Testosterone propionate

Pharmacological properties

Testosterone propionate has a specific androgenic effect: it stimulates the development and function of the external genital organs, prostate gland, seminal vesicles, as well as secondary sexual characteristics in men (voice, hair). participates in the formation of the constitution of the body and sexual behavior in men, enhances libido and potency, stimulates spermatogenesis. reduces the production of lh and fsg. Testosterone is an antagonist of female sex hormones - estrogen, has an antitumor effect in breast tumors in women. It has an anabolic effect, which is manifested by stimulation of protein synthesis, a decrease in fat deposition, a delay in the body necessary for the synthesis of protein of potassium, phosphorus, sulfur, increased fixation of calcium in the bones and increase muscle mass. with sufficient protein nutrition stimulates the production of erythropoietin.

Pharmacokinetics After i / m or s / c administration, it is slowly absorbed at the injection site. Testosterone circulating in the blood enters the target organs, where it is restored to 5-α-dihydrotestosterone, which interacts with cell membrane receptors and penetrates the cell nucleus. Up to 98% of the drug in plasma binds to proteins, mainly to globulins. It is metabolized in the liver to inactive and inactive metabolites that are excreted in the urine. Approximately 6% of the drug is excreted in the feces in an unchanged state.

Indications

Replacement therapy for primary and secondary hypogonadism, eunuchoidism, impotence of endocrine genesis, postcastration syndrome, male menopause, infertility due to impaired spermatogenesis, oligospermia, osteoporosis due to androgen deficiency, breast cancer, menopausal dysfunctions, in combination with bleeding with hyperestrogenism, mastopathy, accompanied by premenstrual painful tension of the mammary glands, endometriosis, uterine fibroids.

Application

For men with eunuchoidism, congenital maldevelopment of the sex glands, their removal by surgery or as a result of trauma, as well as with acromegaly, the drug is prescribed IM or s / c 25-50 mg every other day or 2 days later. the duration of the course of treatment depends on the effectiveness of therapy and the nature of the disease. after improving the clinical picture of testosterone, propionate is administered in maintenance doses of 5-10 mg daily or every other day.

With impotence of endocrine genesis, as well as with male menopause, accompanied by vascular and nervous disorders, Testosterone propionate is prescribed 10 mg daily or 25 mg 2-3 times a week for 1-2 months.

For treatment in male infertility, the drug is used in a dose of 10 mg 2 times a week for 4-6 months or 50 mg every other day for 10 days.

With pathological male menopause, the drug is prescribed at 25 mg 2 times a week for 2 months with a monthly break.

At the initial stages of prostatic hypertrophy, 10 mg is administered once every 2 days for 1–2 months.

Women over 45 years of age with dysfunctional uterine bleeding are prescribed 10–25 mg every other day for 20–30 days until the bleeding stops and atrophic cells appear in vaginal smears.

Contraindications

Individual intolerance to the drug, prostate cancer or breast cancer in men, liver tumors currently or in history, severe liver dysfunction, hypercalcemia, hypercalciuria, untreated congestive heart failure, coronary heart disease.

Side effects

From the reproductive system and mammary glands: priapism, increased sexual arousal, increased libido and frequent erection, gynecomastia, pain in the mammary glands.when used in high doses in men, inhibition of spermatogenesis, testicular atrophy is possible. androgens in men can cause prostatic hyperplasia, the growth of malignant tumors of the prostate gland. masculinization (virilism) phenomena can be observed in women: coarsening of the voice, excessive growth of hair on the face and body, face pastiness, inhibition of ovarian function, menstruation irregularities, atrophy of the mammary glands and endometrial tissues, increased oily skin, clitoral hypertrophy. virilization may be irreversible even after stopping the use of testosterone.

From the respiratory system: respiratory disorders, sleep apnea.

From the musculoskeletal system: leg pain, arthralgia, muscle cramps.

Gastrointestinal disturbances: diarrhea, nausea, gastrointestinal bleeding.

Hepatobiliary disorders: increased levels of aminotransferases, impaired liver function, jaundice, cholestatic hepatitis, when used in high doses over a long period, cases of liver tumors have been reported.

