Androcur, tablets 10 mg 15 pcs

Pharmacodynamics

The oral antiandrogenic drug. Inhibits the effect of male sex hormones (androgens), which are also produced in small quantities 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 after an average of 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

Hirsutism, Acne, Acne (vulgaris), Seborrheic dermatitis, Alopecia (alopecia)

In women:

• androgen-induced severe hair loss on the head to baldness (moderate androgenic alopecia);
• hirsutism of moderate severity;
• acne and/or seborrhea of severe to moderate severity.

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Active ingredient

Cyproterone

Composition

Active ingredients:

Cyproterone acetate, micro 20 – 10 mg.

Auxiliary substances:

Lactose monohydrate – 63.4 mg,

Corn starch – 44 mg,

povidone 25,000 – 1.35 mg,

colloidal silicon dioxide micronized – 1 mg,

magnesium stearate – 0.25 mg.

How to take, the dosage

Performance in women

In case of moderate androgenism, the drug is taken in the form of 10 mg tablets daily from the 1st to the 15th day of the menstrual cycle in a dose of 10 mg once a day. Androcur in the form of tablets 10 mg is taken together with the preparation Diane-35 in order to obtain the necessary contraceptive effect and to prevent intermenstrual bleeding.

In order to stabilize the cycle and for reliable contraception, patients with androgenization phenomena additionally take Diane-35 1 tablet/day on the same hours from days 1 to 21 of the cycle. Both drugs should be started on the 1st day of the cycle (the first day of bleeding). After stopping the intake of Androcur (10th or 15th day of a cycle) during the next days of a cycle take the remaining tablets of the calendar pack of Diane-35 (21 days in total). Then there is a break of 7 days, during which bleeding must occur. After the 7-day break, you should continue taking tablets from the next Androcourt and Diane-35 calendar packs, regardless of whether bleeding has stopped or continues. If there is no bleeding after the end of the pills, treatment should be stopped and an examination should be performed.

The duration of treatment is set by the doctor and depends on the type as well as the severity of the androgenization pathological phenomena and the results of treatment. Acne and seborrhea are usually cured earlier than alopecia.

The Androcur tablets are taken orally after a meal with a small amount of liquid.

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, drowsiness, and decreased ability to concentrate may be observed while taking Androcur.

Contraindications

• Liver disease;
• jaundice;
• A history of persistent itching or herpes during pregnancy;
• Doubin-Johnson syndrome;
• Rotor syndrome;
• existing or previous liver tumors (in prostate carcinoma only if not caused by metastases);
• current or previous liver tumorscachexia (except in patients with prostate carcinoma);
• severe chronic depression;
• previous or existing thromboembolic processes;
• severe diabetes with vascular complications;
• Sick cell anemia;
• pregnancy;
• pregnancy (breastfeeding);
• high sensitivity to the drug.

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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, feeling of inner restlessness, impaired ability to concentrate; when using 100 mg tablets at the beginning of therapy, increased fatigue, apathy, restlessness, reduced 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

Cyproterone-Teva