Androcurus

Androcur (cyproterone) is a drug that is often used in hormonal therapy, especially in gynecology and endocrinology. It is widely known for its androgen-blocking and anti-estrogenic effects. 

Cyproterone is an androgen antagonist that acts by blocking androgen receptors and inhibiting testosterone synthesis. It also has anti-estrogenic properties by blocking estrogen receptors.

Indications Androcura

Androcur can be used to treat hormonal disorders such as hyperandrogenism and hormone-dependent tumors, as well as a component in hormonal therapy in transgender people.

Release form

Androcur is available in various forms, including oral tablets.

Pharmacodynamics

1. Androgen-blocking action: Androcur is an androgen antagonist and blocks receptors for androgens such as testosterone and dihydrotestosterone (DHT). This results in decreased tissue exposure to androgens, which may be beneficial in various conditions associated with androgen excess, such as hyperandrogenism or hormone-dependent tumors.
2. Antiestrogen action: In addition to blocking androgens, Androcur also has the ability to block estrogen receptors. This may be useful in some conditions associated with excess estrogen or when it is necessary to reduce estrogen levels in the body.
3. Additional effects: In addition to its hormonal activity, Androcur may also have an antigonadotropic effect, that is, it reduces the production of gonadotropin hormones (gonadotropin-releasing hormones) by the pituitary gland, which can lead to decreased gonadal secretion and decreased production of gonadal hormones.
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4. Therapeutic effects: All of the above pharmacodynamic properties of Androcur ensure its effectiveness in the treatment of various conditions, such as hyperandrogenism, polycystic ovary syndrome, acne, hormone-dependent tumors and in hormonal therapy in transgender people.

Pharmacokinetics

1. Absorption: Cyproterone is generally absorbed from the gastrointestinal tract following oral administration. Absorption may be variable and depend on the presence of food in the stomach.
2. Metabolism: Cyproterone is metabolized in the liver, mainly by hydroxylation and conjugation. The main metabolite is 15β-hydroxycyproterone, which also has anti-androgen activity.
3. Distribution: Cyproterone binds to blood plasma proteins, mainly albumin. It can also accumulate in tissues that are high in fat, such as adipose tissue.
4. Excretion: Cyproterone and its metabolites are excreted from the body primarily through the kidneys, both in the form of unchanged drug and in the form of metabolites. Part of the drug can also be excreted with bile through the intestines.
5. Semi-terminal period: The half-term period of cyproterone may vary depending on the individual characteristics of the body and the dosage of the drug. Usually it lasts several hours.

Dosing and administration

1. Hormonal therapy:

   • To reduce androgen levels and treat hyperandrogenism in women: Typically, the initial dose is 25-50 mg of cyproterone per day. The dose may be increased to 100 mg per day depending on response to treatment and tolerance. The drug is usually taken during a certain period of the menstrual cycle or continuously in combination with estrogens.
   • For decreased libido and androgen stimulation in men: The initial dose is usually 50-100 mg of cyproterone per day, but can be increased to 200 mg per day as needed.

2. Hormonal therapy in gender medicine:

   • For androgen suppression in transgender women (MtF): Dosage may vary depending on individual needs, but is usually 50-200 mg of cyproterone per day in combination with estrogens.
   • For libido suppression and androgen stimulation in transgender men (FtM): Dosage is usually 100-200 mg of cyproterone per day, but may be adjusted as needed.

3. Use in the treatment of acne: For the treatment of acne, the dosage may vary from 50 to 100 mg of Androcur per day, taken over a period of time.

Use Androcura during pregnancy

1. Effect on fetal development:

   • Studies in mice have shown that use of cyproterone acetate during pregnancy may slow fetal growth and increase the incidence of congenital anomalies such as cleft palate and urinary tract abnormalities. This was due to the antiandrogenic and progestogenic effects of the drug (Saal, 1978).

