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Androkur

Androkur (Androcur)

International name: ciproterone;

Main physical and chemical characteristics: tablets of white color;

structure:

1 tablet contains 50 mg of a tsiproteron of acetate.

other components: lactoses monohydrate, starch corn, polividon 25000, colloid anhydrous silicon dioxide, magnesium stearate.

Form of release of medicine. Tablets.

Farmakoterapevtichesky group. Hormones and also analogs. Anti-androgens.

Code of automatic telephone exchange Y03H A01.

Pharmacological properties.

Androkur represents hormonal drug of anti-androgenic action that blocks influence of androgens which in insignificant quantities are developed as well by an organism of women. Besides, it has gestagenny and anti-gonadotropic effect.

Tsiproterona acetate competitively blocks effect of androgens on bodies which is an androgen - dependent as, for example, protecting a prostate from influence of androgens of gonads and/or bark of epinephral glands. At men at Androkur's reception weakening of sexual desire and potentiality, and also small egg depression of function is observed. These shifts after a suspension of treatment disappear.

At women at Androkur's reception both the pathological excessive hairiness of a body (hirsutism), and the hair loss on the head caused by androgens (an androgenzavisimy alopecia) decrease. Besides, hyperfunction of sebaceous glands decreases and function of ovaries is slowed down during the treatment period.

Pharmacokinetics

After oral administration of a tsiproteron acetate is completely soaked up. Absolute bioavailability almost full (88% of the accepted dose). After oral administration of 50 mg of a tsiproteron of acetate the maximum concentration in a blood plasma of 140 ng/ml is observed about 3 hours. Further concentration of drug in plasma decreases within 24 – 120 hours, with an elimination half-life of 43,9±12,8 hours. The clearance of a tsiproteron of acetate makes 3,5±1,5 ml of a blood plasma / minut./kg. The tsiproterona acetate in the different ways, including hydroxylations and conjugation is metabolized. The main metabolite in a blood plasma - 15b-hydroxy derivative.

Some the part of the accepted dose is removed in an invariable view with bile. Metabolites are removed with urine (30%) and bile (70%). The elimination half-life of metabolites makes 1,7 days of plasma.

Tsiproterona acetate almost completely contacts only blood albumine. About 3,5-4% of the general level remain to a steroid in a stand-at-ease. As linkng with proteins not specific, change of level to globulin that connects sex hormones, does not influence pharmacokinetics of a tsiproteron of acetate.

Indications for use.

Purpose of drug to men.

Treatment by anti-androgens in the presence of an inoperable prostate cancer.

Pathological deviations in the field of sexual desire that cause the necessity lowered sexual requirement.

Purpose of drug to women.

The expressed androgenozation symptoms, such as pathological excessive hairiness of the person and body (vysokostupenevy hirsutism), caused by androgens strong a hair loss on the head to formation of a bald head (a heavy alopecia) that often is followed by severe forms of an acne and/or seborrhea.

Way of use and dose.

Purpose of drug to men.

Treatment by anti-androgens in the presence of an inoperable prostate cancer:

a) for the purpose of an exception of action of androgens of bark of epinephral glands:

- after an orkhiektomiya – on 2 tablets 1-2 times a day (a daily dose of-100-200 mg);

- without orkhiektomiya – on 2 tablets 2-3 times a day (a daily dose of 200-300 mg).

Pill should be taken after reception of food, washing down them with liquid.

At improvement or remission of a disease it is not necessary to change the appointed dose of drug or to interrupt treatments.

b) for the purpose of decrease increase of level of male sex hormones in an initiation of treatment LG-RG agonists:

at first only two tablets of Androkur 2 times a day (200 mg) within 5 - 7 days, then within 3 - 4 weeks 2 tablets of Androkur (200 mg) together with LG-RG agonist in the instruction the manufacturer to a dose 2 times a day.

c) for the purpose of an exception of action of androgens of bark of epinephral glands at treatment by LG-RG agonists:

it is necessary to continue treatments by anti-androgens by reception of 2 tablets of Androkur 1-2 times a day (100-200 mg).

Pathological deviations in the field of sexual desire that cause the necessity lowered sexual requirement.

Necessary the dose of drug is appointed by the doctor. A pill should be taken after food, washing down them with liquid.

The initial dose makes, as a rule, 1 tablet of Androkur 2 times a day (100 mg). The dose if necessary can be raised to 2 tablets 2 times a day (200 mg) or, quickly, to 3 times a day (300 mg). At achievement of a by-product of treatment the therapeutic effect has to be supported by means of the minimum dose. At the majority of cases reception of a half of a tablet 2 times a day is sufficient. It is necessary to enter a maintenance dose and to cancel drug not at once, and gradually. At the same time the day dose with an interval of several weeks decreases on 1 or, better, by a half of a tablet. For stabilization of therapeutic effect administration of drug for a long time, for opportunities with simultaneous carrying out psychotherapy is necessary.

Purpose of drug to women.

Androkur's reception is contraindicated under pregnancy time. Therefore prior to treatment it is necessary to be convinced of lack of pregnancy at the patient.

Women who reached puberty have to begin administration of drug in the first day of a cycle (the first day menstrual bleedings). Only women with an amenorrhea have to begin is appointed the doctor of treatment immediately. At the same time the first day of administration of drug is considered in the first afternoon of a cycle. Further treatment is carried out for below the recommended schedule of reception.

With 1st on 10 2 tablets of Androkur on 50 mg accept day of a cycle (10 days) daily once a day after reception of food, washing down them with liquid. In addition these women for stabilization of a menstrual cycle and necessary contraception receive gestagen-estrogenosoderzhashchy drug: from a cycle, 1st to 21 day (21 days) of 1 dragee of Diane-35 in day.

