Testosterone propionate (Solution) Instructions for Use

ATC Code

G03BA03 (Testosterone)

Active Substance

Testosterone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Androgenic drug – depot form

Pharmacotherapeutic Group

Sex hormones and modulators of the genital system; androgens; derivatives of 3-oxoandrost-4-ene

Pharmacological Action

A hormone of the male gonads. It possesses androgenic activity. It promotes the formation of the genital organs and the development of secondary sexual characteristics in men. In hypogonadism of various etiologies, exogenous Testosterone compensates for the deficiency of the endogenous hormone.

Testosterone also has an anabolic effect: it stimulates protein synthesis in the body, accelerates bone calcification. It causes retention of nitrogen, potassium, calcium, sulfur, phosphates, as well as sodium, chlorine, and water in the body. It stimulates erythropoiesis.

In women, Testosterone causes suppression of the gonadotropic function of the pituitary gland, the function of the ovaries and mammary glands, and atrophy of the endometrium.

Pharmacokinetics

After intramuscular administration, C_max in plasma is reached between 2.5-5 hours. In the blood, Testosterone binds (about 98%) with a specific fraction of globulins that bind Testosterone and estradiol.

It is metabolized mainly in the liver, forming the weakly active androsterone and the inactive etiocholanolone. It is excreted in the form of metabolites, mainly by the kidneys and through the intestines (about 6%). T_1/2 from plasma is 3-4 hours.

After application to the skin, the degree of testosterone absorption is 9-14%.

Indications

For parenteral use: in men – replacement therapy for primary and secondary hypogonadism (delayed puberty, hypopituitarism, post-castration syndrome, eunuchoidism, oligospermia); in women – progressive inoperable breast cancer.

For topical use: in men – replacement therapy for hypogonadism in men, when testosterone deficiency is confirmed by clinical symptoms and laboratory tests.

ICD codes

Dosage Regimen

For intramuscular injection only. Administer deep into the gluteal muscle. A single dose ranges from 25 mg to 100 mg. The frequency of administration is determined by the specific treatment regimen and individual patient response.

For male hypogonadism, typical regimens involve administration two to three times per week to maintain stable physiological testosterone levels. Adjust the dose based on periodic clinical evaluation and serum testosterone concentration measurements.

For inoperable breast cancer in women, use higher doses, typically 50 mg to 100 mg, administered two to three times weekly. Continue therapy as long as a therapeutic response is observed.

For topical use, apply the appropriate formulation according to its specific instructions. Apply to clean, dry, intact skin on the back, abdomen, upper arms, or thighs. Rotate application sites daily. Avoid application to genital areas. Wash hands thoroughly after use.

Monitor serum testosterone levels at the initiation of therapy and at regular intervals thereafter. Titrate the dosage to achieve and maintain levels within the eugonadal range. In prepubertal adolescents, monitor bone age regularly to prevent premature epiphyseal closure.

In elderly patients or those with concurrent conditions such as coronary artery disease, hypertension, or renal impairment, initiate therapy with caution and at the lower end of the dosing range. Observe for signs of fluid retention or worsening of underlying conditions.

Adverse Reactions

From the blood and lymphatic system often – polycythemia; infrequently – increased hematocrit, increased hemoglobin, increased red blood cell count.

From the immune system infrequently – hypersensitivity, allergic reactions.

From the endocrine system infrequently – in women – menstrual cycle disorders, amenorrhea, inhibition of gonadotropin secretion, masculinization, hirsutism; in men – gynecomastia, priapism, oligospermia, impaired spermatogenesis; in boys – precocious puberty, premature closure of bone epiphyses, weight gain, breast and testicular pain.

From metabolism infrequently – retention of sodium salts and water, increased levels of cholesterol and triglycerides in blood plasma, hypercalcemia, increased appetite, increased content of glycosylated hemoglobin.

Mental disorders infrequently – depression, emotional disturbances, insomnia, anxiety, aggressiveness, irritability.

From the nervous system infrequently – dizziness, headache, migraine, tremor.

From the cardiovascular system infrequently – increased blood pressure, impaired cardiovascular function.

From the respiratory system infrequently – bronchitis, sinusitis, cough, dyspnea, snoring, dysphonia.

From the digestive system infrequently – nausea, diarrhea, cholestatic jaundice, abnormal liver function tests, increased AST activity.

From the skin and subcutaneous tissues infrequently – acne, seborrhea, dry skin, alopecia, erythema, rash, papular rash, itching.

From the musculoskeletal system infrequently – myalgia, arthralgia, pain in extremities, muscle spasms, muscle tension, musculoskeletal rigidity, increased blood CPK activity.

From the urinary system infrequently – urinary retention, nocturia, dysuria, decreased urine output, impaired urinary tract function.

