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 antiestrogenic effects.

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

Indications Androcura

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

Release form

Androcur is available in various forms, including tablets for oral use.

Pharmacodynamics

1. Androgen-blocking action: Androcur is an androgen antagonist and blocks receptors for androgens such as testosterone and dihydrotestosterone (DHT). This results in a reduction in the effect of androgens on tissues, which may be useful in various conditions associated with androgen excess, such as hyperandrogenism or hormone-dependent tumors.
2. Antiestrogenic action: In addition to blocking androgens, Androcur also has the ability to block estrogen receptors. This can 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, i.e. it may reduce the production of gonadotropic hormones (gonadotropin-releasing hormones) by the pituitary gland, which may lead to a decrease in gonadal secretion and a decrease in the production of gonadal hormones.
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 after oral administration. Absorption may be variable and depends on the presence of food in the stomach.
2. Metabolism: Cyproterone is metabolized in the liver, primarily by hydroxylation and conjugation. The main metabolite is 15β-hydroxycyproterone, which also has anti-androgen activity.
3. Distribution: Cyproterone binds to plasma proteins, primarily albumin. It may also accumulate in tissues with a high fat content, such as adipose tissue.
4. Excretion: Cyproterone and its metabolites are excreted primarily via the kidneys, both as unchanged drug and as metabolites. Some of the drug may also be excreted in the bile via the intestine.
5. Half-life: The half-life of cyproterone can vary depending on individual characteristics and dosage. It is usually several hours.

Dosing and administration

1. Hormonal therapy:

   • To reduce androgen levels and treat hyperandrogenism in women: The usual starting dose is 25-50 mg 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 starting dose is usually 50-100 mg 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 typically 50-200 mg cyproterone per day in combination with estrogens.
   • For suppression of libido and androgen stimulation in transgender men (FtM): Dosage is usually 100-200 mg cyproterone per day, but can 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 the use of cyproterone acetate during pregnancy may slow fetal growth and increase the incidence of congenital anomalies such as cleft palate and urinary tract anomalies. 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).

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 supported by data on its ability to cause severe congenital anomalies in animal fetuses (Saal, 1978).

Contraindications

1. Hormone-dependent tumors: Androcur may stimulate tumor growth, 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, so 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 (elevated potassium levels in the blood), so it is contraindicated in cases of electrolyte imbalance or 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 during breastfeeding is also not recommended.
7. Hypersensitivity to the drug: The drug should be avoided in case of known hypersensitivity to cyproterone or any of its components.

Side effects Androcura

1. Thromboembolic complications: Includes 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 developing breast cancer in women.
3. Liver dysfunction: Includes increased liver enzymes, hepatitis, and even liver failure.
4. Renal impairment: Increased blood creatinine levels and other renal impairment may occur.
5. Electrolyte imbalances: Includes hyperkalemia, hypernatremia, and other electrolyte imbalances.
6. Decreased libido and sexual function: Men and women may experience decreased libido, erectile dysfunction, anorgasmia, and other sexual dysfunctions.
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 health disorders.
10. Sleep disturbances: Insomnia and other sleep disturbances may occur.

Overdose

1. Drowsiness or feeling weak.
2. Dizziness or loss of consciousness.
3. Heart rhythm disturbances, including fast or slow heartbeats.
4. Digestive upsets such as nausea, vomiting, diarrhea or abdominal pain.
5. Hyperkalemia (high levels of potassium in the blood).
6. Other adverse effects associated with the drug.

Interactions with other drugs

1. Anticoagulants: Androcur may enhance the effects 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 co-administered.
2. Drugs with hyperkalemic effect: 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) can 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 that affect cardiotoxicity: Concomitant use of Androcur with drugs that may enhance cardiotoxicity (eg, 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.