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HRM > Female reproduction drugs > Flashcards

Female reproduction drugs Flashcards

1
Q

What is clomiphene citrate used for?

A

Clomiphene citrate promotes folliculogenesis

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2
Q

What is the MoA of clomiphene citrate?

A

Clomiphene citrate is a hypothalamic estrogen receptor antagonist

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3
Q

How does antagonizing hypothalamic estrogen receptors promote folliculogenesis?

A

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

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4
Q

What side effects are possible with clomiphene citrate?

A

Hot flashes

Ovarian hyperstimulation syndrome

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5
Q

What are menotropins used for?

A

Menotropins promote ovulation in anovulatory women and production of multiple follicles

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6
Q

What are menotropins?

A

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

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7
Q

What is usually given in sequence with menotropins? Why?

A

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

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8
Q

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

A

Urofolitropin promotes ovulation in polycystic ovarian disease patients

(unless clomiphene citrate worked)

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9
Q

What is urofolitropin?

A

Similar to menotropins…but only FSH; no LH

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10
Q

What are follitropin a and b?

A

Recombinant FSH…induces follicular development

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11
Q

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

A

Hyperstimulation –> multiple fetuses

Ovarian hyperstimulation syndrome –> shift of vascular fluids to abdominal and thoracic regions

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12
Q

What is leuprolide?

A

Leuprolide is a synthetic GnRH

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13
Q

What is leuprolide used for?

A

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

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14
Q

What is seen with leuprolide nonpulsatile administration?

A

Initially transiently increases FSH and LH…then suppresses them

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15
Q

What are cetrorelix and ganirelix?

A

Cetrorelix and ganirelix are GnRH antagonists

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16
Q

What are cetrorelix and ganirelix used for?

A

Fertility: prevent endogenous LH surge while giving exogenous gonadotropins

Prostate/breast cancer: inhibit steroid production

Benign uterine diseases (fibroids)

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17
Q

What is seen with cetrorelix and ganirelix administration?

A

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

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18
Q

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

A

Ethinyl estradiol (has a C-17 addition)

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19
Q

What are the metabolic effects of estrogen?

A

Sodium and water retention

Increases HDL and decreases LDL

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20
Q

What are some uses of estrogen?

A

Oral contraceptives
Hormone replacement therapy
Dysmenorrhea

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21
Q

How is estrogen used as an oral contraceptive?

A

In combination with progestins…interferes with LH surge and ovulation

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22
Q

What is given with estrogen for hormone replacement therapy?

A

Progesterone and estrogen are given for hormone replacement therapy

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23
Q

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

A

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

24
Q

Where is estradiol valerate metabolized? Excreted?

A

Estradiol valerate is metabolized in the liver

Conjugates are excreted in urine or bile

25
Q

What does circulating estradiol bind to?

A

SHBG binds to estradiol…estradiol increases synthesis of SHBG

26
Q

What are three Selective Estrogen Receptor Modulators (SERMs)?

A

Tamoxifen
Raloxifene
Toremifene

27
Q

Are SERMs estrogen agonists or antagonists?

A

SERMs are BOTH estrogen agonists and antagonists

28
Q

Where does tamoxifen act as an estrogen antagonist?

A

Breast

Vasculature

29
Q

Where does tamoxifen act as an estrogen agonist?

A

Uterus
Bone
Lipoproteins

30
Q

Can tamoxifen be used in premenopausal women?

A

Yes…unlike other SERMs/SERDs

31
Q

What is tamoxifen used to treat?

A

Estrogen positive breast cancer (and infertility)

32
Q

What are some potential side effects of tamoxifen?

A 
N/V
Skin rashes
Hot flashes
Thromboembolic events
Endometrial cancer
33
Q

What are some differences between tamoxifen and raloxifene?

A

Antagonist sites (R only breast and uterus)

Side effects (R only DVT and leg cramps)

34
Q

Where does toremifene work?

A

Toremifene is an estrogen antagonist in breast

35
Q

What are some potential side effects of toremifene?

A

Hot flashes
Lowers LDL
Raises HDL

36
Q

What is fulvestrant?

A

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

37
Q

What is the action of fulvestrant?

A

Fulvestrant is an estrogen antagonist in all tissues

38
Q

What is fulvestrant used for?

A

Estrogen positive breast cancer treatment

39
Q

Where is fulvestrant excreted?

A

Feces (it is oxidized and conjugated)

40
Q

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

A

Fulvestrant is given IM

The SERMs discussed are oral

41
Q

What are the potential side effects of fulvestrant?

A

GI disturbances
Hot flashes
Thromboembolism

42
Q

What aromatase inhibitors re non-steroidal and reversible?

A

Anastrozole and letrozole

43
Q

What aromatase inhibitor is steroidal and nonreversible?

A

Exemestane

44
Q

What are aromatase inhibitors used for?

A

Estrogen receptor positive cancer in postmenopausal women

45
Q

What side effects are expected with aromatase inhibitors?

A

Hot flashes

Long-term…unknown

46
Q

What are natural and synthetic progestins used for?

A

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

47
Q

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

A

Medroxyprogesterone

48
Q

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

A

Norethindrone

49
Q

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

A

Levonorgestrel (more potent)

50
Q

How do progestins work?

A

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

51
Q

What are some advantages to using progestins?

A

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

52
Q

What are some disadvantages to using progestins?

A

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
Q

What are mifepristone and ulipristal acetate?

A

Mifepristone and ulipristal acetate are progesterone antagonists

54
Q

What is mifepristone used for?

A 
Emergency contraceptive (low dose)
Termination of early pregnancy w/prostaglandin (higher dose)
55
Q

What are some side effects of mifepristone use?

A

Vomiting, diarrhea, and abdominal pain

Heavy vaginal bleeding

56
Q

What is ulipristal used for?

A

Emergency contraception

57
Q

How do progesterone antagonists work?

A

Interferes with or delays ovulation

Also alters endometrium

HRM (40 decks)

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