Tsiproteron

General characteristics. Structure:

Active ingredient: 50 mg of a tsiproteron in 1 tablet.

Drug with the expressed anti-androgenic, progestagenny and antineoplastic action.

Pharmacological properties:

Pharmacodynamics. Competitively blocks androgenic receptors, action of androgens on cells of target organs oppresses. Inhibits release of gonadotrophins, reduces synthesis of endogenous androgens and their level in blood.

Pharmacokinetics. After intake it is completely soaked up from a GIT (bioavailability — about 100%). Cmax in blood — in 3–4 h, elimination has two-phase character with T1/2 of 3–4 h up to 2 days. After introduction of depot form in oil (bioavailability — 100%) Cmax in a blood plasma — in 1–3 days; T1/2 — 4 days; equilibrium concentration in a blood plasma is established after 4 injections. Linkng with blood proteins (it is preferential with albumine) — about 96%. It is metabolized in a liver. Collects in fatty tissue. Gets into breast milk (at a lactation of 0,2% it can be removed with breast milk). It is removed generally in the form of metabolites with bile (to 70%) and urine (to 30%), a small amount is removed with bile in not changed look.

Reduces or completely eliminates effects of androgens — protects a prostate from influence of androgens of gonads and/or bark of adrenal glands. At men reduces unhealthy sexual desire, reduces a potentiality, reduces function of testicles (changes have reversible character and disappear after the treatment termination).

As a result of anti-gonadotropic effect brakes an ovulation. At women reduces a hair loss on the head and their overgrowth on a face and other parts of a body. Besides, reduces the increased function of sebaceous glands.

Indications to use:

Men have a metastasizing or inoperable prostate cancer (without and after an orkhiektomiya, and also in combination with agonists a hormone gonadotrophin-rileasing — GNRG), hyper sexuality. Women have expressed androgenization phenomena (including a heavy hirsutism, a heavy androgenozavisimy alopecia, severe forms of an acne and seborrhea). Children have a premature sexual development.

Route of administration and doses:

In oil, inside. The mode of dosing is set individually depending on a disease. The dose decline and cancellation of treatment are made gradually. Prostate cancer: in oil — on 300 mg of 1 times in 1–2 weeks, inside — on 50–100 mg 1–3 times a day.

Hyper sexuality at men: inside — on 50 mg 2 times a day (if necessary — on 100 mg 2–3 times a day); at achievement of effect the dose is reduced to the minimum supporting — on 25 mg 2 times a day; in oil — on 300–600 mg of 1 times in 10–14 days.

The expressed androgenization phenomena at women: inside, on 100 mg of 1 times a day from 1st to the 10th day of a menstrual cycle (purpose of gestagen-oestrogenic drug from 1st to the 21st day of a cycle is at the same time shown).

In 21 days from the beginning of therapy in reception the break for 7 days during which there comes menstrualnopodobny bleeding becomes.

To children: inside, on 25–50 mg 2 times a day.

Features of use:

Contraindicated at pregnancy (before therapy of the woman have to undergo all-medical and gynecologic examination, a condition of the beginning of therapy is lack of pregnancy). For the period of treatment it is necessary to stop breastfeeding (gets into breast milk).

During treatment control of function of a liver, bark of adrenal glands and a picture of peripheral blood is necessary. At emergence of signs of a hepatotoxic administration of drug should be stopped. At patients with a diabetes mellitus dose adjustment of insulin or other hypoglycemic means can be required (it is necessary more often than usually to carry out control of level of glucose to blood). During treatment it is necessary to refrain from occupation types of activity, requiring special attention. The children receiving high doses of drug at loadings of high intensity can have a need for replacement therapy by glucocorticoids (because of the hidden adrenal insufficiency).

At alcohol intake along with treatment at patients with patholologically the raised sexual desire decrease in effect of therapy can be observed.

In extremely exceptional cases against the background of use of a tsiproteron of acetate benign and extremely seldom malignant tumors of a liver can be observed.

Side effects:

Abdominal pain, nausea, increased fatigue, xeroderma, concern or depression, fatigue, decline in the ability of concentration of attention, liquid delay in an organism, change of body weight, allergic reactions; at high doses — an abnormal liver function.

Men have a suppression of a spermatogenesis (decline in the ability to fertilization, is usually recovered in 3–4 months after drug withdrawal), a gynecomastia (including in combination with the increased tactile sensitivity and morbidity of nipples).

Women have a feeling of tension in mammary glands, suppression of an ovulation.

Children have an oppression of bark of adrenal glands (at high-dose therapy), a liver failure. At bystry introduction in oil — cough, short wind.

Interaction with other medicines:

Anti-gonadotropic action of a tsiproteron amplifies at a combination to GNRG agonists. Against the background of a tsiproteron the need for peroral hypoglycemic means or insulin can change.

Contraindications:

Hypersensitivity, heavy liver failure, liver tumors, including in the anamnesis (except for metastatic damage of a liver at a prostate cancer), a syndrome the Cudgel — Johnson, the Rotor syndrome, a depression (severe forms), a thromboembolic syndrome, pregnancy, feeding by a breast.

Restrictions to use. It is necessary to estimate individually possible advantage and risk of development of negative effects of treatment at the solution of a question of purpose of drug by the patient with a prostate carcinoma in the presence of heavy diabetes with vascular complications, a sickemia, a thromboembolism in the anamnesis, a cachexia (if it is not connected with a prostate cancer).

Teenage age (before end of the period of puberty), herpes of pregnant women (in the anamnesis), idiopathic jaundice of pregnant women (in the anamnesis).

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:

Tablets of 50 mg, 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.