Week 11: Androgens and Anti-Androgens

Question 1

Testosterone MOA/Indications:

Answer 1

• principle endogenous androgen: effects acne, hair growth, weight gain
• highly protein bound
  Indications: hypogonadism, delayed male puberty, hormone therapy in transgender males, endometriosis and postmenopausal symptoms in women

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
Prostates disorders
Sleep apnea
Erythrocytosis (increased Hct)
Hard on the liver - metabolized by CYP450
Hypoglycemia
Testosterone causes increased sodium retention, increased fluid retention, and edema
Testosterone is metabolized to DHT which increases prostate cell size (can cause elevated PSA)

Question 4

Testosterone contraidications

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

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

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 Analogues MOA and indications

Answer 8

Leuprolide (Lupron)
- Anti-androgen - shuts down the pituitary axis - blocks the release of LH which stops the production of testosterone and estrogen -
Indications: treatment of advanced prostate CA, breast CA, mgmt of endometriosis - 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
• hirsutism

Question 11

Spironolactone ADRs

Answer 11

• GI upset
• Gynecomastia
• Preg. Cat. X
  Men (s/s of androgen deficiency): reduced sperm levles, gynecomastia, decreased libido, depression
  Women: menstrual irregularities, virilization