International name:Testosterone [mixture of esters] (Testosterone)
Group Affiliation: Androgen
Active ingredient description (INN): Testosterone [mixture of esters].
Pharmaceutical form: solution for intramuscular injection
Pharmacological action: Androgenic agent, also has an anabolic effect. In the target cells (skin, prostate, seminal vesicles, epididymis) it is reduced by 5-alpha-reductase to 5-alpha-dihydrotestosterone, which specifically interacts with the membrane receptors on the cell surface and penetrates into the nucleus. In some tissues (including the hypothalamus) it is converted to estradiol. In men it stimulates development and activity of gonads, prostate gland, seminal vesicles, formation of secondary male characteristics (height, low voice, growth of beard and mustache), increases libido and potency; indirectly, through CNS, influences sexual behavior. Reduces fat deposition and excretion of micronutrients. Inhibits the production and release of pituitary LH and FSH. It has anabolic effects: it participates in the growth of the skeleton, increases the mass of skeletal muscles; it induces retention of nitrogen, phosphorus, K+, sulfur, which are necessary for protein synthesis. The testosterone esters contained in the product have different rates of absorption and excretion, which ensures rapid development of the effect and prolonged action (up to 4 weeks) after a single injection: testosterone propionate remains effective during the first 24 hours, phenylpropionate and isocaproate - 24 hours after injection.
Indications:
In men - replacement therapy for primary and secondary hypogonadism (delayed puberty, hypopituitarism, eunuchoidism, postcastric syndrome, oligospermia); male menopause, impotence (impotentia generandi virilis); androgen deficiency (Addison's disease, adiposogenital syndrome, pituitary nanism), infertility (spermatogenesis disorder). In women - osteoporosis (against a background of androgen deficiency), breast cancer, ovarian cancer, dysfunctional bleeding in hyperestrogenism, uterine myoma, endometriosis, menopausal disorders in women (together with estrogen), premenstrual syndrome, breast cancer (late metastatic forms), osteoporosis.
Contraindications:
Hypersensitivity, prostate cancer and/or breast cancer, gynecomastia, nephrosis or nephrotic stage of nephritis, prostatic hypertrophy with symptoms of urinary retention, hepatic/renal insufficiency, hypercalcemia, edema, CHF, diabetes, myocardial infarction in anamnesis, common atherosclerosis, pregnancy, lactation. With caution. Asthenic constitution, old age in men; adolescence in boys (before puberty).
Side effects:
Acne, seborrhea, edema, allergic reactions, increased libido, frequent erections, reduced ejaculate volume; hypercalcemia; impaired spermatogenesis and sperm maturation; priapism, premature puberty in boys, increased penile size, premature closure of bone epiphyses; Na+ and water retention, dizziness, nausea; pain, itching, hyperemia at the injection site; GI bleeding, metrorrhagia, thrombophlebitis, cholestatic jaundice, increased activity of "liver" transaminases. If it is used for a long time in women - viril syndrome (coarsening of voice, excessive growth of facial and body hair), breast atrophy, amenorrhea.
Overdose. Symptoms: priapism. Treatment: discontinuation of therapy until the symptoms disappear, with subsequent prescription of smaller doses.
Dosage and administration:
V/m. Men - 100-200 mg 1 time in 15 days, the course of treatment - 10-15 injections; in impotence and climacteric syndrome - 0.1 g 1 time in 15 days, the course of treatment - 5 injections. Women with climacteric syndrome are prescribed 0.1 g 1 time 2-3 weeks, with breast and ovarian cancer - 100-200 mg every 1-2 weeks, treatment - long term.
Cautions:
Patients with arterial hypertension, migraine, epilepsy during treatment it is necessary to have regular medical supervision.
Interaction:
Simultaneous use with inducers of microsomal oxidation enzymes (barbiturates, rifampicin and others) may decrease the effectiveness of testosterone.
