021315 female pharm

Question 1

physiological effects of estrogen

Answer 1

• enhances skeletal maturation and epiphyseal growth plate closure
• feedback regulation of gonadotropin release
• positive effects on bone mass
• increases clotting
• changes bile composition (increases saturation of bile with cholesterol-can cause gallstones)
• increases amt of cervical mucus and water content (facilitates sperm penetration of cervix)
• promotes endometrial proliferation
• increases tubal contractility and favors uterine myometrium contractions

Question 2

progesterone and estrogen bioavailability

Answer 2

low oral bioavailability

half life of minutes due to first pass effect

Question 3

physiologic effects of progesterone

Answer 3

• decreases frequency of GnRH pulses (suppresses gonadotropin release)
• decreases estrogen-driven endothemetrial proliferation and leads to development of secretory endomerium
• changes cervical mucous to scant viscid material (sperm has difficulty penetrating)
• maintenance of pregnancy

Question 4

main determinant for onset of menstruation

Answer 4

abrupt decline in progesterone at end of cycle

Question 5

mestranol is converted by the body to

Answer 5

ethinyl estradiol

Question 6

ethinyl estradiol

Answer 6

synthetic estrogen
orally bioavailable (limits first pass effect)

Question 7

uses of estrogen

Answer 7

combination oral contraceptives (ethinyl estradiol or mestranol)

postmenopausal hormone replacement (equine estrogens, estradiol)

failure of pituitary fxn and ovarian development

Question 8

adverse and toxic effects of estrogen

Answer 8

gallbladder disease
oral estrogens increase risk of thromboembolic dis
nausea and vomiting-initial use
breast swelling
migraine

Question 9

contraindications to estrogen use

Answer 9

pregnancy
estrogen-dependent cancers
undiagnosed uterine bleeding
thromboembolic disorders

Question 10

clomiphene

Answer 10

racemic mixture of two isomers (weak estrogen agonist and potent antagonist)

Question 11

use of clomiphene

Answer 11

induce ovulation (infertility due to anovulation)

Question 12

MOA of clomiphene

Answer 12

inhibits action of stronger estrogens–inhibiting feedback on pituitary and hypothalamus. increases pulsatile gonadotropin release amplitude

Question 13

side effects of clomiphene, tamoxifen, raloxifene, aromatase inhibitors

Answer 13

hot flashes

Question 14

SERMs MOA

Answer 14

mixed estrogenic and antiestrogenic effects (tissue specific)

it’s anti-estrogenic in breast

Question 15

use of tamoxifen

Answer 15

tx and prevention of breast cancer

Question 16

raloxifene MOA

Answer 16

estrogen agonist in bone

Question 17

use of raloxifene

Answer 17

prophylaxis of osteoporosis

breast cancer

Question 18

aromatase inhibitors

Answer 18

letrozole
anastrozole
exemestane

Question 19

suicide inhibitor that irreversibly inactivates aromatase

Answer 19

exemestane

Question 20

uses of aromatase inhibitors

Answer 20

breast cancer

Question 21

medroxyprogesteron

Answer 21

progesterone analog

Question 22

norethindrone

Answer 22

19 nortestosterone derivative
primarily progestational rather than androgenic activity

ethinyl subsituent at C17 slows hepatic metabolism

Question 23

norgestrel

Answer 23

racemic mixture of inactive isomer and active isomer Levonorgestrel

13 ethyl substituent results in more potent progestin with less androgenic activity than norethindrone

Question 24

drospirenone

Answer 24

spironolactone analogue

has ANTI-MINERALCORTICOID and progestin activity

Question 25

use of drospirenone

Answer 25

pregnancy prevention

emotional and physical symptoms of premenstural dysphoric disorder (to reduce tendency toward edema)

moderate acne vulgaris

Question 26

uses of progestins

Answer 26

hormonal contraceptives

post menopausal hormone replacement therapy (with an estrogen b/c want to limit the proliferation that would occur with estrogen alone)

others-secondary amenorrhea, endometrial hyperplasia

Question 27

adverse effects of progestins

Answer 27

headache
breakthrough bleeding
androgenic actions-acne, hirsutism

Question 28

mifepristone

Answer 28

competitive progesterone receptor modulator. mainly an antagonist

Question 29

use of mifepristone

Answer 29

pregnancy termination

Question 30

MOA of mifepristone

Answer 30

causes decidual breakdown

sensitizes myometrium to contractile actions of PGs

Question 31

how is mifepristone administered

Answer 31

in combo with PG (misoprostol) to ensure expulsion of blastocyst

Question 32

ulipristal

Answer 32

selective progesterone receptor modulator

partial agonist

Question 33

use of ulipristal

Answer 33

emergency contraception

Question 34

MOA of ulipristal

Answer 34

inhibits ovulation by inhibiting LH release which inhibits LH-induced follicular rupture in ovary

Question 35

emergency contraception

Answer 35

combined oral contraceptives (levonorgestrel and ethinyl estradiol)

levonorgestrel alone

ulipristal