Testosteroni propionas

General characteristics. Structure:

Active ingredient: testosterone propionate;

1 ml of solution contains Testosteroni propionas in terms of 100% substance of 50 mg;

excipient: ethyl oleate.

Pharmacological properties:

Pharmacodynamics. Testosteroni propionas has specific androgenic effect: stimulates development and function of external genitals, a prostate, seed bubbles, and also secondary sexual characteristics in men (a voice, indumentum). Participates in formation of the constitution of a body and a sexual behavior at men, strengthens a libido and a potentiality, stimulates a spermatogenesis. Reduces production of luteotropic and follicle-stimulating hormones. Testosterone is an antagonist of female sex hormones – estrogen, possesses antineoplastic action at tumors of a mammary gland at women. Has anabolic effect that is shown in stimulation of synthesis of protein, reduction of an adiposity, a delay in an organism necessary for synthesis of protein of potassium, phosphorus, sulfur, strengthening of fixing of calcium in bones and increase in muscle bulk. At sufficient proteinaceous nutrition stimulates production of erythropoetin.

Pharmacokinetics. After intramuscular or hypodermic introduction it is slowly absorbed from the place of an injection. Testosterone circulating in blood gets into target organs where it is recovered to 5-α-дигидротестостерона which interacts with receptors of a cellular membrane and gets into a cell kernel. To 98% of drug in a blood plasma contacts proteins, generally globulins. It is metabolized in a liver to low-active and inactive metabolites which are brought out of an organism with urine. About 6% of drug are removed by intestines in not changed state.

Pharmaceutical characteristics

Main physical and chemical properties: oily liquid of light green or light yellow color with a specific smell.

Indications to use:

Replacement therapy at primary and secondary hypogonadism, an eunuchoidism; impotence of endocrine genesis, postkastratsionny syndrome, men's climax; infertility owing to disturbance of a spermatogenesis, an oligospermatism; the osteoporosis caused by insufficiency of androgens; breast cancer; climacteric frustration at women (in combination with estrogen); dysfunctional uterine bleedings at a hyperestrogenism; the mastopathies which are followed by the premenstrual painful tension of mammary glands; endometriosis, hysteromyomas.

Route of administration and doses:

To men at an eunuchoidism, an inborn underdevelopment of gonads, removal their surgical way or as a result of an injury, and also at an acromegalia to appoint drug intramusculary or subcutaneously on 25-50 mg every other day or in 2 days. Duration of a course of treatment depends on efficiency of therapy and the nature of a disease. After improvement of the clinical picture Testosteroni propionas to enter in maintenance doses 5-10 mg daily or every other day. At impotence of endocrine genesis, and also at the men's climax which is followed by vascular and nervous breakdowns propionate to appoint Testoteron on 10 mg daily or on 25 mg 2-3 times a week for 1-2 months. For treatment of male infertility to use drug in doses on 10 mg 2 times a week within 4-6 months or on 50 mg every other day within 10 days. At a pathological men's climax to appoint drug on 25 mg 2 times a week within 2 months with a monthly break. At initial stages of a prostatauxe to enter 10 mg once in 2 days for 1-2 months.

To women 45 years at dysfunctional uterine bleedings are more senior to appoint 10-25 mg every other day within 20-30 days before the termination of bleeding and emergence of atrophic cells in vulval smears.

Features of use:

As well as all Solutio oleosa, Testosteroni propionas it is entered intramusculary. It is necessary to watch that substance which is entered did not get to a vessel carefully. At very slow administration of solution it is possible to avoid emergence of the short-term reactions which sometimes are noted in time or right after Solutio oleosa injection (desires to cough, fits of coughing, respiratory depression).

With care to appoint the patient with heart failure, arterial hypertension, epilepsy, migraine, a renal failure.

With cordial, renal or hepatic disturbances in the anamnesis use of androgens can cause a complication in the form of hypostases with congestive heart failure in patients or without it. It is necessary to adhere to care at use of drug for patients with the states causing a delay of liquid and causing development of hypostases. With care to use drug at patients with a porphyria.

During treatment by drug it is necessary to control indicators of functions of a liver and kidneys, a thyroid gland and sugar level in blood.

Before an initiation of treatment at men it is necessary to exclude the diagnosis of a prostate cancer as at drug use androgens increase risk of development of a hyperplasia of a prostate. With the preventive purpose it is recommended to conduct regular examinations of a prostate.

At the patients accepting androgens during the long period in addition to laboratory measurements of concentration of Testosterone, it is necessary to check the following laboratory indicators: hemoglobin, a hematocrit (in the beginning – each 3 months, then – once a year) and functional trials of a liver.

Due to the possible tendency to a thrombogenesis with care men should appoint drug after recently undergone operation or an injury.

