Estrogen & Progestin Inhibitors

Question 1

clomiphene

Answer 1

MOA: estrogen receptor partial agonist

Rx: fertility drug

SE: multiple births (ovulation) / hot flashes (↑ LH + FSH)

Question 2

tamoxifen

Answer 2

Selective Estrogen Receptor Modulator

Rx: Estrogen Receptor+ Breast Cancer

Agonist: bone
partial agonist: endometrium
Antagonist: breast / HPG axis

SE: hot flashes / endometrial CA / N/V

Question 3

raloxifene

Answer 3

Selective Estrogen Receptor Modulator

Rx: Cancer / Postmenopausal bone loss

Agonist: bone
Antagonist: breast / uterine / HPG axis

SE: hot flashes / N/V

Question 4

danazol

Answer 4

Estrogen Inhibitor
Rx: endometriosis / breast fibrocystic dz

MOA: inhibit gonadal function

SE: ↑ weight / edema / oily skin + acne (agonist activity on androgens) / hirsutism / hotflashes

Question 5

Anastrozole

Answer 5

Estrogen Inhibitor
Rx: Breast CA

MOA: aromatase inhibitor (no transformation into estrogen)

SE: GI / hot flashes /lethargy

Question 6

letrozole

Answer 6

Estrogen Inhibitor
Rx: Breast CA

MOA: aromatase inhibitor (no transformation into estrogen)

SE: GI / hot flashes /lethargy

Question 7

Mifepristone

Answer 7

Abortifacient (RU 486)

MOA: progesterone antagonist (blocks transcription)

1st: mifepristone
2nd: misoprostol 48 hrs later

Question 8

Ulipristal

Answer 8

“Emergency” Contraceptive

MOA: Progesterone partial agonist

Used up to 5 days after intercourse

Question 9

Anti-progesterones Mechanisms of Action

Answer 9

Inhibit progesterone receptors

Uterine Contractions

Shedding of uterus lining

opens cervix