Androgens And Related Drugs

Front 1

What converts testosterone to DHEA?

Back 1

1. 5a reductase

Front 2

What are the physiological effects of androgens?

Back 2

1. Pubertal transformation

2. Spermatogenesis

3. Anabolic effects

4. EPO effects

Front 3

What are the clinical uses of androgens?

Back 3

1. Male hypogonadism

2. Delayed puberty

3. Wasting in AIDS patients

4. Anemia

Front 4

What is the clinical use of androgens in females?

Back 4

1. Palliative tx in breast cancer

Front 5

What are the testosterone esters?

Back 5

1. Testosterone cypionate

2. Testosterone enanthate

Front 6

What are the 17a alkylated androgens?

Back 6

1. Fluoxymesterone

2. Methyltestosterone

3. Oxandrolone

Front 7

What is the disadvantage of 17a alkylated androgens over testosterone esters?

Back 7

1. More hepatotoxic

Front 8

What is the effect of esterifying 17B hydroxyl in testosterone?

Back 8

1. Makes it more lipophilic

Front 9

How are most testosterones metabolized?

Back 9

1. Rapid first-pass metabolism

Front 10

What are the ssx of primary hypogonadism in males?

Back 10

1. Low testosterone production by testes

Front 11

How do you tx male primary hyopgonadism?

Back 11

1. Replacement tx

2. IM injections or gels

Front 12

What is the goal of androgen replacement tx (ART) in males?

Back 12

1. Restore libido and sexual function

2. Increase muscle mass and bone density

3. Decrease fat

Front 13

What is the use of ART in females?

Back 13

1. Hypoactive sexual desire disorder

Front 14

How do you tx delayed puberty?

Back 14

1. Short course of androgens

Front 15

How do you tx wasting in AIDs patients?

Back 15

1. Increase muscle mass and strength--- androgens

Front 16

What are the adverse effects of androgens?

Back 16

1. Premature epiphyseal closure

2. Hepatotoxicty from 17a

3. Lower HDL and raise LDL

4. Gynecomastia

Front 17

What is the pregnancy category of androgens?

Back 17

1. X--- DO NOT USE

Front 18

Is testosterone supplementation for older men with low testosterone supported by current evidence?

Back 18

1. NO!!!

Front 19

What are the categories of clinical androgens?

Back 19

1. Testosterone

2. Testosterone esters

3. 17a alkylated androgens

4. Testolactone

Front 20

What are the available delivery systems for androgens?

Back 20

1. IM

2. Transdermal patch

3. Gel

4. Implantable pellets

5. Buccal tablets

6. Oral

Front 21

What is the effect of androgen abuse in athletes?

Back 21

1. Use 6-8x normal levels

2. Increase muscle mass

Front 22

What are the anabolic steroids?

Back 22

1. 17a-alkylated compounds

2. MUCH MORE HEPATOTOXIC

Front 23

What are the adverse effects of androgen abuse in males?

Back 23

1. Testicular atrophy

2. Sterility

3. Gynecomastia

4. Acne

5. Raise LDL and lower HDL

Front 24

What are the adverse effects of androgen abuse in females?

Back 24

1. Menstrual irregularities

2. Virilization

Front 25

What is the adverse effect of androgen abuse by athletes?

Back 25

1. Premature epiphyseal closure

Front 26

What is the efficacy of GH and IGF-1 abuse by athletes?

Back 26

1. Evidence is purely anecdotal

Front 27

What is the indication of minoxidil?

Back 27

1. Topical formulation for androgenic alopecia

Front 28

What is the MOA of mionxidil?

Back 28

1. Not well understood

Front 29

What causes male pattern baldness and BPH?

Back 29

1. Blocks 5a reductase, inhibiting conversion of testosterone and DHEA

Front 30

What are the 5a reductase inhibitors?

Back 30

1. Finasteride

2. Dutasteride

Front 31

What are the indications of finasteride?

Back 31

1. BPH

2. Androgenic alopecia

Front 32

What is the clinical indication for dutasteride?

Back 32

1. BPH

Front 33

What are the PDE 5 inhibitors?

Back 33

1. Sildenafil citrate--- viagra

2. Tadalafil

3. Avanafil

Front 34

What is the indication for sildenafil citrate?

Back 34

1. Erectile dysfunction

2. Pulmonary arterial hypertension

Front 35

What is the MOA of sildenafil citrate?

Back 35

1. Inhibits PDE5 in corpus cavernosum

2. NO binds to guanylate cyclase receptors

3. Increased cGMP-- smooth muscle relaxation

Front 36

What is onset of action of sildenafil citrate?

Back 36

1. 1 hour

2. 1/2 life-- 3-4 hours

Front 37

How do PDE5 inhibitors interact with nitrates?

Back 37

1. Nitrates cannot be given for about 6 half lives (24 hours)

Front 38

How is sildenafil metabolized?

Back 38

1. P450 3A4 and 2C9

Front 39

What are the adverse effects of sildenafil citrate?

Back 39

1. Vision problems

2. Severe hypotension

3. Sudden hearing loss

Front 40

What classes of drugs are approved to tx BPH?

Back 40

1. a-blockers

2. 5a-reductase inhibitors

3. Combo-- dutasteride + tamsulosin

4. PDE5 inhibitor

Front 41

What a-blockers can be used to tx BPH?

Back 41

1. Terazosin

2. Doxazosin

3. Tamsulosin

4. Alfuzosin

5. Silodosin

Front 42

What is the MOA of a1 blockers?

Back 42

1. Promote prostate smooth muscle relaxation

Front 43

Why would you want to suppress androgens?

Back 43

1. Prostate cancer

Front 44

What drugs can you use to suppress androgens?

Back 44

1. GnRH agonist

2. Androgen receptor blockers

3. GnRH antagonist

4. Estrogens

Front 45

What is the GnRH agonist?

Back 45

1. Leuprolide

Front 46

What is the MOA of leuprolide?

Back 46

1. Initial increase in testosterone synthesis

2. GnRH receptors desensitize

Front 47

What are the androgen receptor blockers?

Back 47

1. Flutamide

2. Bicalutamide

3. Nilutamide

Front 48

With what are androgen receptor blockers combined in order to tx prostate cancer?

Back 48

1. GnRH agonist

Front 49

What are the GnRH antagonists?

Back 49

1. Degarelix

2. Abarelix

Front 50

What is the MOA of GnRH antagonists?

Back 50

1. Blocks GnRH receptors in the pituitary--- decrease LH---- decrease testosterone