On the part of the blood system and lymphatic system: isolated cases of polycythemia, tendency to thrombosis, increased hematocrit, inhibition of blood coagulation factors.

From the skin and its derivatives: various skin reactions, including acne, seborrhea, baldness, itching.

Metabolic and nutritional disorders: weight gain, hypercalcemia, impaired glucose metabolism, increased LDL levels, decreased HDL levels.

Neurological disorders: dizziness, sweating, headache, nervousness, depression.

General disorders and disorders at the injection site: pain at the injection site, subcutaneous hematoma at the injection site; long-term treatment with testosterone propionate or its use in high doses can sometimes lead to an increase in the frequency of fluid retention and edema; hypersensitivity reactions, including in the form of fever, chills and sensations of heat throughout the body.

special instructions

Like all oil solutions, testosterone propionate is administered in oil. Care must be taken to ensure that the substance that is administered does not enter the vessel. with a very slow administration of a solution, short-term reactions can sometimes be avoided, sometimes noted during or immediately after an injection of an oil solution (urging to cough, coughing attacks, respiratory depression).

Use caution in patients with heart failure, hypertension, epilepsy, migraine, impaired renal function.

In patients with impaired heart, kidney, or liver function, the use of androgens can cause a complication in the form of edema with or without congestive heart failure. Caution should be exercised when using the drug in patients with conditions that cause fluid retention and cause the development of edema. Use with caution in patients with porphyria.

During treatment with the drug, liver and kidney, thyroid, and blood glucose levels should be monitored.

Before starting treatment in men, it is necessary to exclude prostate cancer, since with the use of the drug androgens increase the risk of prostatic hyperplasia. For preventive purposes, it is recommended to conduct regular examinations of the prostate gland.

In patients taking androgens for a long period, in addition to laboratory measurements of testosterone concentration, it is necessary to check the following laboratory parameters: hemoglobin level, hematocrit (at first every 3 months, then 1 time per year) and liver function tests.

In connection with a possible tendency to thrombosis, the drug should be prescribed to men with caution after a recent surgery or injury.

Drug abuse or addiction.Androgens cannot be used to enhance muscle development in healthy people and to increase physical abilities.

Use during pregnancy or lactation. There is insufficient data on the use of the drug during pregnancy or lactation. Given the characteristic virilizing effect of the drug on the fetus, its use is contraindicated during pregnancy or lactation. The use of the drug should be discontinued when diagnosing pregnancy.

Children. Safety and efficacy in children have not been studied, therefore, the drug is not recommended for use in pediatric practice. The use of testosterone in children, along with masculinization, can cause accelerated growth and maturation of bone tissue, as well as premature closure of the growth zone of the pineal gland, which will result in a decrease in final growth.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. While taking the drug should refrain from driving vehicles and working with other mechanisms.

Interactions

When combined with substances that are inducers of microsomal liver enzymes (barbiturates, rifampicin, carbamazepine, phenylbutazone, phenytoin), the effect of testosterone may be weakened. with pronounced hypogonadism of testosterone, propionate can be combined with drugs that stimulate thyroid function, estrogens.

Enhances the action of anabolic agents, vitamins, preparations containing calcium, phosphorus, slows down the elimination of cyclosporine.

Androgens can increase glucose tolerance and reduce the need for insulin or oral antidiabetic drugs in people with diabetes.

Androgens can affect the metabolism of other drugs (an increase in plasma concentrations of oxyphenbutazone was noted). In addition, it was reported that testosterone and its derivatives increase the activity of oral anticoagulants, which may require dose adjustment. Regardless of this fact, you should always adhere to the restrictions regarding IM injections in patients with acquired or hereditary bleeding disorders.

The simultaneous use of Testosterone and ACTH or corticosteroids may increase the risk of edema.

Barbiturates and alcohol decrease testosterone activity.

Overdose

When using the drug in high doses or for a long time, the side effects described in the corresponding section may develop. in this case, the drug should be discontinued, and after the disappearance of androgen-dependent side effects continue in lower doses. if necessary, carry out symptomatic treatment.

An overdose of the drug can lead to the cessation of menstruation.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° c.