Composition, structure and packing
Tablets 1 tab. cyproterone acetate 10 mg 15 pcs.
Tablets 1 tab. cyproterone acetate 50 mg tablets kapsulovidnye, from white to light yellow in color, with both sides risk stamped "LA", on the back side - hexagon.
1 tab. cyproterone acetate 100 mg.
Excipients: lactose, corn starch, povidone 25 000, magnesium stearate.
Clinico-pharmacological group: anti-androgenic drug.
Pharmacological action
Oral anti-androgenic drug. Hinders effect of male sex hormones (androgens), in small quantities produced by the body and also women. It has a gestagen, and antigonadotropnym antiandrogenic action. The men on the background of the drug observed weakening of libido and potency, and reduced function of the testes. These changes disappear after cessation of treatment.
The drug reduces or completely eliminates the influence of androgens on target organs (including on the prostate gland). The women at reception Androkura decreases as pathologically excessive hair growth on face and body, and hair loss caused by androgens in the head. In addition, reduced the increased function of the sebaceous glands and is inhibited during the treatment period, ovarian function.
Pharmacokinetics
Absorption after taking the drug cyproterone acetate inside is completely absorbed from the gastrointestinal tract. After receiving 10 mg Cmax is achieved in 1.5 h and at 75 ng / ml, after administration of 50 mg - 140 mg / ml. After receiving the tablets 100 mg Cmax achieved after an average of 2.8 ± 1.1 h. Bioavailability is 88%.
Distribution and metabolism
Binding to plasma proteins is about 96%. Biotransformiruetsya in the liver by hydroxylation and conjugation, the main metabolite, determined in human blood plasma, - 15β-Hydroxyl derivative.
Withdrawal
T1 / 2 tablets of 10 mg and 50 mg is equal to 43.9 ± 12.8 h for 100 mg - 42.8 ± 9.7 hours is derived from bile and urine mainly as metabolites in the ratio of 3:7.
Statement
Tablets containing 100 mg of cyproterone acetate:
For men: - metastatic or inoperable prostate cancer (without and after testectomy, as well as in combination with agonists gonadotropin-releasing hormone / GnRH /).
Tablets containing 50 mg cyproterone acetate:
For men: - pathological abnormalities in the area of sexual behavior, causing the need to reduce sexual desire - inoperable cancer of the prostate gland.
Tablets containing 10 mg cyproterone acetate:
For women: - caused by androgens strong loss of hair on his head to baldness (androgenic alopecia moderate);
moderate hirsutism;
acne and / or seborrhoea severe and moderate severity.
Dosage regimen
Application men
During pathological abnormalities in sexual behavior, causing the need to reduce sexual desire, dose Androkura pick in each case individually. In the early course of drug taking 50 mg 2 times / day. If necessary, the dose may be increased to 100 mg 2 times / day, and for a time - up to 3 times per day.
When the therapeutic effect of lower dose to the minimum maintenance. In most cases it is sufficient to 25 mg 2 times / day.
This dose reduction should be gradual, over several weeks, change the dose of 1 or better at 1 / 2 tablets per week. To stabilize the therapeutic effect of medication taken for a long time, for several months, possibly with simultaneous psychotherapy.
In the treatment of antiandrogens with unresectable carcinoma of the prostate prescribe the drug in a dose of 100 mg 2-3 times / day. Regardless of whether there is improvement in the patient or remission of the disease, it is necessary to continue taking the drug at the prescribed dose.
To reduce the increased production of male sex hormones in the early treatment of GnRH agonists initially prescribe medication in a dose of 100 mg 2 times / day for 5-7 days, then in the next 3-4 weeks - at the same dose in combination with a GnRH agonist. With the purpose of therapy in the treatment of hot flushes GnRH agonists or after testectomy drug appoint 50-150 mg / day, if necessary increase the dose to 300 mg / day (100 mg 3 times / day). In metastatic or unresectable cancer of the prostate gland can assign Androkura tablets containing 100 mg of cyproterone acetate in doses of 200-300 mg / day, divided into 2-3 reception.
The drug is intended for long-term daily administration. If signs of disease progression, the drug should be abolished.
Application women
When events androgenization moderate drug taking in the form of tablets of 10 mg daily from 1 st to 15 th day of the menstrual cycle in a dose of 10 mg 1 time per day. Androkur in the form of tablets of 10 mg taken together with the drug Diane-35 to obtain the necessary contraceptive effect and exceptions intermenstrual bleeding. To stabilize the loop and in order to reliable contraception patients with symptoms of androgenization additionally take from 1 st to 21 th days of the cycle the drug Diane-35 to 1 tablet / day in the same clock.
