Pharmacology

Question 1

What are the clinical uses of estrogens?

Answer 1

Treat female hypogonadism
HRT
Prevents bone loss
Component of hormonal contraceptives

Question 2

What are the clinical uses of progesterones?

Answer 2

Hormonal contraceptives (alone or with estrogen)
Component of HRT to lower risk of endometrial cancer
Assisted reproductive technology

Question 3

What enzyme converts testosterone to DHT?

Answer 3

5α-reductase

Question 4

What drugs inhibit 5α-reductase?

Answer 4

Finasteride

Dutasteride

Question 5

Why do supraphysiologic levels of testosterone lead to testicular atrophy and decreased spermtogenesis?

Answer 5

Inhibit LH/FSH

Question 6

Paradoxically, supraphysiologic doses of testosterone can result in gynecomastia. Why does this occur?

Answer 6

Aromatization of testosterone to estrogen

Question 7

What are the sites of action of anti-androgens?

Answer 7

GnRH receptor
CYP17 (17α-hydroxylase)
5α-reductase
Androgen receptor

Question 8

What drug is a GnRH analog?

Answer 8

Leuprolide

Question 9

What is the anti-androgen MOA of ketoconazole?

Answer 9

Inhibits desmolase
Inhibits 17α-hydroxylase
(synthesis inhibitor)

Question 10

What drugs are androgen receptor antagonists?

Answer 10

Bicalutamide

Spironolactone

Question 11

What is the anti-androgen MOA of leuprolide?

Answer 11

GnRH analog

Question 12

What is the anti-androgen MOA of dutasteride?

Answer 12

Inhibits 5α-reductase

Question 13

What is the anti-androgen MOA of bicalutamide?

Answer 13

Androgen receptor antagonist

Question 14

What is the anti-androgen MOA of finesteride?

Answer 14

Inhibits 5α-reductase

Question 15

What class of drug(s) can be used to treat prostate cancer?

Answer 15

GnRH agonist

Androgen receptor antagonist

Question 16

What is the anti-androgen MOA of spironolactone?

Answer 16

Androgen receptor antagonist

Question 17

When would you use a 5α-reductase inhibitor to treat BPH?

Answer 17

Very large prostate

Intolerance of α-1 blockers

Question 18

How can you treat precocious puberty in boys?

Answer 18

GnRH agonist

Question 19

A woman with PCOS has hirsutism, what anti-androgen drug can be given to treat this condition?

Answer 19

Spironolactone

Question 20

What drugs are SERMs?

Answer 20

Tamoxifen
Raloxifene
Clomiphene

Question 21

Detail the antagonist actions of tamoxifen.

Answer 21

Breast cancer receptors

Hot flases

Question 22

Detail the agonist actions of tamoxifen.

Answer 22

Endometrial receptors
Venous thrombosis
Prevents osteoperosis

Question 23

Compare/contrast raloxifene with tamoxifen.

Answer 23

Raloxifen is like tamoxifen, however, it does not have agonist activity at the endometrium

Question 24

What is clomiphene used for?

Answer 24

Induces ovulation- selectively blocks estrogen receptors at pituitary which increases FSH/LH output

Question 25

What drug is a pure estrogen receptor antagonist?

Answer 25

Fulvestrant

Question 26

Estrogen is not used alone to treat menopausal symptoms. What is given with estrogen and why?

Answer 26

Progesterone | Decreased risk of endometrial cancer

Question 27

What drugs are aromatase inhibitors?

Answer 27

Anastrozole | Exemestane

Question 28

What are aromatase inhibitors used to treat?

Answer 28

Breast cancer that is ER positive

Question 29

What is the MOA of anastrozole?

Answer 29

Aromataste inhibitor

Question 30

What drug is a competitive inhibitor of progestins at progesterone receptors used to terminate pregnancy?

Answer 30

Mifepristone

Question 31

What drug is administered with mifepristone and what is its MOA?

Answer 31

Misoprostol- PGE1 analog

Question 32

What is the MOA of exemestane?

Answer 32

Aromatase inhibitor

Question 33

What is the MOA of estrogen-progesterone OCPs that inhibits ovulation?

Answer 33

Inhibit LH/FSH, thus prevent estrogen surge. Without the estrogen surge there is no LH surge and no ovulation.

Question 34

How do OCPs inhibit pregnancy?

Answer 34

Inhibit ovulation Progesterones- Thicken cervical mucus Inhibit endometrial proliferation

Question 35

What is the MOA of mifepristone?

Answer 35

Inhibits progestins

Question 36

A drug with β2-agonist activity will have what effect at the uterus?

Answer 36

Relaxation

Question 37

What drugs are uterine β2-agonists given to decrease contraction frequency during labor?

Answer 37

Terbutaline | Ritodrine