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ER Week 4 > Female Reproductive Pharmacology > Flashcards

Female Reproductive Pharmacology Flashcards

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1
Q

For women who have hypohtalamic anovulatory function, what should you give with daily injections?

A

FSH and LH

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2
Q

What will injections of FSH and LH on days 2-3 of menstrual cycle do in normal ovulatory women?

A

superovulation

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3
Q

For women with endogenous estrogen activity and normal hypothalamic pituitary-ovarian junction, you can use what drug to antagonist estrogen in order to induce FSH secretion?

A

clomiphene citrate

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4
Q

In all these cases, what do you give IM or SC when the follicle reaches 1.8-2.0 cm?

A

hCG

and sometimes progesterone

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5
Q

What are the two drugs that are urinary derived human gonadotropins pooled from postmenopausal women, concentrate and purified?

A

menotropin (both FSH and LH)

urofolitropin (FSH activity)

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6
Q

Who gets menotropin?

A

anovulatory women

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7
Q

Who gets urofolitropin?

A

women with polycystic ovarian disease

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8
Q

Recombinant human gonadotrpoins are also available - what are they?

A

follitropin A

follitropin B

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9
Q

What are the main gonadotropin stimulator side effects?

A
  1. hyperstimulation with multiple fetuses

ovarian hyperstimulation syndrome

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10
Q

Describe ovarian hyperstimulation syndrome

A

shift of vascular fluids to abdominal and thoracic cavities

usually mild symptoms, but occasionally severe.

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11
Q

What is clomiphene citrate

A

estrogen antagonist in hypothalamus

a SERM - nonsetoirdal selecive estrogen receptor modulator

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12
Q

What does climiphene citrate stimulate then?

A

release of GnRH and gonadotropins

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13
Q

It’s used as a fertility drug - about what percentage of patients will ovulate and what percentage will become pregnany?

A

80% of anovulatory women will ovulate

35% will become pregnant

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14
Q

What are the toxicities for clomiphene citrate?

A

hot flashes

ovarian hyperstimulatory syndrome

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15
Q

What is the 2-step ovulation induction?

A
  1. follicular stimulation using FSH, FSH and LH or clomiphene
  2. folow with hCG to stimulate the LH surge
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16
Q

WHat is the name of recombinant hCG?

A

choriogonadotropin alpha

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17
Q

What does hCG do in this context?

A
  1. binds to LH receptor to have LH-like induction of ovulation
  2. sitmulates estrogen primed follicle to induce meiotic resumption of oocytes
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18
Q

What is the synthetic GnRH we should know?

A

Leuprolide

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19
Q

Leuprolide given in nonpulsatile administration leads to what?

A

suppression of FSH and LH after an initial transient rise

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20
Q

What are the three reasons to give leuprolide?

A
  1. to hust down HPO and paired with a FSH/LH or clomiphene to stimulate follicle production
  2. For reducing symptoms of uterine fibroids (including bleeding)
  3. For controlling hormone dependent prostate and breast cancers
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21
Q

Pulsatile administration of leuprolide will cause what?

A

release of FSH and LH - used to induce follicle development

just mimics the normal axis

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22
Q

What are the two GnRH antagonists?

A

Ganirelix

Cetrorelix

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23
Q

What do Ganirelix and Cetrorelix do to gonadotropin release?

A

they anatonize GnRH, so they decrease LH/FSH secretion

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24
Q

Why are the GnRH antagonists used in fertility?

A

they prevent the endogenous LH surge, while promoting folliculogenesis with exogenous gonadotropins (used to suppress the woman’s own system if it’s not working and replace it with synthetic hormones)

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25
Q

Why are GnRH antagonists used in prostate an dbreast cancer?

A

inhibit steroid production

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26
Q

So if GnRH antagonists and continuous use of the GnRH agonists both cause decreased FSH/LH secreiton, what’s the difference?

A

you don’t see the transient increase in FSH/LH with the GnRH antagonists

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27
Q

What are the three natural estrogens?

A

17beta estradiol (E2) - this is prominent
estrone (E1)
estriol (E3)

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28
Q

What are the general effects of estrogen?

A

development, growth and maintenance of sex accessary tissue

skeletal growth and development of body shape (help the epiphyseal growth plates close - mutation makes you tall)

key regulator of the HPO axis and therefore in maintaining the menstrual cycle

29
Q

What are the metabolic effects on estrogen?

A

sodim and water retention

increase in HDL and decreased LDL (heart protective)

30
Q

What are the main uses of estrogen?

