Androgens and antiandrogens

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A 32-year-old woman comes to the physician due to significant pain during her menstrual cycles. The patient tells the physician that this started eight months ago and has been interfering with her activities of daily living. After an appropriate workup, the diagnosis of endometriosis is made. The physician decides to start the patient on a medication that has pro-androgenic effects and anti-estrogenic effects. Which of the following is the most likely medication used in this patient?  

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Androgens are a class of steroid hormones that act as agonists to androgen receptors.

Testosterone is the principal endogenous androgen, while synthetic androgens include testosterone derivatives and anabolic steroids.

They bind to and activate androgen receptors and are used in the treatment of conditions where testosterone levels in the body drop lower than normal, such as primary or secondary hypogonadism.

Now, antiandrogens or androgen antagonists include androgen receptor inhibitors, 5α-reductase inhibitors, and inhibitors of testosterone synthesis.

They prevent the biological effects of androgens like testosterone in the body and are used in the treatment of prostate cancer, benign prostatic hyperplasia, hair loss in males, and hirsutism in females.

Testosterone, the primary male hormone, is an androgen, andro meaning male and gen meaning “to produce,” which means testosterone helps generate the characteristics associated with male sexuality.

The effects of testosterone are first seen in the fetus, where it guides development of the male urogenital tract and external genitalia, as well as testicular descent through the inguinal canal.

Testosterone is primarily secreted by the fetal testicles.

The fetal ovaries also secrete testosterone but at much lower levels, and this largely explains the differences in fetal development between boys and girls.

In puberty, the hypothalamic-pituitary axis regulates testosterone levels and gonadal function.

Resumen

Androgens are hormones that are important in the development of male characteristics and reproduction. Common examples of androgens include testosterone and its metabolite dihydrotestosterone (DHT). Antiandrogens are drugs that block the effects of androgens. They are often used to treat conditions such as prostate cancer, benign prostatic hyperplasia (BPH), and hirsutism (excessive hair growth).

Androgens are produced by the testes, ovaries, adrenal glands, and fat tissue. Examples of antiandrogens include drugs like apalutamide, bicalutamide, and darolutamide.

Fuentes

  1. "Katzung & Trevor's Pharmacology Examination and Board Review,12th Edition" McGraw-Hill Education / Medical (2018)
  2. "Rang and Dale's Pharmacology" Elsevier (2019)
  3. "Goodman and Gilman's The Pharmacological Basis of Therapeutics, 13th Edition" McGraw-Hill Education / Medical (2017)
  4. "Effect of Anabolic−Androgenic Steroids and Glucocorticoids on the Kinetics of hAR and hGR Nucleocytoplasmic Translocation" Molecular Pharmaceutics (2010)
  5. "Sex Hormones (Male): Analogs and Antagonists" Encyclopedia of Molecular Cell Biology and Molecular Medicine (2006)
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