Eralphon, 2000 me 1 ml 10 pcs

ATX code: WHOHA

Pharmacological properties

Pharmacodynamics

Epoetin alfa is a glycoprotein specifically stimulating erythropoiesis, activates cytosis and erythrocyte maturation from erythrocyte progenitor cells. Recombinant epoetin alfa is synthesized in mammalian cells, in which the gene encoding human erythropoietin is embedded. By its composition, biological and immunological properties epoetin alpha is identical to natural human erythropoietin. Administration of epoetin alfa leads to increased levels of hemoglobin and hematocrit, improved blood supply to tissues and heart function. The most pronounced effect of epoetin alfa administration is observed in anemia caused by chronic renal failure. In very rare cases during long-term use of erythropoietin for therapy of anemic conditions formation of neutralizing antibodies to erythropoietin with development of partial red cell aplasia or without it may be observed.

Pharmacokinetics

In intravenous administration of epoetin alfa in healthy persons and patients with uremia the elimination half-life is 5-6 hours. When epoetin alfa is administered subcutaneously its concentration in blood increases slowly and reaches maximum in 12 to 18 hours after administration, the period of semi-elimination is 16-24 hours. Bioavailability of epoetin alfa when administered subcutaneously is 25-40%. It does not cumulate.

Indications

– anemia in patients with chronic renal failure, including those on hemodialysis;

– prevention and treatment of anemia in patients with solid tumors, whose anemia was a consequence of antitumor therapy;

– prevention and treatment of anemia in patients infected with the human immunodeficiency virus (HIV) caused by the use of zidovudine, with endogenous erythropoietin levels less than 500 IU/ml;

– prevention and treatment of anemia in patients with multiple myeloma, low-grade non-Hodgkin lymphoma, chronic lymphocytic leukemia, in patients with rheumatoid arthritis;

– treatment and prevention of anemia in premature babies born with low body weight up to 1.5 kg;

– as part of a predeposit program before major surgery in patients with a hematocrit level of 33-39%, to facilitate the collection of autologous blood and reduce the risk associated with the use of allogeneic blood transfusions if the expected need for transfusion exceeds the amount that can be obtained by autologous collection without the use of epoetin alfa;

– before major surgery with an expected blood loss of 900-1800 ml in adult patients without anemia or with mild to moderate anemia (hemoglobin level 100-130 g/l) to reduce the need for allogeneic blood transfusions and facilitate the restoration of erythropoiesis.

Pharmacological effect

ATC code: VOZHA

Pharmacological properties

Pharmacodynamics

Epoetin alpha is a glycoprotein that specifically stimulates erythropoiesis, activates the cytosis and maturation of erythrocytes from erythrocyte precursor cells. Recombinant epoetin alfa is synthesized in mammalian cells into which the gene encoding human erythropoietin is integrated. In its composition, biological and immunological properties, epoetin alfa is identical to natural human erythropoietin. The administration of epoetin alfa leads to an increase in hemoglobin and hematocrit levels, improving blood supply to tissues and heart function. The most pronounced effect of the use of epoetin alfa is observed in anemia caused by chronic renal failure. In very rare cases, with long-term use of erythropoietin for the treatment of anemic conditions, the formation of neutralizing antibodies to erythropoietin may be observed with or without the development of partial red cell aplasia.

Pharmacokinetics

With intravenous administration of epoetin alfa in healthy individuals and patients with uremia, the half-life is 5-6 hours. With subcutaneous administration of epoetin alfa, its concentration in the blood increases slowly and reaches a maximum in the period from 12 to 18 hours after administration, the half-life is 16-24 hours. The bioavailability of epoetin alfa when administered subcutaneously is 25-40%. Does not cumulate.

Special instructions

During treatment, it is necessary to monitor blood pressure weekly and perform a complete blood count (including platelets, hematocrit, ferritin). In the pre- and postoperative period, hemoglobin levels should be monitored more often if the initial level was less than 140 g/l. It must be remembered that epoetin alfa in the treatment of anemia does not replace blood transfusion, but reduces the need for its repeated use.

In patients with controlled hypertension or a history of thrombotic complications, increased doses of antihypertensive drugs and/or anticoagulants may be required, respectively. When prescribed to patients with liver failure, a slowdown in the metabolism of epoetin alfa and a pronounced increase in erythropoiesis are possible. The safety of the drug in this category of patients has not been established. Although the drug stimulates erythropoiesis, the possibility of epoetin alfa affecting the growth of certain types of tumors, including bone marrow.

The possibility that a preoperative increase in hemoglobin levels may predispose to the development of thrombotic complications should be considered. Before undergoing elective surgery, patients should receive adequate prophylactic antiplatelet therapy. In the pre- and postoperative period, the drug is not recommended for use in patients with an initial hemoglobin level of more than 150 g/l.

In adult patients with chronic renal failure, clinically significant coronary heart disease or chronic heart failure, the hemoglobin level should not exceed 100-120 g/l.

Before starting treatment, possible causes of an inadequate reaction to the drug should be excluded (deficiency of iron, folic acid, cyanocobalamin, severe poisoning with aluminum salts, concomitant infections, inflammatory processes and injuries, hidden bleeding, hemolysis, bone marrow fibrosis of various etiologies) and, if necessary, adjust the treatment.

