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Flashcards in Female reproduction drugs Deck (57):
1

What is clomiphene citrate used for?

Clomiphene citrate promotes folliculogenesis

2

What is the MoA of clomiphene citrate?

Clomiphene citrate is a hypothalamic estrogen receptor antagonist

3

How does antagonizing hypothalamic estrogen receptors promote folliculogenesis?

Estrogen works via feedback inhibition to reduce FSH levels...FSH causes follicular maturation

4

What side effects are possible with clomiphene citrate?

Hot flashes
Ovarian hyperstimulation syndrome

5

What are menotropins used for?

Menotropins promote ovulation in anovulatory women and production of multiple follicles

6

What are menotropins?

Menotropins are gonadotropins (FSH and LH) purified and concentrated from postmenopausal women's pee

7

What is usually given in sequence with menotropins? Why?

hCG is given in sequence with menotropins because it helps induce ovulation via LH-like surge

8

What drug is given to induce ovulation in women with polycystic ovarian disease?

Urofolitropin promotes ovulation in polycystic ovarian disease patients

(unless clomiphene citrate worked)

9

What is urofolitropin?

Similar to menotropins...but only FSH; no LH

10

What are follitropin a and b?

Recombinant FSH...induces follicular development

11

What side effects would be expected with follitropin a or b?

Hyperstimulation --> multiple fetuses
Ovarian hyperstimulation syndrome --> shift of vascular fluids to abdominal and thoracic regions

12

What is leuprolide?

Leuprolide is a synthetic GnRH

13

What is leuprolide used for?

Shut down HPO and paired with FSH/LH or clomiphene to stimulate follicle production

Reducing symptoms (like bleeding) of uterine fibroids

Controlling hormone dependent prostate and breast cancers

14

What is seen with leuprolide nonpulsatile administration?

Initially transiently increases FSH and LH...then suppresses them

15

What are cetrorelix and ganirelix?

Cetrorelix and ganirelix are GnRH antagonists

16

What are cetrorelix and ganirelix used for?

Fertility: prevent endogenous LH surge while giving exogenous gonadotropins

Prostate/breast cancer: inhibit steroid production

Benign uterine diseases (fibroids)

17

What is seen with cetrorelix and ganirelix administration?

Decrease in endogenous FSH and LH...NO transient rise (seen with GnRH agonist)

18

What is an orally available 17β estradiol (E2)?

Ethinyl estradiol (has a C-17 addition)

19

What are the metabolic effects of estrogen?

Sodium and water retention
Increases HDL and decreases LDL

20

What are some uses of estrogen?

Oral contraceptives
Hormone replacement therapy
Dysmenorrhea

21

How is estrogen used as an oral contraceptive?

In combination with progestins...interferes with LH surge and ovulation

22

What is given with estrogen for hormone replacement therapy?

Progesterone and estrogen are given for hormone replacement therapy

23

What form of estrogen is given as a transdermal patch, topical gel, or vaginal ring?

Estradiol valerate can be given as a patch, gel, or ring

24

Where is estradiol valerate metabolized? Excreted?

Estradiol valerate is metabolized in the liver

Conjugates are excreted in urine or bile

25

What does circulating estradiol bind to?

SHBG binds to estradiol...estradiol increases synthesis of SHBG

26

What are three Selective Estrogen Receptor Modulators (SERMs)?

Tamoxifen
Raloxifene
Toremifene

27

Are SERMs estrogen agonists or antagonists?

SERMs are BOTH estrogen agonists and antagonists

28

Where does tamoxifen act as an estrogen antagonist?

Breast
Vasculature

29

Where does tamoxifen act as an estrogen agonist?

Uterus
Bone
Lipoproteins

30

Can tamoxifen be used in premenopausal women?

Yes...unlike other SERMs/SERDs

31

What is tamoxifen used to treat?

Estrogen positive breast cancer (and infertility)

32

What are some potential side effects of tamoxifen?

N/V
Skin rashes
Hot flashes
Thromboembolic events
Endometrial cancer

33

What are some differences between tamoxifen and raloxifene?

Antagonist sites (R only breast and uterus)

Side effects (R only DVT and leg cramps)

34

Where does toremifene work?

Toremifene is an estrogen antagonist in breast

35

What are some potential side effects of toremifene?

Hot flashes
Lowers LDL
Raises HDL

36

What is fulvestrant?

Fulvestrant is a Selective Estrogen Receptor Down-regulator (SERD)

37

What is the action of fulvestrant?

Fulvestrant is an estrogen antagonist in all tissues

38

What is fulvestrant used for?

Estrogen positive breast cancer treatment

39

Where is fulvestrant excreted?

Feces (it is oxidized and conjugated)

40

What is a major (very broad sense) difference between fulvestrant and the SERMs?

Fulvestrant is given IM
The SERMs discussed are oral

41

What are the potential side effects of fulvestrant?

GI disturbances
Hot flashes
Thromboembolism

42

What aromatase inhibitors re non-steroidal and reversible?

Anastrozole and letrozole

43

What aromatase inhibitor is steroidal and nonreversible?

Exemestane

44

What are aromatase inhibitors used for?

Estrogen receptor positive cancer in postmenopausal women

45

What side effects are expected with aromatase inhibitors?

Hot flashes
Long-term...unknown

46

What are natural and synthetic progestins used for?

Oral contraceptives
Hormone replacement therapy
Treatment of dysmenorrhea
Luteal support for implantation and pregnancy

47

There are three types of synthetic progestins; progestanes, estranes, and gonanes. What is an example of a progestane?

Medroxyprogesterone

48

There are three types of synthetic progestins; progestanes, estranes, and gonanes. What is an example of an estrane?

Norethindrone

49

There are three types of synthetic progestins; progestanes, estranes, and gonanes. What is an example of a gonane?

Levonorgestrel (more potent)

50

How do progestins work?

Progesterone suppresses ovulation (likely via feedback inhibition of HPO/HPG axes)

51

What are some advantages to using progestins?

Reliable contraception
Decrease risk of endometrial and ovarian cancer
Decrease incidence of ectopic pregnancy
Menses regulation

52

What are some disadvantages to using progestins?

Daily administration
No STD protection
Increased risk of breast cancer with triphasic oral E & P
Other side effects (depression, wt. gain, nausea, HTN, DVT)

53

What are mifepristone and ulipristal acetate?

Mifepristone and ulipristal acetate are progesterone antagonists

54

What is mifepristone used for?

Emergency contraceptive (low dose)
Termination of early pregnancy w/prostaglandin (higher dose)

55

What are some side effects of mifepristone use?

Vomiting, diarrhea, and abdominal pain
Heavy vaginal bleeding

56

What is ulipristal used for?

Emergency contraception

57

How do progesterone antagonists work?

Interferes with or delays ovulation
Also alters endometrium