Block 2

Question 1

what is the mechanism of action of estrogen

Answer 1

diffuse across membrane
bind to intracellular receptors
hormone receptor complex binds to a hormone response element

Question 2

what is the effect of estrogen on the bone

Answer 2

decreases osteoclast activity

Question 3

what is the effect of estrogen on the RAAS system

Answer 3

increases angiotensinogen

Question 4

what is the effect of estrogen having high enterohepatic circulation

Answer 4

increases the synthesis of clotting factors and plasma angiotensinogen

Question 5

does estrogen or progesterone have a favorable effect on the lipid profile

Answer 5

estrogen: increases HDL, decreases LDL

Question 6

what are 7 uses of estrogen

Answer 6

primary hypogonadism in females
androgen dependent prostatic tumors
menopause hormonal therapy
hirsutism
PCOS
acne
menopause hormonal therapy

Question 7

what drug can be used in women with a history of breast cancer when estrogens are contraindicated

Answer 7

Paroxetine (SSRI)

Question 8

name 5 adverse effects of estrogen use

Answer 8

increased risk of endometrial/breast cancer
thromboembolism
migraine
postmenopausal bleeding
edema

Question 9

estrogen use is contraindicated in situations such as (6)

Answer 9

liver disease
untreated hypertension
porphyria cutanea tarda
thromboembolism disorders
high risk for breast cancer
estrogen dependent neoplasms/endometrial hyperplasia

Question 10

name 5 uses of progesterone

Answer 10

contraception
menopause hormone therapy
endometrial hyperplasia/cancer
increase appetite (megestrol acetate in cancer or AIDS)
prevent recurrent miscarriages

Question 11

what is the effect of progesterone on bone

Answer 11

can cause osteoporosis

Question 12

what is the effect of progesterone on the lipid profile

Answer 12

increases LDL, decreases HDL

Question 13

adverse effects of progesterone use include (5)

Answer 13

changes in libido
hirsutism
acne
osteoporosis
change in libido

Question 14

what are 2 examples of drugs which act as antiestrogens

Answer 14

Clomiphene
Fulvestrant

Question 15

what is the mechanism of action of fulvestrant

Answer 15

increases intracellular degradation of ERalpa receptor which protecting ERbeta–>decreases estrogen effect

Question 16

Fulvestrant, an antiestrogen, is used in what 2 conditions

Answer 16

breast cancer in women resistant to Tamoxifen and aromatase inhibitors
breast cancer with endometrial risk

Question 17

what is the mechanism of action of Clomiphene

Answer 17

partial agonist at estrogen receptors causes interference of negative feedback on the hypothalamus and pituitary, leading to increased FSH/LH, allowing for an increase in ovulation and pregnancy

Question 18

what is Clomiphene used for

Answer 18

infertility (ovulation induction)

Question 19

what are 3 adverse effects of Clomiphene, an antiestrogen

Answer 19

multiple births
visual disturbances
increased risk of ovarian cancer/ovarian enlargement

Question 20

what are 2 examples of selective estrogen receptor modulators

Answer 20

Tamoxifen
Raloxifene

Question 21

what is the mechanism of action of selective estrogen receptor modulators

Answer 21

estrogenic in some issues, antiestrogenic in others

Question 22

what is the mechanism of action of tamoxifen, a selective estrogen receptor modulator

Answer 22

competitive antagonist for estrogen receptors in breast tissue
agonist in bone and endometrium

Question 23

how is tamoxifen metabolism

Answer 23

it’s a prodrug converted to active form in the liver by CYP2D6/3A4

Question 24

what is tamoxifen, a selective estrogen receptor modulator, used for

Answer 24

estrogen receptor positive breast cancer

Question 25

what are 5 adverse effects of tamoxifen

Answer 25

thromboembolism/pulmonary embolism increased risk for endometrial cancer hypercalcemia cataracts bone pain

Question 26

what is the mechanism of action of Raloxifene, a selective estrogen receptor modulator

Answer 26

agonist effect on bone antagonist effect on endometrium and breast

Question 27

what are 2 uses of Raloxifene, a selective estrogen receptor modulator

Answer 27

prevention of osteoporosis in postmenopausal women reduce risk of invasive breast cancer in postmenopausal women

