Pharmacology of Androgens

Question 1

GnRH is released by the ______, which stimulates release of _____ and _____ from the ant. pituitary.

Answer 1

Hypothalamus

LH and FSH

Question 2

LH stimulates ____ cells to produce testosterone.

Answer 2

Leydig cells

Question 3

Testosterone promotes production of _____ by sertolli cells.

Answer 3

Sperm

Question 4

Testosterone is converted to DHT by?

Answer 4

5 alpha reductase

Question 5

Testosterone is converted to estradiol by?

Answer 5

aromatase

Question 6

Testosterone and DHT work on what receptors?

Answer 6

Androgen receptors

Question 7

Estradiol works on what receptors?

Answer 7

Estrogen receptors

Question 8

Testosterone is the most important androgen in _____ and _____.

Answer 8

Muscle and liver

Question 9

Testosterone levels peak at what time?

Answer 9

8-10 am

Question 10

Normal testosterone levels are between ____ and ____ at their peak.

Answer 10

500-700 ng/dl

Question 11

Hypogonadism is marked by testosterone levels of _____.

Answer 11

<200ng/dl

Question 12

DHT is the predominant androgen in ____ and _____.

Answer 12

Prostate and reproductive tissue.

Question 13

T/F? DHT can be converted to estradiol by aromatase.

Answer 13

False - only testosterone is the only substrate for aromatase.

Question 14

The most significant action mediated by estrogen receptors occurs in ______.

Answer 14

Bone

Question 15

What are the clinical uses for androgens?

Answer 15

Hypogonadal men/boys
Osteoporosis
Muscle wasting in AIDS pts
Hormone replacement therapy in aging men

Question 16

What are symptoms of androgen deficiency?

Answer 16

Low libido
Low bone mineral density
Gynecomastia

Question 17

T/F? Testosterone can help treat impaired spermatogenesis.

Answer 17

False - Testosterone suppression of gonadotropin secretion would further impair spermatogenesis

Question 18

What should be recommended to patients with low normal T levels?

Answer 18

Diet, lifestyle changes, and weight loss

Question 19

IM dosing of testosterone provides what benefits?

Drawbacks?

Answer 19

Less frequent injections but higher fluctuation in T levels.

Question 20

Oral testosterone is hardly ever used do to what side effects?

Answer 20

Hepatic side effects

Question 21

What adverse effect of a testosterone patch requires discontinuance in up to 1/3 of patients trying the patch?

Answer 21

Severe skin rash

Question 22

List the adverse effects of testosterone.

Answer 22

Decreased HDL and increased LDL
Hypomania (roid rage)
Cardiovascular risks

Question 23

T/F? All anabolic hormones also have androgenic side effects.

Answer 23

True

Question 24

Pulsatile administration of GnRH ______ (increases/decreases) LH and FSH release.
Continuous administration of GnRH _______ LH and FSH release.

Answer 24

Increases

Blocks

Question 25

Targets for Anti-Androgen drug action include?

Answer 25

GnRH receptors CYP17 (testosterone synthesis) 5 alpha reductase Androgen receptors

Question 26

Give an example of a CYP17 inhibitor.

Answer 26

Ketoconazole

Question 27

Give an example of a 5 alpha reductase inhibitor.

Answer 27

Finasteride

Question 28

Give an example of an androgen receptor inhibitor.

Answer 28

Flutamide | Spironolactone

Question 29

List the clinical uses of anti-androgens.

Answer 29

BPH Androgenic alopecia Prostate cancer Hirsutism of polycystic ovarian syndrome

Question 30

List 3 alpha blockers for BPH treatment.

Answer 30

Tamsulosin (flomax) - uroselective Silodosin (rapaflo) - uroselective Doxazosin - non selective.

Question 31

Common side effect of alpha blockers?

Answer 31

Orthostatic hypotension

Question 32

For BPH patients who cannot tolerate alpha blockers, what medications would you recommend?

Answer 32

5 alpha reductase inhibitors FInasteride Dutasteride

Question 33

Adverse effects of 5 alpha reductase inhibitors?

Answer 33

decreased libido ejaculatory or erectile dysfunction weakness

Question 34

What oral medication is available for treatment for androgenic alopecia?

Answer 34

Finasteride

Question 35

Is there a difference in dose of finasteride for treatment of BPH vs androgenic alopecia?

Answer 35

Yes BPH - 1mg Androgenic alopecia - 5mg

Question 36

What topical medication is available for androgenic alopecia?

Answer 36

Minoxidil (Rogaine)

Question 37

What class of medications used to treat prostate cancer is associated with an initial flare of bone pain and urinary tract symptoms?

Answer 37

GnRH agonists

Question 38

What medications are examples of GnRH agonists used to treat prostate cancer?

Answer 38

Leuprolide (Lupron) | Histrelin (Supprelin)

Question 39

What is the preferred androgen receptor blocker used for prostate cancer?

Answer 39

Bicalutamide

Question 40

Role of bicalutamide in prostate cancer?

Answer 40

Reduces flare symptoms

Question 41

When are GnRH antagonists indicated for prostate cancer?

Answer 41

Advanced prostate cancer

Question 42

T/F? GnRH antagonists are associated with flare symptoms.

Answer 42

False

Question 43

First line treatment for hirsutism of PCOS?

Answer 43

Combined oral contraceptive.

Question 44

Your patient you are treating for hirsutism of PCOS has had a suboptimal response to a COC. What medication would you consider adding?

Answer 44

Spironolactone