Both medications should be started in the 1 st day of the cycle (first day of bleeding). After discontinuation Androkura (10 th or 15 th day of the cycle) in the next days of the cycle take the remaining tablets from the calendar packaging of the drug Diane-35 (total 21 days). Then follows a break in the last 7 days, during which bleeding must occur.
After a 7-day pause, continue receiving the following calendar packs of drugs Androkur and Diane-35, irrespective of whether the bleeding is over or still going on. If after taking pills bleeding occurred, treatment should be discontinued and a survey.
Duration of treatment is established by a doctor and depends on the type and severity of pathological phenomena androgenization and treatment results. Acne and seborrhea are usually treatable before alopecia. Tablets Androkur ingest after a meal, washed down with a small amount of liquid.
Side effect
On the part of the musculoskeletal system: men rarely - osteoporosis.
On the part of the endocrine system: receiving Androkura for several weeks in males leads to a decrease in fertilization rate (the suppression of spermatogenesis, a reversible decrease in libido and potency), which is completely restored within 3-4 months after stopping treatment, and in rare cases - gynecomastia, sometimes combined with increased tactile sensitivity in the nipple of the breast.
The women sometimes - feeling tension in the breasts, changes in body weight. Combination therapy with Androkurom causes suppression of ovulation and prevents conception.
From the side of the central nervous system: women in isolated cases - reducing mood and depression, feeling of anxiety that the ability to focus, the application of 100 mg tablets at the beginning of therapy may be fatigue, apathy, anxiety, reduced ability to concentrate.
On the part of the digestive system: the application of 100 mg tablets at the beginning of therapy may be nausea, abdominal pain and in rare cases - violations of liver function.
Other: Using 100 mg tablets at the beginning of therapy can dry skin and in rare cases when used in high doses - a sense of lack of air.
Contraindications
liver disease;
jaundice;
constant itching or herpes during pregnancy in history;
Dubin-Johnson syndrome;
Rotor syndrome;
existing or previously transferred tumor of the liver (with carcinoma of the prostate - only in cases where the tumor is not due to metastases);
cachexia (except for patients with carcinoma of the prostate gland);
severe chronic depression;
previous or existing thromboembolic processes;
severe diabetes with vascular complications;
sickle cell anemia;
Pregnancy
lactation (breastfeeding);
Hypersensitivity to the drug.
Pregnancy and lactation
Androkur contraindicated in pregnancy. If necessary, the appointment during lactation should resolve the issue of termination of breastfeeding.
Cautions
In patients with carcinoma of the prostate and the presence of severe diabetes with vascular changes, sickle-cell anemia or preceding thromboembolic events when deciding on the appointment of the drug Androkur be individually weigh the potential benefits and risks of adverse effects of treatment. Patients before therapy Androkurom must undergo general medical and patient further gynecological examination to exclude pregnancy. At the same time taking the drug Androkur Diane-35 and the patient should be informed that with the passage of the reception Androkura and / or tablets of Diane-35 in normal times should take the drug within the next 12 hours
By exceeding the above time, the contraceptive effect for a given cycle is not guaranteed. Pills or tablets Androkur Diane-35 should continue in the period started from packages, omitting the forgotten pill and / or pills, that in this cycle to prevent premature bleeding.
In addition to the end of this cycle is necessary to use other, non-hormonal methods of preventing conception. If this cycle does not stop bleeding, you should stop therapy and a survey.
With simultaneous use of alcohol, providing action inhibitor, in patients with pathologically increased sexual attraction may be a reduction in the effect of therapy Androkurom.
Monitoring of laboratory parameters
During the period of treatment with careful monitoring of liver function and pattern of peripheral blood.
Effects on ability to drive vehicles and management mechanisms
Patients whose work requires more attention should be borne in mind that when you receive Androkura may experience fatigue, lethargy, reduced ability to concentrate.
Overdose
Studies of acute toxicity Androkura showed that cyproterone acetate can be attributed to substances with very low toxicity. In case of accidental ingestion of several tablets Androkur of intoxication should be expected.
Drug Interactions
When applied simultaneously with the drug Androkur may change the effectiveness of hypoglycemic drugs and insulin. Anti-androgenic action of cyproterone acetate increases with its joint application with GnRH agonists, the action cyproterone acetate reduced the initial increase in testosterone GnRH agonists.
Terms and Conditions of storage
Specific requirements for storage conditions not. Shelf life - 5 years.
