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Description
pharmacological effect
Epoetin beta is a glycoprotein that specifically stimulates erythropoiesis, activates mitosis and maturation of erythrocytes from erythrocyte progenitor cells. Recombinant epoetin beta is synthesized in mammalian cells into which the gene encoding human erythropoietin is inserted. Due to its composition, biological and immunological properties, epoetin beta is identical to natural human erythropoietin. The introduction of epoetin beta leads to an increase in hemoglobin and hematocrit, an improvement in tissue blood supply and cardiac function. The most pronounced effect of epoetin beta use is seen in anemia caused by chronic renal failure. Very rarely, with prolonged 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 aplasia of red blood cells.
Even a person who is far from medicine understands the important role that the refuge plays in ensuring the normal functioning of the body. In sports, where physical activity has gone beyond the limits that are even remotely accessible to a simply physically developed person, it is simply impossible to overestimate the influence of the blood system on sports results.
An increase in hemoglobin levels by 10-30% leads to such a significant increase in sports performance, that it can act as the main reason for victory. Of course, the greatest use of erythropoietin preparations and other hematopoietic stimulants was found in cyclic sports focused on general endurance and strength.But methods to limit the development of sarcoplasmic and mitochondrial hypertrophy, which have recently become popular, make it quite appropriate to use these groups of drugs in strength sports technologies.
An increase in the number of red blood cells while maintaining the rheological properties of blood (ie, fluidity) leads to an increase in the supply of tissues with oxygen and nutrients, as well as a pronounced stimulation of metabolic processes, in particular anabolic, in blood. the athlete's body. This results in a dramatic increase in athletic performance.
Of course, it will very tantalizingly increase the ability of the blood to bind and transport oxygen and carbon dioxide, increase the buffering properties of the blood and help increase the volume of circulating blood and achieve a monstrous 'pump'. About ten years ago, a sensational report appeared in one of the Canadian newspapers that a synthetic drug had been invented and tested on athletes, which, when introduced into the blood stream, completely repeats the properties of the red blood cells – which it eats. it is capable of capturing and transferring everything the royal shelter carries, but much more efficiently. Sports circles immediately responded with calls to improve the quality and accuracy of doping control. The actual situation with synthetic erythrocyte substitutes is unknown, but medical practice has accumulated a great deal of experience in stimulating erythroposis due to proven and effective drugs, the most effective of which is erythropoietin.
As always, in this case, the traditional logic worked – what is good for the sick can be useful for the very healthy. Opinions began to appear in fresh tourism publications that erythropoietin could replace the massive use of anabolic steroids.Of course, these opinions are based on the experience of using EPO in other sports. In professional sports, this agent is traditionally used in combination with stanozolone, insulin and growth hormone. The determination of it and its metabolites in urine remains extremely difficult. However, the EPO is classified as doping by the IOC Medical Committee.
Human erythropoietin is sold under a variety of trade names. It is a recombinant glycoprotein that is a mitosis-stimulating factor (stimulating the division of erythrocyte lineage precursors) and a differentiation hormone that promotes the formation of erythrocytes from stem cells. The drug is produced by genetic engineering. It is produced by various pharmaceutical companies in three forms: alpha, beta, and delta.
Erythropoietin-delta is the most effective antiallergic and has the highest degree of purity. The use of the drug leads to an increase in the hematocrit (the percentage of the cellular component of the blood) and the level of hemoglobin in the blood, an improvement in the blood supply to the tissues and cardiac function, and a decrease in the symptoms of amic ischemia. In traditional medicine, recombinant human erythropoietin is used to replace its own hormone deficiency in patients with renal anemia undergoing hemodialysis treatment. It is also possible to use EPO in cases of anemia, when blood transfusion is contraindicated for one or another medical, social or religious reason (in this case, washed erythrocytes or mass of erythrocytes).
Typically, the drug is administered subcutaneously, and the starting dose is approximately 20 IU per kilogram of body weight three times a week, or 10 IU per kilogram of body weight daily.In case of insufficient efficacy of the drug, the dose can be increased by 20 IU per kilogram of body weight three times a week every four weeks (60 IU per 1 kg per week). When administered intravenously, the initial dose is 40 IU per 1 kg of body weight 3 times a week, after four weeks the dose can be doubled. Regardless of the route of administration, the maximum dose should not exceed 720 units per kilogram of body weight per week. In the future, the maintenance dose is selected so that the hematocrit does not exceed 35 percent by volume. When using erythropoietin, it is necessary to keep in mind that it is extremely important to provide the body with an adequate amount of all essential nutrients (macronutrients), as well as vitamins, minerals, especially iron, vitamin B12 and folic acid.
Side effects: When EPO is used for vital indications, side effects are not taken into account, and are corrected by special means during treatment. When treated with recombinant human epithropostin, blood pressure may increase, headache, weakness, dizziness, muscle pain (especially at the beginning of treatment). There is a probability of developing thrombosis and microthrombosis, as well as jaundice. Individual drug intolerance is possible.
Contraindications for the use of EPO are: hypersensitivity to the drug, arterial hypertension, difficult to treat, pregnancy and lactation. The freshly prepared solution should be stored in a refrigerator and used for everyday life.
When EPO is used in sports, it is necessary to carefully monitor the hematocrit level, the rheological properties of the blood, the aggregation capacity of erythrocytes and platelets to exclude the possibility of thrombus formation.In professional cycling, where EPO preparations are used very widely, a hematocrit level of 50% and above is the basis for eliminating an entrant early on.
