Testosterone Propionate

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

The drug has specific androgenic properties: it stimulates the activity and developmental processes of the genitals, the prostate with seminal vesicles, and at the same time 2 male sexual characteristics (hair and voice). Is a participant in the formation of the body constitution, as well as male sexual behavior, enhances 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 case of sexual underdevelopment or disorders in the functioning of the reproductive system, and in addition, with menopause (it can develop in people over 50 years old - a condition when a man becomes infertile ) and the nervous and vascular disorders caused by it. It is also prescribed in the case of acromegaly (a disease that affects the pituitary gland; with it, there is an increase in the size of internal organs, feet with hands and a nose with a lower jaw, as well as metabolic disorders) and prostate hypertrophy.

For women, the medication is prescribed 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 (persons under the age of 60). In addition, it is used for pathological bleeding from the uterus (caused by a disorder of the ovarian function) in elderly patients.

Release form

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

Pharmacodynamics

Testosterone is a female gonadosteroid (estrogen) antagonist; it demonstrates an antitumor effect on breast neoplasms in women. It has anabolic activity - it stimulates protein binding, reduces the amount of stored fat, retains sulfur and potassium with phosphorus required for protein binding inside the body, and in addition potentiates calcium fixation inside bones and increases muscle mass.

In the case of a sufficient amount of protein nutrition, the medication stimulates the production of erythropoietin. [2]

Pharmacokinetics

With s / c or i / m injections, the substance is absorbed at a low speed from the injection site. Testosterone circulating inside the bloodstream penetrates into the target organs, recovering there to 5-a-dihydrotestosterone, which interacts with the endings of the cell wall, and then passes into the cell nucleus.

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

Metabolic processes are realized inside the liver with the formation of metabolic components excreted together with urine, which have weak (or do not have at all) therapeutic activity. About 6% of unchanged drugs are excreted through the intestines.

Dosing and administration

For men with acromegaly, eunuchoidism, congenital underdevelopment of the gonads and their removal due to injury or during 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 medication begins to be administered in maintenance doses - 5-10 mg (daily or every other day).

In the case of impotence, which is of an endocrine nature, and andropause (against its background, nervous and vascular disorders are noted), 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.

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

In the 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 applied at 1-month intervals for a period of 1-2 months.

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

• Application for children

There is no data on the effectiveness of Testosterone propionate and its safety in pediatrics, which is why it is not prescribed for children.

The use of testosterone in pediatrics can lead to accelerated maturation and growth of bone tissue, masculinization, and at the same time to premature closure of the growth epiphyseal zone, which will decrease the final growth of the child.

Use Testosterone Propionate during pregnancy

There is not enough information regarding the use of the drug during lactation and pregnancy. Taking into account the characteristic virilizing effect on the fetus, it should not be prescribed for HB or pregnancy. If the patient was diagnosed with conception, the use of drugs must be stopped.

Contraindications

The main contraindications:

• strong sensitivity to medication;
• carcinoma of the prostate or breast in men;
• neoplasms in the liver (also present in the history);
• severe disorders of hepatic activity;
• hypercalciuria or -calcemia;
• CHF that has not been cured, as well as IHD.

Side effects Testosterone Propionate

Among the side effects:

• lesions associated with the mammary glands and reproductive function: increased sexual arousal, priapism, gynecomastia, increased erection frequency and libido potentiation, as well as chest pain. The use of large portions leads to suppression of spermatogenesis and testicular atrophy in men. The action of androgens can provoke the growth of malignant neoplasms in the area of the prostate and its hyperplasia. In women, signs of virilism may develop: an increase in hair on the body and face, coarsening of the sound of the voice, suppression of ovarian activity, facial pastiness, atrophy of endometrial tissues and breasts, menstrual irregularities, clitoral hypertrophy and epidermal fatness. The virilization process may be incurable even after the withdrawal of testosterone administration;
• respiratory problems: respiratory distress or sleep apnea;
• disorders in the work of the musculoskeletal structure: arthralgia, pain affecting the legs, and muscle cramps;
• disorders of the gastrointestinal tract: nausea, diarrhea, or bleeding in the gastrointestinal tract;
• lesions affecting the hepatobiliary system: jaundice, an increase in aminotransferase rates, cholestatic hepatitis, a disorder in the liver. With prolonged administration of large portions, tumors in the region of the liver may be noted;
• disorders associated with the blood system and lymph: polycythemia is observed singly; 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, a decrease in HDL levels or an increase in LDL levels, weight gain and a disorder of glucose metabolism;
• neurological signs: hyperhidrosis, depression, dizziness, nervousness and headaches;
• systemic disorders and problems in the area of the injection: hematoma under the skin or pain in the area of injection of drugs. With prolonged use of the medication or the introduction of high dosages, the frequency of the development of puffiness and cases with fluid retention sometimes increases. Symptoms of intolerance may occur, including chills, fever and fever throughout the body.

Overdose

The use of drugs in high portions or over a long period of time can provoke the appearance of the symptoms indicated in the "side effects".

With such a violation, it is necessary to cancel the medication, and when the negative signs associated with androgen disappear, continue its use in reduced portions. If necessary, symptomatic actions are performed.

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 the case of a pronounced intensity of hypogonadism, the medication can be combined with substances that stimulate the activity of the thyroid gland and estrogens.

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

Androgens can increase glucose tolerance, as well as weaken the insulin requirement (or the need for the use of oral hypoglycemic drugs) in diabetics.

Androgens also affect the metabolic processes of other medicines (an increase in serum values 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. It is required to constantly observe all restrictions on injections in persons with blood clotting disorders (hereditary or acquired).

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

Alcohol and barbiturates reduce the effects of testosterone.

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

There are no clinical symptoms of deterioration in the activity of the thyroid gland.

Storage conditions

Testosterone propionate must be kept out of the reach of children. Temperature values - no more than 25 ° С.

Shelf life

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

Analogs

The analogs of the drug are the substances Androgel, Methyltestosterone with Sustanon, as well as Testanat and Testosterone andecanoate.