Description
Latin name
EPOCRIN
Form release
Solution for intravenous and SC administration.
Packing
In an ampoule of 1 ml of solution. In a blister strip packaging of 10 ampoules. In cardboard packaging 1 blister strip packaging.
Pharmacological action
Pharmacodynamics
Stimulant of erythropoiesis, recombinant human erythropoietin, glycoprotein.
Activates mitosis and red blood cell maturation from erythrocyte progenitor cells. Recombinant epoetin alpha is synthesized in mammalian cells into which a gene encoding human erythropoietin is inserted. In its composition, biological and immunological properties, epoetin alpha is identical to natural human erythropoietin. The introduction of epoetin alpha leads to an increase in the level of hemoglobin and hematocrit, and an improvement in the blood supply to tissues and heart function.
The most pronounced effect of the use of epoetin alpha is observed in anemia, caused by chronic renal failure.
In very rare cases, with prolonged use of epoetin alpha for the treatment of anemic conditions, the formation of neutralizing antibodies to erythropoietin with the development of partial red cell aplasia with or without it can be observed.
Pharmacokinetics
Absorption and distribution of
After s / c administration, the concentration of the active substance in the blood increases slowly, Cmax is reached within 12-18 hours. Bioavailability with s / c administration is 25-40%.
Excretion of
After sc administration of T1 / 2 is 16-24 hours.
After iv administration of T1 / 2 in healthy individuals and patients with uremia is 5-6 hours.
Indications
Anemia in patients with chronic renal failure (including hemodialysis)
prevention and treatment of anemia in patients with solid tumors resulting from antitumor therapy
prevention and treatment of anemia caused by the use of zidovudine in HIV-infected patients (AIDS)
prevention and treatment of anemia in patients with myeloma, non-Hodgkin ² ¢s lymphomas low malignancy, chronic lymphocytic leukemia, in patients with rheumatoid arthritis
prevention and treatment of anemia in premature babies born with low body weight ( up to 1500 g)
to reduce the volume of transfused blood during extensive surgical interventions and acute blood loss.
Contraindications
Partial red cell aplasia after previous treatment with any erythropoietin
uncontrolled arterial hypertension
inability to conduct adequate anticoagulant therapy
during the period of 1 month after severe cardiomyopathy blood collection before surgery
porphyria
hypersensitivity to components Reparata.
Caution: the drug should be prescribed to patients with thrombosis (history), with malignant neoplasms, with sickle cell anemia, in patients with moderate anemia without iron deficiency, in patients with refractory anemia, epilepsy and chronic liver failure.
Use during pregnancy and lactation
Since experience with the use of epoetin alfa during pregnancy and lactation in humans is insufficient, Epocrin ® should be prescribed only in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus or infant.
When using epoetin alfa in women of reproductive age with anemia in the presence of chronic renal failure, menstruation can resume. The patient should be warned about the possibility of pregnancy and the need to use reliable methods of contraception before starting therapy.
Composition
1 ml of the solution contains:
Active substances:
human epoetin alfa epoetin 2000 recombinet.
Excipients:
albumin (in the form of albumin, solution for infusion 10%) – 2.5 mg,
sodium citrate pentaesquihydrate – 5.8 mg or sodium citrate dihydrate – 4.776 mg,
sodium chloride – 5.84 mg,
citric acid monohydrate – 0.057 mg,
water d / i – up to 1 ml.
Dosage and administration of
In the treatment of anemia in patients with chronic renal failure, Epocrin ® is administered sc or iv in patients on hemodialysis through an arteriovenous shunt at the end of the dialysis session. When the method of administration is changed, the drug is administered in the previous dose, then the dose is adjusted if necessary (when s / c administration of the drug Epocrin ®, to achieve the same therapeutic effect, a dose of 20-30% is required than with iv administration). Epocrine treatment includes 2 stages.
1. Stage of correction. When s / to the introduction of the drug Epocrin ®, the initial dose is 30 IU / kg 3 times a week. With the on / in the introduction of the drug Epocrin ®, the initial dose is 50 IU / kg. The correction period lasts until the optimal hemoglobin level (100-120 g / l in adults and 95-110 g / l in children) and hematocrit (30-35%) are reached. These indicators must be monitored weekly.
The following situations are possible:
Hematocrit increase from 0, 5% to 1% per week
Do not change the dose until optimal parameters are achieved
Hematocrit growth rate less than 0.5% per week
Increase single dose 1.5 times
Hematocrit growth rate more than 1% per week
Reduce single dose 1.5 times
Hematocrit remains low or decreases
It is necessary to analyze the causes of
resistance. The effectiveness of therapy depends on a correctly selected individual treatment regimen.
2. Stage of maintenance therapy. To maintain a hematocrit of 30-35%, the dose of Epocrin ® used at the correction stage should be reduced by 1.5 times. Then, the maintenance dose of Epocrin ® is selected individually, taking into account the dynamics of hematocrit and hemoglobin. After stabilization of hematological parameters, it is possible to switch to the administration of the Epocrin ® preparation once every 1-2 weeks.
