Androgens

Question 1

Danazol

Answer 1

Given orally, weakly androgenic and interacts with progesterone as well as androgen receptor.
Suppresses the pituitary-ovarian axis; depresses the output of FSH, LH
Causes Pancreatitis

Question 2

Spironolactone

Answer 2

Anti Androgen
weak inhibitor of the binding of androgen to the androgen receptor, primarily inhibits androgen synthesis
Reduces conc of cytochrome P450 17 a hydroxylase C17-20 lyase complex in testicular resulting in decline of testosterone
used to treat hirsutism

Question 3

Abiraterone

Answer 3

Inhibits 17 a hydroxylase/ C17, 20 lyase
Tx of patients with metastatic castration- resistant prostate cancer
SE: mineralocorticoid excess, adrenocortical insufficiency, Hepatotoxicity

Question 4

Flutamide

Answer 4

non steroidal antiandrogen devoid of other activity hormonal activity
potent competitive inhibitor of the binding of DHT to androgen receptor
used to treat prostate cancer with GnRH blockade or estrogen

Question 5

Ketoconazole

Answer 5

Interferes w/ C17-20 lyase, leading to decreased testosterone levels
used in high doses to treat prostate cancer
can be hepatotoxic

Question 6

Cimetidine

Answer 6

H2 receptor antagonist
In high doses, cimetidine can compete for the androgen receptor
Males who are treated for Zollinger-Ellison Syndrome can develop gynecomastia
Used to treat hirsutism

Question 7

Finasteride

Answer 7

Blocks conversion of testosterone to DHT
preferentially block 5a reductase 2 but also inhibits the 1 isozyme as well
Used to treat prostatic hyperplasia (BPH)
used to treat male pattern baldness

Question 8

Sildenafil, Vardenafil, Tadalafil

Answer 8

NO activates guanylyl cyclase, which form cGMP from GTP. cGMP produces smooth muscle relaxation. All 3 drugs inhibit PDE-5, responsible for the termination of cGMP in corpus cavernosum
Absolute contraindication against the use of concurrent organic nitrates

Question 9

Alprostadil

Answer 9

Form of prostaglandinE1 (PGE1) and affects blood flow
When administered via intracavernosal injection, alprostadil acts locally to relax trabecular smooth muscle of corpora cavernous and the cavernosal arteries. This causes swelling and elongation of penis when arterial blood flows into the corpus cavernous to expand the lacunar spaces
SE: hypotension, dizziness, bradycardia