ETALFA

Active material: Alfacalcidol
When ATH: A11CC03
CCF: Preparation, regulates the exchange of calcium and phosphorus
ICD-10 codes (testimony): E20.0, E20.1, E55, E55.0, E58, E83.3, E89.2, M81.0, M81.1, M81.2, M81.4, M81.8, M82, M83, N25.0
Manufacturer: LEO PHARMACEUTICAL PRODUCTS (Denmark)

Pharmaceutical form, composition and packaging

Capsules soft gelatin, Oval, yellowish-white; contents of capsules – You oily mass from colorless to light yellow in colour.

Excipients: sesame oil refined, a-токоферол (wreathed. IS).

The composition of the shell: gelatin, glycerol, potassium sorbate, Titanium dioxide.

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Capsules soft gelatin, Oval, dark brown; contents of capsules – You oily mass from colorless to light yellow in colour.

Excipients: sesame oil refined, a-токоферол (wreathed. IS).

The composition of the shell: gelatin, glycerol, potassium sorbate, iron oxide black, iron oxide red.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Drops for intake Colorless, clear or slightly opalescent.

Excipients: citric acid monohydrate, ethanol, makrogolglicerolgidroksistearat, metilparagidroksiʙenzoat, sodium citrate, sorbitol, a-токоферол (wreathed. IS), Purified water.

20 ml – dark glass bottles with a dropper (1) – packs cardboard.

The solution for the on / in the colorless, clear.

Excipients: citric acid monohydrate, ethanol, sodium citrate, propylene glycol, water d / and.

0.5 ml – vials of dark glass (10) – trays, plastic (1) – packs cardboard.
1 ml – vials of dark glass (10) – trays, plastic (1) – packs cardboard

Pharmacological action

Alfacalcidol (1α-gidroksivitamin (D)₃) quickly turns into a liver in 1.25-digidroksivitamin D₃ – metabolite of vitamin D, which acts as the regulator of calcium and phosphorus. Insufficient endogenous synthesis in the kidneys-1.25 digidroksivitamina (D)₃ leads to violations of metabolism of mineral salts. The drug increases the absorption of calcium and phosphorus in the gut, increases their reabsorbqiyu in the kidneys, increases bone mineralization, decreases in the blood concentration of parathyroid hormone.

The main advantages of Jetalfa compared with vitamin D – fast action and the possibility of a more precise dose management, that reduces the risk of hypercalcemia.

Pharmacokinetics

Absorption and metabolism

Zhirorastvorim alfacalcidol, its bioavailability when administered – about 100%.

After intake alfacalcidol metabolised in the liver with the formation of the active metabolita 1.25-digidroksivitamina D₃. FROM_max 1.25-digidroksivitamina (D)₃ plasma levels achieved after 8-12 hours after a single dose alfakalzidola.

Deduction

T_1/2 1.25-digidroksivitamina (D)₃ – about 35 no. Report kidneys and jelchew roughly the same number of.

Testimony

Disease, caused by the exchange of calcium and phosphorus due to insufficient endogenous synthesis of 1.25-digidroksivitamina D₃:

— Renal osteodistrofia;

- Osteoporosis (incl. postmenopauzny, senile, steroidal);

-postsurgical or idiopathic hypoparathyreosis;

— psevdogipoparatireoz;

-Vitamin D-dependent rickets (incl. congenital);

-Vitamin D-resistant rickets;

-rickets, associated with malabsorbziei and malnutrition;

- Osteomalacia;

- Hypocalcemia;

-of calcium malabsorption.

Dosage regimen

The drug is prescribed inside (regardless of the meal) or / 1 time / day. Duration of treatment is determined by the physician individually in each case and depends on the nature of the disease and the effectiveness of therapy.

Ampoule before use it is necessary to shake a few times.

Drops should not be diluted before use.

Adult

At osteomalacia drug prescribed oral dose 1-3 mg / day.

At gipoparatireoze – 2-4 mg / day.

At osteodystrophies in patients with chronic renal insufficiency – to 2 mg / day.