Abuse of drug or accustoming. Androgens cannot be applied to strengthening of development of muscles in healthy people and to increase in physical abilities.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

During administration of drug it is necessary to abstain from control of motor transport and work with other mechanisms.

Side effects:

From reproductive system and mammary glands: a priapism, the raised sexual excitement, strengthening a libido and a frequent erection, a gynecomastia, mammary gland pain. At use of high doses for men oppression of a spermatogenesis, an atrophy of testicles is possible. Androgens can cause a prostate hyperplasia, growth of malignant tumors of a prostate in men. At women the phenomena of a masculinization (virilism) can be observed: voice coarsening, excess growth of hair in the face and body, pastosity of the person, oppression of function of ovaries, frustration of periods, atrophy of mammary glands and fabrics of an endometria, fat content of skin, clitoris hypertrophy. Virilescence can be irreversible even after testosterone phase-out.

From respiratory system: respiratory disturbances, an apnoea in a dream.

From a musculoskeletal system: onychalgia, arthralgia, myotonia.

gastroкишечныенарушения: diarrhea, nausea, gastrointestinal bleeding. Gepatobiliarny disturbances: increase in level of aminotransferases, abnormal liver functions, jaundice, cholestatic hepatitis, at use of high doses throughout the long period was reported about cases of tumors of a liver.

From system of blood and lymphatic system: isolated cases of a polycythemia, tendency to fibrinferments, increase in a hematocrit, oppression of blood-coagulation factors.

From skin and its derivatives: various skin reactions, including an acne, seborrhea, baldness, an itch.

Metabolic and alimentary disturbances: increase in body weight, hypercalcemia, glucose exchange disturbance, increase in level of lipoproteids of low density, decrease in level of lipoproteids of high density.

Neurologic disturbances: dizziness, the increased sweating, a headache, nervousness, a depression.

General disturbances and condition of the place of an injection: pain in the place of an injection, a hypodermic hematoma in the place of an injection; long treatment by Testosteroni propionas or its use in high doses can sometimes lead to increase in frequency of cases of a delay of liquid and hypostases; hypersensitivity reactions, including in the form of temperature increase, a fever and feeling of heat in all body.

Interaction with other medicines:

At the combined use with the substances which are inductors of microsomal enzymes of a liver (barbiturates, rifampicin, carbamazepine, phenylbutazone, Phenytoinum), the effect of testosterone can be weakened. At sharply expressed hypogonadism Testosteroni propionas can be combined with the drugs stimulating function of a thyroid gland, estrogen.

Strengthens action of anabolic means, vitamins, drugs, calciferous, phosphorus, slows down cyclosporine elimination.

Androgens can increase tolerance to glucose and reduce the need for insulin or for peroral antidiabetic drugs at the persons suffering from a diabetes mellitus.

Androgens can influence metabolism of other medicines (growth of serumal concentration of an oksifenbutazon was noted). Besides, it was reported that testosterone and its derivatives increase activity of peroral anticoagulants that can demand dose adjustment. Irrespective of this fact it is always necessary to adhere to the restrictions concerning intramuscular injections, to patients with the acquired or inherited disorders of coagulability of blood.

Simultaneous use of Testosterone and adrenocorticotropic hormone or corticosteroids can increase risk of emergence of hypostases.

Barbiturates and alcohol reduce activity of testosterone.

Contraindications:

Individual intolerance of drug, prostate cancer or breast cancer at men, liver tumors now or in the anamnesis, heavy abnormal liver functions, a hypercalcemia, a hypercalcuria, not treated congestive heart failure, coronary heart disease.

Overdose:

At use of drug in the raised doses or for a long time the side effects described in appropriate section can develop. In this case drug should be cancelled, and after disappearance of androgenzavisimy side effects to continue in smaller doses. If necessary to carry out a symptomatic treatment.

The overdose of drug can lead to the termination of periods.

Use during pregnancy of an ilikormleniye a breast

 

There are no sufficient data about use of drug during the periods of pregnancy or feeding by a breast. Considering characteristic virilizuyushchy influence of drug on a fruit use it is contraindicated during the periods of pregnancy or feeding by a breast. Use of drug should be stopped when diagnosing pregnancy.

Children

Safety and efficiency of use to children were not studied therefore it is not recommended to use drug in pediatric practice. Testosterone use to children together with a masculinization can become the reason of the accelerated growth and ripening of a bone tissue, and also premature closing of region of growth of an epiphysis that as a result will lead to decrease in final growth.

Storage conditions:

Period of validity. 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule. On 5 or 10 ampoules in a pack. On 5 ampoules in the blister. On 1 or 2 blisters in a pack.