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Understanding Androgens: Function, Pharmacology, and Clinical Applications

This chapter explores androgens, primarily testosterone, produced by the testes, ovaries, and adrenal cortex. They are known for promoting male sex characteristics and have significant physiologic effects unrelated to sex. Key clinical applications include managing androgen deficiency in males, with potential adverse effects like virilization and hepatotoxicity. It discusses testosterone biosynthesis, its effects on both males and females, and various therapeutic uses, including treatment for hypogonadism, delayed puberty, and specific cancers. The chapter also addresses the misuse of anabolic steroids by athletes and associated risks.

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Understanding Androgens: Function, Pharmacology, and Clinical Applications

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  1. Chapter 65 Androgens

  2. Androgens • Produced by the testes, ovaries, and adrenal cortex • Major endogenous androgen is testosterone • Noted most for their ability to promote expression of male sex characteristics • Significant physiologic and pharmacologic effects unrelated to sex

  3. Androgens • Primary clinical application is management of androgen deficiency in males • Principal adverse effects are virilization and hepatotoxicity

  4. Fig. 65–1. Structural formulas of representative androgens.

  5. Testosterone • Biosynthesis and secretion • Males: testosterone • Females: preandrogens • Effects on sex characteristics in males • Pubertal transformation • Spermatogenesis

  6. Testosterone • Effects on sex characteristics in females • Clitoral growth • Anabolic effects • Skeletal muscle • Erythropoietic effects • Synthesis of erythropoietin • Men have greater hematocrit than women

  7. Clinical Pharmacology of the Androgens • Two basic categories • Testosterone and testosterone esters • 17-Alpha-alkylated compounds

  8. Clinical Pharmacology of the Androgens • Therapeutic uses • Male hypogonadism • Replacement therapy • Delayed puberty • Breast cancer • Replacement therapy in menopausal women • Wasting in patients with AIDS • Anemias

  9. Clinical Pharmacology of the Androgens • Adverse effects • Virilization • Premature epiphyseal closure • Hepatotoxicity • Effects on cholesterol levels • Use in pregnancy • Prostate cancer • Edema • Gynecomastia • Abuse potential (athletic performance)

  10. Clinical Pharmacology of the Androgens • Androgen preparations for male patients • Hypogonadism • Oral androgens • Intramuscular testosterone ester • Transdermal testosterone patches • Transdermal testosterone gels • Implantable testosterone pellets • Testosterone buccal tablets

  11. Androgen (Anabolic Steroid) Abuse by Athletes • Many athletes use to enhance athletic performance • Significant risks • Hypertension, suppression of release of LH and FSH, testicular shrinkage, sterility, gynecomastia, acne, reduction in HDL and increase in LDL • Hepatotoxicity with 17-alpha-alkylated compounds • Renal damage • Psychologic effects • Mentally healthy: minimal impact • Psychologically unbalanced: could intensify aggression

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