Overview
During treatment, monitoring of liver function, adrenal cortex, and peripheral blood picture is necessary. In patients with diabetes mellitus, a dose adjustment of insulin or other hypoglycemic drugs may be required (blood glucose concentration should be monitored more often than usual).
In women, before starting treatment, it is necessary to exclude pregnancy and conduct a general medical and gynecological examination (including examination of the mammary glands and examination of a smear of cervical mucus). During treatment, women of childbearing age, along with oral contraceptives, it is recommended to use barrier methods of contraception. In case of termination of the menstrual cycle during treatment, it is necessary to cancel the drug related pill pregnancy is excluded. Avoid getting the drug into the vessels and its quick administration with i / m injection.
There was no negative effect of the drug on fertility after discontinuation of treatment.
In rare cases, against the background of treatment with sex hormones, the development of liver tumors was observed (the connection with the drug was not proved), therefore, in the case of severe abdominal pain, enlarged liver or signs of intra-abdominal bleeding, when making a differential diagnosis, the possibility of a tumor should be considered.
In rare cases, the occurrence of thrombosis and thromboembolism was noted after the use of cyproterone (a causal relationship has not been established).
In the treatment of androgenization in women in the case of combined treatment with a drug containing ethinyl estradiol + cyproterone, if smearing bleeding is observed within 3 weeks of taking the drug, treatment is not interrupted. With persistent or repeated irregular bleeding, it is necessary to conduct a gynecological examination to exclude organic disease. Patients with organic brain and mental illnesses are usually resistant to treating hypersexuality. In case of impaired fertility, sperm analysis must be performed before treatment.
With epilepsy, multiple sclerosis, porphyria, otosclerosis, tetanus, hypertension, the risk of side effects increases.
During the treatment period, you should refrain from engaging in activities requiring increased attention.
Content
Pharmacological properties of the drug Cyproterone
Cyproterone belongs to synthetic antiandrogens - antagonists of male sex hormones. It is an antiandrogenic steroid structure. Cyproterone acetate, through competitive binding, blocks tissue receptors of male sex hormones - androgens (testosterone, dihydroepiandrosterone, androstenedione, etc.). Using to eliminate the phenomena of androgenization in women, the correction of deviations in the genital area in men, antiandrogen therapy for prostate carcinoma.
Androgens in small quantities are also formed in the body of women, mainly in the adrenal glands, ovaries and skin. Androgen-dependent skin derivatives (sebaceous glands and hair follicles) with an increase in the level of androgen production increase sebum secretion, which is a pathogenetic factor in the development of seborrhea and acne (acne), there is an excess of male hair growth in women (hirsutism) with simultaneous hair loss on the head (androgenic alopecia). Cyproterone reduces these signs of androgenization in women, which is clinically manifested by healing or preventing the formation of acne, and by reducing excessive sebum on the scalp and facial skin. Cyproterone also has gestagenic properties - it inhibits the secretion of gonadotropic hormones in the pituitary gland and inhibits ovulation, which causes its contraceptive effect.
In men, excessive androgen production causes increased testicular function, increased potency and libido, and with such an androgen-dependent disease as prostate carcinoma, the disease progresses. The introduction of the drug reduces excessive sex drive, protects the prostate gland (target organ for androgens) from exposure to androgens, and inhibits the growth of prostate tumors.
Used in the form of tablets and a prolonged depot form for Brenda-35 / m administration.
Indications for use of the drug Cyproterone
Moderately pronounced androgenization phenomena in women (hirsutism, severe or moderate forms of androgenetic alopecia and acne) with resistance to other types of therapy. Assign Brenda-35 severe androgenization phenomena. Men are prescribed for antiandrogen therapy in case of inoperable carcinoma of the prostate gland both without previous orchiectomy and after it; in the treatment of prostate carcinoma by agonists of the Russian Federation LH; for the correction of painful or pathological deviations in the field of sexual desire, necessitating a decrease in sexual activity.
The use of the drug Cyproterone
Women with moderate androgenization phenomena are prescribed orally at 10 mg / day, as a rule, in combination with a progestogen-estrogen preparation to simultaneously prevent pregnancy and prevent the development of intermenstrual bleeding. Both drugs are taken from the 1st day of the menstrual cycle, cyproterone is taken at 10 mg / day from the 1st to the 15th day of the menstrual cycle. A progestogen-estrogenic drug is taken daily from the 1st to the 21st day of the cycle, 1 dragee per day. Then they take a 7-day break during which menstrual bleeding occurs. In the absence of bleeding, medication can be continued only after exclusion of pregnancy. After a break, treatment is continued with the above method. In case of amenorrhea, cyproterone is taken from any day and the 1st day of the drug is conventionally taken for the 1st day of the menstrual cycle. The duration of treatment is usually several months. Acne and seborrhea can be treated more quickly than hirsutism and alopecia. After clinical improvement, stop taking cyproterone and continue to take only progestogen-estrogen drug.
