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Pharmachologic 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 in which the gene encoding human erythropoietin is inserted. By 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 heart function. The most pronounced effect of the use of epoetin beta is observed in anemia caused by chronic renal failure. In very rare cases, with prolonged use of erythropoietin for the treatment of anemic conditions, the formation of neutralizing antibodies to erythropoietin can be observed with or without the development of partial red cell aplasia.
Even a person who is far from medicine understands the important role that shelter plays in ensuring the normal functioning of the body. In sports, where physical activity has long 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, which 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 and strength endurance. But the methods of the limiting development of sarcoplasmic and mitochondrial hypertrophy, which have recently become popular, make it quite appropriate to use these groups of drugs in the technologies of strength sports.
An increase in the number of red blood cells while maintaining the rheological properties of blood (i.e., fluidity) leads to an increase in the supply of tissues with oxygen and nutrients, as well as a pronounced stimulation of metabolic, in particular anabolic, processes in the athlete's body. This gives rise to a dramatic increase in sports performance.
Of course, it will very temptingly increase the ability of the blood to bind and carry oxygen and carbon dioxide, increase the buffering properties of the blood and help to increase the volume of circulating blood and achieve a monstrous "pumping". 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, being introduced into the bloodstream, completely repeats the properties of red blood cells - it eats is capable of capturing and transferring everything that real shelter transports, but much more efficient. Sports circles immediately responded with calls to improve the quality and accuracy of doping control. The actual situation with synthetic substitutes for erythrocytes is unknown, but medical practice has accumulated quite a wealth 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 may turn out to be useful for the very healthy. Opinions began to appear in cool-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. Determination of it and its metabolites in urine is still extremely difficult. However, EPO is classified as a doping by the IOC Medical Committee.
Human erythropoietin is sold under a variety of commercial 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 anti-allergenic and has the highest degree of purity. The use of the drug leads to an increase in 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 tissues and heart function, and a decrease in the symptoms of anemic ischemia. In traditional medicine, human recombinant erythropoietin is used to replace the deficiency of its own hormone 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 reasons (in this case, washed erythrocytes or erythrocyte mass).
Typically, the drug is administered subcutaneously, and the initial dosage is about 20 IU per kilogram of body weight three times a week, or 10 IU per kilogram of body weight daily. In case of insufficient effectiveness of the drug, the dose may 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 dosage 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 dosage 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 take into account 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 using EPO for vital indications, side effects are not taken into account, and are corrected by special means during therapy. When treating with recombinant human epitropostin, arterial pressure may increase, headache, weakness, dizziness, muscle pain may be observed (especially at the beginning of treatment). There is a likelihood of developing thrombosis and microthrombosis, as well as jaundice. Individual drug intolerance is possible.
Contraindications to 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 using EPO in sports, it is necessary to carefully control the hematocrit level, the rheological properties of the blood, the aggregation ability of erythrocytes and platelets to exclude the possibility of thrombus formation. In professional cycling, where EPO preparations are very widely used, a hematocrit level of 50% and higher is the basis for removing a participant from the start.
We believe that at certain stages of training top-level bodybuilders, the competent use of EPO can have quite a serious rationale and will significantly affect the athletic performance. But, given the extreme closedness 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 remains 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 medications 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 immunity stimulants, such as interferon and amiksin, as well as preparations for active and passive immunization of the body, including various specific vaccines and serums. It is clear that none of these medicines will be recommended for independent uncontrolled use without the participation of a qualified pharmacologist.
Whole truth about erythropoietin, how doping works on athletes
Erythropoietin is a glycopeptide hormone produced by the adrenal glands and, in small quantities, by the liver. It is involved in regulating the production of red blood cells synthesized in the bone marrow. The task of erythrocytes, in turn, is to supply cells with oxygen. The effect of erythropoietin on the hematopoietic ability of a person is of interest to scientists and sports coaches, as it makes it possible to increase the resources of the human body.
How erythropoietin works.
Erythropoietin or, as it is usually 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. Amino acid constituent elements 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, entering the blood, converts reticulacites into red blood cells, significantly increasing their number, respectively, increasing the oxygen they carry. As the oxygen level rises, the pressure in the arteries rises and the blood becomes more viscous.
EPO is not only produced during hypoxia; glucocorticoid, synthesized by the adrenal gland, in a stressful situation also becomes a stimulator of its release. Such a feature of the body allows it in a few seconds to increase the strength and speed of muscle tissues, and the flow of acid provides endurance.
The metabolism working in this way allowed man as a species to survive, since there were plenty of natural enemies in the wild, primitive nature. When attacked by a predator, a person managed to escape or win in a fight with a strong animal.
True, such a surge in the activity of the synthesis of blood cells leads to 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. Ancient man replenished his supply of iron and copper by eating the defeated animal.
Reasons for deviation of 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 range of hormone content 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.
The presence of all the pathologies and diseases mentioned 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 such a situation is eliminated.
The use of erythropoietin in therapy
Many diseases and conditions are treated with hormonal therapy, including drugs with erythropoietin. Any treatment in this direction is prescribed by an endocrinologist, since even the smallest deviation in the dosage of the drug can lead to a dangerous excess or, conversely, an underestimation of the number of red blood cells.
The 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.
