Cyproterone-Teva, tablets 50 mg 50 pcs

Pharmacotherapeutic group: antiandrogen

Pharmacological properties

Pharmacodynamics. Cyproterone has the ability to compete with
tissue androgen receptors in target organs, reducing or completely
eliminating the effects of androgens (both endogenous and exogenous origin) in
target organs of men and women. In addition to the antiandrogenic effect,
cyproterone has a powerful antigonadotropic and progestogenic effect.
In men, while taking cyproterone, there is a weakening of sexual desire and
a decrease in testicular function. Cyproterone reduces or completely eliminates the effects
of androgens on the prostate gland.
The use of cyproterone in women reduces the symptoms of androgenization
regardless of what causes these symptoms – increased
production of androgens or increased sensitivity of receptors to circulating
androgens. Reduces hirsutism, androgenetic alopecia, reduces the secretion of the
secretion of the sebaceous glands of the skin. Cyproterone inhibits ovulation, which causes its
contraceptive effect.

After you stop taking cyproterone, all of its effects disappear.

Pharmacokinetics.

Cyproterone in a wide range of doses after oral administration
is completely absorbed. The absolute bioavailability of cyproterone after
oral administration is about 88%. When taking 50 mg of cyproterone, its maximum
concentration in blood serum after 3 hours is 140 mg / ml. Then there is a
two-phase decrease in concentration (within 24-120 hours). The final
half-life is 43.9±12.8 hours. The total serum clearance of cyproterone is 3.5±1.5
ml/min/kg. Cyproterone undergoes biotransformation in the liver, mainly with the
participation of the CYP3A4 isoenzyme of cytochrome P450. Metabolism occurs mainly
by hydroxylation and conjugation. 15beta-hydroxy derivative is the main
metabolite in human plasma.
Cyproterone is excreted mainly in the form of metabolites with bile and kidneys, part of
cyproterone is excreted unchanged. The ratio of cyproterone in urine and bile
is 3:7. The half-life (T1 / 2) with bile and kidneys is 1.9 days. Metabolites
are excreted from blood plasma at approximately the same rate (T1 / 2 – 1.7 days).
Cyproterone is almost completely bound to plasma albumin. Only 3.5-4%
is in the blood in a free form. Since the connection (non-specific) with
plasma proteins is more important, changes in the content of
sex hormone-binding globulin do not affect the pharmacokinetics of cyproterone.
Due to the long-term nature of the elimination of cyproterone from blood plasma during its
daily intake should be expected to accumulate cyproterone in serum 3 times
greater when using repeated doses in one cycle of treatment

Composition

Indications

Use during pregnancy and lactation

Contraindications

Side effects

Interaction

How to take, course of administration and dosage

Overdose

Special Instructions