Antiandrogens

Definition - What does Antiandrogens mean?

Anti-androgens are a diverse group of medicines that counteract the effects of excess amounts of androgens or male sex hormones, namely testosterone and dihydrotestosterone. They are used to treat a variety of androgen excess states in both males and females.

Androgen excess states in women include excess male-pattern hair growth (or hirsutism), acne, polycystic ovary syndrome (PCOS), and menstrual disorders. These medications are harmful to the fetus, and therefore, women of childbearing age need adequate contraception while using them.

In males, anti-androgens are primarily used to treat prostate cancer, but tend to cause enlargement of the breast tissues due to reduced blood levels of male hormones.


FertilitySmarts explains Antiandrogens

Some of the commonly prescribed anti-androgens include:

  • Cyproterone acetate: This is the most commonly used medication, has progesterone-like effects, and is often used in combination with an estrogen to treat multiple abnormalities in women with PCOS and prostate cancer in men.
  • Spironolactone: Although a water pill, it can also benefit women with hirsutism.
  • Flutamide, bicalutamide, nilutamide: These are mostly used to treat prostatic cancer.
  • 5α-reductase inhibitors like finasteride and dutasteride: These medications block the enzyme 5α-reductase that converts testosterone to its active form. They are used in the treatment of prostate disorders like benign prostate hyperplasia in males as well as PCOS in females.
  • Leuprolide (Lupron): It is prescribed in endometriosis because it considerably lowers estrogen levels. It is also used for in vitro fertilization (IVF) to facilitate the recruitment of ovarian follicles by halting the development of the dominant follicle. In men, Leuprolide is used to treat prostate cancer.

In PCOS, the antiandrogens not only benefit excessive hair growth and menstrual irregularities but also appear to reduce body fat, improve the blood lipid profile, and optimize ovulation by minimizing the insulin resistance. The improvement in ovulation can help with infertility that is a major problem in women with PCOS. Although contraceptives are usually given along with antiandrogen therapy, doctors usually prescribe antiandrogens with an approach to maintain the antiandrogenic effects even after the antiandrogen and contraceptive medications are discontinued. This allows for the ovulation-promoting effect of antiandrogens while limiting the actions of the contraceptive.

Side effects associated with the use of antiandrogens are as follows:

In women:

  • Cessation of menses (amenorrhea) or irregular periods during the childbearing age: Antiandrogens lower the levels of estrogens (the primary female sex hormones) in females. This is because of the lower availability of androgens to be converted to estrogens in the body via an enzyme, called aromatase
  • Osteoporosis: Due to the loss of protective effect of androgens and estrogens on bone
  • Liver function derangement
  • Breast pain/tenderness
  • Malformations in babies if taken while being pregnant

In men:

  • Erectile dysfunction: Anti-androgens can interfere with erectile performance
  • Reduced volume of semen and reduced count of sperms: Both of which affect a man’s ability to conceive
  • Reduced muscle mass and strength
  • Reduced hair growth
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