Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that block the biological effects of androgens such as testosterone and dihydrotestosterone (DHT) in the body. They work by blocking the androgen receptor (AR) and/or inhibiting androgen production. Antiandrogens can be seen as the functional opposite of androgens. Their application range covers a variety of androgen-dependent diseases and has therapeutic effects on both men and women.
Antiandrogens can be divided into three main types: androgen receptor antagonists, androgen synthesis inhibitors, and antigonadotropins.
1. Androgen receptor antagonistsAndrogen receptor antagonists directly block the effects of androgens, while androgen synthesis inhibitors and antigonadotropins work by reducing androgen levels.
This class of drugs blocks the effects of testosterone and DHT by binding directly to the androgen receptors. They include steroidal and nonsteroidal resistance agents. The effects of steroid receptor antagonists may affect other hormones, while nonsteroid receptor antagonists are more selective and have no effect on other hormones.
2. Androgen synthesis inhibitorsThis type of drug directly inhibits the biosynthesis of testosterone and DHT. These inhibitors can effectively reduce the level of androgens in the body, thereby helping to improve diseases caused by excess androgens, such as prostate cancer and polycystic ovary syndrome.
3. Antigonadotropin agentsAntigonadotropins inhibit the production of androgens by suppressing the release of gonadotropins. This type of drug is often used to treat male prostate cancer and precocious puberty in adolescents and has significant therapeutic effects.
Antiandrogens are widely used in the treatment of various diseases. In men, they are often used to treat problems such as prostate cancer, benign prostatic hyperplasia, and excessive sexual desire.
In women, anti-androgen drugs are used to treat androgen-related diseases such as acne, hirsutism, and polycystic ovary syndrome.
Testosterone and DHT play a key role in the development of prostate cancer. Antiandrogens, by reducing the effects of these androgens, can significantly slow the progression of the disease.
For example, 5α-reductase inhibitors such as finasteride are used to treat benign prostatic hyperplasia because they are effective in reducing prostate enlargement and associated symptoms.
Antiandrogens are also useful for female skin problems such as acne and hirsutism, which are related to excess androgens.
As in polycystic ovary syndrome, anti-androgens also help reduce symptoms and prevent women from developing masculine characteristics.
The side effects of antiandrogens vary depending on the type of drug. For men, common side effects include breast swelling, sexual dysfunction, etc., while women tolerate it relatively well.
However, it should be noted that anti-androgens may cause estrogen levels to be too low in some cases, causing symptoms such as hot flashes and irregular menstruation.
The mechanism of action of anti-androgens is part of their therapeutic advantage. Not only can they target different types of symptoms, but they can also be adjusted and different drugs can be selected according to individual needs.
As research into anti-androgens deepens, we may see more application development for these drugs and how to reduce possible side effects while protecting patient health.
In this rapidly developing medical field, will the progress of anti-androgens change our understanding of sex hormones and how to formulate future treatment guidelines? This is worth our consideration.