm.

In order to prevent the development of hyperphosphataemia in patients with bone lesions of renal genesis, Etagol's preparation can be administered together with phosphate binding agents.

Effect on the ability to drive transp. cf. and fur:

Ethalph has little or no effect on the ability to drive and complex machinery.

Form release / dosage:

Solution for intravenous administration.

Packaging:

For 0.5 ml or 1 ml of the drug in the ampoule of a neutral brown light-protective glass (type I). The ampoule has a dot for the fracture of the ampoule.

10 ampoules in a plastic pallet with instructions for use are placed in a cardboard box.

Storage conditions:

At a temperature of 2 to 8 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012029 / 03

Date of registration:28.10.2011

Date of cancellation:2017-11-27

The owner of the registration certificate:Leo Pharmaceutical Products Co., Ltd. A / S (Leo Pharma A / S) Leo Pharmaceutical Products Co., Ltd. A / S (Leo Pharma A / S) Denmark

Manufacturer: & nbsp

LEO Pharmaceutical Products Ltd. A / S (LEO Pharma A / S) Denmark

Representation: & nbspNycomed Distribution Ltd.Nycomed Distribution Ltd.

Information update date: & nbsp27.11.2017

Illustrated instructions

Instructions

Ethal® (Etalpha®)