In the prevention and treatment of anemia in patients with solid tumors, it is recommended to determine the level of endogenous erythropoietin before using the drug. When the concentration of serum erythropoietin is less than 200 IU / ml, the initial dose of Epocrin ® with iv administration is 150 IU / kg. With sc administration, the initial dose of Epocrin ® can be reduced to 100 IU / kg. If there is no response, a dose increase of up to 300 IU / kg is possible. A further increase in dose seems inappropriate. It is not recommended to prescribe Epocrine ® for patients with a serum content of endogenous erythropoietin of more than 200 IU / ml.
For the prevention and treatment of anemia caused by the use of zidovudine in patients with HIV infection, iv administration of Epocrin ® at a dose of 100-150 IU / kg 3 times a week is effective provided that the level of serum endogenous erythropoietin is less than 500 IU / ml and the dose of zidovudine is less than 4.2 g per week. With sc administration, the dose of Epocrin ® can be reduced by 1.5 times.
The feasibility of using Epocrin ® for the prevention and treatment of anemia in patients with myeloma, non-Hodgkin s lymphomas of low malignancy, chronic lymphocytic leukemia is due to inadequate synthesis of endogenous erythropoietin against the background of the development of anemia. With a hemoglobin content of less than 100 g / l and serum erythropoietin below 100 IU / ml, Epocrin ® is administered subcutaneously at an initial dose of 100 IU / kg 3 times a week. Laboratory monitoring of hemodynamic parameters is carried out weekly. If necessary, the dose of Epocrin ® is adjusted in the direction of increasing or decreasing every 3-4 weeks. If upon reaching a weekly dose of 600 IU / kg there is no increase in hemoglobin, Epocrin ® should be discontinued, as its further use is ineffective.
The advisability of using the Epocrin ® preparation for the prevention and treatment of anemia in patients with rheumatoid arthritis is due to the fact that in this disease there is a suppression of the synthesis of endogenous erythropoietin under the influence of an increased concentration of pro-inflammatory cytokines. Epocrin ® is administered subcutaneously at a dose of 50-75 IU / kg 3 times a week. With an increase in hemoglobin content of less than 10 g / l after 4 weeks of treatment, the dose of Epocrin ® is increased to 150-200 IU / kg 3 times a week. A further increase in dose seems inappropriate.
For the prevention and treatment of anemia in premature infants born with low birth weight, Epocrin ® is administered s.c. at a dose of 200 IU / kg 3 times a week, starting from 6 days of life until the target hemoglobin and hematocrit are reached, but not more than 6 weeks.
For the prevention of anemia with extensive surgical interventions and acute blood loss, Epocrin ® is administered iv or sc 3 times a week at a dose of 100-150 IU / kg until the hematocrit and hemoglobin normalize.
Side effects
Flu-like syndrome: in some cases, at the beginning of therapy – dizziness, drowsiness, fever, headache, myalgia, arthralgia.
From the cardiovascular system: possible dose-dependent arterial hypertension, worsening of the course of arterial hypertension (more often in patients with uremia) in some cases – a hypertensive crisis, a sharp increase in blood pressure with symptoms of encephalopathy (headache, confusion) and generalized tonic-clonic seizures .
On the part of the metabolism: a decrease in serum ferritin concentration is possible, decrease in serum iron metabolism in patients with uremia possible hyperkalemia and hyperphosphatemia.
Allergic reactions: possibly mild or moderate skin rash, urticaria, pruritus, angioedema, eczema.
Local reactions: hyperemia, burning, mild or moderate soreness at the injection site are possible (more often with s / c administration).
Other: thrombocytosis in some cases – shunt thrombosis (in patients on hemodialysis, with a tendency to hypotension or with aneurysm, stenosis) symptoms associated with respiratory failure or unstable blood pressure are very rare – immune reactions (induction of the formation of antibodies with the development of partial red cell aplasia or without it), exacerbation of porphyria.
Drug Interaction
When concomitant administration of Epocrine ® with cyclosporine increases the binding of the latter to erythrocytes (dose adjustment of cyclosporine may be required).
Based on the clinical experience of Epocrine ® to date, no pharmacological incompatibility with other medicinal products has been identified. However, to avoid possible incompatibility or decrease in activity, Epocrine ® should not be mixed with solutions of other medicines.
Overdose
Symptoms: side effects may increase.
Treatment: in the case of an increase in blood pressure, antihypertensive agents are prescribed, with the ineffectiveness of the latter, Epocrine should be canceled. At high levels of hemoglobin and hematocrit blood flow is shown.
Storage conditions
Keep out of the reach of children at temperatures from 2 ° to 8 ° C.
Expiration
2 years.
Active e substance
epoetin alfa
Dosage Form A dosage form
injection and infusion
Research Institute for Highly Clean Biological Products, Russia
