Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:B.03.X.A Other stimulators of hemopoiesis
B.03.X.A.02 Darbepoetin alfa
Pharmacodynamics:Darbepoetin alfa is produced using gene technology in Chinese hamster ovary cells (CHO-K1). Stimulates erythropoiesis by the same mechanism as endogenous erythropoietin.
Darbepoetin alfa stimulates the proliferation and differentiation of erythroid progenitor cells, promotes the release of reticulocytes from the bone marrow into the blood. Darbepoetin alfa forms peritubular cells of the kidneys (90%) and, in a smaller amount, liver cells (10%). The formation of erythropoietin is significantly enhanced with tissue hypoxia. Darbepoetin alfa stimulates the production of erythrocytes under hypoxic conditions by binding and activation of high affinity receptors (EpoR), which are expressed predominantly on the surface of immature erythroid cells. In chronic kidney diseases, the synthesis of erythropoietin is disrupted.
Pharmacokinetics:In connection with the increased content of carbohydrates, the concentration of circulating blood darbepoetin alfa exceeds the minimum concentration,necessary for the stimulation of erythropoiesis for a longer time, compared with equivalent doses of recombinant human erythropoietin, which reduces the incidence of darbepoetin alfa with an equivalent level of biological response.
The half-life for chronic renal failure is 21 hours after intravenous administration and 49 hours after subcutaneous administration.
Indications:Anemia in chronic renal failure, with neoplasms, with other chronic diseases.
III.D60-D64.D63.0 * Anemia in neoplasm (C00-D48 +)
III.D60-D64.D63.8 * Anemia in other chronic diseases classified elsewhere
XIV.N17-N19.N18.9 Chronic renal failure, unspecified
Contraindications:Hypersensitivity, uncontrolled arterial hypertension.
Carefully:Sickle-cell anemia, hepatic insufficiency, epilepsy.
Pregnancy and lactation:Category FDA - C. Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted. With caution and after careful evaluation of the expected benefit of therapy for the mother and the potential risk to the fetus, the drug should be given to pregnant women.
If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
Dosing and Administration:Introduction subcutaneous or intravenous. Treatment should be conducted by a doctor who has already had experience with this drug. Darbepoetin alfa is supplied ready for use in pre-filled syringes. The standard dose of the drug is 0.45 μg / l - a single or weekly injection. If the patient on dialysis - the dose can be increased to 0.75 mkg / kg, in extreme cases, in the absence of therapeutic effect, an increase in the dose by another 25% is possible.
Side effects:From the cardiovascular system: increased blood pressure, thromboembolism (including pulmonary arteries).
From the nervous system: headache, stroke, convulsions.
From the skin: erythema, rash.
On the part of the body as a whole: pain at the injection site, swelling, allergic reactions, anaphylactic reactions.
Overdose:The maximum tolerated dose of darbepoetin alfa is not determined. Possible polycythemia. Treatment - cancellation of the drug.
Interaction:Clinical data obtained to date do not contain indications of the interaction of darbepoetin alfa with other substances.However, it is known that its interaction with drugs characterized by a high degree of affinity for erythrocytes, such as ciclosporin, tacrolimus. With the simultaneous administration of darbepoetin alfa with any such drugs, the level of serum levels in the blood serum should be monitored with a dose modification in case of an increase in the hemoglobin concentration.
In view of the fact that compatibility studies have not been conducted, the drug should not be mixed or administered as an infusion along with other medications.
Special instructions:During treatment, monitoring of arterial pressure, hemoglobin, water-electrolyte balance, ferritin concentration in plasma, plasma transferrin level, monitoring of renal function and neurological status is required.