Androfarm

General characteristics. Structure:

Active ingredient: cyproterone;

1 ml of drug contains a tsiproteron of acetate of 100 mg in terms of 100% substance;

excipients: benzyl benzoate, castor oil.

Pharmacological properties:

Pharmacodynamics. Androfarm – hormonal drug with anti-androgenic activity.

At use of a tsiproteron of acetate for men sexual desire and a potentiality decreases, and also function of gonads is oppressed. After drug withdrawal these effects disappear.

Tsiproterona acetate competitively oppresses influence of androgens on an androgen - dependent target organs, for example, protects a prostate from influence of androgens which are developed in gonads and/or bark of adrenal glands.

Tsiproterona acetate has the central inhibiting effect. The anti-gonadotropic effect causes decrease in synthesis of testosterone in testicles and, as a result, reduction of concentration of this hormone in blood serum.

At use of high doses of a tsiproteron of acetate insignificant increase in level of prolactin was sometimes observed.

Pharmacokinetics. After intramuscular introduction of a tsiproteron acetate is gradually released from solution. Bioavailability of a tsiproteron of acetate makes 100%. Its maximum level in blood serum is reached in 2-3 days. After that hormone level in blood serum decreases with a final elimination half-life 4±1,1 days. The full clearance of a tsiproteron of acetate makes 2,8±1,4 ml/min. of blood serum.

Tsiproterona acetate almost completely contacts blood plasma albumine. About 3,5-4% of the general level of a steroid remain in a stand-at-ease. As linkng with proteins not specific, change of level of the globulin connecting sexual steroids does not influence pharmacokinetics of a tsiproteron of acetate.

Tsiproterona acetate is metabolized in the different ways, including a hydroxylation and conjugation. The main metabolite – 15β-гидроксипроизводное. Metabolism of the first phase is catalyzed, mainly by CYP3A4 enzyme of P 450 cytochrome.

Insignificant part of the accepted dose is removed in not changed view with bile. The most part of substances is excreted in the form of metabolites with urine and bile.
Pharmaceutical characteristics.

Main physical and chemical properties: yellow or flavovirent oily liquid with a specific smell.
Incompatibility.

Drug should not be mixed with other medicines in one syringe.

Indications to use:

For treatment of an inoperable prostate cancer.

For decrease in a sexual inclination at pathological deviations in the sexual sphere at men.

Route of administration and doses:

Drug is used intramusculary. The injection should be done very slowly.

It is necessary to watch that substance which is entered did not get to a vessel carefully.

Treatment of an inoperable prostate cancer.

The drug in a dose of 3 ml is administered deeply intramusculary once a week.

At improvement of a state or remission of a disease it is not necessary to change the appointed dose of drug or to stop treatment.

For decrease in a sexual inclination at pathological deviations in the sexual sphere at men.

3 ml of drug enter each 10-14 days deeply intramusculary. In exceptional cases, if the effect of treatment is insufficient, it is possible to enter 6 ml of drug (about 3 ml in the right and left gluteuses are desirable) each 10-14 days.

After achievement of satisfactory therapeutic effect it is reasonable to reduce a dose by gradual increase in an interval between injections. It is necessary to apply Androfarm to stabilization of therapeutic effect a long time and if it is possible, along with use of psychotherapeutic actions.
Patients of advanced age.

There are no data testimonial of need for dose adjustment for patients of advanced age.

Patients with a liver failure. Drug use Androfarm is contraindicated to patients with liver diseases (so far parameters of function of a liver will not return to norm).

Patients with a renal failure. There are no data testimonial of need of dose adjustment for patients with a renal failure.

Features of use:

Use during pregnancy or feeding by a breast.

The Androfarm solution is not applied to treatment of women.
Children.

The Androfarm is not appointed before completion of puberty. The negative impact of drug on growth and endocrine system of the patient therefore drug is not recommended for use to children and teenagers is not excluded.

In some cases during drug use the Androfarm in high doses can be observed an asthma, it needs to be considered when carrying out differential diagnosis. It is considered that such states do not demand treatment.

There are messages on development of anemia at use of a tsiproteron of acetate. Considering it, it is regularly necessary to control blood indicators with obligatory determination of quantity of erythrocytes throughout the entire period of treatment.

Patients with a diabetes mellitus demand careful medical observation during treatment by Androfarm as there can be a need for correction of a dose of peroral antidiabetic means or insulin.

It was reported about development of the thromboembolic phenomena in patients who applied a tsiproteron acetate though the interrelation with administration of drug is not established.

Patients with arterial or venous тромботическими / the thromboembolic phenomena (for example, a deep vein thrombosis, an embolism of a pulmonary artery, a myocardial infarction) or cerebrovascular diseases in the anamnesis and patients with tumors at a late stage belong to group of the increased risk of development further of the thromboembolic phenomena. It is necessary to approach with extra care purpose of drug a sick inoperable prostate cancer with the thromboembolic phenomena in the anamnesis. In each separate case it is necessary to weigh the expected advantage of treatment and potential risk.

The Androfarm has kortikosteroidopodobny effect therefore throughout the entire period of treatment it is necessary to check function of bark of adrenal glands regularly.