A
  1. oral contraceptives (usually with progestins)

2. Hormone replacement therapy

31
Q

Estradiol 17b is the prinicpal natural hormone, what do we add to reduce metabolism and make orally active in a medication? What is this called?

A

OH at C17

this is ethinyl estradiol

32
Q

What are the 4 general routes of admission?

A

injeciton
transdermal patch
topical gel
vaginal ring

33
Q

How is ethinl estradiol metaolized?

A

mby the liver, excreted in kidney or bile

34
Q

Circulating estradiol is bound to what?

A

steroid hormone binding globulin

35
Q

Clomiphene citrate is a SERM. Is it an antagonist or agonist at the level of the hypothalmus

A

antagonist

36
Q

What is clomiphene citrate used for?

A
  1. ovulatory dysfunction in patients who are not pregnant
  2. polycystic ovarian syndrome
  3. amenorrhea
37
Q

What are the side effects of clomiphene citrate?

A

nausea, vomiting, skin rashes
hot flashes
thromboembolic events (esp those who smoke)
endometrial cancer

38
Q

What is Tamoxifen?

A

also a selective estrogen receptor modulator

39
Q

Where is tamosifen an anatonist?

A

breast and vasculature

40
Q

Where is tamoxifen an agonist? good or bad

A

uterus (bad - endometriosis)

bone (good - less osteoporotsis)

41
Q

What additional thing do we use tamoxifen fo?

A

treatment and prevention so festrogen positive breast cancers

42
Q

What are two other SERMs?

A

Raloxifene

Toremifene

43
Q

Where is Raloxifene an agonist and why is it better than Tamosifen?

A

agonist in bone and lipoprotein (good), but not in the uterus - which is why it’s sometimes preferred to tamoxifen

44
Q

WHat is the selective estrogen receptor down regulator?

A

Fulvestrant

45
Q

What are the side effects of fulvestrant?

A

GI disturbances
hot flashes
thromboembolism

46
Q

How is fulvestrant administered?

A

IM injection once a month - helpful for compliance

47
Q

What are the three aromatase inhibitors we know?

A

anastrozole
letrozole
exemestane

48
Q

What are the two nonsteroidals? Reversible?

A

anastrozole
letrozole

are reversible

49
Q

Which one is a steroid? Reversible?

A

exemesate is steroidal, not reversible

50
Q

WHat are the aromatase inhibitors used for?

A

treat ER+ cancer in postmenopausal women

this is because in postmenopausal women, most estrogen is not made in the ovaries, it’s made by aromatase in the periphery

51
Q

What are the actions of progesterone?

A

development and maintenance of secretory endometrium

promotes uterine relaxation during pregnanty - withdrawn during late pregnancy

prepares breast for lactation

52
Q

What are the receptors for progesterone?

A

PR-A ad PR-B

53
Q

What are the main uses for synthetic progestins?

A
  1. OCPs
  2. Hormone replacement
  3. Treatment of dysmenorrhea
  4. Luteal support for impoanation and pregnancy
  5. As plan B to interfere with ovulation
54
Q

What is the natural progestin?

A

progesterone C21

55
Q

What synthesizes progesteron?

A

Corpus luteum
placenta
testes and adrenal

56
Q

What are the three progestins we should know for her?

A

medroxyprogesterone acetate
Norethindrone
Levonorgestrel

57
Q

Which is the progestane?

A

medroxyprogesterone acetate

58
Q

Whish is the estrane?

A

norethindrone

59
Q

Which is the gonane?

A

levonorgestrel

60
Q

Progestins are absorbed readily, but significantly metabolized in first pass. What will retard this?

A

17C substitutions

61
Q

THey are metabolized and conjugated in the liver and excreted ….

A

by kidney and bile

62
Q

Progesterone will bind to what in the serum

A

cortisol binding globulin

63
Q

How about 19-nor progestins?

A

steroid hormone binding globulin

64
Q

What are the two treatment modality for emergency contraception and abortefacient?

A

progesterone agonist: levonogestrel

Progesterone antagonist: mifepristone and ulpristal acetate

65
Q

What is the plan B progestin?

A

levonogestrel

66
Q

Can plan B terminate a pregnancy?

A

no - high dose progestin is required to maintain a pregnancy

67
Q

What is Ella?

A

ulipristal - efficacy upt o 5 days

68
Q

What is mifepristone?

A

it’s a weak anti-progesterone; a 19-nortestosterone analog which is used as emergency contraception or abortifacent

ER Week 4 (15 decks)

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