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ER Week 4 > Female Reproductive Pharmacology > Flashcards

Female Reproductive Pharmacology Flashcards

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
Why are GnRH antagonists used in prostate an dbreast cancer?
inhibit steroid production
26
So if GnRH antagonists and continuous use of the GnRH agonists both cause decreased FSH/LH secreiton, what's the difference?
you don't see the transient increase in FSH/LH with the GnRH antagonists
27
What are the three natural estrogens?
17beta estradiol (E2) - this is prominent estrone (E1) estriol (E3)
28
What are the general effects of estrogen?
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
What are the metabolic effects on estrogen?
sodim and water retention increase in HDL and decreased LDL (heart protective)
30
What are the main uses of estrogen?
1. oral contraceptives (usually with progestins) | 2. Hormone replacement therapy
31
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?
OH at C17 this is ethinyl estradiol
32
What are the 4 general routes of admission?
injeciton transdermal patch topical gel vaginal ring
33
How is ethinl estradiol metaolized?
mby the liver, excreted in kidney or bile
34
Circulating estradiol is bound to what?
steroid hormone binding globulin
35
Clomiphene citrate is a SERM. Is it an antagonist or agonist at the level of the hypothalmus
antagonist
36
What is clomiphene citrate used for?
1. ovulatory dysfunction in patients who are not pregnant 2. polycystic ovarian syndrome 3. amenorrhea
37
What are the side effects of clomiphene citrate?
nausea, vomiting, skin rashes hot flashes thromboembolic events (esp those who smoke) endometrial cancer
38
What is Tamoxifen?
also a selective estrogen receptor modulator
39
Where is tamosifen an anatonist?
breast and vasculature
40
Where is tamoxifen an agonist? good or bad
uterus (bad - endometriosis) bone (good - less osteoporotsis)
41
What additional thing do we use tamoxifen fo?
treatment and prevention so festrogen positive breast cancers
42
What are two other SERMs?
Raloxifene | Toremifene
43
Where is Raloxifene an agonist and why is it better than Tamosifen?
agonist in bone and lipoprotein (good), but not in the uterus - which is why it's sometimes preferred to tamoxifen
44
WHat is the selective estrogen receptor down regulator?
Fulvestrant
45
What are the side effects of fulvestrant?
GI disturbances hot flashes thromboembolism
46
How is fulvestrant administered?
IM injection once a month - helpful for compliance
47
What are the three aromatase inhibitors we know?
anastrozole letrozole exemestane
48
What are the two nonsteroidals? Reversible?
anastrozole letrozole are reversible
49
Which one is a steroid? Reversible?
exemesate is steroidal, not reversible
50
WHat are the aromatase inhibitors used for?
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
What are the actions of progesterone?
development and maintenance of secretory endometrium promotes uterine relaxation during pregnanty - withdrawn during late pregnancy prepares breast for lactation
52
What are the receptors for progesterone?
PR-A ad PR-B
53
What are the main uses for synthetic progestins?
1. OCPs 2. Hormone replacement 2. Treatment of dysmenorrhea 4. Luteal support for impoanation and pregnancy 5. As plan B to interfere with ovulation
54
What is the natural progestin?
progesterone C21
55
What synthesizes progesteron?
Corpus luteum placenta testes and adrenal
56
What are the three progestins we should know for her?
medroxyprogesterone acetate Norethindrone Levonorgestrel
57
Which is the progestane?
medroxyprogesterone acetate
58
Whish is the estrane?
norethindrone
59
Which is the gonane?
levonorgestrel
60
Progestins are absorbed readily, but significantly metabolized in first pass. What will retard this?
17C substitutions
61
THey are metabolized and conjugated in the liver and excreted ....
by kidney and bile
62
Progesterone will bind to what in the serum
cortisol binding globulin
63
How about 19-nor progestins?
steroid hormone binding globulin
64
What are the two treatment modality for emergency contraception and abortefacient?
progesterone agonist: levonogestrel Progesterone antagonist: mifepristone and ulpristal acetate
65
What is the plan B progestin?
levonogestrel
66
Can plan B terminate a pregnancy?
no - high dose progestin is required to maintain a pregnancy
67
What is Ella?
ulipristal - efficacy upt o 5 days
68
What is mifepristone?
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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