We believe that at certain stages of training of high-level bodybuilders, the competent use of EPO can have a rather serious reason and significantly affect athletic performance. But, given the extreme closure of information about erythropoietin and the complete reluctance of doctors, coaches and athletes from those sports in which a decent experience of using EPO has been accumulated, shares the methods of using this drug, the question still open. Experiments with this drug are considered extremely dangerous and its use without experienced and qualified medical support is not possible. Although, this thought can be attributed to any other drug.
In addition to EPO, other drugs can also be used to stimulate hematopoiesis, such as various forms of iron, vitamin B12 and its coenzyme form – cobamamide, folic acid, methyluracil, sodium nucleinate, leucogen. The list of drugs could be significantly expanded, but we deliberately did not do this, since the effectiveness of their use is very doubtful, although with their help it is possible to correct certain vitamin and mineral disorders in the blood serum. Some exceptions can be made for drugs that have immunomodulatory properties and stimulate the body's defenses at the peak of sports form and approaches to it. These include preparations of the thymus gland, nonspecific stimulants of immunity, such as interferon and amiksin, as well as preparations for active and passive immunization of the body, including various vaccines and specific serums. It is clear that none of these drugs is recommended for independent uncontrolled use without the involvement of a qualified pharmacist.
The whole truth about erythropoietin, how doping works in athletes
Erythropoietin is a glycopeptide hormone produced by the adrenal glands and, in small amounts, by the liver. Participates in the regulation of the production of red blood cells synthesized in the bone marrow. The task of the erythrocytes, in turn, is to supply oxygen to the cells. The effect of erythropoietin on the hematopoietic capacity of a person is of interest to scientists and sports trainers, since it allows to increase the resources of the human body.
How does erythropoietin work?
Erythropoietin or, as it is called in medicine, EPO begins to be produced even with the smallest oxygen deficiency. The hormone is transferred throughout the body by a complex iron-containing protein, hemoglobin.
Oxygen is used by the body for a variety of functions. Without it, the synthesis of cholesterol, bile acid, steroid hormones would be impossible. Constituent elements of amino acids and so on. In addition, oxygen breaks down into harmless elements, toxins, poisons and unnecessary drugs.
With hypoxia, oxygen starvation, internal organs, the cardiovascular system, and most importantly the brain are destroyed. That is, severe cases of hypoxia end in death.
The hormone erythropoietin, getting into the blood, converts reticulocytes into red blood cells, significantly increasing their number, respectively, increasing the oxygen they carry. As the oxygen level increases, the pressure in the arteries increases and the blood becomes more viscous.
EPO is not only produced during hypoxia, glucocorticoids, synthesized by the adrenal gland, in a stressful situation also become a stimulator of their release. Such a feature of the body allows you in a few seconds to increase the strength and speed of muscle tissues, and the flow of acid provides resistance.
Metabolism working in this way enabled man as a species to survive, as there were plenty of natural enemies in the wild and primitive nature. When attacked by a predator, a person managed to escape or win a fight with a strong animal.
True, such an increase in the activity of blood cell synthesis leads to the depletion of reserves of iron, copper, vitamins B9 and B12, therefore, after a stressful situation, it is necessary to restore the balance of these substances in the body. Body. Ancient man replenished his supply of iron and copper by eating the defeated animal.
Reasons for the deviation of the EPO from the norm
In the human body, the level of various hormones is extremely precisely balanced, the same applies to erythropoietin. For women, the hormone content range from 8 to 30 IU / l is taken as the norm. In men, respectively, 5.6 to 28.9 IU / L. If there is a deviation from the norm in a larger or smaller direction, this may mean the presence of some pathologies.
- With an increased level of erythropoietin, the number of erythrocytes should be high, but if it is low, this indicates anemia, which suppresses hematopoietic function of the bone marrow.
- Erythropoietin levels can be depleted by the environment, such as high altitude, low oxidation conditions.
- Oxygen depletion, despite high levels of erythropoietin, can occur as a result of poisoning the body with smoke, for example from cigarettes.
- Decreased erythropoietin levels can be caused by kidney failure or the presence of a cyst or tumor in the adrenal glands. The kidneys also stop producing the necessary hormone in case of urolithiasis or the presence of multiple cysts in the parenchyma of the organ.
- Tumors can also affect the bone marrow, so a high level of erythropoietin in this situation does not cause an influx of red blood cells.
- The bone marrow is susceptible to a variety of pathologies, from various forms of anemia to leukemia, all of which are accompanied by low levels of red blood cells, white blood cells, or platelets.
- If, at an elevated level of erythropoietin, oxygen in the blood still does not increase, this may be due to diseases of the lungs or the cardiovascular system.
- Damage to the brain by hemangioblastoma, leads to a violation of the level of erythropoietin in the blood.
- Acquired immunodeficiency syndrome.
- Following transplantation of any organ, especially bone marrow, there is significant hormonal failure, accompanied by a deficiency of red blood cells.
- Donated blood leads to a deficiency of red blood cells, despite the high level of erythropoietin.
The presence of all the mentioned pathologies and diseases becomes the reason for a long and laborious therapy, during which not only the hormonal and oxygen balance in the body is put in order, but the very reason for the occurrence of diseases is eliminated. such situation.
The use of erythropoietin in therapy
Many diseases and conditions are treated with hormone therapy, including erythropoietin medications. Any treatment in this direction is prescribed by an endocrinologist, since even the smallest deviation in the dose of the drug can lead to a dangerous excess or, conversely, an underestimation of the number of red blood cells.
Treatment is carried out both with the help of subcutaneous and intravenous drugs. During treatment, the patient is regularly checked for blood composition, hemoglobin level, and erythropoietin content in the blood.
