Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:G.03.H.A.01 Cyproterone
Pharmacodynamics:Synthetic antiandrogen. Similar to the chemical structure with natural androgens, it has the ability to competitively bind to the tissue receptors of these hormones in target organs. Reduces or eliminates the effects of androgens, including those associated with excessive production of male sex hormones.
Has gestagenic activity and antigonadotropic properties.
Pharmacokinetics:After oral administration, it is slowly absorbed from the digestive tract. Maximum concentration in plasma is achieved after 3-4 hours. The final half-life is about 38 hours.
Cyproterone is metabolized in the liver. The main metabolite, 15β-hydroxyciproterone, possesses antiandrogenic activity.
About 35% of the dose is excreted in the urine in the form of free and conjugated metabolites. The rest is excreted with feces.
Indications:For men: correction of pathological abnormalities in sexual behavior (if necessary to reduce sexual activity), metastatic or inoperable prostate cancer (without and after orchiectomy, and in combination with gonadotropin-releasing hormone agonists).
For women: androgenic alopecia of moderate severity; hirsutism of medium severity; acne and / or seborrhea of severe and moderate severity; contraception (as part of combined drugs).
II.C60-C63.C61 Malignant neoplasm of prostate
XII.L60-L75.L64 Androgenic alopecia
IV.E20-E35.E28.1 Excess androgens
IV.E20-E35.E30.1 Premature puberty
V.F50-F59.F52.7 Increased libido
XII.L20-L30.L21.8 Other seborrheic dermatitis
XII.L60-L75.L68.0 Hirsutism
XII.L60-L75.L70.8 Other acne
Contraindications:Hypersensitivity, severe hepatic insufficiency, liver tumors, including history (with the exception of metastatic liver damage in prostate cancer), Dubin-Johnson syndrome, Rotor syndrome, depression (severe forms), thromboembolic syndrome, pregnancy, breast-feeding.
Carefully:It is necessary to individually evaluate the possible benefits and risk of developing negative effects of treatment when deciding on the prescription of the drugpatients with carcinoma of the prostate in the presence of severe diabetes with vascular complications, sickle-cell anemia, history of thromboembolism, cachexia (if it is not associated with prostate cancer).
Adolescence (until the end of the puberty period), herpes of pregnant women (in the anamnesis), idiopathic jaundice of pregnant women (in the anamnesis).
Pregnancy and lactation:Category of recommendations for FDA is not defined. Contraindicated in pregnancy (before the therapy, women should undergo general medical and gynecological examination, the condition for the initiation of therapy is the absence of pregnancy). For the duration of treatment, breastfeeding should be stopped (penetrates into breast milk).
Dosing and Administration:Intramuscularly, orally. The dosage regimen is set individually depending on the disease. Dose reduction and cancellation of treatment is gradual. Prostate cancer: intramuscularly - 300 mg once every 1-2 weeks, inside - 50-100 mg 1-3 times a day.
Hypersexuality in men: inside - 50 mg twice a day (if necessary - 100 mg 2-3 times a day); when the effect is achieved, the dose is reduced to a minimal maintenance dose of 25 mg twice a day; intramuscularly - 300-600 mg once every 10-14 days.
Expressed androgenization phenomena in women: inside 100 mg once a day from the 1st to the 10th day of the menstrual cycle (at the same time, the appointment of a gestagen-estrogen preparation from the 1st to the 21st day of the cycle is shown). After 21 days from the beginning of therapy in the reception, a break is made for 7 days, during which menstrual bleeding occurs.
Children: inside 25-50 mg 2 times a day.
Side effects:From the side endocrine system: a change in body weight is possible. In men - suppression of spermatogenesis, gynecomastia; in women - a feeling of tension in the chest; in children when used in high doses, the hypothalamus may be adversely affected, leading to suppression of the adrenal cortex.
From the side CNS: possible anxiety, depression, fatigue, impaired ability to concentrate.
From the side digestive system: in some cases, when used in high doses - a violation of liver function.
From the side respiratory system: with rapid administration of a cough, shortness of breath.
Overdose:Symptoms: nausea, vomiting.
Treatment: symptomatic.
Interaction:The antigonadotropic effect of cyproterone is enhanced when combined with gonadotropin-releasing hormone agonists.
Against the background of cyproterone, there may be a change in the need for oral hypoglycemic agents or insulin.
Special instructions:During the treatment, it is necessary to monitor liver function, adrenal cortex and peripheral blood picture. If signs of hepatotoxicity appear, the drug should be discontinued. Patients with diabetes may require a dose adjustment of insulin or other hypoglycemic agents (more often than usual to monitor blood glucose levels). During the treatment period, it is necessary to refrain from engaging in activities requiring increased attention. In children receiving large doses of the drug, under high-intensity loads, there may be a need for replacement therapy with glucocorticoids (due to latent adrenal insufficiency).
When alcohol is taken concomitantly with treatment in patients with pathologically elevated sexual desire, a decrease in the effect of therapy may be observed.
In extremely rare cases against the background of the use of cyproterone acetate, benign and extremely rare malignant liver tumors can be observed.
During treatment should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.