Hemax Mechanism of Action

ATC Code: B03XA01.
Pharmacology: Pharmacodynamics: Mechanism of Action: Erythropoietin induces erythropoiesis by stimulating the division and differentiation of erythroid progenitors in the bone marrow, causing the enhancement of the globular mass and, in turn, the hematocrit. Erythropoieitn also stimulates the release of reticulocytes from the bone marrow into the bloodstream, where they mature into erythrocytes. The normal concentration of endogenous erythropoietin is 10-30 mU/ml and it is regulated by the levels of tissue oxygenation. When such levels decrease, the erythropoietin concentration increases up to 100- and 1000-fold. This is also observed in anaemic patients.
Pharmacokinetics: Epoetin alpha, Hemax active ingredient, is indicated for parenteral (subcutaneous or intravenous) administration. The initial enhancement in the reticulocyte count occurs within 7 to 10 days following administration. Red cell count, hematocrit and haemoglobin levels increase significantly generally within 2 to 6 weeks following epoetin alpha administration. The range and extent of the response will depend on the dose and availability of iron stores. The maximum plasma concentration is achieved 15 minutes following the administration of a unique intravenous dose and between 5 to 24 hours following subcutaneous administration as a single dose. Peak concentrations following SC administration may remain for 12 to 16 hours and detectable amounts can be observed for at least 24 hours following administration. Epoetin alpha half-life is 4 to 13 hours post intravenous or subcutaneous administration. Elimination half-life is generally longer after the administration of the first doses than after two or more weeks of treatment. Generally, after 24 hours, erythropoietin plasma levels return to their basal levels. Following epoetin subcutaneous administration, the maximum concentration is observed between 5 to 24 hours post administration and its decline is slower.
In adult healthy volunteers, half-life following intravenous administration was 20% lower than in patients with renal failure. In a trial that involved healthy volunteers, Hemax half-life, administered by SC route, was 20.8±6.3 hours. Once the treatment is withdrawn, hematocrit may start decreasing after 2 weeks.
Toxicology: Preclinical safety data: Carcinogenesis and mutagenesis: Carcinogenic potential of Hemax has not been evaluated. Epoetin does not induce bacterial gene mutations or chromosomal aberrations in mammalian cells.
Fertility: In female rats treated with epoetin at 100 to 500 IU/kg intravenously, there was a trend for slightly increased foetal wastage.