At patients who applied a tsiproteron acetate cases of development of a hepatotoxic, including jaundice, hepatitis and liver failure are registered that sometimes led to a lethal outcome. The majority of these cases concerned treatment of men with a widespread prostate cancer. Toxicity of drug depends on a dose and develops usually after several months of treatment. Before an initiation of treatment, it is regular throughout the entire period of treatment and if any symptoms of a hepatotoxic are observed, it is necessary to conduct researches of function of a liver. If a hepatotoxic is confirmed, in the absence of other reason of its emergence (for example, in the presence of metastasises), use of a tsiproteron of acetate is recommended to be cancelled. Treatment can be continued if the advantage of therapy exceeds possible risk.

In isolated cases development high-quality was observed, and is even more rare – malignant tumors of a liver. In some cases the intra belly bleedings caused by these tumors threatened life. At emergence of pain in an upper part of a stomach, increase in a liver or symptoms of intra belly bleeding during treatment by Androfarm it is necessary to consider probability of existence of a tumor of a liver.

It was reported about emergence of the meningiomas (one or multiple) associated with prolonged use (within several years) a tsiproterona of acetate in a dose of 25 mg a day or above. If the meningioma is diagnosed for the patient who is treated by drug Androfarm, treatment needs to be stopped.

It is recommended to administer the drug only intramusculary, very slowly. The pulmonary microembolism caused by introduction of Solutio oleosa can lead to development of such symptoms as cough, an asthma and a stethalgia. Emergence of vazovagalny reactions, such as an indisposition, a hyperhidrosis, dizziness, paresthesias and a syncopal state is also possible. These reactions can arise in time or right after an injection and are reversible. The maintenance therapy, for example, administration of oxygen is also usually applied.

During treatment by Androfarm it is not necessary to take alcohol.

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

During treatment by Androfarm increased fatigue, oppressed mood can be observed that has to be considered by patients whose activity is connected with control of vehicles or with other mechanisms.

Side effects:

Frequency of side reactions is defined as it is very frequent (≥1/10), is frequent (≥1/100, <1/10), infrequently (≥1/1000, <1/100), is rare (≥1/10000, <1/1000) and is very rare (<1/10000).

New growths: very seldom – benign and malignant tumors of a liver; frequency is unknown – high-quality cerebral meningiomas in connection with prolonged use (within several years) drug in a dose of 25 mg or above.

Frustration from circulatory and lymphatic systems: frequency is unknown – anemia.

Frustration from immune system: seldom – hypersensitivity reactions.

Metabolic and alimentary disturbances: often – increase or a degrowth of a body.

Mental disorders: very often – decrease a libido, erectile dysfunction (these phenomena disappear after the treatment termination); often – oppressed mood, concern (temporarily).

Vascular disturbances: frequency is unknown – the thromboembolic phenomena (the causal interrelation with administration of drug is not established).

Frustration from respiratory system: often – an asthma.

Frustration from digestive tract: frequency is unknown – intra belly hemorrhage.

Frustration from gepatobiliarny system: often – a hepatotoxic, including jaundice, hepatitis, a liver failure.

Frustration from skin and hypodermic cellulose: infrequently – rash.

Frustration from a musculoskeletal system and connecting fabric: frequency is unknown – osteoporosis.

Disturbances from reproductive system and mammary glands: very often – reversible oppression of a spermatogenesis (after the treatment termination it is gradually recovered for several months); often – a gynecomastia (sometimes in a combination with hypersensitivity of nipples at a touch) that, as a rule, passes after drug withdrawal.

General frustration and local reactions: often – increased fatigue, heat inflows, the strengthened sweating.

Interaction with other medicines:

At treatment Androfarmy there can be a need for dose adjustment of peroral anti-diabetic drugs or insulin.

In spite of the fact that clinical trials of interaction of drug with medicines were not conducted, but as it is metabolized with the participation of CYP3A4 enzyme, it is expected that кетаконазол, итраконазол, Clotrimazolum, ритонавир and other strong CYP3A4 inhibitors oppress metabolism of a tsiproteron of acetate. On the other hand, the inductors CYP3A4, such as rifampicin, Phenytoinum and medicines containing a St. John's Wort can reduce the level of a tsiproteron of acetate.

Based on results of the research in vitro, it is possible to assume that at use of high therapeutic doses of a tsiproteron of acetate (100 mg three times a day) the inhibition of such enzymes of system of P 450 cytochrome as CYP2C8, 2C9, 2C19, 3A4 and 2D6 is possible.

At simultaneous use of HMGCoA inhibitors (statines) and high therapeutic doses of a tsiproteron of acetate because of an identical way of metabolism of these substances the risk of a myopathy or rabdomioliz associated with statines can increase.

Contraindications:

Hypersensitivity to any of drug components; liver diseases; syndrome Cudgel Johnson, Rotor syndrome; liver tumors, including in the anamnesis (only in that case when the tumor is not caused by metastasises of a prostate cancer); a meningioma nayavny or in the anamnesis; a serious general condition (if it is not connected with an inoperable prostate cancer); heavy chronic depression; the diagnosed thromboembolic states.

At use for the purpose of decrease in a sexual inclination at pathological deviations in the sexual sphere at men, except the above-stated contraindications: severe forms of a diabetes mellitus with vascular complications; sickemia.

Overdose:

Tsiproterona acetate almost nontoxic substance. After single use in a dose which several times exceeds therapeutic cases of acute toxicity were not noted.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 3 ml in an ampoule. On 3 ampoules in a pack.