Aquatest

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of testosterone.

Excipients: benzyl alcohol, миристил-γ-пиколиния chloride, a macrogoal 400, sodium chloride, water for injections. 

Androgenic hormone.

Pharmacological properties:

Pharmacodynamics. Testosterone is primary male sex hormone synthesized and emitted by testicles. It stimulates growth and development of men's generative organs and secondary sexual characteristics (maturing of a prostate, seed bubbles, a penis and a scrotum), distribution of hair on men's type on a face, a pubis, a breast), development of a throat, muscles of a body and fat distribution. Nitrogen, sodium, potassium and phosphorus detains, strengthens anabolism and reduces a catabolism of proteins. Premature increase in concentration of testosterone in a blood plasma during the period before puberty causes closing of an epiphysis and suspension of growth. Stimulates products of erythropoetin and erythrocytes. On a negative feedback mechanism (feedback) oppresses secretion of luteinizing and follicle-stimulating hormones of a hypophysis and the spermatogenesis oppresses.

testosterone has biological and medicinal properties of natural hormone, but is more slowly soaked up and testosterone is more resistant in an organism, than. Testosterone is appointed mainly to men at a sexual underdevelopment, functional disturbances in a reproductive system, a menopausal syndrome, at an acromegalia. In some cases testosterone gives positive effect at a prostatauxe: the general state improves, frustration of an urination, etc. decrease. Testosterone can also have positive effect at angioneurotic forms of stenocardia. The positive effect is connected with improvement of blood circulation and processes of exchange in a cardiac muscle; also favorable shifts of a lipidic ratio in blood, increase in coefficient lecithin/cholesterol are observed.

Administration of testosterone to women causes braking of gonadotropic function of a hypophysis, oppression of function of the follicular device and ovaries, an endometria atrophy, suppression of function of mammary glands. Shows beneficial effect at complaints of a climacteric.

Pharmacokinetics. Testosterone begins the action right after an injection and works during 24 h. In blood of nearly 98% of testosterone contacts the specific fraction of globulins connecting testosterone and oestradiol. Biotransformation occurs in a liver to various 17 ketosteroids which after conjugation with glucuronic or sulphuric acid are allocated with urine (about 90%). About 6% of the absorbed drug are removed with a stake in an untied look.

Indications to use:

Men have an androgenic insufficiency after castration, an eunuchoidism, impotence of a hormonal origin, symptoms of a men's climax (decrease in a libido, intellectual and physical activity), at an acromegalia; at a prostatauxe; the osteoporosis caused by androgenic insufficiency; at angioneurotic forms of stenocardia.

At women – at climacteric vascular and nervous breakdowns when oestrogenic drugs are contraindicated (at tumors of generative organs and mammary glands, uterine bleedings); along with radiation therapy at a breast cancer and ovaries (usually at women aged up to 60 years); at dysfunctional uterine bleedings at elderly women.

Route of administration and doses:

Intramusculary, it is deep in a gluteus. The dose is established individually depending on indications and reaction of the patient.

To men at an eunuchoidism, an inborn underdevelopment of gonads, their removal a surgical way or as a result of an injury, and also at an acromegalia appoint 25 mg daily or on 50 mg every other day or in 2 days. The term of treatment depends on efficiency of therapy and the nature of a disease. Usually treatment is carried out for a long time. After improvement of a clinical picture enter testosterone in maintenance doses: 5-10 mg daily or every other day.

At impotence in connection with functional insufficiency of gonads, overfatigue and nervous exhaustion, and also at a men's menopausal syndrome appoint 10 mg daily or on 25 mg 2-3 times a week within 1-2 months.

At a prostatauxe in an initial stage accept 10 mg every other day within 1-2 months.

At patients with stenocardia the positive effect at use of testosterone on 10 - 12,5 mg is sometimes observed once a week; at good tolerance number of injections increase to two in a week (during 3 - 5 weeks). By the end of treatment the dose and quantity of injections are reduced again. The course of treatment consists of 15-20 injections.

To women 45 years at dysfunctional uterine bleedings are more senior appoint 10-25 mg every other day within 20-30 days before the termination of bleeding and emergence of atrophic cells in vulval smears. Previously it is necessary to exclude malignant new growths of a uterus.

At vascular and nervous breakdowns of a climacteric origin at women and existence of contraindications to use of estrogen, enter testosterone on 10 mg every other day or on 25 mg 2 times a week during 2-3 weeks.

At malignant tumors of a mammary gland or ovaries testosterone enter in a dose 50 mg daily within several months, then (depending on results of treatment) reduce a dose and for a long time appoint maintenance doses. As addition to surgical intervention or radiation therapy drug is appointed to women up to 60 years (women of more advanced age are recommended to accept estrogen).

The highest doses intramusculary for adults: one-time 50 mg, daily 100 mg.

The drug cannot be administered intravenously!

Features of use:

In case of androgenzavisimy side reactions treatment by testosterone should be stopped. After disappearance of side effects to resume treatment in lower doses.

Patients with the latent or expressed heart failure, a renal failure, hypertensia, epilepsy or migraine (or existence of these states in the anamnesis) are subject to constant observation as androgens can cause a delay of sodium and water in some cases. At long reception to check functions of a liver. At patients with cancer of a mammary gland, a hypernephroma, lung cancer with metastasises in bones to check calcium level in blood and urine.

At boys in the prepubertatny period androgens have to be applied with care in order to avoid premature closing of an epiphysis and the accelerated sexual development.

Side effects:

- priapism and other signs of excess sexual stimulation (frequent erection);
- boys in the prepubertatny period have an accelerated sexual development, increase in frequency of erections, increase in a penis and premature closing of an epiphysis;
- damage of a spermatogenesis and disturbance of maturing of spermatozoa, oligospermatism and decrease in volume of an ejaculate;
- anomalies of a prostate;
- women have a bleeding from patrimonial ways, strengthening of a libido; at long use of drug virilescence symptoms are possible;
- hirsutism, gynecomastia;
- seborrhea, eels, fat skin, the accelerated hair loss;
- delay of sodium and water, hypostases;
- hypercalcemia symptoms;
- thrombophlebitis;
- nausea, cholestatic jaundice, increase in level of aminotransferases of a liver (in process of the termination of reception are normalized);
- headache, depression, aggression, alarm, sleep disorder, paresthesias.

Pain, itch and hyperemia in the place of an injection are possible.

Interaction with other medicines:

Increases efficiency of anticoagulants and hypoglycemic means (it is necessary to change doses), inhibits cyclosporine removal. Inductors of liver enzymes (barbiturates, rifampicin, carbamazepine, phenylbutazone, Phenytoinum) reduce effect of testosterone.

Contraindications:

The increased individual sensitivity to drug components, a carcinoma of a prostate or mammary gland; nephrosis or nephrotic phase of nephrite, hypostases; hypercalcemia; abnormal liver function; diabetes mellitus; heart and coronary failure, a myocardial infarction in the anamnesis, atherosclerosis at elderly men; pregnancy, feeding by a breast.

Overdose:

At acute overdose toxicity of testosterone extremely low.

At chronic overdose development of a priapism is possible. In this case treatment should be stopped, and after disappearance of symptoms - to begin in smaller doses.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Suspension for injections of 50 mg/ml or 100 mg/ml. On 1 ml or 2 ml in ampoules; on 1 ml, 2 ml or 5 ml in bottles.