Androcur, tablets 50 mg 20 pcs

Pharmacodynamics

The oral antiandrogenic drug. Inhibits the effect of male sex hormones (androgens), which are also produced in small amounts by the female body. It has gestagenic, anti-androgenic and antigonadotropic action.

In men against the background of taking the drug there is a weakening of libido and potency as well as a decrease in the function of the testes. These changes disappear after discontinuation of treatment. The drug reduces or completely eliminates the effect of androgens on the target organs (including the prostate gland).

In women, taking Androcur reduces both pathologically excessive growth of facial and body hair and androgen-induced hair loss on the head. In addition, increased sebaceous gland function is reduced and ovarian function is inhibited during the treatment period.

Pharmacokinetics

Intake

After oral administration, ciproterone acetate is completely absorbed from the GI tract. After taking 10 mg C_max is reached after 1.5 hours and is 75 ng/ml, after taking 50 mg – 140 mg/ml. After taking 100 mg tablet C_max is reached on average in 2.8±1.1 h. The bioavailability is 88%.

Distribution and metabolism

The binding to plasma proteins is about 96%. It is biotransformed in the liver by hydroxylation and conjugation; the main metabolite determined in human plasma is the 15β-hydroxyl derivative.

T_1/2 for 10 mg and 50 mg tablets is 43.9±12.8 h, for 100 mg it is 42.8±9.7 h. It is excreted with bile and urine mainly as metabolites in the ratio 3:7.

Indications

In men:

Active ingredient

Composition

Active substances:

Cyproterone acetate micro 20 – 50 mg.

Auxiliary substances:

Lactose monohydrate – 110.5 mg,

Corn starch – 59.5 mg,

Polyvidone 25,000 – 2.5 mg,

Silica colloidal anhydrous – 2 mg,

Magnesium stearate – 0.5 mg.

How to take, the dosage

Application in men

In case of pathological deviations in the sphere of sexual behavior, causing the need to reduce sexual desire, the dose of Androcur is selected in each individual case. At the beginning of the course the drug is taken 50 mg 2 times a day. If necessary, the dose may be increased to 100 mg 2 times a day, and temporarily to 3 times a day. When therapeutic effect is achieved, the dose is reduced to the minimum maintenance dose. In most cases, 25 mg 2 times/day is sufficient. At the same time, the dose reduction should be gradual, over several weeks, with a change in dose by 1 or better by 1/2 tablet per week. To stabilize the therapeutic effect, the drug is taken long term, over several months, if possible with simultaneous psychotherapy.

In treatment with anti-androgens for inoperable prostate carcinoma, the drug is prescribed in a dose of 100 mg 2-3 times a day. Whether the patient’s condition improves or the disease remits, it is necessary to continue taking the drug in the prescribed dose.

In order to decrease increased production of male sex hormones at the start of treatment with GnRH agonists, the drug is initially prescribed in a dose of 100 mg twice daily for 5 to 7 days, and then in the next 3-4 weeks in a combination with a GnRH agonist at the same dose.

For the treatment of hot flashes during treatment with GnRH agonists or after orchiectomy, the drug is prescribed at 50-150 mg/day; if necessary, the dose is increased to 300 mg/day (100 mg 3 times/day).

In metastatic or inoperable prostate cancer, Androcur tablets containing 100 mg of cyproterone acetate may be prescribed at a dose of 200-300 mg/day divided into 2-3 doses. The drug is intended for long-term daily administration. If there are signs of disease progression, the drug should be discontinued.

Interaction

Concomitant use of Androcur may change the effectiveness of hypoglycemic drugs and insulin.

The antiandrogenic effect of cyproterone acetate is enhanced when used together with GnRH agonists; the initial increase in testosterone production by GnRH agonists is reduced by cyproterone acetate.

Special Instructions

In patients with prostatic carcinoma and the presence of severe diabetes with vascular changes, sickle cell anemia, or prior thromboembolic events, the possible benefits and risks of developing adverse effects of treatment must be individually weighed when deciding whether to prescribe Androcur.

Patients should undergo general medical and gynecologic examinations to rule out pregnancy before starting therapy with Androcur.

If patients simultaneously take Androcur and Diane-35, they should be informed that if they do not take Androcur and/or Diane-35 pills at the usual time, they should take the medicine within the next 12 hours. If the above mentioned time is exceeded, the contraceptive effect for this cycle is not ensured. You should continue taking Androcur or Diane-35 pills or dragees at the time of starting, skipping the forgotten pills and/or dragees in order to prevent premature bleeding in this cycle. Additionally, other, non-hormonal methods of preventing conception should be used until the end of this cycle. If this cycle does not end with bleeding, the therapy should be interrupted and a checkup should be performed.

The simultaneous use of alcohol, which has a disinhibiting effect, in patients with pathologically increased libido may be observed to reduce the effect of Androcur treatment.

Control of laboratory parameters

During treatment with the drug, careful monitoring of liver function and peripheral blood counts is necessary.

Impact on ability to operate vehicles and other mechanisms requiring increased attention

Patients whose activities require increased attention should be aware that increased fatigue, lethargy, and decreased ability to concentrate may be observed while taking Androcur.

Contraindications

Side effects

Musculoskeletal system: in men rarely – osteoporosis.

Endocrine system disorders: taking Androcur for several weeks in men leads to decreased fertility (suppression of spermatogenesis, reversible decrease in libido and potency), which completely recovers in 3-4 months after discontinuation of the drug; in single cases – gynecomastia, sometimes combined with increased tactile sensitivity of the breast nipples. In women, sometimes – a feeling of tension in the mammary glands, changes in body weight.

Combination therapy with Androcur causes suppression of ovulation and prevents conception.

CNS disorders: in women in single cases – decreased mood and depression, internal anxiety, impaired ability to concentrate; when using 100 mg tablets at the beginning of therapy, increased fatigue, apathy, anxiety, decreased ability to concentrate are possible.

Digestive system disorders: nausea, abdominal pain; liver function abnormalities in single cases are possible during the use of 100 mg tablets in the beginning of therapy.

Others: in the use of 100 mg tablets at the beginning of therapy, dry skin may occur; in isolated cases of high doses, feeling of shortness of breath.

Overdose

An acute toxicity study of Androcur has shown that cyproterone acetate can be classified as a very low toxicity substance.

Inadvertent ingestion of multiple Androcur tablets should not be expected to cause intoxication.

Similarities