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

For capsules of 0.25 μg: soft gelatin capsules oval-shaped yellowish white. The contents of the capsules are a transparent oily mass from colorless to light yellow.

For capsules of 1 μg: soft gelatin capsules oval-shaped brown. The contents of the capsules are a transparent oily mass from colorless to light yellow.

Pharmacotherapeutic group:Vitamin - calcium-phosphorus exchange regulator

ATX: & nbsp

A.11.C.C.03 Alfacalcidol

Pharmacodynamics:

Alfacalcidol (1α-hydroxyvitamin D3) quickly turns into a liver in 1,25-dihydroxyvitamin D3 - a metabolite of a vitamin D, which acts as a regulator of calcium and phosphorus metabolism. Inadequate endogenous synthesis in the kidneys of 1,25-dihydroxyvitamin D3 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 parathyroid hormone in the blood. The main advantages of alfacalcidol in comparison with vitamin D - rapid action and the possibility of more precise dose adjustment, which reduces the risk of hypercalcemia.

Pharmacokinetics:

Alfacalcidol is fat-soluble and its bioavailability when taken orally - about 100%.After suction alfacalcidol metabolized in the liver with the formation of an active metabolite dihydroxyvitamin D3. The concentration of 1,25-dihydroxyvitamin D3 in blood plasma reaches a maximum in 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 the components of the drug, including sesame

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; nephrourolythisis in the anamnesis; diseases of the gastrointestinal tract (including gastric ulcer and duodenal ulcer); hypothyroidism; sarcoidosis, tuberculosis or other granulomatosis, as these conditions have a predisposition to increase the sensitivity to vitamin D.

Dosing and Administration:

The drug is used inside regardless of food intake, without chewing, squeezed with enough liquid, once a day. The duration of treatment is determined by the doctor individually in each case and depends on the nature of the disease and the effectiveness of therapy.

Adults and children weighing more than 20 kg

The initial dose of -1 mcg per day

The maintenance dose is 0.25 - 2 μg per day

With rickets and osteomalacia - from 1 to 3 mcg per day;

With hypoparathyroidism -1-4 mcg per day;

In osteodystrophy in chronic renal failure, 0.5 to 2 μg per day;

In osteoporosis (including postmenopausal, senile, steroid, etc.) - 0.5-1 mcg per day.

Begin treatment is recommended 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 μg / 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.

Side effects:

The most common undesirable effects of the drug Etalph® are hypercalcaemia, hypercalciuria and vitamin D-dependent toxicity.

The following are data on adverse adverse reactions, depending on the frequency of their occurrence. Adverse adverse reactions other than signs of hypercalcemia, obtained as separate reports, are also included.

Very often> 1/10 Frequently> 1/100 and <1/10 Not infrequent> 1/1000 and <1/100 Rare> 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 calcifications, hyperphosphataemia, high content of calcium phosphate compounds, anorexia

Frequency unknown:

Hypermagnesemia, decreased appetite, weight loss, dehydration, growth arrest, albuminuria, hypercholesterolemia, increased levels ACT and ALT in serum

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

Rarely:

Disorders of the psyche, hallucinations, coma, apathy

Frequency unknown:

Hyperthermia

Disorders from the cardiovascular system:

Rarely:

Tachycardia, high blood pressure

Disorders from the gastrointestinal tract:

Infrequently:

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

Rarely:

Acute pancreatitis

Frequency unknown:

Ulceration of the tongue, ulceration of the gums, polydipsia

Disturbances from the skin

Often:

Itchy skin

Rarely:

Erythema multiforme, psoriasis

Frequency unknown:

Rash (erythematous, maculopapular, pusteleznaya), exfoliative dermatitis

Impaired sensory organs:

Rarely:

Calcification of the conjunctiva and sclera

Disturbances from the respiratory system:

Frequency unknown:

Rhinitis

Disorders from the urinary system:

Often:

Hypercalciuria, increased serum creatinine and urea levels

Frequency unknown:

Renal failure, nephrocalcinosis, urinary tract infection

Disorders from the reproductive system:

Frequency unknown:

Decreased libido

General disorders:

Rarely:

Calcification, asthenia and fatigue

Overdose:

Early symptoms of vitamin 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 vitamin 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 level 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 stopping the intake of calcium supplements.

