Androcur 10mg #15

User manual for Androcur

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Composition

Androcur tablets have 3 different dosages: one tablet can contain 10 mg, 50 mg or 100 mg of cyproterone acetate (micro 20). Typically, auxiliary compounds such as lactose monohydrate, corn starch, polyvidone 25,000, silicon dioxide, magnesium stearate are used.

Form of issue

    Androcur tablets 10 mg and 50 mg of round form, white or yellowish, have a risk on one side and the engraving of the hexagon, on the other, are distinguished by engraved letters inside the hexagon: "BW" and "BV" respectively. Packed in blisters of 10, 15 tablets. or jars of dark glass to 20, 50 tablets, in one package can be - 15, 20, 50 tablets.
    Tablets Androcur 100 mg capsular form white or yellowish. On both sides of the tablets there are risks and letters "LA", and also with one side - a hexagon. They are packed in blisters for 10 tab., In one pack - 6 blisters.

pharmachologic effect

The preparation is characterized by antiandrogenic and gestagenic effects.

Pharmacodynamics and pharmacokinetics

Androcur is a hormonal antiandrogenic remedy. Due to the competitive displacement of androgens present in the target organs, the symptoms characteristic of androgen-dependent conditions occur, for example, excessive hair growth on the face or body with hirsutism, androgenic alopecia (alopecia) and increased sebaceous glands and acne. The mechanism of action of the drug is based on the antigonadotropic effect of active cyproterone, which effectively reduces the concentration of androgens and additionally provides a therapeutic effect. Changes caused by Androcur therapy are reversible, recovery occurs after discontinuation of the drug.
In combination with Diane-35, ovarian function is suppressed.

Pharmacokinetic data Androcur 10 mg

Cyproterone is fully absorbed after oral ingestion of the tablets, and the absolute bioavailability is approximately 88%. To achieve a maximum concentration of 75 ng / ml, it is necessary that approximately 1.5 hours pass. The half-life is 0.8 hours for the first phase and 2.3 days for the second, with a total plasma clearance of 3.6 ml / min for 1 kg. Metabolized by cyproterone hydroxylation and conjugation, the main metabolite in the bloodstream is the 15β-hydroxy derivative. Further biotransformation occurs in the liver, and excretion of metabolites - together with bile and kidneys (ratio 3: 7), and in unchanged form - only together with bile.
Because of the long half-life, daily taking of tablets leads to a cumulation and increase in the content of cyproterone in the plasma several times.
Indications for use

For tablet dosage of 10 mg

The drug is used in women with manifestations of androgenization of moderate severity, among them:
    hirsutism;
    androgenic alopecia;
    severe and moderate form of acne, accompanied by the formation of nodules, inflammation, seborrhea, risk of scarring.

For tablets, dosages of 50 mg and 100 mg

    treatment of common inoperable or metastatic prostate cancer in order to suppress the action of testosterone, including antiandrogen therapy for an inoperable type of prostate cancer;
    decrease in the severity of hyperandrogenism that occurs during the first stages of therapy with GnRH agonists (hormones - gonadotropins of the releasing factor);
    relief of "hot flashes" in patients with prostate cancer during treatment with GnRH agonists or after an orchiectomy;
    increased sexual desire in patients who have sexual deviations.

Contraindications

    contraindicated during pregnancy and breastfeeding, as well as during adolescence (until the full completion of puberty);
    when hypersensitivity reactions occur on the components of the drug;
    patients with liver diseases such as: Dabin-Johnson syndrome, Rotor, neoplasm or history of liver tumor data);
    with idiopathic jaundice, herpes or persistent itching during the previous pregnancy;
    sickle-cell anemia;
    patients with severe chronic depression;
    meningioma (including the presence of an anamnesis record);
    cachexia;
    severe diabetes mellitus and complications (including diabetic angiopathy);
    patients with thromboembolism, arterial and venous thrombosis, myocardial infarction, stroke, deep vein thrombophlebitis, cerebrovascular disorders (including records in anamnesis);
    Lactase insufficiency or lactose intolerance, glucose-galactose malabsorption disease.

Side effects

Patients taking Androcur may experience:
    bloody discharge from the vagina, change in body weight and mood deterioration;
    the most dangerous adverse reactions are the development of neoplasms in the liver, which can later lead to intra-abdominal bleeding that threatens the life of patients;
    hypersensitivity reactions;
    hyperglycemia;
    depression, increased or decreased libido;
    functional liver disorders, jaundice and hepatitis are possible;
    skin rash;
    strained and painful mammary glands;
    inhibition of ovulation or anovulation (absence - as a result of the impossibility of conception);
    non-menstrual bleeding or the absence of menstrual bleeding.

In men the following undesirable reactions are most often observed:

    decreased libido, reversible suppression of the process - spermatogenesis (restored several months after drug discontinuation);
    impotence;
    the most dangerous adverse reactions are hepatotoxicity, the development of neoplasms in the liver, which can lead to intra-abdominal bleeding or the onset of thromboembolic events;
    anemia;
    hypersensitivity reactions;
    depression and depressed mood, a temporary feeling of anxiety;
    thrombosis and thromboembolism;
    reversible gynecomastia, accompanied by soreness and increased sensitivity of nipples.