At the treatment combined cycling drugs are recommended to be accepted every day at the same time. At a reception delay more, than on 12 hours, contraceptive action on this cycle is not guaranteed. In this case, for prevention of premature bleeding in this cycle, Androkur's reception and/or Diane-35 should be continued according to the recipe, passing the forgotten tablets and/or a dragee. At the same time until the end of a cycle it is necessary to apply dobavochno a non-hormonal birth control (except for a calendar method according to Knausu-Ogino and a temperature method).

Behind the 21-day period of administration of drugs it is necessary to do 7-day having rummaged during which has to come bleeding owing to cancellation of hormones. In 4 weeks after an initiation of treatment, in the same a day of the week, the new cycle of treatment irrespective of begins, bleeding stopped or. If during 7-day the break of bleeding was not, the patient has to see a doctor. Administration of drug should be suspended. Pregnancy has to be excluded then administration of drug can be resumed. At improvement of a condition of the patient the doctor can reduce a daily dose of Androkur that was accepted the first 10 days of the combined treatment, to one or a half of a tablet. Perhaps appointment to the patient only of Diane-35 is sufficient.

We pay your attention to need of acquaintance also with special indications when carrying out the combined cyclic treatment which contain in information which is added to the drug Diane-35. Women in a postmenopause or after a hysterectomy can receive only Androkur. At the same time the day dose of Androkur depending on weight of disturbances makes 1 or 0,5 tablets on 50 mg and is accepted according to the scheme within 21 days with the subsequent 7-day by a break.

Side effect.

Androkur within several weeks of reception gradually lowers a spermatogenesis. After a treatment suspension it renews within several months. Sometimes Androkur's reception leads at patients - men to a gynecomastia, cumulative regarding men with hypersensitivity of chest nipples to contacts. These phenomena, as a rule, disappear after drug withdrawal.

At men at long-term treatment by Androkur, as well as at use of other anti-androgenic drugs in isolated cases the osteoporosis phenomena were observed.

At women against the combined treatment the ovulation is suppressed. The feeling of intensity of mammary glands is possible. Purpose of high doses of Androkur can cause the lowered functions of bark of epinephral glands. At treatment of patients with high doses of Androkur in isolated cases rather heavy abnormal liver functions were observed.

The exhaustion and hypoactivities, in certain cases temporary internal concern or depressive mood can be other epiphenomena. Also change of body weight is possible.

Contraindications.

Pregnancy, lactation; liver diseases, jaundice, a long itch or herpes during pregnancy, a syndrome the Cudgel Johnson, the Rotor syndrome postponed or are available liver tumors (in the presence of a prostate cancer only in a case when the tumor is not caused by metastasises), diseases that lead to a hypotrophy (except for a prostate cancer), the heavy chronic depressions predicted or the existing thromboembolic phenomena, a heavy diabetes mellitus with changes of vessels, a sickemia, hypersensitivity to any of drug components.

Purpose of drug patients with cancer of a prostate with the predicted thromboembolic phenomena, a heavy diabetes mellitus with changes of vessels or a sickemia should solve questions about expediency after careful estimation of possible useful and negative effects.

Before purpose of the combined cyclic treatment women with the expressed symptoms of an androgenozation need to study special information that it is added to the drug Diane-35 which is applied in this case.

Overdose.

Studying of acute toxicity after a single dose was shown that the tsiproteron acetate (active the making Androkura) can be regarded as almost nontoxic. After nonspecial reception several therapeutic doses at the same time acute intoxication was not noted.

Features of use.

Patients who participate in activity which demands special concentration (service of mechanisms, participation in traffic, etc.) have to take in attention Androkur by-effects are possible: exhaustion, decrease of the activity and abilities to concentration.

At simultaneous alcohol intake Androkur's action lowering sexual desire can will decrease owing to rastormazhivayushchy effect of alcohol.

Before completion of puberty Androkur is not appointed as it is impossible to exclude adverse influence of drug on growth of the patient and his endocrine system.

During the entire period of treatment it is necessary to control function of a liver and bark of epinephral glands, and also the patient's blood (including, number of erythrocytes).

The doctor has to be informed by the patient about existence of a diabetes mellitus as this illness demands careful supervision.

Sometimes at Androkur's reception there is a feeling of an asthma. At differential diagnosis it is necessary to take into account the stimulating influence on breath of progesterone and synthetic progestogens that is followed gipokapniyeyu and a compensatory respiratory alkalosis which is not considered by it that demands treatment.

It is sometimes reported about developing of a thrombembolia at simultaneous use of Androkur. Causal interrelations, however is doubtful.

In isolated cases, as well as at use of other sex hormones, liver tumors were observed. They can lead to the bleedings menacing for life in an abdominal cavity. Therefore the patient should inform the doctor if there are unusual complaints from upper parts of an abdominal cavity which do not pass themselves. The possibility of a tumor of a liver has to be taken into account at differential diagnosis.

Women prior to treatment have to be subject to careful general and gynecologic inspection. At patients who reached puberty at the same time it is necessary to be convinced of lack of pregnancy. If against the combined treatment by Androkur and Diane-35 during the 3-week period of administration of drugs bleeding comes easy "out of turn", reception should not be interrupted; and if there comes strong bleeding, the patient has to see a doctor. In this case it is necessary to conduct examination for the purpose of an exception of an organic disease.

In need of additional purpose of Diane-35 it is necessary to adhere to all indications of Diane-35 specified in the instruction for medical use.

Interactions with other medicines.

The need for peroral anti-diabetic drugs or insulin can change.

Terms and storage conditions. To store in ordinary conditions, in the place, unavailable to children. Period of storage - 5 years.

 
"Androzhel   Androkur of depot"