Question 28

what is an adverse effect of Raloxifene, a selective estrogen receptor modulator

Answer 28

thromboembolism

Question 29

what is Toremifene used for

Answer 29

metastatic breast cancer

Question 30

-ozole is a suffix used for what drug class what are 2 other drugs in this class

Answer 30

aromatase inhibitors Exemestane, Testolactone

Question 31

what is the mechanism of action of aromatase inhibitors

Answer 31

block the conversion of androgens-->estrogen leads to increase in GnRH with increases FSH and LH

Question 32

name 3 uses of aromatase inhibitors

Answer 32

estrogen dependent postmenopausal breast cancer metastatic breast cancer ovulation induction

Question 33

name 2 adverse effects of aromatase inhibitors

Answer 33

osteoporosis with prolonged use acne

Question 34

what drug class is used for prepubertal cryptorchism

Answer 34

gonadotropins (FSH/LH)

Question 35

what drug class can be used to aid with infertility in hypogonadal men

Answer 35

gonadotropins (FSH/LH)

Question 36

what are 3 adverse effects of gonadotropin use

Answer 36

multiple pregnancies ovarian hyperstimulation syndrome gynecomastia

Question 37

what is the mechanism of action of gonadotropin agonists

Answer 37

pulsatile release increases FSH/LH release continuous release increases FSH/LH release for 7-10 days, then decreases

Question 38

what is an example of a gonadotropin analog

Answer 38

gonadorelin

Question 39

what type of action does gonadorelin have

Answer 39

short acting gonadotropin-->increased FSH and LH release

Question 40

what are the uses of gonadorelin, a short acting gonadotropin

Answer 40

diagnosis of hypogonadism infertility

Question 41

what type of drug action does goserelin have

Answer 41

long acting continuous release-->decreased FSH/LH

Question 42

in what 5 situations is goserelin, a long acting gonadotropin analog, used

Answer 42

endometriosis uterine leiomyoma precocious puberty breast/ovarian cancer early pubertal transgender adolescents

Question 43

what are 3 adverse effects of gonadotropin analogues

Answer 43

symptoms of menopause gynecomastia in men osteoporosis with long term use

Question 44

GnRH receptor antagonists have the suffix ___

Answer 44

-relix

Question 45

what is the mechanism of action of combined oral contraceptives

Answer 45

negative feedback to reduce levels of FSH/LH --> decreased ovulation, atrophy of glands, slowing of tubal motility and ova transport, thickens cervical mucus

Question 46

in combined oral contraceptive pills, estrogen reduced __, progesterone reduced __

Answer 46

estrogen reduces FSH progesterone reduces LH

Question 47

what are 5 uses of combined oral contraceptives

Answer 47

endometriosis hirsutism PCOS reduce endometrial/ovarian/colorectal cancer primary dysmenorrhea

Question 48

if severe adverse effects such as __ (4) occur with combined oral contraceptive use, use must be immediately withdrawn

Answer 48

thromboembolism hepatic adenoma depression increased risk of breast cancer/cerebrovascular disorders

Question 49

combined oral contraceptive use is contraindicated if a patient has __ (9)

Answer 49

thromboembolic disease coronary disease cerebrovascular disease smoking migraines undiagnosed vaginal bleeding mild hypertension gallbladder disease convulsive disorders

Question 50

combined oral contraceptives should be avoided with use of what other drugs

Answer 50

enzyme inducers antibiotics

Question 51

mini pills are classified as __ only pills

Answer 51

progesterone

Question 52

what is the mechanism of action of mini pills (progesterone only pills)

Answer 52

decrease frequency of GnRH release-->decreased midcycle LH surge thickening of cervix mucus

Question 53

__ drugs are used when estrogen is contraindicated

Answer 53

mini (progesterone only)

Question 54

in what 5 cases are mini pills uses

Answer 54

chronic smokers hepatic disease hypertension psychosis history of thromboembolism

Question 55

what are 2 adverse effects of mini pill (progesterone only) use

Answer 55

doesn't completely suppress ovulation-->irregular fertile periods amenorrhea