Testosterone propionate

Testosterone propionate exhibits significant anabolic and androgenic effects (regulates the activity of male gonads and protein binding).

The drug has specific androgenic properties: it stimulates the activity and development of the genitals, prostate with seminal vesicles, and along with this, 2-nd sexual characteristics of the male type (hair and voice). It is a participant in the processes of formation of the body constitution, as well as male sexual behavior, helps to increase potency and libido, and in addition, stimulates the process of spermatogenesis. Reduces the volume of produced FSH and prolactin. [ 1 ]

Indications Testosterone propionate

It is used in men in cases of sexual underdevelopment or disorders in the functioning of the reproductive system, as well as in menopause (can develop in people over 50 years of age - a condition when a man becomes infertile ) and the nervous and vascular disorders caused by it. It is also prescribed in cases of acromegaly (a disease affecting the pituitary gland; it is characterized by an increase in the size of internal organs, feet with hands and nose with lower jaw, as well as metabolic disorders) and prostate hypertrophy.

The drug is prescribed to women for neurovascular disorders caused by the onset of menopause (if it is impossible to use estrogenic substances or female gonadosteroids), and ovarian and breast carcinoma (in people under 60 years of age). In addition, it is used for pathological uterine bleeding (caused by ovarian dysfunction) in elderly patients.

Release form

The medicinal substance is released in the form of an injection liquid, inside ampoules with a capacity of 1 ml. The box contains 5 or 10 ampoules of the medicine.

Pharmacodynamics

Testosterone is an antagonist of female gonadosteroids (estrogens); it demonstrates an antitumor effect in neoplasms in the breast area in women. It has anabolic activity - it stimulates protein binding, reduces the volume of deposited fat, retains sulfur and potassium with phosphorus required for protein binding in the body, and in addition, it potentiates calcium fixation in bones and increases muscle mass.

In case of sufficient protein intake, the drug stimulates the production of erythropoietin. [ 2 ]

Pharmacokinetics

With subcutaneous or intramuscular injections, the substance is absorbed at a low rate from the injection site. Testosterone circulating in the bloodstream penetrates into target organs, being reduced there to 5-a-dihydrotestosterone, which interacts with the ends of the cell wall, after which it passes into the cell nucleus.

About 98% of the drug is synthesized with protein in the blood plasma (most of it with globulins).

Metabolic processes are realized inside the liver with the formation of metabolic components excreted with urine, which have weak (or no) therapeutic activity. About 6% of unchanged drug is excreted through the intestine.

Dosing and administration

For men with acromegaly, eunuchoidism, congenital underdevelopment of the gonads and their removal due to injury or surgery, a dosage of 25-50 mg is required, which is administered subcutaneously or intramuscularly with a frequency of every other day or 2 days. The duration of such a treatment cycle is determined by the nature of the pathology and the effectiveness of the drug. When symptoms of improvement appear, the drug is administered in maintenance doses - 5-10 mg (daily or every other day).

In case of impotence of endocrine origin and andropause (against which nervous and vascular disorders are observed), the medication is used in a dosage of 10 mg daily or in a portion of 25 mg 2-3 times a week for 1-2 months.

For infertility in men, the drug is administered in doses of 10 mg 2 times a week for 4-6 months or in the amount of 50 mg (every other day) for a period of 10 days.

In case of pathological andropause, Testosterone propionate is used 2 times a week at a dosage of 25 mg, for 2 months. It can also be used at 1-month intervals for a period of 1-2 months.

Women are prescribed it in combination therapy for breast carcinoma – 0.1 g is administered 2-3 times a week.

• Application for children

There is no data regarding the efficacy of Testosterone propionate and its safety in pediatrics, which is why it is not prescribed to children.

The use of testosterone in pediatrics can lead to accelerated maturation and growth of bone tissue, masculinization, and along with this, to premature closure of the growth epiphyseal zone, which will reduce the final height of the child.

Use Testosterone propionate during pregnancy

There is not enough information regarding the use of the drug during lactation and pregnancy. Given the characteristic virilizing effect on the fetus, it cannot be prescribed during breastfeeding or pregnancy. If the patient has been diagnosed with conception, the use of the drug should be stopped.