2. Teratogenic effects:

   • Another study in mice found that cyproterone acetate administered early in pregnancy could cause a dose-dependent decrease in fetal weight and an increase in the incidence of congenital anomalies such as exencephaly and cardiac anomalies (Eibs et al., 1982).
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3. Feminization of male fetuses:

   • Cyproterone acetate may cause feminization of male fetuses due to its antiandrogenic properties, making its use during pregnancy undesirable (Neumann & Kj, 1975).

4. Use during pregnancy:

   • Due to possible teratogenic effects and effects on fetal development, cyproterone acetate is not recommended for use during pregnancy. This is confirmed by data on its ability to cause severe congenital anomalies in animal fetuses (Saal, 1978).

Contraindications

1. Hormone-dependent tumors: Androcur can stimulate the growth of tumors, so it is contraindicated in the presence or suspicion of hormone-dependent tumors, such as breast or endometrial cancer.
2. Thromboembolic complications: Taking Androcur may increase the risk of thromboembolic complications, therefore it is contraindicated in patients with a predisposition to thrombosis or with a history of thrombophlebitis or thromboembolism.
3. Liver failure: The drug is metabolized in the liver, so its use may be contraindicated in severe liver failure.
4. Diabetes mellitus: Taking Androcur may affect blood glucose levels, so it should be used with caution in patients with diabetes mellitus.
5. Hyperkalemia: The drug may cause hyperkalemia (increased levels of potassium in the blood), so it is contraindicated if you have electrolyte imbalance or are taking other drugs that can increase potassium levels in the blood.
6. Pregnancy and lactation: The drug may have a teratogenic effect on the fetus, so its use during pregnancy is contraindicated. Its use is also not recommended during breastfeeding.
7. Hypersensitivity to the drug: The drug should be avoided in cases of known hypersensitivity to cyproterone or any of its components.

Side effects Androcura

1. Thromboembolic complications: Include thrombosis and embolism of various vessels, such as venous thrombosis, pulmonary embolism and other thromboembolic events. This is one of the most serious side effects of cyproterone.
2. Increased risk of breast cancer: Androcur may increase the risk of breast cancer in women.
3. Liver dysfunction: Includes elevated liver enzymes, hepatitis, and even liver failure.
4. Kidney dysfunction: Possible increased creatinine levels in the blood and other kidney dysfunction.
5. Electrolyte disturbances: Includes hyperkalemia, hypernatremia and other electrolyte disturbances.
6. Decreased libido and sexual function: Men and women may experience decreased libido, erectile dysfunction, anorgasmia and other sexual dysfunction.
7. Weight changes: Weight gain or loss may occur.
8. Menstrual irregularities: Women may experience menstrual irregularities, including amenorrhea and abnormal bleeding.
9. Mood disorders: Includes depression, anxiety, mood changes and other mental disorders.
10. Sleep disorders: Insomnia and other sleep disorders may occur.

Overdose

1. Sleepy or weak.
2. Dizziness or loss of consciousness.
3. Irregular heartbeats, including fast or slow heartbeat.
4. Digestive problems, such as nausea, vomiting, diarrhea, or abdominal pain.
5. Hyperkalemia (high potassium levels in the blood).
6. Other drug-related side effects.

Interactions with other drugs

1. Anticoagulants: Androcur may increase the effect of anticoagulants such as warfarin, which may lead to an increased risk of bleeding. Careful monitoring of prothrombin time (PT) and international normalized ratio (INR) is necessary when used together.
2. Drugs with hyperkalemic effects: Concomitant use of Androcur with drugs that can increase the level of potassium in the blood (for example, potassium-sparing diuretics or angiotensin-converting enzyme inhibitors) may lead to the development of hyperkalemia.
3. Drugs metabolized by cytochrome P450: Androcur may alter the activity of cytochrome P450 enzymes in the liver, which may affect the metabolism of many other drugs, such as cyclosporine, theophylline, tacrolimus and others.
4. Drugs affecting cardiotoxicity: Concomitant use of Androcur with drugs that can increase cardiotoxicity (for example, aminoglycoside antibiotics or antiarrhythmic drugs) may increase the risk of cardiac complications.
5. Drugs affecting liver function: Androcur may interact with other drugs that also affect liver function, which may lead to increased hepatotoxicity.