Male Reproductive drugs

Question 0

testosterone

Answer 0

androgen, main male sex hormone (physiologically).

a) given topical, IM, or transdermal as replacement Tx
b) abused orally for athletic benefit

Question 1

Dihydrotestosterone (DHT)

Answer 1

More potent form of testosterone, responsible for dvpt of external male genitalia in fetus.

Question 2

Finasteride, Dutasteride

Answer 2

5 alpha reductase = block DHT synthesis
Finasteride –l type II only
Dutasteride –l type I & II, may be more effective but not proven
Use: reduce prostate size in BPH,
& male pattern baldness (Finasteride only)
SE: erectile dysfunction, ejaculation problems

Question 3

Flutamide, Bicalutimide, Nilutimide, Enzalutimide

Answer 3

androgen R antagonists,
Use: w/ GnRH analog for metastatic prostate cancer
* limited solo use bc increased LH –> testosterone (some)
SE: hepatotoxicity, hot flashes, gynecomastia

Question 4

Abiraterone acetate

Answer 4

Androgen R antagonist, blocks CYP17A1

Use: lower testosterone levels

Question 5

Cytoproterone acetate

Answer 5

progestin + anti-androgen
(competes w/ DHT for androgen R)
Use: Reduce LH –> reduce testosterone

Question 6

Leuprolide, Goserelin

Answer 6

inhibit testosterone synth. by inhibiting LH,
Use: prostate cancer, endometriosis
*block GnRH if chronic use
SE: impotence, decreased libido, hot flashes, osteoporosis

Question 7

testosterone cypionate
testosterone ethanate
testosterone propionate

Answer 7

testosterone 17-b analogs (de-esterified).
IM or transdermal for testosterone replacement
* transdermal has lower, more stable blood levels

Question 8

Sildenafil

Answer 8

PDE5 inhibitor,
for Erectile dysfunction
(makes smooth muscle relax by blocking cGMP –> GMP)

Question 9

Tadalafil, Avanafil

Answer 9

PDE5 inhibitor,
for Erectile dysfunction
(makes smooth muscle relax by blocking cGMP –> GMP)

Question 10

Vardenafil

Answer 10

PDE5 inhibitor,
for Erectile dysfunction
(makes smooth muscle relax by blocking cGMP –> GMP)

Question 11

Testosterone synthesis pathway

Answer 11

Cholesterol –> pregnenolone –> progesterone –> 17hydroxyprogesterone -> androstenedione -> Testosterone

Question 12

3 phases associated with gynecomastia

Answer 12

1. Newborns - w/ remaining effect from mother’s estrogen
2. Puberty (increased testosterone and estrogen)
3. Aging (more fat mass = more testosterone to estrogen conversion)