Androgen Drugs

Question 1

Ketoconazole

Answer 1

Inhibition of testosterone synthesis by blocking 17a-hydroxylase

Question 2

Finasteride

Answer 2

Inhibits type II 5a-reductase = no dihydrotestosterone synthesis
Use: BPH if alpha blocker not working. Androgenetic alopecia

Question 3

Flutamide

Answer 3

Blocks androgen binding at receptor

Question 4

Leuprolide

Answer 4

GnRH analog
Continuous use: prostate cancer, precocious puberty in boys
SC or IM

Question 5

Degarelix and Ganirelix

Answer 5

GnRH antagonist

Use for advanced prostate cancer

Question 6

Dutasteride

Answer 6

Inhibits type I and II 5a-reductase = no dihydrotestosterone synthesis
Use: BPH if alpha blocker not working.
Slower onset and longer half life

Question 7

Bicalutamide

Answer 7

Androgen receptor antagonist.
Use with GnRH agonists in prostate cancer.
Preferred. Oral, once daily.

Question 8

Spironolactone

Answer 8

Androgen receptor antagonist.
Use with GnRH agonists in prostate cancer. PCOS hirsutism.
Oral tid

Question 9

Leuprolide SE

Answer 9

Headache, nausea, hypogonadism

Question 10

Finasteride & Dutaseride SE

Answer 10

Down libido. Erectile dysfunction

Question 11

Bicalutamide SE

Answer 11

Loss of libido, gynecomastia, nausea, transient abnormal LFTs

Question 12

Spironolactone

Answer 12

High K, gynecomastia

Question 13

Testosterone ethanate/cypionate

Answer 13

IM. Increased lipophilicity = goes in tissue for gradual release
Every 1-3 weeks
More fluctuations