Ph2010.03.12- Estrogens & Progestins

Front 1

List 3 naturally occurring estrogens by their potency

Back 1

estradiol (E2) > estrone (E1) > estriol (E3)

Front 2

Contrast synthetic steroidal and nonsteroidal estrogens

Back 2

steroidals have a cholesterol backbone

Front 3

List 3 synthetic steroidal and 3 synthetic nonsteroidal estrogens

Back 3

Front 4

Enzyme responsible for conversion of testosterone to estrogen

Back 4

aromitase

Front 5

1. primary location of estrogen receptors in cell
2. long term effect (in general)
3. short term effect (in general)

Back 5

1. nucleus

2. receptors homodimerize, bind ERE on multiple genes, affect protein synthesis

3. activate kinase systems and Ca mobility

Front 6

5 reproductive effects of estrogen

Back 6

1. primary & secondary female sex characteristics

2. puberty changes

3. neuroendo regulation of menstruation

4. endometrial growth

5. secretion of thin cervical mucous

Front 7

Source of estrogen and progesterone during the NL menstrual cycle & their effect on endometrium

Back 7

estrogen: maturing follicles in ovary, promotes endometrial prolif

progesterone: corpus luteum, maintains thickened endometrium

Front 8

Metabolic effects of estrogen:
1. cholesterol
2. blood pressure
3. thrombotic activity
4. bone
5. liver

Back 8

1. increase HDL, decrease LDL, increase bile excretion

2. increase BP via renin

3. promote thrombosis

4. decrease resorption

5. increase protein synthesis

Front 9

5 major clinical uses of estrogens

Back 9

Front 10

5 drug preparations of estrogen

Back 10

1. conjugated
2. estradiol (PO)
3. estradiol (TD)
4. ethinyl estradiol
5. DES

Front 11

7 contraindications of using estrogen preparations

Back 11

Front 12

Tamoxifen:
--indication
--MOA in breast, endometrium, bone
--6 SEs

Back 12

Front 13

Tamoxifen:
1. 2 contraindications
2. 2 tx considerations

Back 13

1. hx of DVT/PE, pregnancy

2. 4-6 increase in endometrial cancer incidence, use < 5 yrs to minimize endometrial risk

Front 14

Clomiphene:
1. 1 indication
2. MOA in hypothalamus/pituitary, ovaries
3. 4 SEs

Back 14

1. female infertility from ovulatory ds

2. estrogen antag in hypoth/pituitary (increase GnRH/FSH/LH), partial agonist in ovaries

3. thromboembolism, ovarian cysts/hypertrophy, flushing/vasomotor sxs, abd discomfort

Front 15

Clomiphene:
--6 contraindications
--1 tx consideration

Back 15

Front 16

Raloxifene:
1. indication
2. MOA in breast, uterus, bone
3. 4 SEs

Back 16

1. osteoporosis prevention/tx

2. estrogen agon in bone, antag in uterus & breast

3. retinal vascular occlusion, venous thromboembo, hot flashes, leg cramps

Front 17

Raloxifene:
1. 2 contraindications
2. 1 tx consideration

Back 17

1. preg, hx of venous thromboembo

2. decrease risk of invasive breast cancer in postmenopausal women w/ osteoporosis

Front 18

Fulvestrant:
--indication
--MOA
--5 SEs

Back 18

Front 19

Fulvestrant:
1. 1 contraindication
2. 1 tx consideration

Back 19

1. preg

2. pure estrogen antag w/ no agon activty

Front 20

4 aromatase inhibitors and their MOAs (2)

Back 20

anastrozole (compet inhib)
letrozole (compet inhib)
exemestane (irrev inhib)
formestane (irrev inhib)

Front 21

Drug indication of aromatase inhibitors

Back 21

Tx/prevention of estrogen receptor positive early-stage, locally advanced, and metastatic breast cancer

Front 22

Describe 4 physiological actions of progesterone

Back 22

1. neuroendo reg of menstrual cycle

2. induce secretory uterine endometrium (implantation)

3. thick cervical mucus

4. increase body temp

Front 23

3 clinical uses of progestins

Back 23

1. in OCPs (w/ or w/out ethinyl estradiol)

2. component of HRT in menopause

3. Rx for dys/oligomenorrhea, endometriosis, PCOS

Front 24

MOA of progestin-only contraceptives (primary & secondary)

Back 24

primary: decrease GnRH pulse frequency & GnRH responsiveness of AP

secondary: alter tubal peristalsis, endometrium, cervical mucous (thick)

Front 25

Key concept of using combined OCPs (E2 + P)

Back 25

mimic neg feedback on gonadotropin secretion in luteal phase

Front 26

Mefepristone (RU-486):
1. drug indication
2. MOA

Back 26

1. abortion (through day 49 of pregnancy)

2. blocks progesterone receptor binding

Front 27

Consequences of estrogen deficiency:
--4 early
--4 intermediate
--3 long term

Back 27

Front 28

4 major indications for female HRT

Back 28

1. vasomotor instability
2. mood changes
3. urogenital atrophy
4. osteoporosis