Jetalfa is introduced in the/in gemodialise after each session in the form of bolusa approximately 30 s return line apparatus to maximally distance from patient, because absorption alfakalzidola plastic can occur undesired reduction of dosage.

The initial dose – 1 ug 1 dialysis session. The maximum dose – 6 mcg for dialysis session and no more than 12 micrograms per week. For the solution of the drug Jetalfa not required additional breeding.

At postmenopauzne, senilnom, steroidnom and other types of osteoporosis daily dose is 0.5-1 g.

It is recommended to begin treatment with minimal doses, controlling 1 Once a week the concentration of calcium and phosphorus in the blood plasma. Dose can be increased to 0.25 or 0.5 mcg/day to stabilize the biochemical parameters. When you reach the minimum effective dose to control the concentration of calcium in the blood plasma every 3-5 weeks.

In young children recommended use of the drug Jetalfa in the form of drops (dispensing and receiving medication in capsule form is difficult).

At body weight <20 kg the drug is prescribed on the basis of 0.01-0.05 ug / kg / day.

At body mass index ≥ 20 kg – 1 mg / day (except in the case of renal osteodystrophies).

At renal osteodystrophy children dose is 0.04-0.08 ug / kg / day. Dose determined in accordance with the dynamics of biochemical parameters in order to prevent gipercalziemii.

Side effect

Metabolism: giperfosfatemiя, a small increase in blood HDL, hypercalcemia symptoms: diarrhea, constipation, nausea, vomiting, dry mouth, anorexia, metallic taste in mouth, pancreatitis, gastralgia, clouding of urine, nephrolithiasis, thamuria / nocturia, hypercalciuria, polyuria, polydipsia; headache, dizziness, confusion, drowsiness, rarely – psychosis (a change of mentality and mood), myalgia, ostealgias, heart rhythm disturbance, increased blood pressure; fatiguability, generalized weakness, conjunctival hyperemia, photophobia, itching, calcification of soft tissues, blood vessels and internal organs (incl. kidney, light), weight loss, renal and cardiovascular collapse until death (most often arise when acceding to the gipercalziemii giperfosfatemii), dysplasia in children.

From the urinary system: nephrocalcinosis, renal failure, mild-to-moderate severity (with prolonged hypercalcemia).

For the skin: itching, rash, hives.

Contraindications

- Hypercalcemia;

- hypervitaminosis D;

— giperfosfatemia (except giperfosfatemii at gipoparatireoze);

- Gipermagniemiya;

- Hypersensitivity to the drug (incl. by propilenglikolu, part of the solution for injection).

FROM caution You should apply at nefrolitiaze, atherosclerosis, Heart Failure, renal failure, Sarcoidosis, in patients with a high risk of hypercalcemia, especially when there urolithiasis, patients, receiving cardiac glycosides or drugs naperstanki (in gipercalziemii increases the risk of arrhythmia).

Pregnancy and lactation

Clinical experience of use in pregnancy and lactation is missing, Therefore, the issue of the appointment of the drug in this category of patients, the physician decides individually. As a result of hypercalcemia during pregnancy possible fetal defects.

Cautions

Be wary appoint patients, predisposed to the development of hypercalcemia, especially when there urolithiasis.

During treatment may develop hypercalcemia, Therefore, patients should be informed about the clinical symptoms of this condition.

During treatment requires regular monitoring of the concentration of calcium and phosphorus in serum. Calcium concentration should be measured once a week or a month, depending on the clinical situation. More frequent definition of calcium requires early treatment, especially in States without significant bone lesions, eg, gipoparatireoze, and, If the content of calcium in plasma already promoted, as well as in the later stages of treatment if there are signs of recovery of bone structure. The risk of hypercalcemia is determined by factors such, as the degree of bone demineralization, functional ability of kidneys and a dose of Jetalfy.

Occurrence of hypercalcemia may be due to, that timely and adequate dose is not reduced when there are biochemical signs of recovery of bone structure (normalization of ALP in blood). Should prevent prolonged hypercalcemia, especially in chronic renal failure, focusing on such indicators, as the concentration of serum calcium, Alkaline phosphatase, parathyroid hormone, the amount of calcium, excreted with urine, radiological and histological data.

