

Androcur - antiandrogenic, gestagennoe.
Pharmacodynamics
Oral anti-androgenic drug. Inhibits the effects of male sex hormones (androgens), in small amounts also produced by the woman’s body. It has a gestagenic, antiandrogenic and antigonadotropic action.
In men, while taking the drug, there is a weakening of sexual desire and potency, as well as a decrease in the function of the testes. These changes disappear after cessation of treatment. The drug reduces or completely eliminates the effect of androgens on the target organs (including the prostate gland).
In women, while taking Androcur, both pathologically excessive hair growth on the face and body, and hair loss caused by androgens, is reduced. In addition, the increased function of the sebaceous glands is reduced and ovarian function is inhibited during the treatment period.
Pharmacokinetics
Suction
After taking the drug inside cyproterone acetate is completely absorbed from the gastrointestinal tract. After taking 10 mg Cmax is reached in 1.5 hours and is 75 ng / ml, after taking 50 mg - 140 mg / ml. After taking the pill 100 mg Cmax reaches an average of 2.8 ± 1.1 hours. Bioavailability is 88%.
Distribution and metabolism
Plasma protein binding is about 96%. Biotransformed in the liver by hydroxylation and conjugation, the main metabolite, as determined in human plasma, is a 15β-hydroxyl derivative.
Removal
T1/2 for pills of 10 mg and 50 mg, it is equal to 43.9 ± 12.8 hours; for 100 mg, it is 42.8 ± 9.7 hours. It is excreted in bile and urine mainly as metabolites in the ratio 3: 7.
Manifestations of moderate androgenization in women, such as:
1 tablet contains:
Active substances: cyproterone acetate, micro 20 - 10 mg;
Excipients: lactose monohydrate - 63.4 mg, corn starch - 44 mg, povidone 25 000 - 1.35 mg, colloidal micronized silicon dioxide - 1 mg, magnesium stearate - 0.25 mg.
Cyproterone is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Androcur | Bayer Pharma AG | Germany | pills |
Cyproterone-Teva | Teva | Israel | pills |
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Antiandrogenic therapy for inoperable prostate cancer: At 200-300 mg / day (1 tablet 2-3 times a day, for a long time).
If you improve or achieve remission, you should not interrupt treatment or reduce the dosage.
To reduce the initial increase in androgen levels in GnRH agonist therapy:First, 200 mg per day (1 tablet 2 times a day) as monotherapy for 5–7 days, then 200 mg per day for 3–4 weeks in combination with a GnRH agonist in the dosage recommended by the manufacturer.
For the treatment of hot flashes during therapy with GnRH analogues or after orchiectomy: At 50-100 mg / day (0.5-1.5 pills per day), if necessary, followed by increasing the dose to 300 mg per day (1 tablet 3 times a day).
From the hemopoietic system: frequency unknown - anemia.
On the part of the immune system: rarely, hypersensitivity reactions.
Mental Disorders: often - depression, depressed mood, anxiety (temporarily).
From the side of the vessels: frequency unknown - thrombosis and thromboembolism.
Carefully: if patients with inoperable prostate cancer have a thrombosis and thromboembolism in history, severe diabetes mellitus with angiopathy, sickle cell anemia® appointed only after assessing the individual balance of benefit and risk in each case.
The antigonadotropic effect of cyproterone acetate is enhanced by its combined use with gonadotropin-releasing hormone agonists.
Under the action of cyproterone acetate, the initial increase in testosterone production caused by gonadotropin-releasing hormone agonists is reduced.
Contraindicated in pregnancy and during breastfeeding.
Treatment with Androcur should be carried out under the control of the liver, adrenal cortex and peripheral blood.
If there is evidence of hepatotoxicity, the drug should be discontinued.
In patients with diabetes mellitus, dosage adjustment of insulin or other hypoglycemic drugs may be required (glucose monitoring should be performed more often than usual).
The negative impact of Androcur on fertility after cessation of treatment is not marked.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
During the period of treatment it is necessary to refrain from activities requiring increased attention.
Cyproterone is practically non-toxic.
In case of an unintended single dose in a dose that is many times higher than the therapeutic one, one should not expect acute intoxication.