Testosterone Propionate
Description of the dosage form
Transparent oily liquid of light yellow color.
Note. During storage, crystals may fall out or the entire contents of the ampoule may crystallize. In case of crystal precipitation or crystallization of the entire contents of the ampoule, the ampoule should be heated in a boiling water bath with shaking. If the crystals disappear and the solution becomes clear, and when cooled to 36-38 ° C the crystals do not fall out again, the drug is suitable for use.
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Pharmacokinetics
Suction
the maximum concentration after intramuscular administration of the drug is observed after 2.5-5 hours
Distribution
in the blood, testosterone binds (about 98%) to a specific fraction of globulins that bind testosterone and estradiol.
Metabolism
Testosterone is metabolized mainly in the liver with the formation of inactive androsterone and inactive etiocholanolone.
Derivation
excreted as metabolites, mainly by the kidneys and intestines (about 6%). The elimination half-life is 3-4 hours.
Pharmacodynamics
Androgenic agent, also has an anabolic effect. In target cells (skin, prostate, seminal vesicles, epididymis) it is reduced by 5-alpha-reductase to 5-alpha-dihydrotestosterone, which specifically interacts with receptors on the cell surface and penetrates the nucleus. In some tissues (including the hypothalamus) it is converted to estradiol. In men, stimulates the development and activity of the gonads, prostate, seminal vesicles, the formation of secondary male characteristics (growth, low voice, growth of beard and mustache), increases libido and potency; indirectly, through the central nervous system, affects sexual behavior. Reduces fat deposition and micronutrient excretion. Inhibits the production and release by the pituitary gland of luteinizing hormone and follicle-stimulating hormone. Has anabolic effects: participates in skeletal growth, increases skeletal muscle mass; causes a delay of nitrogen, phosphorus, potassium ions, sulfur, necessary for protein synthesis.
Indications
In men: replacement therapy for primary and secondary hypogonadism (delayed puberty, hypopituitarism, eunuchoidism, post-castration syndrome, oligospermia).
In women: progressive inoperable metastatic breast cancer.
Contraindications
Asthenic physique, old age in men, in men with hypertension, in patients with epilepsy, in patients with migraine, in patients with coronary heart disease prone to edema, adolescence in boys (before puberty), benign .
