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Antiandrogens: What Are They?

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Antiandrogens are drugs that block the effects of male sex hormones and are used to treat prostate cancer, acne, male pattern baldness, and hirsutism. They can also be used in sex reassignment therapy and to treat male sexual disorders. There are two types of antiandrogens, pure and steroidal, and they can have side effects such as nausea, decreased sex drive, and liver problems. They are contraindicated during pregnancy as they can cause permanent demasculinization in male fetuses.

Antiandrogens are hormone receptor antagonists. These compounds work by blocking the biological effects of androgens, or male sex hormones, through blockage or competition for cellular binding sites. By inhibiting the ability of testosterone to bind, these androgen antagonists cause a decrease in overall testosterone production in the body.

Doctors prescribe antiandrogens to treat a variety of problems, including prostate cancer, acne, and male pattern baldness. They have shown success in treating polycystic ovary syndrome (PCOS) and are commonly used to relieve symptoms of hirsutism or excessive hair growth. They are used by transgender women during sex reassignment therapy and to treat male sexual disorders. Some registered sex offender programs administer antiandrogens to offenders to reduce sex drive and the risk of recidivism.

During the treatment of prostate cancer, antiandrogens reduce testosterone production. Hormone receptor antagonists are often given before and after radiation therapy. In combination with other hormone therapies, antiandrogens slow the progression of prostate cancer and can relieve pain if the cancer has spread to nearby bones. Research has shown that the use of androgen antagonists increases the survival rate for men diagnosed with prostate cancer.

There are two types of these antiandrogens: pure or non-steroidal and steroidal. Flutamide is an example of a pure antiandrogen. It is one of the main drugs prescribed during prostate cancer treatment and lowers excess androgen levels in women with PCOS.

Spironolactone is classified as a steroidal androgen antagonist. This diuretic is commonly prescribed in the treatment of hirsutism. Women suffering from PCOS often experience a successful reduction in symptoms of acne or hair loss. When given to males, this drug should not be accompanied by potassium supplementation to reduce the risk of hyperkalemia or abnormally high blood potassium levels.

Ketoconazole, another commonly prescribed antiandrogen, works as a broad-spectrum antifungal. Drugs such as finasteride and dudasteride treat male pattern baldness. Other synthetic steroid antiandrogens are included in birth control pills.

Side effects caused by antiandrogen treatment include nausea, diarrhea, decreased sex drive, erection difficulties, low red blood cell count, breast enlargement, and liver problems. Long-term use can lead to osteoporosis, a disease that causes bones to become brittle and break.

Antiandrogens are absolutely contraindicated during pregnancy. Research clearly shows that male fetuses exposed to androgen antagonists in utero undergo permanent demasculinization. Side effects noted by male badger studies include genital malformations such as hypospadias and cleft phallus, absent or reduced accessory sex glands, and nipple retention.

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