Patients with F / M-transsexualism in the treatment of the underlying disease receive lifelong replacement therapy with high doses of androgens. Androgen therapy is carried out for the purpose of acquiring features (constitutional, mental) characteristic of the opposite sex, and after bilateral oophorectomy for changing sex, it prevents the development of osteoporosis and the manifestations of post-structural syndrome.
Large doses of androgens are administered in the form of testosterone preparations – Omnadren-250 and Sustanon-250, containing 4 different testosterone esters: propionate, phenylpropionate, capronate and isocapronate. The testosterone esters of the preparations have different absorption and excretion rates, which ensures a quick and long-lasting (up to 4 weeks) effect after a single injection: testosterone propionate is effective for 1 day, the effect of testosterone phenylpropionate and isocapronate begins 24 hours after injection and lasts up to 2 weeks. Assign 1 ml intramuscularly 1 time in 2-4 weeks.
In the first days after the injection of Sustanon-250 or Omnadren-250, there is an increase in testosterone above the supraphysiological level, which may cause a number of side effects of testosterone treatment: an increase in hemoglobin, erythrocytes and hematocrit. Due to the direct impact on the bone marrow and activation of the synthesis of erythropoietin in the kidneys, testosterone stimulates erythropoiesis.
An adult bone marrow produces about 2.3 million red blood cells every second, or 138 million every minute. This process (erythropoiesis) is regulated by a glycoprotein hormone, erythropoietin (EPO), which is formed in the kidneys and circulates in the blood at a concentration of about 1/100 of most other hormones.
When entering the bone marrow, EPO binds to erythroid progenitors (PFU-E and CFU-E), which have receptors for EPO (EPO-P) on their surface. When EPO binds to its receptors on BFU-E cells, they proliferate in CFU-E, which are extremely sensitive to EPO. Proerythroblasts proliferate and differentiate into erythroblasts, and the latter into normoblasts and reticulocytes, which mature and, becoming erythrocytes, enter the circulating blood.
The main function of the EPO / EPO-P system is the regulation of erythropoiesis through the production of a hormone in the kidney, its entry into the blood circulation and binding to specific EPO-P on the erythroid progenitors of the bone marrow. The result of this endocrine function of EPO is the formation of red blood cells in accordance with the body’s need for oxygen.
The effect of EPO-P is well studied in erythroid cells, and traditionally there was an opinion that EPO acts only on these cells. However, it has recently become clear that EPO-P is expressed in many organs and tissues, including the brain, heart, endothelium, uterus, ovaries, oviducts, and testicles. In particular, it is assumed that EPO-P may be necessary for
functioning of neurons.
Although research in this direction has just begun, it is becoming increasingly clear that erythroid cells are not the only targets of EPO.
Thus, there are probably three different systems of action of EPO:
endocrine hormonal system, in which EPO acts as a hormone (it is produced in one tissue and transported in plasma to the target tissue);
paracrine system, where cells produce EPO, which binds to the receptor on adjacent cells; autocrine system in which the cell itself produces and uses EPO.
It has been clinically proven that androgens stimulate erythropoiesis, as well as actively affect blood clotting processes, enhancing thrombosis and aggregation of red blood cells.
In the ENTs of the Russian Academy of Medical Sciences, 73 patients with female transsexualism, receiving HRT Omnadren-250 and Sustanon-250 1 every 1-3 weeks, hemodynamic parameters were investigated. In 25 patients, an increase in hemoglobin, erythrocyte, hematocrit levels was observed above the upper physiological norm of men and fibrinolysis factors, which leads to hypercoagulation. The mean values in these patients were as follows: НЬ 163 g / l, Rf 5.12х1012 / l, Н1: 48.9%.
The effect of androgen therapy on hemodynamic parameters was also shown when examining patients with terminal chronic renal failure, type 1 diabetes mellitus who were on programmed bicarbon hemodialysis. For the correction of anemia, patients received erythrostym in a dose of 8000 ± 2000 units. per week, and, given the presence of pronounced testosterone deficiency, they were prescribed Sustanon-250 at a dose of 1.0 ml 1 time in 2 weeks. within 3 months After 1.5 months against the background of therapy with androgens, it was possible to reduce the erythrostim dose to 2000 units in Week. Correction of anemia with testosterone hormone replacement therapy is realized through the stimulation of the synthesis of EPO, as well as the action on androgen-sensitive EPO-P in the red bone marrow. It is also impossible to exclude the conversion of testosterone to estrogens, which have a self-stimulating effect on the red sprout of the BONE marrow.
Thus, the control of these indicators is mandatory during androgen therapy. Most authors recommend reducing the dose of the drug at a hematocrit of 51% and the complete abolition of androgen replacement therapy with a hematocrit of more than 54%. We hope that with the advent of new, non-peak androgenic drugs, this side effect will be eliminated.