Androcur^® (Tablets, Solution) Instructions for Use

ATC Code

G03HA01 (Cyproterone)

Active Substance

Cyproterone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antiandrogenic drug

Pharmacotherapeutic Group

Antiandrogen

Pharmacological Action

Synthetic antiandrogen. It is similar in chemical structure to natural androgens and has the ability to competitively bind to tissue receptors of these hormones in target organs. It reduces or eliminates the effects of androgens, including those associated with excessive production of male sex hormones.

It has gestagenic activity and antigonadotropic properties.

Pharmacokinetics

After oral administration, it is slowly absorbed from the gastrointestinal tract. C_max in plasma is reached after 3-4 hours. The terminal T_1/2 is about 38 hours.

Cyproterone is metabolized in the liver. The main metabolite, 15β-hydroxycyproterone, has antiandrogenic activity.

About 35% of the dose is excreted in the urine in the form of free and conjugated metabolites. The remaining part is excreted in the feces.

Indications

For men: correction of pathological deviations in the sphere of sexual behavior (if it is necessary to reduce sexual activity), metastatic or inoperable prostate cancer (without and after orchiectomy, as well as in combination with GnRH agonists).

For women: moderate androgenic alopecia; moderate hirsutism; severe and moderate acne and/or seborrhea; contraception (as part of combined preparations).

ICD codes

Dosage Regimen

Establish the dosage individually based on the specific indication, clinical response, and patient tolerance.

For inoperable prostate cancer, administer 100 mg to 200 mg daily, typically in two or three divided doses. Continue therapy until disease progression is evident.

For the reduction of sexual drive in men, initiate with a dose of 50 mg twice daily. Adjust the maintenance dose to the lowest effective amount, which may be as low as a quarter of a 50 mg tablet per day.

For androgen-dependent conditions in women, such as severe acne, hirsutism, or androgenetic alopecia, administer one 10 mg tablet twice daily, typically from day 1 to day 10 of the menstrual cycle. Combine with an estrogen for a cyclic regimen, for example, from day 5 to day 25 of the cycle.

For contraception in women, use only as a component of a fixed-dose combined oral contraceptive product. Adhere strictly to the dosage regimen specified for that particular product.

Take tablets with a small amount of fluid after a meal to improve gastrointestinal tolerance. Do not exceed the prescribed daily dose. Regularly reassess the need for continued therapy.

Adverse Reactions

From the endocrine system: change in body weight is possible. In men – suppression of spermatogenesis, gynecomastia are possible; in women – a feeling of tension in the chest; in children when using high doses, a negative effect on the hypothalamus is possible, leading to inhibition of the adrenal cortex.

From the central nervous system: anxiety, depression, fatigue, deterioration in the ability to concentrate are possible.

From the digestive system: in some cases when using high doses – impaired liver function.

From the respiratory system: with rapid administration, cough, shortness of breath are possible.

Contraindications

Liver diseases, hereditary benign hyperbilirubinemias (Dubin-Johnson and Rotor syndromes); cachexia (except for patients with prostate carcinoma); severe chronic depression; thromboembolic processes or their presence in history; severe diabetes mellitus complicated by angiopathies; sickle cell anemia; adolescence until the completion of puberty; pregnancy, idiopathic jaundice of pregnancy or severe pruritus and herpes of pregnancy in history, lactation period.

Use in Pregnancy and Lactation

Cyproterone is contraindicated for use during pregnancy and during lactation.

In women, before starting therapy, pregnancy should be excluded.

Use in Hepatic Impairment

Contraindicated in liver diseases.

Pediatric Use

Contraindicated in adolescence until the completion of puberty.

In children receiving high doses of cyproterone, with high-intensity loads, replacement therapy with corticosteroids may be required due to the presence of latent adrenal insufficiency.

Special Precautions

Use with caution in patients at risk of developing depressive conditions.

During treatment, careful monitoring of liver function, adrenal cortex and peripheral blood picture, blood glucose levels is necessary.

In patients with diabetes mellitus, dose adjustment of insulin or other hypoglycemic drugs may be required.

In women, before starting therapy, pregnancy should be excluded.

In children receiving high doses of cyproterone, with high-intensity loads, replacement therapy with corticosteroids may be required due to the presence of latent adrenal insufficiency.

Influence on the ability to drive vehicles and mechanisms

During treatment, one should refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.

Drug Interactions

With simultaneous use, a change in the clinical efficacy of oral hypoglycemic drugs and insulin is possible.

With simultaneous use, the effectiveness of cyproterone is reduced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.