Estrogen and Progestin Inhibitors Flashcards

1
Q

MOA of clomiphene

A

estrogen receptor partial agonist - blocks estrogen negative feedback

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2
Q

use of clomiphene

A

fertility drug

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3
Q

adverse effects of clomiphene

A
  • multiple births
  • hot flashes
  • ovary enlargement
  • blurry vision
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4
Q

fxnal consequences of SERM use

A

bone - suppress resoprtion

endometrium - proliferation

pituitary - hot flashes

breast - inhibit proliferation

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5
Q

Tamoxifen MOA

A
  • agonist: bone
  • partial agonist: endometrium
  • antagonist: breast/HPG axis
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6
Q

what is Tamoxifen used for

A

ER+ Breast CA

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7
Q

adverse effects of tamoxifen

A
  • hot flashes
  • endometrial CA
  • nausea, vomiting
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8
Q

what drugs are SERM

A

tamoxifen

raloxifene

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9
Q

MOA of raloxifene

A

agonist: bone
antagonist: breast/uterus/HPG axis

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10
Q

use for raloxifene

A

CA

postmenopausal bone loss

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11
Q

SE of raloxifene

A
  • hot flashes

- N&V

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12
Q

what drug inhibit estrogen by inhibit gonadal function

A

danazol

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13
Q

what is danazol used for

A
  • endometriosis

- breast fibrocystic disease

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14
Q

SE of danazol

A
  • weight gain
  • edema
  • oily skin
  • acne
  • hirsutism
  • hot flashes

danazol metabolite (ethisterone) has mild androgenic effects

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15
Q

which drug inhibits estrogen by inhibiting aromatase

A

anastrazole

letrozole

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16
Q

what is anastrazole and letrozole used for

A

breast cancer

17
Q

SE of anastrazole and letrozole

A
  • GI distrubance
  • hot flashes
  • lethargy
18
Q

what drug is an antiprogesterone (progesterone receptor modulator)?

A

Abortifacient

e.g. Mifepristone

19
Q

what drug is an antiprogesterone (progesterone receptor modulator) that acts as a partial agonist?

A

Emergency contraceptive

Ulipristal

20
Q

dosing for mifepristone?

A

less than 7 weeks gestation:
1st dose of mifepristone

2nd dose of misoprostol 48 hours later

21
Q

Ulipristal can be used as an emergency contraceptive up to ___ days after intercourse

A

5

22
Q

MOA of antiprogesterones

A
  1. inhibit progesterone receptors
  2. uterine contractions
  3. lining of uterus is shed
  4. opens cervix
23
Q

Anti-progesterones other potential clinical uses:

1: disrupt ovulation

Tx 2 and 3 cancer

Induce delivery after 4

induce 5 at end of 3rd trimester

A
  1. contraceptive
  2. breast
  3. endometrial
  4. fetal death
  5. labor