It is a substance of the steroid structure, which, entering the bloodstream in the target tissue, penetrates the cells and acts like other steroid hormones.
It binds to intracellular cytosolic receptors and activates them. The resulting hormone-receptor complex penetrates into the nucleus, where it interacts with specific regions localized in the genes and changes the transcription of the protein genes.In some tissues (in the skin, hair follicles, prostate, seminal vesicles), testosterone under the influence of 5a-reductase is converted into dihydrotestosterone, which in these tissues is an active form of the hormone. Dihydrotestosterone binds more firmly to receptors and its effect is more pronounced.
Effects of androgen hormones
Conditionally it is possible to divide into 2 groups:
– stimulation of development of male genital organs and secondary male sexual characteristics
– stimulation of male sexual behavior
– increased growth and increased muscle mass
– stimulation of erythropoiesis
Indications for use:
· Based on substitution therapy
– Male hypogonadism and lag in sexual development
– Involutional disorders in men associated with the extinction of sexual function
· In the calculation of suppression of the gonadotrophic function of the pituitary gland (suppressive, suppressive therapy)
– tumor diseases of the breast in women.
Undesirable effects of androgenic drugs
· Gynecomastia (due to transformation in peripheral tissues into estrogens)
Oligo and azoospermia (due to oppression according to the negative feedback principle of production of follicle-stimulating hormone of the pituitary gland)
· Reducing the size of the testicles (for the same reason as the previous one)
· Increase in the size of the prostate gland (due to the conversion to a more active dihydrotestosterone)
· Cholestasis and jaundice (due to increased cholesterol content in bile)
Hepatitis (due to cholestasis)
· Adenoma and carcinoma of the liver (more often with methyltestosterone and other 17a-substituted testosterone)
· Increased aggression
· For women – virilization
· In pregnant women, the musculation of the fetus’s external genitalia.
Contraindications to the appointment of androgens:
Tumors of the prostate or mammary gland in men
· Heart failure (due to a delay in the body Na + and water).
Features of pharmacological properties of the main representatives
Natural hormone drug
It is subject to rapid metabolism in the body due to which it is rarely used as a medicine.
Sometimes it is administered intramuscularly in the form of an aqueous suspension 10-50 mg 2-3 times a week for replacement therapy.
FV: 2.5% aqueous suspension in amp. 1 ml each (Aquaviron).
17b-derivative of testosterone. Get synthetically. Being an ether, it is slightly more slowly absorbed by intramuscular injection and lasts longer, in comparison with testosterone.
· Male hypogonadism (in / muscle, 50 mg 2-3 times a week)
· Delayed puberty in adolescent boys (in / mouse 50-100 mg 2-3 times a week)
· Cryptorchidism (doses and administration regimen are the same)
· Male menopause (dose and mode of administration are the same)
· Unprofitable breast cancer in women in the menopausal period (in terms of suppression of the gonadotropic function of the pituitary gland, v / muscle, 100 mg 2-3 times a week)
FV: 1% and 5% of the oil in the amp. 1 ml each.
Testosterone enantate (Testosterone enantate)
Similar in structure and pharmacological properties with testosterone propionate, but the effect develops more slowly, but lasts longer.
It is used for the same indications as testosterone propionate.
It is prescribed intramuscularly for 50-400 mg every 2-4 weeks.
Fv: amp. on 250 mg (Testoviron Depot-250)
Testosterone Decanoate (Testoterone decanoate)
Also testosterone ester.
It is characterized by an even longer duration of action.
It is not used on its own. It is a part of combined androgen-containing drugs.
Sustanon-250 (Sustanon-250, Omnandren-250)
Contains in its composition a mixture of testosterone esters, which differ in their pharmacokinetic properties:
· Testosterone propionate – 30 mg / ml
· Testosterone phenylpropionate – 60 mg / ml
· Testosterone isocaproate – 60 mg / ml
· Testosterone decanoate – 100 mg / ml
Propionates provide a rapid onset, and decanoate – a long-lasting effect.
Used for the same indications as previous androgenic drugs.
Assign intramuscularly 1 ml 1 time per month.
FV: amp on 1 ml.
17a-alkyl substituted testosterone. It differs from previous androgenic drugs with resistance to metabolism in the liver during primary passage, and therefore it is effective when ingested.
By activity inferior to testosterone.
Assign inside, and also for the cheek: with inoperable breast cancer of 25-100 mg, for other indications (male hypogonadism, delayed sexual development, male menopause) – 5-25 mg per day.