From the genital organs and breast often – hot flashes, increased level of prostate-specific antigen, pathological results of prostate examination, benign prostatic hyperplasia; infrequently – increased or decreased libido, breast induration, increased estradiol concentration, increased concentration of free testosterone in blood serum, in men – frequent erection, decreased ejaculate volume, prostatitis, prostatic intraepithelial neoplasia, prostate induration, impaired prostate function.

General reactions infrequently – increased fatigue, asthenia, hyperhidrosis, night sweats

Local reactions often – pain, discomfort, itching, swelling, hematoma, irritation at the injection site. With topical use – dryness and irritation of the skin at the application site.

Contraindications

Breast cancer in men, prostate cancer, gynecomastia, nephrotic stage of chronic glomerulonephritis, prostate hypertrophy with urinary retention, renal failure, hepatic failure, hypercalcemia, chronic heart failure, diabetes mellitus, history of myocardial infarction, widespread atherosclerosis; pregnancy, breastfeeding period.

Not used topically in women.

With caution

Asthenic physique, elderly age in men, arterial hypertension in men, epilepsy, migraine, coronary artery disease in patients prone to edema, adolescent age in boys (before puberty), benign prostatic hyperplasia.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Not used topically in women.

Use in Hepatic Impairment

Contraindicated for use in hepatic failure.

Use in Renal Impairment

Contraindicated for use in the nephrotic stage of chronic glomerulonephritis; in renal failure.

Pediatric Use

When treating prepubertal adolescents, systematic observation is recommended to avoid premature closure of bone epiphyses and precocious puberty.

Geriatric Use

Use with caution in elderly men.

Special Precautions

The concentration of testosterone should be monitored at the beginning of treatment and regularly during treatment. The dose is selected individually to ensure regulation of eugonadal testosterone levels.

Patients with arterial hypertension, migraine, epilepsy require regular medical supervision during treatment. The drug should be used with caution in these patient groups.

In patients suffering from severe cardiac, hepatic or renal failure or coronary artery disease, treatment with testosterone preparations may cause complications characterized by edema with or without chronic heart failure. In this case, treatment should be stopped immediately.

Existing sleep apnea syndrome may worsen, especially in the presence of risk factors such as obesity and chronic respiratory diseases.

Data on the efficacy and safety of testosterone preparations in patients over 65 years of age are limited. There are currently no agreed data on age restrictions for the use of testosterone, but it should be taken into account that with increasing age, the physiological concentration of testosterone in serum decreases.

The use of testosterone for the treatment of children, along with masculinization, can cause accelerated growth and maturation of bone tissue, as well as premature closure of the epiphyseal growth zone, which will ultimately lead to a decrease in final height. Therefore, it is necessary to use with caution in adolescent boys before puberty.

The appearance of common acne is possible.

In women receiving high doses, the development of virilism is possible.

When used by athletes, it must be taken into account that this drug contains an active substance (Testosterone) which may give a positive reaction in anti-doping tests.

Before starting treatment in men, a diagnosis of prostate cancer must be excluded, because the use of androgens increases the risk of developing prostate hyperplasia; the use of androgens may promote the growth of an existing malignant tumor.

During treatment, regular examination of the prostate in men is necessary.

Rare cases of benign and malignant liver tumors with the development of intra-abdominal bleeding have been reported during treatment with sex steroids.

If severe abdominal pain, liver enlargement, or signs of intra-abdominal bleeding occur during treatment, the possibility of a liver tumor should be considered in the differential diagnosis.

In patients taking androgens for a long period, in addition to laboratory measurements of testosterone concentration, the following laboratory parameters should be periodically checked: hemoglobin, hematocrit (to detect polycythemia), liver function tests and lipid profile.

Cases of abuse of testosterone preparations have been reported, usually in doses exceeding those recommended for approved indications and in combination with other anabolic androgenic steroids. Abuse of testosterone preparations can cause dependence, as well as withdrawal syndrome with a significant dose reduction or abrupt discontinuation of use. Abuse of testosterone preparations, along with other anabolic androgenic steroids, can lead to serious adverse reactions from the cardiovascular system (in some cases with fatal outcomes), liver and/or mental disorders. Abuse of testosterone preparations and other anabolic androgenic steroids poses a significant health risk and is strongly discouraged.

Drug Interactions

With simultaneous use with inducers of microsomal oxidation enzymes (including barbiturates, rifampicin), a decrease in the effectiveness of testosterone is possible. It enhances the effect of indirect anticoagulants (warfarin, nicoumalone, phenindione), which may require dose adjustment.

It enhances the effect of hypoglycemic agents.

It inhibits the excretion of cyclosporine and increases the plasma concentration of oxyphenbutazone.

With simultaneous use of testosterone with ACTH or corticosteroids, the risk of developing edema increases.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.