Androgens and Antiandrogens

Question 1

What is hypogonadism

Answer 1

failure of testes to make testosterone

Question 2

What are some health issues with hypogonadism

Answer 2

• loss of energy
• decreased libido
• osteoporosis
• loss of muscle mass
• anemia

Question 3

How is hypogonadism treated

Answer 3

give testosterone or testosterone esters

Question 4

How is testosterone administered to a patient

Answer 4

IM or transdermal

Question 5

How should you not administer testosterone to a patient?

Answer 5

oral

• metabolized by small intestines
• low bioavailability: extensive first pass effects

Question 6

where are testosterone topical gels applied ? how do these topical gels work?

Answer 6

shoulders or upper arms

- 24 hour depot for slow release of hormone in blood

Question 7

When are testosterone topical patches applied

Answer 7

applied daily

Question 8

What is the trade name for testosterone topical patch

Answer 8

Androderm

Question 9

where should androderm not be topically applied? why?

Answer 9

scrotum

- potential to absorb too much testosterone

Question 10

When is the androgderm patch removed and why? side effects of left on?

Answer 10

• MRI test
• patch has aluminum
• can cause burning

Question 11

Why should female partners avoid touching the androderm patch

Answer 11

cause acne or abnormal hair growth

Question 12

Where is the buccal testosterone given?

Answer 12

• placed on gum

- forms gel

Question 13

What is the FDA black box warning for all testosterone gels and topical solutions

Answer 13

virilization can occur in children exposed to topical testosterone
- children should not come in contact with product

Question 14

Name 2 testosterone esters

Answer 14

testosterone cypionate and enanthate

Question 15

How is testosterone ester administered

Answer 15

IM

Question 16

What is an advantage of using testosterone ester over testosterone

Answer 16

• testosterone esters have longer duration

- administered every 2 or 4 weeks

Question 17

Testosterone is used to treat what

Answer 17

1. hypogonadism

2. metastatic breast cancer in women

Question 18

Name 2 17alpha-alkylated testosterone

Answer 18

1. methyltestosterone

2. fluoxymesterone

Question 19

what is the best route of aministration for methyltestosterone and fluoxymesterone

Answer 19

oral

Question 20

What is 17alpha-alkylated testosterone used to treat

Answer 20

1. hypogonadism

2. metastatic breast cancer in women

Question 21

Methyltestosterone and fluoxymesterone has a high abuse potential for what

Answer 21

anabolic activity

Question 22

17alpha-alkylated testosterone is contraindicated for who

Answer 22

• male breast cancer
• prostate cancer
• pregnancy

Question 23

low doses of methyltestosterone and fluoxymesterone have what adverse effects

Answer 23

cholestatic hepatitis

jaundice

Question 24

Testosterone analogues associated with methyltestosterone and fluoxymesterone have the greatest risk of what side effect

Answer 24

hepatotoxicity

Question 25

what are side effects of 17alpha-alkylated testosterone at normal doses

Answer 25

- edema ( salt and water retention) - liver cancer - bleeding due to decline levels of clotting factors II, V, VII, and X

Question 26

what are contraindications for all testosterone analogs

Answer 26

prostate cancer male breast cancer pregnancy

Question 27

MOA for Danazol

Answer 27

depresses preovulatory surge in output of FSH and LH - reduction of ovarian estrogen and progesterone production - suppress midcycle surge of FSH and LH resulting in anovulation

Question 28

Why would women not want to take Danazol

Answer 28

- weight gain

Question 29

What is Danazol used for

Answer 29

- Endometriosis - hereditary angioedema - fibrocystic breast disease

Question 30

What are adverse effects of Danazol

Answer 30

- weight gain - acne - thrombosis - mood swings - hepatic dysfunction

Question 31

what is Danazol contraindicated in

Answer 31

pregnancy | breast feeding

Question 32

MAO for Stanazolol

Answer 32

17-alpha-alkylated derivative of testosterone | - increases mRNA levels and protein levels of C1 INH and C4

Question 33

Who is Stanazolol contraindicated in

Answer 33

1. pregnancy 2. male breast or prostate cancer 3. female breast cancer with hypercalcemia

Question 34

What is Stanazolol used for

Answer 34

Hereditary angioedema

Question 35

What are adverse effects of Stanazolol

Answer 35

HEPATIC TOXICITY edema acne virilization in women , baldness

Question 36

MOA for Oxandrolone

Answer 36

- synthetic testosterone derivative | - high anabolic to andgrogenic ratio

Question 37

What is Oxandrolone used for

Answer 37

- weight gain patients who have undergone 1. extensive surgery 2. severe trauma 3. long-term corticosteroid therapy and cannot gain weight

Question 38

side effects of Oxandrolone

Answer 38

- edema - hypertension - irritability

Question 39

Oxandrolone is contraindicated in who

Answer 39

- breast cancer - prostatic cancer - pregnancy

Question 40

Overall MOA for Finasteride and Dutasteride

Answer 40

reduce levels of dihydrotestosterone

Question 41

What enzyme converts testosterone to dihydrotestosterone

Answer 41

5alpha-reductase

Question 42

Specific MOA for Finasteride

Answer 42

-competitive inhibitor of type 2 form of 5alpha-reductase

Question 43

Specific MOA for Dutasteride

Answer 43

- competitive inhibitor for Type 2 and 1 forms of 5alpha-reductase

Question 44

What are antiandrogens used for

Answer 44

- benign prostatic hyperplasia | - may take 6 months to reduce size of prostate

Question 45

Finasteride can be used in combination with other drugs

Answer 45

- Tamsulosin or Alfuzosin

Question 46

What is the MOA of Tamsulosin and Alfuzosin

Answer 46

alpha1-adrenergic receptor inhibitors | - decreases smooth muscle tone in prostate and bladder neck

Question 47

What is the specific MOA for Tamsulosin

Answer 47

- inhibits smooth muscle contraction - decreases muscle tone in bladder neck and prostatic urethra, reduces urethral pressure and resistance which lessens bladder outlet obstruction

Question 48

What are adverse effects of Finasteride and Dutasteride

Answer 48

- gynecomastia - decrease PSA values ( lower levels in males by 50%) - decrease dihydrotestosterone - elevated testosterone

Question 49

when should Fnasteride be used with caution

Answer 49

hepatic dysfunction

Question 50

Who is contraindicated for Finasteride and Dutasteride

Answer 50

- women and children - pregnancy category X - pregnant women and breast feeding women should not handle tablets

Question 51

MOA for Leuprolide

Answer 51

- GnRH agnoist - down regulation of LH and FSH - decrease levels of circulating testosterone in males

Question 52

what is Leuprolide used for

Answer 52

prostatic cancer | endometriosis

Question 53

Adverse effects of Leuprolide

Answer 53

- hot flashes - edema - gynecomastia

Question 54

MOA for Fltuamide

Answer 54

intereferes with binding of testosterone and dihydrotestosterone

Question 55

what is Fltuamide used for? route of administration?

Answer 55

``` prostatic cancer ( oral ) acne ( topical) ```

Question 56

Side effect of Fltuamide

Answer 56

- gynecomastia | - elevated liver function tests