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Androgen blockers or Anti-androgen was discovered to prevent androgens like dihydrotestosterone and testosterone from expressing their biological effects in responsive tissues. Anti-androgens alter the androgen pathway by affecting androgen production or by blocking the appropriate receptors.

Prescribed Anti-androgen drugs can be taken to treat various androgen-dependent conditions. In men the drugs are mostly used to treat prostate cancer. In women also the drug is used to decrease levels of male hormones that cause symptoms of hypoandrogenism.

Uses of anti-androgen

Anti-androgen medications work by blocking the male hormone testosterone from binding to androgen receptor and are useful in treating prostate cancer. The reason being prostate cancer cells require testosterone to grow. Anti-androgen medications can be used in combination with LHRH (lutenizing hormone releasing hormone) antagonists or alone known as anti-androgen monotherapy (AAM) to reduce the amount of testosterone produced in the body. Other uses of the medicine include:

  • Acne: Acne can be caused because of several reasons. One of the reasons being excessive production of sebum which is a a whitish semi liquid greasy substance that is produced by certain glands in the skin. Anti-androgen will help by slowing down the secretion of sebum and thereby clearing acne.
  • Amenorrhea: Amenorrhea is a situation that is used to describe absence of menstrual periods in females. This is caused because of excessive high levels of androgens in the blood. Taking the medicine may help in restoring the normal menstrual periods.
  • Gender reassignment: As part of hormonal treatment that comes with gender reassignment surgery, anti androgen drugs are prescribed
  • Paraphilias: This is a condition in men where they have strong sexual urge or behaviours. The drug is prescribed to lower blood serum levels of testosterone and help them control their sexual urges.
  • Virilization: it is a condition suffered by females which is marked by changes such as male pattern baldness, overdevelopment of skeletal muscles, voice changes and so on. The drug may be prescribed to correct this condition.
  • Hirsutism: It is a condition in which women develop excess body and facial hair in patterns that are usually associated with adult males. This takes place because of excess amount of androgens in the blood. It may also result from oversensitivity of hair follicles to normal levels of androgens. Hirsutism may indicate PCOS in women.

Side effects of anti-androgen

The medication though helpful in treating prostate cancer has several side effects such as:

  • Mood/Cognitive Changes: Patients on anti-androgen drugs can experience changes in their cognitive ability or experience mood swings. When the person is being treated feeling of depression may also come
  • Muscle mass and strength: Because of anti-androgen therapy muscle strength and mass gets affected.
  • Sexual side effects: Sexual side effects such as loss of libido may also result with anti-androgen therapy
  • Gynecomastia: It is the condition where size of male breasts increases in size and become painful and tender. This is a common side effects of anti-androgen therapy.
  • Other side effects: Other side effects resulting from the disease are dizziness, loss of appetite, trouble sleeping and headache.

Anti- androgen drugs

Some of the popular anti-androgen medicines that are used in anti-androgen treatments are:

  • Leuprolide: The medicine is used to lowers the level of testosterone in the bloodstream. It also reduces levels of estrogens in women and girls and may be used to treat tumours in uterus. The medicine however should not be given to nursing women or those who are pregnant, patients diagnosed with spinal compression or those allergic to drug.  Side effects of the medicine include pain in groin, chest or legs, hot flashes, impotency, loss of interest in sex, sleep disturbance, mood change, and loss of interest in sex. Side effects experienced by women may include irregular menstrual periods, burning or itching sensation in vagina, and loss of bone density and so on.
  • Goserelin and Triptorelin: The medicines work the same way as Leuprolide. Triptorelin. Is however not usually given to women. Goserelin should not be given during lactation or during pregnancy. Side effects of Goserelin may include vomiting an nausea.   Side effects of Triptorelin may include difficulty urinating, cloudy or bloody urine, pain in lower or side back, headaches or hot flashes, vomiting or diarrhoea, unusual tiredness, depression or mood change and so on.
  • Abarelix: It is a new drug that works by blocking hormone receptors in pituitary gland. Recommended for treatment of prostate cancer. The medicine should not be given to children or women. The side effects of this medicine include irregular heartbeat, loss of bone density, hot flashes, sleep disturbances, pain in nipples or breasts.
  • Ketoconazole: It is an anti fungal drug that is used in treating hirsutism. The medicine should not be given to those who are allergic to it and also to those who consume alcohol. Also, those taking the medicine should have their liver functioning monitored at regular intervals. Side effects of Ketoconazole include loss of appetite, vomiting, nausea, skin rash, uterine bleeding, hair loss, breast pain, decline in sperm production, loss of interest in sex and so on.
  • Nilutamide, Bicalutamide and Flutamide: Flutamide is nonsteriodal anti-androgen medicine that blocks the use of androgen by the body. Bicalutamide and Nilutamide also work the same way. Flutamide and Bicalutamide should not be given to pregnant women. Liver functioning should also be monitored at regular intervals when taking these medicines. They should notify to the doctor about any pain in the upper right side of the abdomen or yellowish colour of eyes or skin. These are signs of liver damage. Nilutamide drugs should not be given to those who suffer from respiratory problems or those who have liver disorder.

Flutamide causes several side effects such as breast tenderness and gynecomastia in men, nausea, fatigue, flu like symptoms, indigestion, dark urine, dry skin, liver damage, dizziness. Nilutamide and Bicalutamide also suffer from the same side effects. In addition Nilutamide may affect the eye’s ability to adjust to sudden changes in light intensity; it may cause difficulty in breathing also.

  • Cyproterone acetate: The steroidal anti androgen drug works by lowering testosterone production and also by blocking the body's use of androgens. The drug should not be used during pregnancy or lactation or by those with liver disease. The side effects that can be experienced when taking the medicine are, it may cause cause gynecomastia, loss of interest in sex, impotency, deep venous thrombosis and it may also result in damage to cardiovascular system.
  • Spironolactone: The medicine is usually given to woman when there is excess of androgen. The drug should not be given to those with kidney failure, liver disease or with those with high levels of potassium. Taking the medicine may result in side effects such as headaches, fatigue, and drowsiness, impotency in men, nausea, diarrhoea, or loss of appetite, vomiting, skin itching or rashes.

The list of medicines is not exhaustive. There may be other medicines, uses as well as side effects also.

Diagnosis of disease

Diagnosis of the disease will be done by your doctor after examining you thoroughly. You may be asked about your medical history, sign and symptoms that you are facing. Your doctor may prescribe you with various test to identify the root cause of the health issues that you are facing.


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