Tablets 1 tab. cyproterone acetate 10 mg 15 pcs.
Tablets 1 tab. cyproterone acetate 50 mg tablets kapsulovidnye, from white to light yellow in color, with both sides risk stamped "LA", on the back side - hexagon.
1 tab. cyproterone acetate 100 mg.
Excipients: lactose, corn starch, povidone 25 000, magnesium stearate.
Clinico-pharmacological group: anti-androgenic drug.
Pharmacological action
Oral anti-androgenic drug. Hinders effect of male sex hormones (androgens), in small quantities produced by the body and also women. It has a gestagen, and antigonadotropnym antiandrogenic action. The men on the background of the drug observed weakening of libido and potency, and reduced function of the testes. These changes disappear after cessation of treatment.
The drug reduces or completely eliminates the influence of androgens on target organs (including on the prostate gland). The women at reception Androkura decreases as pathologically excessive hair growth on face and body, and hair loss caused by androgens in the head. In addition, reduced the increased function of the sebaceous glands and is inhibited during the treatment period, ovarian function.
Pharmacokinetics
Absorption after taking the drug cyproterone acetate inside is completely absorbed from the gastrointestinal tract. After receiving 10 mg Cmax is achieved in 1.5 h and at 75 ng / ml, after administration of 50 mg - 140 mg / ml. After receiving the tablets 100 mg Cmax achieved after an average of 2.8 ± 1.1 h. Bioavailability is 88%.
Distribution and metabolism
Binding to plasma proteins is about 96%. Biotransformiruetsya in the liver by hydroxylation and conjugation, the main metabolite, determined in human blood plasma, - 15β-Hydroxyl derivative.
Withdrawal
T1 / 2 tablets of 10 mg and 50 mg is equal to 43.9 ± 12.8 h for 100 mg - 42.8 ± 9.7 hours is derived from bile and urine mainly as metabolites in the ratio of 3:7.
Statement
Tablets containing 100 mg of cyproterone acetate:
For men: - metastatic or inoperable prostate cancer (without and after testectomy, as well as in combination with agonists gonadotropin-releasing hormone / GnRH /).
Tablets containing 50 mg cyproterone acetate:
For men: - pathological abnormalities in the area of sexual behavior, causing the need to reduce sexual desire - inoperable cancer of the prostate gland.
Tablets containing 10 mg cyproterone acetate:
For women: - caused by androgens strong loss of hair on his head to baldness (androgenic alopecia moderate);
moderate hirsutism;
acne and / or seborrhoea severe and moderate severity.
Dosage regimen
Application men
During pathological abnormalities in sexual behavior, causing the need to reduce sexual desire, dose Androkura pick in each case individually. In the early course of drug taking 50 mg 2 times / day. If necessary, the dose may be increased to 100 mg 2 times / day, and for a time - up to 3 times per day.
When the therapeutic effect of lower dose to the minimum maintenance. In most cases it is sufficient to 25 mg 2 times / day.
This dose reduction should be gradual, over several weeks, change the dose of 1 or better at 1 / 2 tablets per week. To stabilize the therapeutic effect of medication taken for a long time, for several months, possibly with simultaneous psychotherapy.
In the treatment of antiandrogens with unresectable carcinoma of the prostate prescribe the drug in a dose of 100 mg 2-3 times / day. Regardless of whether there is improvement in the patient or remission of the disease, it is necessary to continue taking the drug at the prescribed dose.
To reduce the increased production of male sex hormones in the early treatment of GnRH agonists initially prescribe medication in a dose of 100 mg 2 times / day for 5-7 days, then in the next 3-4 weeks - at the same dose in combination with a GnRH agonist. With the purpose of therapy in the treatment of hot flushes GnRH agonists or after testectomy drug appoint 50-150 mg / day, if necessary increase the dose to 300 mg / day (100 mg 3 times / day). In metastatic or unresectable cancer of the prostate gland can assign Androkura tablets containing 100 mg of cyproterone acetate in doses of 200-300 mg / day, divided into 2-3 reception.
The drug is intended for long-term daily administration. If signs of disease progression, the drug should be abolished.
Application women
When events androgenization moderate drug taking in the form of tablets of 10 mg daily from 1 st to 15 th day of the menstrual cycle in a dose of 10 mg 1 time per day. Androkur in the form of tablets of 10 mg taken together with the drug Diane-35 to obtain the necessary contraceptive effect and exceptions intermenstrual bleeding. To stabilize the loop and in order to reliable contraception patients with symptoms of androgenization additionally take from 1 st to 21 th days of the cycle the drug Diane-35 to 1 tablet / day in the same clock.
