Hormones Wu

Question 1

What is the most important structure for selective, high affinity binding to estrogen receptor?

Answer 1

Phenolic A ring

Question 2

What is the key enzyme in estrogen synthesis?

Answer 2

aromatase

Question 3

What is the major source of estrogen in premenopausal women?

Answer 3

granulosa cells of ovary

Question 4

What is the major source of estrogen in men?

Answer 4

adipose tissue

Question 5

Estrogen’s role in metabolic actions?

Answer 5

Salt and water retention, edema

DEC LDL INC HDL but inc coag factors and HT

Question 6

Who has the highest risk of osteoporosis?

Answer 6

Smokers who are thin, caucasian, inactive, low calcium intake, family history

Question 7

Estrogen Hormone replacement therapy increases risks for?

Answer 7

invasive BC, heart attack, stroke, venous thromboembolism. AAAAND MORE

Question 8

When should estrogens be contraindicated?

Answer 8

estrogen dependent neoplasm, undiagnosed geneital bleeding/liver disease/history of thromboembolic disorder, during pregnancy!

Question 9

What are two synthetic estrogens?

Answer 9

diethylstilbestrol + ethinyl estradiol

Question 10

Tamoxifen and Clomiphene are WHAT?

Answer 10

Estrogen receptor competitive antagonists

Question 11

What role does the stereochemistry play in tamoxifen and clomiphene function?

Answer 11

TRANS- antagonists

CIS- agonist

Question 12

What role does clomiphene play in humans?

Answer 12

blocks the estrogen receptor, disrupting negative feedback… enlargement of the ovaries! so tx infertility

Question 13

What should we give someone to treat their estrogen receptor positive, estrogen-dependent breast cancer?

Answer 13

tamoxifen for palliative treatment

Question 14

What is the MOA of leuprolide?

Answer 14

GnRH are desensitized, leading to decrease in gonadotropin and steroid release. acts as antiestrogen!

Question 15

What is an example of a steroidal substrate analog to aromatase?

Answer 15

exemestane! acts as suicide inhibitor to irreversibly inactivate aromatase

Question 16

Non steroidal aromatase inhibitors?

Answer 16

LETROZOLE and ANASTROZOLE! interact with heme groups of CYPS

post menopausal BC and induction of ovulation with infertility

Question 17

What causes the 1*C temperature rise at midcycle?

Answer 17

Progesterone secretion increase

Question 18

DRUGS FOR PROGESTINS

Answer 18

medroxyprogesterone, norethindrone, norgestrel, ethynodiol

Question 19

MOA of mifepristone?

Answer 19

Competitive antag at progesterone and glucocorticoid receptors.

• prevents ovulation by blocking progesterone receptors at pituitary or hypothal
• luteal phase, block progesterone action on the uterus resulting in release of prostaglandins from endometrium + menstrual bleeding\
• increased adrenal steroidogenesis

Question 20

What drugs are used as abortifacient in early pregnancy?

Answer 20

Mifepristone with prostaglandin

Question 21

Morning after pill contents-

Answer 21

Norgestrel/ethinyl estradio or straight up norgestrel or single dose 600 mg mifepristone

Question 22

How do estrogen and progestin interfere with fertility?

Answer 22

INHIBIT OVULATION! suppress plasma concentrations of FSH and LH

Question 23

Cardiovascular risks when taking contraceptives?

Answer 23

increased risk of thrmboembolism, increased platelet aggregation and accelerated clotting, milk hypertension

Question 24

How does one decrease their risk of endometrial and cervical cancer when on oral contraceptives?

Answer 24

take estrogen-progesterone combination preparation instead of just estrogen.

Question 25

what are the three periods of life when testosterone is highest?

Answer 25

embryogenesis
neonatal period
puberty

Question 26

What is the anabolic effect of testosterone?

Answer 26

Nitrogen retaining activity. all anabolic steroids tested are also androgenic.

Question 27

Can steroids really make you stronger???

Answer 27

Promote muscle growth in women and immature boys but no benefit at therapeutic doses

Question 28

What role does testosterone play in the bloooood?

Answer 28

stimulates erythropoietin formation! so use to treat refractory anemia.

Question 29

What androgen is used to treat endometriosis? why?

Answer 29

DANAZOL!! weak progestin and androgen activity. suppresses ovarian function by inhibiting midcycle surge of LH and FSH

Question 30

How do we manage hyperplasia and carcinoma of the prostate?

Answer 30

block the synthesis/action of androgens

Question 31

What is the most effective inhibitor of testosterone synthesis?

Answer 31

GnRH analog LEUPROLIDE– decreased plasma LH and decreased testosterone

Question 32

MOA Finasteride

Answer 32

Inhibits 5alpha reductase!Q converts tesosterone to DHT

Question 33

What acts as a competitive antag of DHT for androgen receptor

Answer 33

cyproterone acetate

Question 34

What two drugs are NON STEROIDAL anti androgens?

Answer 34

comp antag of androgen receptor

flutamide + bicalutamide

Question 35

SPIRONOLACTONE?? whats the role here?

Answer 35

Compet antag for androgen receptor. treat female hirsutism.

Question 36

general uses for anti-androgens?

Answer 36

Treat hirsuitism and male-pattern baldness in women, treat men with excessive sex drive, treat precocious puberty in boys

Question 37

What causes endometriosis?

Answer 37

Excess estrogen created each month

Question 38

What are two GnRH anaglos for endometriosis?

Answer 38

leuprolide! Nafarelin!!!!

Question 39

What are uterine fibroids?

Answer 39

benign tumors that grow in muscle layers of the uterus

Question 40

What meds can we give to shrink fibroids?

Answer 40

leuroplide and nafarelin

OR cetrorelix acetate (GnRH antagonist)

Question 41

Based on the properties of oxytocin, how can we clinically treat preterm labor?

Answer 41

• increase hydration to power plasma concentration of oxytocin
• give ATOSIBAN oxytocin antagonist!