Week 11: Androgens and Anti-Androgens

Question 1

Testosterone Indications:

Answer 1

• indication: primary hypogonadism (testicular disease), pituitary or hypothalamic condition, chronic illness (diabetes, cirrhosis, CKD, steroids/opioids) delayed puberty, hormone therapy in transgender males, endometriosis and postmenopausal symptoms in women **only for deficiency, NOT for impaired spermatogenesis (can suppress spermatogenesis) and infertility

Question 2

Androgen/Testosterone deficiency signs and symptoms

Answer 2

• low libido
• decreased spontaneous morning erections
• low bone mineral density
• gynecomastia
• small testes
• loss of body hair
• fatigue, depression, anemia, reduced muscle mass (sarcopenia), increased fat mass

Question 3

Testosterone ADRs

Answer 3

• Acne
• testosterone is metabolized to DHT which increases prostate cell size (can cause elevated PSA) = prostates disorders
• sleep apnea
• erythrocytosis (increased Hct)
• hard on the liver
• metabolized by CYP450
• hypoglycemia
• increased sodium retention, increased fluid retention, and edema

Question 4

Testosterone contraindications

Answer 4

• prostate or male breast cancer - severe BPH - erythrocytosis (hct > 50) - severe untreated sleep apnea - uncontrolled CHF - preg cat X

Question 5

Testosterone drug interactions

Answer 5

• anticoagulants (warfarin) - protein bound and CYP450 leads to increased effect of warfarin (increased INR) - diabetic agents - increased risk of hypoglycemia - corticosteroids - potential for enhanced fluid retention

Question 6

Testosterone monitoring? when is effect seen?

Answer 6

• check testosterone (1st thing in the morning) 2-3 months after starting treatment then every 6-12 months once stable - monitor for prostate CA 3mo and 1yr after starting treatment - monitor Hct 3-6mo after starting treatment, then annually - effects seen in 3-6 months; bone density in 2 years

Question 7

5-Alpha Reductase Inhibitors MOA and indications

Answer 7

Finasteride (Proscar, Propecia) - Anti-androgen

• inhibits 5-alpha reductase enzymes that convert testosterone to DHT
• treats BPH and male pattern baldness
• takes 6 months to work and should decrease PSA levels

Question 8

GnRH (gonadotropin releasing hormone) Analogues MOA and indications

Answer 8

Leuprolide (Lupron)

• Anti-androgen
• blocks LH release which stops the production of testosterone and estrogen
• Indications: advanced prostate CA, breast CA, management of endometriosis & fibroids, puberty suppression in transgender pts, precocious puberty

Question 9

Aldosterone Antagonists MOA

Answer 9

Spironolactone

• Anti-androgen
• inhibits the 5-alpha reductase enzyme and is also an aldosterone antagonist

Question 10

Spironolactone Indications

Answer 10

• polycystic ovarian syndrome
• acne (PCOS) - hirsutism

Question 11

Spironolactone ADRs

Answer 11

• GI upset - Gynecomastia
• Preg. Cat. X
• Men (s/s of androgen deficiency): reduced sperm levels, gynecomastia, decreased libido, depression

Women: menstrual irregularities, virilization