Androgen Pharm

Question 1

What cells produce Testosterone in men and women?

Answer 1

Leydig Cells

Question 2

How often is GnRH secreted?

Answer 2

every 30-120 minutes

Question 3

Where does negative feedback for Testosterone take place?

Answer 3

Anterior Pituitary and Hypothalamus

Question 4

What is the enzyme int the Leydig cells that converts androstendione testosterone?

Answer 4

17B hydroxysteroid dehydrogenase (17B-HSD)

Question 5

What proteins is Test. normally bound to?

Answer 5

Albumin (bioavailable)

SHBG sex hormone binding globulin (unavailable)

Question 6

What are the 2 functions of Testosterone?

Answer 6

Anabolic 
Androgenic (sexual repro and 2ndry male sex char.)

Question 7

What are the anabolic Effects of Androgens?

Answer 7

Inc. RMR
Lower Blood Glucose
Inh. Lipid acc. in adipocytes
Skel- Enhances bone formation
closure of  epi Gr Plate
RBCs- Inc production of EPO
Muscle- Inc. Protein synth and Inh. Protein Breakdown

Question 8

What are the Theraputic uses of androgens?

Answer 8

Endometriosis
Delayed puberty
Hypogonadism
Aging
Anabolic Effects

Question 9

What is Hypogonadism?

Answer 9

Androgen deficiency

Question 10

What is Primary Androgen Def?

Answer 10

Testicular dysfunction. Dec. T

Loss of Neg. FB

Question 11

What is Secondary Androgen Def?

Answer 11

Hypothalamus
Morbid obesity
Dec in circulating gonadotropins
Low T with low LH andFSH

Question 12

What are the theraputic androgen preparations?

Answer 12

Methyltestosterone (Oral or SL)
Test. Enanthate (IM)
Testosterone (TD or topical)

Question 13

What are the adverse effects of Androgen therapy?

Answer 13

Premature epiphyseal closure
Inc Musc/tend injuries
Hepatic Dysfunction
Lipid metabolism
Edema, Fluid retention
Polycythemia
Mental Disturbances

Question 14

Waht are the theraputic uses of Antiangrogens?

Answer 14

F- Hirsuitism
M-Precocious Puberty
-BPH
-Prostate Cancer
-Alopecia

Question 15

What are the different types of anti-androgens?

Answer 15

Androgen Receptor inhibitors
GnRH Agonists
GnRH Antagonists
Steroid Synthesis Inhibitors

Question 16

Waht are the drugs included in the And. Rec. Antagonists?

Answer 16

Flutamide

Bicalutamide

Question 17

What is the Use of And. Rec. Antagonists?

Answer 17

Tx for Prostate cancer

Question 18

What is are the SA of And. Rec. Antagonists?

Answer 18

Gynecomastia
Rev. Liver Tox
Limited effects when used alone
Admin prior to GnRH analog Tx

Question 19

What is the purpose of GnRH Receptor agonists?

Answer 19

Prostate Cancer Tx

Question 20

What drugs are GnRH Receptor agonists?

Answer 20

Leuprolide

Goserelin

Question 21

What are the SAs of GnRH agonists?

Answer 21

Sexual Dys
Bone mineral density loss
Anemia 
Fatigue
Initial Surge in T levels that can cause growth of Pros. Cancer

Question 22

What are the defferences between Degarelix and other GnRH receptor agonists?

Answer 22

Faster
No LH (test) surge
Red LH/FSH prod
Dec Test Production. More effective T supression

Question 23

What is the drug in the Androgen Biosynth Inhibitors?

Answer 23

Abiraterone

Question 24

What is the use of Abiraterone?

Answer 24

Mets prostate cancer

Used with prednisone

Question 25

SA ofAbiraterone

Answer 25

Hepatic Tox | HTN, Hyper K and fluid retention

Question 26

What are the 5a reductase inhibitors?

Answer 26

Finasteride and dutasteride

Question 27

What is the use of 5a-reductase inhibitors?

Answer 27

BPH | Male pattern baldness

Question 28

What is the Mechanism of Tx of Androgenic Alopecia?

Answer 28

Balding people have increased androgen receptor and 5a-reductase (DHT)levels DHT cause baldness by inducing apoptosis in dermal papilla

Question 29

What are the SA of 5a reductase inhibitors.

Answer 29

Impotence and Gynecomastia Lower PSA levels -False neg in PC screening -PSA values should be doubled for comparison.

Question 30

What is the Mechanism of Penile Erection?

Answer 30

``` Nitric Oxide Act. Guanylyl cyclase cGMP Relaxation ofSM of corpus cavernosum Inc. BF erection ```

Question 31

Waht is the MOA of ED Tx Drugs?

Answer 31

Increase in cGMP

Question 32

What are the PDE5 inhibitor drugs?

Answer 32

Sildenafil Vardenafil Tadalafil

Question 33

Which Pts respond the least well to PDE5 inhibitors?

Answer 33

Cavernous nerve dysfunction | Diabetics and Prostatectomies

Question 34

What are the SA of PDE5 inhibitors?

Answer 34

Serious crdiac events Dangerous combo with nitrates/nitrites. Dangerously Low BP Priapism Sudden vision loss

Question 35

How are Testosterone esters made and used?

Answer 35

``` FA conjugated to Test. (C17 w/ ester bond) Increases lipophilicity Dissolved in oil, given IM Slow Release Ester hydrolysed in vivo Slower metabilism(liver) Longer duration ```

Question 36

What are the properties and risks of 17 alkylated derivatives of Test?

Answer 36

Slower Liver Cat. Oral Liver and Hepatic Tox can occur (higher risk than with unmod T or Test Esters)

Question 37

What is the MOA of the Androgen receptor Antagonists?

Answer 37

Inhibits nuclear translocation of AR Blocks DNA binding Blocks coactivator recruitment

Question 38

What is the MOA of the GnRH receptor agonists?

Answer 38

Increased receptor affinity and decreased proteolysis compared to GnRH Increases LH and test. production Desensitization and Dn Reg of GnRH receptors on pituitary gonadotropes

Question 39

What must be added to the GnRH agonists in Tx of prostate cancer?

Answer 39

AR Receptor antagonist | prevents initial Test. Surge that can inc. cancer growth