Androgens

Question 1

Testosterone, Methyltestosterone, Fluoxymesterone, Oxymethalone, Oxandrolone

Answer 1

1. Tx, Men:
   - testicular deficiency, aging and impotence (androgens should be avoided due to incidence of prostate cancer in this group).
   - Anemia.
2. Tx, Women:
   - Female hypopituitarism is tx with both androgens and estrogens.
   - Methyltestosterone is used in combination w/diethystillbesterol.
3. Both sexes:
   - short stature when long bone stimulation is requried w/out masculinization.
   - Hypoproteinemia of nephrosis
   - used in debilitated post op pts/burn pts/premature infants all have negative nitrogen balance.
4. SE: Men:
   - inhibits release of LH and FSH –> dec testosterone production/spermatogenesis
   - may inc growth of prostate cancer in elderly men
   SE Women:
   - masculinization,
   - loss of gonadotropins,
   - pseudohermaphroditism if given in pregnant women.
   Both sexes:
   - Facial hair, baldness,
   - fluid retention, oily skin/acne
   - decreased HDL and in LDL,
   - psychological changes (roid rage)
5. CI: Pregnancy, androgen-dependent neoplasms, aplastic anemia, hepatic carcinomas, growing children.

Question 2

Antiandrogens

Answer 2

Prevent or depress action of androgens

• tx of hirsutism in women
• prostate tumors in men
• gynecomastia is a common SE in men

Question 3

Ketoconazole

Answer 3

1. Androgen synthesis inhibitor.

- Anti fungal that inhibits synthesis of androgens in very high doses (4x antifungal dose is used).

Question 4

Spironolactone

Answer 4

1. Reduces 17alpha hydroxylase activity
   - Mineralocorticoid antagonist
   - partially blocks androgen receptor, also inhibits synthesis of androgens, high doses,
   - indications: hirsutism and PMS in women

Question 5

Flutamide, Bicalutamide, Nilutamide

Answer 5

1. Androgen Receptor antagonists: reduces male sex accessory organ function.
2. Non-steroidal androgen receptor antagonist.
3. Tx:
   - prostate cancer, in combination w/long acting GnRH agonist.
   - May be used topically for hirsutism and male pattern baldness
   - Bicalutamide is replacing flutamide due to less hepatotoxicity and once a day dosing.
4. SE: Flutamide mild reversible hepatotoxicity. Will effect libido.

Question 6

Finasteride, Dutasteride

Answer 6

1. 5a-Reductase inhibitors (enzyme that converts testosterone to DHT).
2. TX: benign prostatic hyperplasia, male pattern baldness
3. SE: sexual dysfunction, impotence, dec libido, decreased ejaculate volume, ejaculation dysfunction, breast enlargment, gynecomastia
4. CI: Reduced PSA may mask detection of prostate carcinoma. Teratogenic! (women cannot handle these pills and men taking this cannot give blood).