In cases of severe androgenization in women, cyproterone is used from the 1st to the 10th day of the menstrual cycle, 100 mg once a day in combination with the administration of a progestogen-estrogen preparation from the 1st to the 21st day of the cycle. The treatment regimen is similar to the above. After clinical improvement, the dose of cyproterone can be reduced to 25-50 mg / day. In women after menopause or with a removed uterus, only cyproterone monotherapy is carried out at a dose of 25-50 mg / day according to the scheme: 21 days - intake, 7 days - break.
In high doses of inoperable carcinoma of the prostate gland (to exclude the influence of androgens of the adrenal cortex after orchiectomy), cyproterone is prescribed 100 mg 1-2 times a day or is administered intramuscularly as an injection-depot 300 mg once every 2 weeks. If an orchiectomy has not been performed, 100 mg of cyproterone is prescribed 2-3 times a day or is administered IM once a week. With the improvement of the condition or remission of the disease, cyproterone is continued. The duration of therapy is determined individually and is about 6 months.
In the treatment of patients with inoperable carcinoma of the prostate, agonists of the Russian Federation LH are previously prescribed only cyproterone for 5-7 days, 100 mg 2 times a day, and in the next 3-4 weeks, an agonist of the Russian Federation LH is added. To limit the action of androgens of the adrenal cortex during treatment with agonists of the Russian Federation, LH cyproterone continues to be taken 100 mg 1-2 times a day.
In the treatment of pathological deviations of sexual desire, the dose of cyproterone is selected individually. Usually, at the beginning of the course, 50 mg are prescribed 2 times a day or depot injections of 300 mg IM once every 10-14 days; if necessary, the dose for oral administration is increased to 100 mg 2 times a day, and temporarily - up to 3 times a day or up to 600 mg of the depot form once every 10-14 days IM. In the case of a satisfactory therapeutic effect, a single dose is reduced to the minimum maintenance. In most cases, 25 mg Brenda-35 times a day is enough for this. In this case, the dose reduction should be gradual, over several weeks. To stabilize the therapeutic effect, cyproterone is usually used for a long time, for several months.
Contraindications to the use of the drug Cyproterone
Pregnancy, severe liver dysfunction, hereditary benign hyperbilirubinemia (Rotor syndrome, Dubin-Johnson syndrome), liver tumors, a tendency to thrombosis, severe diabetes mellitus with vascular complications, sickle cell anemia, a history of herpes, idiopathic jaundice itching during pregnancy, severe chronic depression. With prostate carcinoma, the above diseases (with the exception of primary liver tumors and severe depression) are a relative contraindication and the question of the use of cyproterone is decided individually. The use of cyproterone under the age of 18 is not recommended (until the end of puberty).
Side effects of the drug Cyproterone
Sometimes it is possible to change body weight and sex drive, a feeling of anxiety, depressed mood, depression, increased fatigue, weakening of attention.
In women, combination therapy with cyproterone causes a temporary suppression of ovulation and prevents conception, sometimes breast engorgement, and very rarely liver dysfunction.
With the use of cyproterone in men, the ability to fertilize is reduced, recovering 3-4 months after stopping treatment. Very rarely, liver dysfunctions, gynecomastia are noted, sometimes together with an increase in the tactile sensitivity of the mammary nipples.
In rare cases, with the use of cyproterone, benign and very rarely malignant tumors of the liver develop.
Special instructions for the use of the drug Cyproterone
Before starting treatment of the phenomena of androgenization in women, a general medical and gynecological examination (including mammary glands) is recommended, and pregnancy should also be excluded.
When intermenstrual bleeding occurs, treatment should not be interrupted, usually it stops on its own. With heavy and repeated bleeding, a gynecological examination is necessary to exclude organic diseases of the female genital organs.
During treatment, liver function, adrenal cortex, and peripheral blood composition should be regularly monitored.
During pregnancy and lactation, the use of cyproterone is contraindicated. Taking the drug during pregnancy can cause signs of feminization in male infants.
Drug Interactions Cyproterone
Due to the effect of steroid hormones on carbohydrate metabolism and glucose tolerance when taking cyproterone, dose adjustment of insulin and other antidiabetic drugs may be required.
Instruction manual
Tradename
Androcourt®
International Nonproprietary Name
Dosage form
Structure
One tablet contains
active substance - cyproterone acetate 50 mg,
Excipients: lactose monohydrate, corn starch, povidone 25000, colloidal silicon dioxide, magnesium stearate.
Description