With the development of hypercalcemia drug should be lifted immediately so far, While calcium concentration in the serum is not normalized (usually within a week), then you can assign product again in a dose, component of the half from the previous.

Patients with lesions of bone (In contrast to patients with renal insufficiency) can carry the drug in higher doses without signs of hypercalcemia. The absence of rapid increase in the calcium content in the serum of patients with osteomalacia does not necessarily mean, that should be increased dose, tk. Calcium can penetrate into demineralised bone due to its increased absorption in the gut.

In order to prevent the development of giperfosfatemii in patients with bone lesion of renal origin, drug Jetalfa may be nominated together with fosfatsvjazyvajushhimi means.

In osteoporosis use Jetalfy you can combine with estrogenami and antirezorbtivei drugs. Jetalfu should not be administered concomitantly with other drugs vitamin D and its derivatives.

Effects on ability to drive vehicles and management mechanisms

When taking the drug in the therapeutic dose effects on driving and complicated mechanisms have been identified.

Overdose

Symptoms: early symptoms gipervitaminoza (D) (due to hypercalcemia) – diarrhea, constipation, nausea, vomiting, dry mouth, anorexia, metallic taste in mouth, hypercalciuria, polyuria, polydipsia, thamuria / nocturia, headache, fatiguability, generalized weakness, myalgia, ostealgias; later symptoms gipervitaminoza (D) – dizziness, confusion, drowsiness, clouding of urine, heart rhythm disturbance, itching, increased blood pressure, conjunctival hyperemia, nephrolithiasis, weight loss, photophobia, pancreatitis, gastralgia, rarely – psychosis (a change of mentality and mood); symptoms of chronic intoxication vitamin D – calcification of soft tissues, blood vessels and internal organs (kidney, light), renal and cardiovascular collapse until death, dysplasia in children.

Treatment: the drug should be discontinued. In the early stages of acute overdose taken inside the drug – gastric lavage and/or the appointment of mineral oil (Vaseline), conducive to reducing the intake and increase the excretion of faeces. In severe cases, you may need to support healing events – with the introduction of infusion hydration salt solutions (forced diuresis), in some cases – GCS assignment, “loop” diuretics, ʙisfosfonatov, calcitonin and dialysis using solutions with low calcium. We recommend that you control the content of electrolytes in the blood, kidney function and condition of the heart (According to ECG) especially in patients, receiving digoxin.

Drug Interactions

Together with the appointment of barbiturates or anticonvulsants, which activate enzymes mikrosomalnogo oxidation in the liver, You may need a higher dose of Jetalfy.

Alfacalcidol increases the risk of heart rhythm problems when taken against the backdrop of cardiac glycosides and drugs naperstanki.

Calcitonin, derived etidronovoy and Pamidronic acids, plikamicin, Gallium nitrate and GKS reduces effect alfakalzidola.

Suction decreases when its alfakalzidola joint application with kolestiraminom, kolestipolom, mineral oil, sukralfatom, antaцidami.

Concomitant therapy magnisoderjasimi antacids and vitamin D can cause increasing the concentration of magnesium in the blood, and with antatidami aljuminijsoderzhashhimi – increasing the concentration of aluminum in the blood, especially in chronic renal failure.

Kalcijsoderzhashhie drugs in high dose and thiazide diuretics in combination with vitamin D increases the risk of hypercalcemia. Phosphorus-containing drugs combined with the high dose vitamin D increases the likelihood of giperfosfatemii. The simultaneous use of different analogues of vitamin D is accompanied by the additive effect with the development of hypercalcemia.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

Preparation in the form of capsules should be stored at a temperature of no higher than 25° c, in the form of drops reception inside and solution for injection – at a temperature of from 2 ° to 8 ° C.. Keep out of the reach of children. Shelf life – 3 year.

An opened bottle of liquor for the reception inside should be retained for 28 days at a temperature of from 2 ° to 8 ° C..