ANDROGENS & anti-ANDROGENS

Question 1

TESTOSTERONE (1:1): (drug names)

Answer 1

1. testosterone
2. testosterone cypionate
3. testosterone enanthate

Question 2

testosterone DERIVATIVES: (drug names)

Answer 2

1. fluoxymesterone (1:2)
2. oxymetholone (1:3)
3. oxandrolone (1:3-1:13)
4. nandrolone decanoate (1:2.5-1:4)

Question 3

androgens → pharmacokinetics:

Answer 3

1. ineffective taken ORALLY → testosterone is given IM or as patches, gels, buccal tablets
2. derivatives are alkylated on 17a position → allows oral administration, longer t1/2

Question 4

androgens → indications:

Answer 4

1. primary hypogonadism
2. secondary hypogonadism (failure of hypothalamus or pituitary)
3. chronic wasting (HIV, cancer)
4. aging
5. endometriosis
6. anemia
7. osteoporosis
8. growth stimulation (delayed puberty)
9. protein anabolic agent
10. used by athletes & body builders to increase lean body mass, muscle strength & endurance

Question 5

androgens → CONTRAindications:

Answer 5

1. breast, prostate carcinoma
2. pregnancy expectation
3. avoid in infants & young children
4. caution in renal & cardiac disease predisposed to edema

Question 6

androgens → side effects in WOMEN:

Answer 6

1. hirsutism, acne, baldness
2. deep voice
3. excessive muscle development
4. depression
5. endometrial bleeding

Question 7

androgens → side effects in MEN:

Answer 7

1. priapism
2. impotence
3. decreased spermatogenesis
4. gynecomastia
5. cosmetic change
6. prostate growth

Question 8

androgens → side effects in CHILDREN:

Answer 8

1. abnormal sexual maturation

2. growth disturbances

Question 9

androgens → other side effects:

Answer 9

1. atherosclerosis
2. sodium retention and edema
3. hepatic dysfunction, cholestasis
4. sleep apnea, aggression
5. erythrocytosis

Question 10

anti-ANDROGENS: (drug names)

Answer 10

1. leuprolide
2. finasteride
3. dutasteride
4. flutamide
5. nilutamide
6. enzalutamide
7. bicalutamide

Question 11

leuprolide → mechanism of action:

Answer 11

GnRH analog + AR antagonist

Question 12

finasteride & dutasteride → mechanism of action:

Answer 12

inhibit 5a reductase → decreased DHT

Question 13

flutamide + nilutamide + enzalutamide + bicalutamide → mechanism of action:

Answer 13

competitive inhibitors of androgens at target cell

Question 14

finasteride & dutasteride → indications:

Answer 14

1. BPH
2. prostate cancer
3. male baldness

Question 15

flutamide + nilutamide + enzalutamide + bicalutamide → indications:

Answer 15

ORAL treatment for prostate cancer