Both medications should be started in the 1 st day of the cycle (first day of bleeding). After discontinuation Androkura (10 th or 15 th day of the cycle) in the next days of the cycle take the remaining tablets from the calendar packaging of the drug Diane-35 (total 21 days). Then follows a break in the last 7 days, during which bleeding must occur.
After a 7-day pause, continue receiving the following calendar packs of drugs Androkur and Diane-35, irrespective of whether the bleeding is over or still going on. If after taking pills bleeding occurred, treatment should be discontinued and a survey.
Duration of treatment is established by a doctor and depends on the type and severity of pathological phenomena androgenization and treatment results. Acne and seborrhea are usually treatable before alopecia. Tablets Androkur ingest after a meal, washed down with a small amount of liquid.
Side effect
On the part of the musculoskeletal system: men rarely - osteoporosis.
On the part of the endocrine system: receiving Androkura for several weeks in males leads to a decrease in fertilization rate (the suppression of spermatogenesis, a reversible decrease in libido and potency), which is completely restored within 3-4 months after stopping treatment, and in rare cases - gynecomastia, sometimes combined with increased tactile sensitivity in the nipple of the breast.
The women sometimes - feeling tension in the breasts, changes in body weight. Combination therapy with Androkurom causes suppression of ovulation and prevents conception.
From the side of the central nervous system: women in isolated cases - reducing mood and depression, feeling of anxiety that the ability to focus, the application of 100 mg tablets at the beginning of therapy may be fatigue, apathy, anxiety, reduced ability to concentrate.
On the part of the digestive system: the application of 100 mg tablets at the beginning of therapy may be nausea, abdominal pain and in rare cases - violations of liver function.
Other: Using 100 mg tablets at the beginning of therapy can dry skin and in rare cases when used in high doses - a sense of lack of air.
Contraindications
liver disease;
jaundice;
constant itching or herpes during pregnancy in history;
Dubin-Johnson syndrome;
Rotor syndrome;
existing or previously transferred tumor of the liver (with carcinoma of the prostate - only in cases where the tumor is not due to metastases);
cachexia (except for patients with carcinoma of the prostate gland);
severe chronic depression;
previous or existing thromboembolic processes;
severe diabetes with vascular complications;
sickle cell anemia;
Pregnancy
lactation (breastfeeding);
Hypersensitivity to the drug.
Pregnancy and lactation
Androkur contraindicated in pregnancy. If necessary, the appointment during lactation should resolve the issue of termination of breastfeeding.
Cautions
In patients with carcinoma of the prostate and the presence of severe diabetes with vascular changes, sickle-cell anemia or preceding thromboembolic events when deciding on the appointment of the drug Androkur be individually weigh the potential benefits and risks of adverse effects of treatment. Patients before therapy Androkurom must undergo general medical and patient further gynecological examination to exclude pregnancy. At the same time taking the drug Androkur Diane-35 and the patient should be informed that with the passage of the reception Androkura and / or tablets of Diane-35 in normal times should take the drug within the next 12 hours
By exceeding the above time, the contraceptive effect for a given cycle is not guaranteed. Pills or tablets Androkur Diane-35 should continue in the period started from packages, omitting the forgotten pill and / or pills, that in this cycle to prevent premature bleeding.
In addition to the end of this cycle is necessary to use other, non-hormonal methods of preventing conception. If this cycle does not stop bleeding, you should stop therapy and a survey.
With simultaneous use of alcohol, providing action inhibitor, in patients with pathologically increased sexual attraction may be a reduction in the effect of therapy Androkurom.
Monitoring of laboratory parameters
During the period of treatment with careful monitoring of liver function and pattern of peripheral blood.
Effects on ability to drive vehicles and management mechanisms
Patients whose work requires more attention should be borne in mind that when you receive Androkura may experience fatigue, lethargy, reduced ability to concentrate.
Overdose
Studies of acute toxicity Androkura showed that cyproterone acetate can be attributed to substances with very low toxicity. In case of accidental ingestion of several tablets Androkur of intoxication should be expected.
Drug Interactions
When applied simultaneously with the drug Androkur may change the effectiveness of hypoglycemic drugs and insulin. Anti-androgenic action of cyproterone acetate increases with its joint application with GnRH agonists, the action cyproterone acetate reduced the initial increase in testosterone GnRH agonists.
Terms and Conditions of storage
Specific requirements for storage conditions not. Shelf life - 5 years.
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