Contraindications

Main contraindications:

• severe sensitivity to the drug;
• prostate or breast carcinoma in men;
• neoplasms in the liver area (also present in the anamnesis);
• severe liver dysfunction;
• hypercalciuria or -calcemia;
• CHF that was not treated, as well as coronary heart disease.

Side effects Testosterone propionate

Side effects include:

• lesions associated with the mammary glands and reproductive function: increased sexual arousal, priapism, gynecomastia, increased frequency of erections and potentiation of libido, as well as chest pain. The use of large doses leads to suppression of spermatogenesis and testicular atrophy in men. The action of androgens can provoke the growth of malignant neoplasms in the prostate area and its hyperplasia. In women, signs of virilism may develop: increased hair on the body and face, coarsening of the voice, suppression of ovarian activity, facial pastosity, atrophy of the endometrial tissue and breasts, menstrual irregularities, clitoral hypertrophy and epidermal fat. The virilization process may be incurable even after discontinuation of testosterone administration;
• respiratory problems: respiratory distress or sleep apnea;
• disorders of the musculoskeletal system: arthralgia, pain affecting the legs, and muscle cramps;
• gastrointestinal disorders: nausea, diarrhea or bleeding in the gastrointestinal tract;
• lesions affecting the hepatobiliary system: jaundice, increased aminotransferase levels, cholestatic hepatitis, liver dysfunction. With prolonged administration of large doses, tumors in the liver area may be observed;
• disorders associated with the blood system and lymph: polycythemia is observed sporadically; the hematocrit index may increase or the blood clotting factor may be suppressed. A tendency to thrombosis also develops;
• problems with the epidermis and its derivatives: various epidermal symptoms, including seborrhea, acne, itching and alopecia;
• alimentary and metabolic disorders: hypercalcemia, decreased HDL levels or increased LDL levels, weight gain and glucose metabolism disorders;
• neurological signs: hyperhidrosis, depression, dizziness, nervousness and headaches;
• Systemic disorders and problems at the injection site: hematoma under the skin or pain at the injection site. With prolonged use of the drug or administration in high doses, the incidence of swelling and cases of fluid retention sometimes increases. Symptoms of intolerance may occur, including chills, increased temperature, and fever throughout the body.

Overdose

Using the drug in high doses or over a long period of time may cause symptoms listed in "side effects".

In case of such a violation, the medication should be discontinued, and when the negative signs associated with androgen disappear, its use should be continued in reduced doses. Symptomatic actions are performed if necessary.

Interactions with other drugs

Administration together with drugs that induce intrahepatic microsomal enisms (rifampicin, phenytoin with barbiturates, phenylbutazone and carbamazepine) may reduce the effect of testosterone.

In cases of severe hypogonadism, the medication can be combined with substances that stimulate thyroid activity and estrogens.

Testosterone propionate potentiates the activity of anabolic steroids, vitamins and medications that contain phosphorus or calcium, and also reduces the rate of elimination of cyclosporine.

Androgens can enhance glucose tolerance and reduce insulin requirements (or the need for oral hypoglycemic drugs) in diabetics.

Androgens also affect the metabolic processes of other medications (an increase in serum levels of oxyphenbutazone is noted).

There is evidence that testosterone and its derivatives increase the effect of oral anticoagulants, which may require a change in dosage. All restrictions regarding injections in individuals with blood clotting disorders (hereditary or acquired) must be observed at all times.

The combination of testosterone with corticotropin or corticosteroids increases the likelihood of developing edema.

Alcohol and barbiturates reduce the effects of testosterone.

Androgens are able to reduce the indices of thyroxine-binding globulin, which causes a decrease in the total values of thyroxine and potentiation of the capture of thyroxine with triiodothyronine. At the same time, the indices of free fractional thyroid hormones do not change.

There are no clinical symptoms of deterioration of thyroid function.

Storage conditions

Testosterone propionate should be stored in a place closed to children. Temperature values - no more than 25°C.

Shelf life

Testosterone propionate can be used within 2 years from the date of manufacture of the pharmaceutical product.

Analogues

Analogues of the drug are the substances Androgel, Methyltestosterone with Sustanon, as well as Testenate and Testosterone anddecanoate.