Estrogen and Progesterone Inhibitors and Antagonists

Question 1

What is Tamoxifen(Nolvadex)?

What is it used for?

Answer 1

a non steroidal SERMS. A partial agonist/antagonist at the estrogen receptor

Used for palliative care of BC patients and as chemoprevention of BC. After 5 years it loses its effectiveness and might even CAUSE uterine cancers.

Question 2

SERMS stands for…?

Answer 2

selective estrogen receptor modulators

Question 3

Name 3 SERMS:

Answer 3

1 Tamoxifen (Nolvadex)

2 Toremifene (Fareston)

3 Roloxifene (Avista)

Question 4

What is Toremifene (Fareston)?

What is it used for?

Answer 4

a non steroidal SERMS. A partial agonist/antagonist at the estrogen receptor

Used for palliative care of BC patients and as chemoprevention of BC. After 5 years it loses its effectiveness and might even CAUSE uterine cancers.

Question 5

What is Roloxifene (Avista) used for?

How does it work?

Answer 5

Approved for postmenopausal osteoporosis.

It is a SERM that has positive effects of bone and lipids however it does NOT stimulate breast and endometrial tissue.

Question 6

Name an ovulation inducing agent

Answer 6

Clomiphene (Clomid, Serophene, milophene)

Question 7

What is Clomiphene (Clomid)?

What is it used for?

Answer 7

An ovulation inducing agent that works as a partial agonist/antagonist thus inhibiting ER in the hypothalamus causing increased release of GnRH> FSH & LH.

Used to induce ovulation in anovulatory women.

Question 8

Describe Mifepristone (RU486):

Answer 8

a 19-norsteroid that is a progesterone receptor antagonist

Question 9

What properties does Mifepristone (RU486) have that can terminate pregnancy?

Answer 9

Luteolytic properties

Question 10

What are 2 uses for Mifepristone (RU486)?

Answer 10

as a post-coital contraceptive/abortifacient

treating Cushing’s syndrome (glucocorticoid receptor antagonist)

Question 11

What doses of Mifepristone (RU486) + misoprostal terminate pregnancy?

How effective is it?

Answer 11

Mifepristone- 800 mg/d for 2 days
misoprostol- 600 mg

> 95% within the first 7 weeks

Question 12

AE’s of Mifepristone?

Answer 12

V/D/abdominal and pelvic pain

in 5% of patients vaginal bleeding might require intervention! (thus only given by physician)

Question 13

What is Lilopristone (ZK 98734)?

Answer 13

experimental drug similar to mifepristone

Question 14

What drug is used for treating endometriosis?

Answer 14

Danazol (Danocrine)

Question 15

How does Danazol work?

Answer 15

Inhibits mid-cycle surge of FSH and LH

Question 16

What receptor(s) does Danazol bind to?

Answer 16

androgen, glucocorticoid and progesterone receptors.

Question 17

Danazol is CI’ed in which patients?

Answer 17

Pregnant (teratogenic)

Liver disease patients

Question 18

What is a negative side effect of Danazol?

Answer 18

hirsuitism (boosted androgenic effects)

Question 19

What 4 drugs can be given to inhibit aromatase in patients with tamoxifen resistance BC?

Answer 19

Anastrozole (Arimidex)

letrozole (Femara)

Exemestane (Aromasin)

Fadrozole (Afema)

Question 20

How does Anastrozole (Arimidex) and letrozole (Femara) work?

Answer 20

non steroidal selective inhibitors of aromatase that treat tamoxifen resistant BC

Question 21

What is Exemestane (Aromasin) and what is it used for?

Answer 21

a steroid molecule that irreversibly inhibits aromatase.

Used to treat advanced BC.

Question 22

Fadrozole (Afema)… what up with this shit?

Answer 22

New oral nonsteroidal aromatast inhibitor or some shit man idk.