Segars: HRT/SERMs

Question 1

What is the cliff notes version of Menopausal hormone therapy?

Answer 1

• when she hits menopause, she stops making estrogen…

- so then we give her estrogen

Question 2

What is Menopausal transition

Answer 2

• they’re entering menopause
• peri-menopause
• increase in FSH, reduction in hormone levels and variation of cycle
• THEY CAN STILL GET PREGGO!!!

Question 3

What is not an effect of menopause?

Answer 3

-heart effects

Question 4

What do estrogens do to endometrium?

Answer 4

-makes it proliferate

Question 5

so, if there is an intact uterus, what do we give her?

Answer 5

• a progestin!

- add that along with the estrogen

Question 6

What are the four estrogens that we use?

Answer 6

• estradiol
• Conjugated estrogens
• Esterified estrogens
• Estropipate (stabilized with piperazine

Question 7

What are the available progestinic components?

Answer 7

• Medroxyprogesterone
• Methyltestosterone
• Progesterone
• dont give her this if she doesn’t have a uterus

Question 8

What is the major effect of estrogen-only hormone therapy?

Answer 8

• Decrased production of anti thrombin 3
• decreased osteoclastic activity
• Increased production of triglycerides and clotting factors

Question 9

What do we not use MHT for?

Answer 9

• bone effects
• heart attack
• anything that isn’t menopause

Question 10

What are the harms of estrogen and progestin therapy in women with uterus?

Answer 10

• stroke
• DVT
• pulmonary embolism
• Invasive breast cancer
• Gallbladder disease
• Dementia
• Self-reported urinary incontinence

Question 11

Should MHT be used to prevent CVD or dementia?

Answer 11

-no it should not

Question 12

What do we do for women who are only having vaginal symptoms?

Answer 12

-topical vaginal estrogen

Question 13

What do we include in a woman who has a uterus?

Answer 13

-progestin

Question 14

does estrogen therapy increase the risk of blood clots?

Answer 14

-yes

Question 15

What kind of cancer is a risk thing 3-5 years of continuous estrogen with progestin therapy?

Answer 15

breast cancer

Question 16

What is SERM?

Answer 16

-selective estrogen receptor modulators

Question 17

What are TSECs?

Answer 17

-tissue-selective estrogen complexes

Question 18

What is the one SERM we have to know about?

Answer 18

-Ospemifene

Question 19

What is the one TSEC we need to know?

Answer 19

-Bazedoxifene

Question 20

Ospemifine

Answer 20

• SERM

- only used for tx of painful intercourse

Question 21

MOA of Ospemifine

Answer 21

• estrogen agonist… binds ERs in vagina
• but also antiestrogenic on breast
• increases vaginal secretions and what not
• Stimulatory endometrial effects

Question 22

Side effects of Ospemifene

Answer 22

• worsening of increase in hot flashes/sweating
• estrogenic-simliar effects on coagulation
• Endometrial thickening and even hyperplasia (estrogen agonist)

Question 23

When is Ospemifine contraindicated?

Answer 23

• -unusal/abnormal vaginal bleeding
• Thromboembolic diseases
• Estrogen-related neoplasia’s (uterine, ovarian, breast)

Question 24

Bazedoxifene

Answer 24

-TSEC!

Question 25

Indications for Bazedoxifene?

Answer 25

• tx of moderate to severe vasomotor symptoms associated with menopause in women with a uterus
• prevention of post-menopausal osteoporosis in women with a uterus

Question 26

Bazedoxifene MOA

Answer 26

• antagonistic activity in endometrium and breast tissue

- but also estrogenic agonist especially in bone

Question 27

Side effects of Bazedoxifene

Answer 27

• all estrogen-related effects

- Bazedoxifene-specific: has the potential of worsening hot flashes. sweating (kinda like ospemifene)

Question 28

When is Bazedoxifene contraindicated?

Answer 28

• in all situations that estrogens are!

- this is a complex with estrogen complex in it!