Pharm 1b

Question 1

whats a SERM? TSEC?

Answer 1

Selective estrogen receptor modulators, Tissue-selective estrogen complexes

Question 2

SERM goal?

Answer 2

Beneficial pro-estrogenic actions in select tissues with beneficial anti-estrogenic actions in other tissues

Question 3

TSEC goal?

Answer 3

combines unique elements of a SERM with an estrogen compound

Question 4

SERMS names? (2 important ones)

Answer 4

Ospemifene, Clomiphene (-ifine sound at end)

Question 5

TSEC name?

Answer 5

Bazedoxifene

Question 6

Ospemifine used for?

Answer 6

mod/severe dyspareunia (painful intercourse) symptom of vulvar and vaginal atrophy of menopause

Question 7

Ospemifene MOA?

Answer 7

Agonist by binding to ERs in vagina but also anti- estrogenic on breast. Increases cell growth vagina increasing secretions and decreasing vaginal pH, reduce pain/discomfort during intercourse

Question 8

Ospemifene increased risk of endometrial cancer?

Answer 8

not known risk still use with caution

Question 9

Ospemifene SE?

Answer 9

worsening hot flashes/sweating
estrogenic similar effects on coagulation (less than estrogen alone)
Endometrial thickening/hyperplasia (not yet cancer)

Question 10

Ospemifene contraindications?

Answer 10

same as estrogen
unusual/abnormal vag bleeding
Thromboembolic diseases
Estrogen related neoplasias

Question 11

Bazedoxifne is complexed with? type of women? indications? 2

Answer 11

W/ CE, for women w/ intact uterus.

1. Treat mod/severe vasomotor symptoms associated with menopause in women w/ uterus
2. prevention of post-menopausal osteoporosis in women w/ uterus

Question 12

Bazedoxifne MOA

Answer 12

Antagonistic activity in endometrium and breast. agonist in bone.

Question 13

Bazedoxifine differs from SERMs and progestin how?

Answer 13

does not stimulate endometrial proliferation.
destroy HER2 malignant cells.
Less vaginal bleeding

Question 14

Bazedoxifne SE? contraindicated?

Answer 14

SE- all estrogen effects. B specific- Worsening hot flashes/ sweating. Contra- all situations estrogens are

Question 15

Anti-estrogens?

Answer 15

Clomiphene

Question 16

Clomiphene indications?

Answer 16

Infertility in anovulatory women (no menses)

Question 17

Clomiphene- MOA

Answer 17

induction of ovulation in women with: amenorrhea, PCOS, and dysfunctional bleeding with anovulatory cycles.
blocks inhib actions of estrogen on hypothalamus GnRH and pituitary gonadotropin release.

Question 18

Clomiphine dosing

Answer 18

Orally between cycle days 5 and 9

Question 19

Clomiphene SE?

Answer 19

multi births
ovarian cysts
hot flashes
luteal phase dysfunction