With prolonged use of Androcur

    can develop osteoporosis, caused by a prolonged androgen deficiency;
    can develop benign cerebral meningioma, subject to prolonged use of the drug for several years at a dose of ≥25 mg.

Instructions for Androcur (Method and Dosage)

Tablets, if necessary, washed down with a small amount of pure water. If during the therapy there are signs of progression of the disease, then the drug is canceled.

Instruction for Androcur 10 mg in combination with Diane-35

The drug is supplemented with Diana-35 therapy for reliable contraception and prevention of irregular bleeding. Begin therapy with both drugs from the 1st day of the menstrual cycle (menstrual bleeding), taking 1 tablet of Androcur and Diana-35 for 15 days. Then in the next 6 days, only Diana-35 should be taken. Next, make a 7-day break, during which the patient should have menstrual bleeding (otherwise - treatment is interrupted until pregnancy is excluded). After this, regardless of the menstrual bleeding ended, the taking of tablets should be resumed.
Passing the reception of Androcur tablets: usually reduces the therapeutic effect and causes menstrual bleeding. A missed tablet should not be taken, so that there is no double dose, you should resume your appointment at the usual time of admission with Diane-35.
Duration of treatment differs depending on the degree of pathological signs of the androgenation process. Complex therapy is recommended for several months. Achieving a therapeutic effect can be faster with acne and seborrhea than with alopecia and hirsutism. When there is a positive dynamics can be tried in the future only take Diana-35.

Scheme of treatment with Androcur

Scheme of antiandrogen therapy for an inoperable type of prostate cancer: take Androcur for a long time, 2 tablets with a 50 mg dose or 1 tablet at a dosage of 100 mg 2-3 times during the day, that is, the daily dose is approximately 200-300 mg. If there is an improvement or remission, then therapy is not recommended to interrupt or reduce dosage.
In the treatment of GnRH agonists in order to reduce the initial increased level of androgens: the initial daily dose is 200 mg (2 tablets 50 mg or 1 tablet 100 mg 2 times daily). Usually monotherapy lasts 5-7 days, then - in combination with the agonist GnRH Androcur take 200 mg per day for 3-4 weeks.
Coping of "tides" during treatment with GnRH agonists or after an orchiectomy: the initial daily dose should not exceed 50-100 mg (1-3 tablets with a dosage of 50 mg or 0.5-1.5 tablets with a dosage of 100 mg during the day). In the following - the daily dose can be increased to 300 mg.
For treatment of increased sexual desire with sexual deviations, one tablet of Androcur should be taken at a dosage of 50 mg twice a day, gradually increasing the dose as necessary to 200-300 mg per day (briefly, and when the result is achieved, try to gradually reduce the dose to a minimally effective maintenance - usually up to 50 mg / day). The course of treatment is long, if possible - simultaneously with psychotherapy.

Overdose

As a result of the conducted toxicity studies, it was found that cyproterone as an active component of Androcur is practically non-toxic compound, therefore the risk of acute intoxication due to a single dose of overdoses of the drug is unlikely.

Interaction

    Therapy by Androcur may require a change in the dosage of oral hypoglycemic agents or insulin.
    Because cyproterone metabolism occurs using the CYP 3A4 isoenzyme, it is suggested that ketoconazole, clotrimazole, itraconazole, ritonavir, and other potent inhibitors of the CYP 3A4 isoenzyme may inhibit cyproterone metabolism, whereas inducers of the CYP 3A4 isoenzyme, for example, Rifampicin, Phenytoin lead to a decrease in the concentration of cyproterone in the bloodstream.
    In men who suffer from chronic alcoholism and who are treated for high doses of the drug, a decrease in the effectiveness of therapy is possible.
    The use in combination with inhibitors of HMG-CoA reductase (so-called statins), also metabolized by the isoenzyme CYP3A4, increases the risk of myopathy and rhabdomyolysis.

Storage conditions

Temperature regime - up to +25 ° Celsius.

Shelf life

Up to 60 months.

In pregnancy and lactation

The use of the drug is contraindicated, since high-dose cyproterone during hormonal-sensitive differentiation of the genital organs leads to the appearance of signs of feminization in putative male fetuses. However, teratogenic effects are absent at the stage of organogenesis, up to the development of the external organs of the reproductive system.

Reviews of Androcur

You can find comments and discussions on this anti-androgen drug in various forums and medical portals. Women's comments about Androcur are positive, but many are concerned about the possibility of getting pregnant and that the drug should be combined with Diane-35. In addition, some complain of nausea and decreased libido and many other side reactions.
Reviews of men about Androcur are few, since in our country the drug is more often used by women in order to reduce masculinization. Men rarely treat advanced sexual treatment, and those who used carcinoma or cancer do not leave comments.