Erythropoietin (epoetin alfa) EPO General Description
EPO is a kidney hormone that is secreted in liver cells. It controls the production of red blood cells. In bodybuilding, the drug is used as a performance-enhancing substance. The production of erythropoietin (EPO) is accomplished by cloning molecules in a cell culture.
Erythropoietin contains 165 different acids, and its molecular mass is 34,000 Da. The drug is produced from rHuEPO, which is developed in mammalian cells, to which the human gene is transfected beforehand using genetic engineering. Therefore, EPO completely clones the human erythropoietin hormone.
The active agent is synthesized in the kidneys, and after entering the blood it begins to affect the bone marrow, stimulating the production of red blood cells. As a result of the maturation of erythroblasts, hemoglobin and reticulocytes concentrations increase. The drug acts at the cellular level, and its effect identifies the action of the polypeptide hormone. EPO also acts as a secondary messenger by performing internalization, which leads to an increase in the concentration of calcium in the cells.
The drug was invented in 1905 in Paris by a professor of medicine called Paul Carnot. According to doctors, blood corpuscles are produced due to hemopoietin, and this substance was later named “erythropoietin”. Further EPO studies showed that the drug was able to raise the level of hematocrit, which allowed it to be used in medicine to treat anemia. The drug began to be used en masse in the 80s for:
• Kidney failure.
• Ulcerative colitis.
• Crohn's disease.
In bodybuilding, EPO is used to increase stamina and supply muscle tissue with oxygen and other beneficial substances that accelerate muscle growth. The effect of EPO is due to the binding of the hormone to EpoR. The drug has high glycosation, which is 40% of the total molecular mass. The half-life of the active agent of the drug lasts up to five hours. The binding of the hormone to the receptors occurs on the surface of the cell, which is highly susceptible to erythropoietin. The receptors themselves are located in the kidneys, nerves, heart and muscles. Red blood cells in blood plasma do not respond to the action of the hormone, however, as their number and duration of life are directly related to the level of erythropoietin.
So that the drug does not lose its effectiveness, it is stored at a temperature of 2-8 degrees above zero for two years from the date of manufacture. Don’t shake before injection and don’t freeze.
Among the positive effects of EPO are:
• Improved nutrition and oxygen delivery to muscles.
• Improved endurance.
• Normalized production of blood cells.
• Improved general condition of the body.
• Increased physical endurance.
• Improved blood circulation.
• Rapid regeneration of damaged tissue.
• Improved function of internal organs.
Due to the ability to increase the level of red blood cells, the drug improves alertness, favorably affects brain activity and improves athletic performance.
EPO Possible Side Effects
EPO rarely causes side effects, but improperly established dosages, as well as individual intolerance to the active agent, may lead to the following: increased blood pressure, thrombosis, aneurysm, stenosis, thromboembolism, red cell aplasia, hyperphosphatemia and hyperkalemia. There may also be a decrease in ferritin levels, migraines, chills, ostalgia, fatigue, itching, hives and body rash.
If any of the above effects is detected, immediately consult a doctor. It is possible to stop using the drug or review the dosage.
EPO Administration and Dosage
The drug is injected subcutaneously or intravenously. Dosage is assigned to each athlete individually and depends on the state of health, weight and height. EPO use is recommended to start with an initial dose of 50-150 IU per 1 kg of athlete's weight. Supportive doses of 17-100 IU per 1 kg of mass are enough. Injections are made three times a week.
Before surgery and blood sampling, the drug is administered once a week for three weeks at a dose of 600 IU.
A method for detecting EPO in athlete’s blood was developed in Sydney in 2000. Doping control was based on the analysis of urine and blood. Despite the fact that the drug is well detected in urine, some organizations still take blood for analysis.
In order to avoid being disqualified and to successfully pass doping control, experienced athletes stop taking erythropoietin seven days before the test. This is enough to affect endurance and pass the testing.
To avoid an anaphylactoid reaction, the first injection is done under the supervision of a doctor. When taking the drug, users should constantly monitor blood pressure and platelet count to avoid issues with the heart and blood vessels. If their number exceeds 150-109 from the initial level of the lymphocyte count, the drug usage is stopped.
If hematocrit increases in the body, a decrease in ferritin is observed. If the level of ferritin is less than 100 mcg/l, iron supplements are prescribed at 200-300 mg per day.
In sports, the drug is used to significantly increase the level of red blood cells, which are responsible for delivering oxygen to all internal organs and muscles. Due to this, endurance increases, which allows athletes to handle more loads to the body and achieve the established fitness goal. Experienced athletes recommend using the drug for no more than six months, and the first positive changes will be visible two weeks after the first injection.
Before using EPO, a blood test should be taken to determine the number of red blood cells and platelets and then set the dosage accordingly, otherwise improper use of the drug can lead to serious health problems.
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