In severe cases of acute accidental overdose and persistent hypercalcemia, general supportive measures should be taken.

In case of an overdose, the drug should be discontinued. In the early periods of acute overdosage, gastric lavage and / or ingestion of mineral oil (vaseline) is shown, which helps to reduce absorption and increase the excretion of the drug through the intestine. In severe cases (serum calcium level> 3 mmol / L), it may be necessary to carry out maintenance treatments - 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.It is mandatory to monitor the content of electrolytes in the blood serum (especially calcium), kidney function and heart condition (according to the electrocardiogram) especially in patients taking digoxin (or other digitalis preparations).

Interaction:

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

With the simultaneous use of alfacalcidol with digitalis drugs, the risk of arrhythmia increases.

Absorption of alfacalcidol 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, derivatives of etidronic and pamidronic acids, 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.

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 accompanied by additive action with the development of hypercalcemia. Ethyl® should not be administered concomitantly with other vitamin preparations D and its derivatives.

Special instructions:

Pay attention to patients taking cardiac glycosides, as 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 effectiveness of alfacalcidol is generally maintained in patients with reduced liver function. In severe hepatic insufficiency, the concentration of the active metabolite of 1,25-dihydroxyvitamin D can be reduced by decreasing the hydroxylation process or by decreasing the enterohepatic circulation. In this case, it may be necessary to administer the drug at higher doses.

When applying the drug in the elderly, dose adjustments are not required

The drug may contribute to the development of hypercalcemia, so patients should inform about the clinical symptoms of this condition (see section "Overdose").

During the use of the preparation of Ethal® it is necessary to regularly monitor the concentration of calcium, phosphate, calcium-phosphate compounds, alkaline phosphatase and the level of parathyroid hormone in the blood 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 bone damage, for example, hypoparathyroidism, and if the calcium content in the plasma is already increased, as well as at later stages of treatment with signs of bone structure restoration. The risk of developing hypercalcemia is determined by such factors as the degree of bone demineralization, the functional capacity of the kidneys and the dose of Ethal®.The appearance of 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 alkaline phosphatase in the blood). It is necessary to prevent the development of prolonged hypercalcemia, especially in chronic renal failure, focusing on such factors as concentration in the serum of calcium, alkaline phosphatase, parathyroid hormone, the amount of calcium excreted in the urine, radiologic and biochemical data.

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

Patients with severe bone damage (in contrast to patients with renal insufficiency) can tolerate higher doses of the drug without signs of hypercalcemia. The lack of a rapid increase in serum calcium 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 on dialysis, the level of parathyroid hormone in serum should be consistent with the current treatment guidelines.

In order to prevent the development of hyperphosphataemia in patients with lesions of the kidneys of the kidney genesis, the preparation of Ethal® can be administered together with phosphate binding means.

In the case of osteoporosis, the use of Ethal® can be combined with estrogens and antiresorptive drugs.

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

Ethal® does not or does not significantly affect the ability to drive and complex machinery.

Form release / dosage:Capsules 0.25 μg, 1.0 μg.

Packaging:

Capsules 0.25 μg:

10 capsules are packed in a blister pack of PVC / aluminum foil, on the one hand, the blister pack is covered with an aluminum foil / PVC film.

For 3 or 10 blister packs are placed in a cardboard box with instructions for use.

Capsules 1 μg:

10 capsules are packed in a blister pack of PVC / aluminum foil, on the one hand, the blister pack is covered with an aluminum foil / PVC film.

For 1, 3 or 10 blister packs are placed in a cardboard box with instructions for use.

Storage conditions:

At a temperature not higher than + 25 ° С.

Keep out of the reach of children.

Shelf life:2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012029 / 01

Date of registration:05.04.2011

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®)