Contraceptives

Question 1

Ethinyl Estradiol & Mestranol MOA

Answer 1

Estrogen; Ethinyl groups greatly decrease hepatic metabolism; often used in oral contraceptive

Question 2

Ethinyl Estradiol & Mestranol Tox (in combo pill)

Answer 2

Estrogen component responsible for breast enlargement, increased excitability

Question 3

Ethinyl Estradiol & Mestranol uses

Answer 3

MC used as combo of estrogen/progestin for oral contraceptive; also in tx of prostate tumors

Question 4

Progestin Drugs

Answer 4

Norethindrone, norgestrel, levonorgestrel

Question 5

Progestin MOA

Answer 5

Progestin; Impairs sperm transport by thickening the cervical mucus, decreases motility of ovules in oviduct, & alters endometrium to impair implantation

Question 6

Progestin Tox (in combo pill)

Answer 6

Progestin component responsible for acne & wt gain

Question 7

What protein is progestin bound to in blood

Answer 7

Transcortin

Question 8

What protein is estrogen bound to in blood

Answer 8

70% bound to SHBG

Question 9

Which estrogen receptor is found in female genital tract

Answer 9

ER-alpha

Question 10

which estrogen receptor is found in prostate and ovary

Answer 10

ER-beta

Question 11

DDI of OCs

Answer 11

Failure w/ Abx, Rifampin, anti-HIV, anti-convulsants, St. John’s wort

Question 12

Which classes of drugs can be used for tx of endometrial cancer

Answer 12

progestin and anti-estrogens

Question 13

which progestin is used in emergency contraceptive

Answer 13

levonorgestrel (2 doses 12 hours apart)

Question 14

Mifepristone MOA

Answer 14

Anti-Progestin; Blocks binding of progesterone to its own receptor

Question 15

Mifepristone uses

Answer 15

Uses: approved by the FDA for termination of pregnancy

Question 16

Onapristone MOA

Answer 16

Anti-Progestin; Blocks binding of progesterone to its own receptor; More pure antagonist than Mifepristone

Question 17

Clomiphene MOA

Answer 17

Anti-Estrogen; SERM w/ antagonistic action in all tissue- binds to ER-alpha & ER-beta: acts on hypothalamus blocking feedback inhibition thus stimulating GnRH release increasing LH/FSH and thus ovulation

Question 18

Copper IUD MOA

Answer 18

copper is spermicidal

Question 19

Copper IUD Tox

Answer 19

Copper may cause cramping; high initial cause

Question 20

Is fertility quickly restored after use with copper containing IUD

Answer 20

Yes

Question 21

how long is a copper IUD useful for? additional uses other than contraceptive?

Answer 21

Effective 15-20 yrs but FDA recommends 10 yrs; FDA approved for dysmenorrhea

Question 22

Androgen (4)

Answer 22

Danazol, Testosterone cypionate, Testosterone transdermal patch, Fluoxymesterone

Question 23

Non patch androgen Tox

Answer 23

Dose-related; virilizing effects on females, feminizing effects in males, suppression of LH & FSH; Decreased HDL, Increased LDL

Question 24

patch androgen tox

Answer 24

Dose-related; virilizing effects on females, feminizing effects in males, suppression of LH & FSH; Decreased HDL, Increased LDL
AND
patch can cause tearing of skin

Question 25

cypoterone acetate MOA

Answer 25

Androgen Receptor Antagonist; Competes w/ DHT for androgen receptor preventing translocation into nucleus

Question 26

Vaginal contraceptive ring MOA

Answer 26

Inserted intravaginally by patient for 3 weeks, one week off; Delivers ethinyl estradiol & progestin

Question 27

vaginal contraceptive ring Tox

Answer 27

h/a, discomfort, vaginal discharge

Question 28

vaginal contraceptive ring PK

Answer 28

Not effective until in place for 7 days; Rapid return to fertility upon removal

Question 29

testosterone cypionate PK

Answer 29

IM & LA

Question 30

Fluoxymesterone PK

Answer 30

oral & SA

Question 31

Danazol PK

Answer 31

IM & LA

Question 32

Danazol uses

Answer 32

tx of endometriosis & PMS (weakly androgenic)