Before starting treatment, iron reserves in the body should be assessed. In most patients with chronic renal failure, in cancer and HIV-infected patients, plasma ferritin concentration decreases simultaneously with an increase in hematocrit level. Ferritin concentrations must be determined throughout the course of treatment. If it is less than 100 ng/ml, oral iron replacement therapy is recommended at a rate of 200-300 mg/day (100-200 mg/day for children). In premature infants, oral iron therapy at a dose of 2 mg/day should be started as early as possible. Patients donating autologous blood and in the pre- or postoperative period should also receive adequate amounts of iron orally at a dose of 200 mg/day.

In patients with chronic renal failure, correction of anemia may result in improved appetite and increased absorption of potassium and protein. Periodic adjustments of dialysis parameters may be required to maintain blood urea, creatinine, and potassium concentrations within normal limits.

In patients with chronic renal failure, it is necessary to monitor the level of electrolytes in the blood serum.

According to available data, the use of epoetin alfa in predialysis patients does not accelerate the progression of chronic renal failure. Due to increased hematocrit, it is often necessary to increase the dose of heparin during hemodialysis. With inadequate heparinization, blockage of the dialysis system and thrombosis of the vascular access are possible, especially in patients with a tendency to hypotension or with complications of an arteriovenous fistula (stenosis, aneurysm, etc.). In such patients, thrombosis prophylaxis is recommended.

When used in women of reproductive age with anemia due to chronic renal failure, menstruation may resume. The patient should be warned about the possibility of pregnancy and the need to use reliable methods of contraception before starting therapy. Experimental studies on rats and rabbits did not reveal a teratogenic effect when administered intravenously in doses up to 500 IU/kg body weight per day; at higher doses, a weak, statistically insignificant decrease in fertility was noted.

During the treatment period, until the optimal maintenance dose is established, patients with chronic renal failure must be careful when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions (increased risk of increased blood pressure at the beginning of therapy).

Considering the possible more pronounced effect of the drug, its dose should not exceed the dose of recombinant erythropoietin used in the previous course of treatment. During the first two weeks, the dose is not changed and the dose/response ratio is assessed. After this, the dose can be reduced or increased according to the above scheme.

Active ingredient

Epoetin alfa

Composition

1 ampoule (1.0 ml) contains Epoetin alfa (recombinant human erythropoietin) 2000 IU as an active substance.

Excipients: sodium chloride, sodium citrate pentasesquihydrate or sodium citrate dihydrate, albumin solution, citric acid monohydrate, water for injection.

Pregnancy

Since there is insufficient experience with the use of erythropoietin during pregnancy and lactation in humans, epoetin alfa should be prescribed only if the expected benefits from its use outweigh the possible risk to the fetus and mother.

Contraindications

– hypersensitivity to the drug or its components;

– partial red cell aplasia after previous therapy with any erythropoietin;

– uncontrolled arterial hypertension;

– impossibility of carrying out adequate anticoagulant therapy;

– for severe occlusive diseases of the coronary, carotid, cerebral and peripheral arteries and their consequences, including acute and recent myocardial infarction and acute cerebrovascular accident (as part of a pre-deposit blood collection program before surgery).

With caution:

Malignant neoplasms, epileptic syndrome (including in the presence of thrombocytosis, thrombosis (history), sickle cell anemia, iron and folate deficiency conditions, porphyria, chronic liver failure. Since there is not enough experience with the use of erythropoietin during pregnancy and in humans, epoetin alfa should be prescribed only if the expected benefits of its use outweigh the possible risk It is not known whether epoetin alfa is excreted in breast milk.

Side Effects

At the beginning of treatment, flu-like symptoms may be observed: dizziness, drowsiness, fever, headache, myalgia, arthralgia.

From the cardiovascular system: dose-dependent increase in blood pressure, worsening of arterial hypertension (most often in patients with chronic renal failure), in some cases – hypertensive crisis, a sharp increase in blood pressure with symptoms of encephalopathy (headache, confusion) and generalized tonic-clonic convulsions.

From the hematopoietic organs: thrombocytosis, in some cases – thrombosis of the shunt or arteriovenous fistula (in patients on hemodialysis with a tendency to arterial hypotension or with an aneurysm, stenosis, etc.), aplasia of the erythrocyte lineage.

Allergic reactions: skin rash (mild or moderate), eczema, urticaria, itching, angioedema.

Local reactions: hyperemia, burning, mild or moderate pain at the injection site (more often occur with subcutaneous administration).

From the laboratory parameters: decrease in serum ferritin concentration, with uremia – hyperkalemia, hyperphosphatemia.

Other: complications associated with respiratory failure or decreased blood pressure, immune reactions (induction of antibody formation), exacerbation of porphyria.

Interaction

Reduces the concentration of cyclosporine due to an increase in the degree of its binding to red blood cells (it may be necessary to adjust the dose of cyclosporine). Pharmaceutically incompatible with solutions of other drugs.

Overdose

Symptoms: increased side effects.

Treatment: symptomatic. With a high level of hemoglobin – bloodletting.

Storage conditions

At temperatures from 2 to 8 °C.

Keep out of the reach of children.

Shelf life

2 years. Do not use after the expiration date stated on the package.

Manufacturer

PharmFirma Sotex, Russia