Menopausal Hormone Therapy; Selective Estrogen Modulators and Tissue Selective Estrogen Complexes

Question 1

what are the symptoms of menopause

Answer 1

hot flashes, night sweats, vaginal dryness (painful intercourse) , sleep disturbances, mood disorders, urinary incontinence

anybody who wants MHT needs 1 or more of these signs

Question 2

what disorders have an increased prevelance in menopause

Answer 2

cardiovascular effects (ACS, MI)

bone effects (osteoporosis, osteopenia)

when a premenopausal/menopausal patient presents to you, you should be asking about these things

Question 3

the primary therapy for menopausal symptoms is _

Answer 3

estrogen

with or without the addition of progestin

Question 4

women with an intact uterus must also be on a _ along with the estrogen)

Answer 4

progestin

Question 5

why do women with an intact uterus going through menopause need to be on both estrogen and progestin?

Answer 5

because unapposed estrogen increases the risk of endometrial hyperplasia/carcinoma

Question 6

pharmacotherapy during peri-menopause can also commonly consist og _ therapy

Answer 6

combinedation hormonal contraceptives

Question 7

combined hormone contraceptive therapy provides _ regulation and _ protection

Answer 7

hormone regulation

pregnancy protection

Question 8

available formed of estrogen (4)

Answer 8

1. estradiol
2. conjugated estrogens
3. esterified estrogens
4. estropipate

Question 9

estradiol is in _ form in the tablet/vaginal ring and _ form in the injectable version

Answer 9

acetate

cypionate

Question 10

conjugated estrogens are a blend of many _ derivatives that are derived from estrogens found in the _

Answer 10

estrogen

urine

Question 11

esterified estrogens are a combination of _ and _

Answer 11

Na+ estrone sulfate (majority)

Na+ equillin sulfate (minority)

Question 12

estropipate is a cyrstalline estrone solubilized sulfate and stabilized with?

Answer 12

piperazine

Question 13

progesting _ (enhance/oppose) estrogen effects

Answer 13

oppose

Question 14

what are the avaibale progestenic components

Answer 14

medroxyprogesterone MPA

methytestosterone

Progesterone

Question 15

medroxyprogesterone MPA is given with what estrogen?

Answer 15

CE: conjugated estrogens

Question 16

methyltestosterone is given with what estrogen?

Answer 16

EE: esterified estrogens

Question 17

what is the MOA of exogenous estrogen?

Answer 17

bind to the estrogen receptors in various tissues and is transferred to the nucleus which results in increase gene and protein expression that give the physiological responses of estrogen

Question 18

estrogen effect on the endometrium

Answer 18

proliferation

increased risk of hyperplasia and carcinoma this is why this is not given alone in someone who still has their uterus

Question 19

estrogen effects on lab results:

cholesterol
antithrombin III
osteoclastic bone activity
triglycerides
clooting factoris
platelet aggregation
sodium/fluid retention
thyroid binding TBG

Answer 19

estrogen will work to decrease cholesterol LDL/TC (this is good)

it will decrease antithrombin III activity (break up a clot)

will decrease osteoclastic acivity

will increase HDL and triglycerides (good)

will increase clotting factors and platelet aggregation (higher chance of clotting-not good)

increase sodium and fluid rentention (bloating and puffy)

increase thyroid binding globulin (TBG)

Question 20

womens health initiative study said that MHTs are benifical or preventative effects are on ? and risks of various _

Answer 20

preventative effects on heart disease, osteoposis related fractures

risk of various cancers though

Question 21

what are the benefits of both combined MHT and estrogen only MHT (people with no uterus)

Answer 21

benefits are a decrease in diabetes and fractures

Question 22

what is a benefit singular to combined MHT (estrogen and progestin in a patient with a uterus)

Answer 22

decerase in colorectal cancer

Question 23

what is a benefit to just estrogen MHT

Answer 23

decrease in invasive breast cancer

Question 24

what are some harms associated with both combination MHT and estrogen only MHT

Answer 24

dementia
gall bladder disease
stroke
VTE
urinary incontience

Question 25

what are some harms associated with just combined MHT

Answer 25

increased risk of breast cancer (invasive) and increased risk of coronoary heart disease

Question 26

MHT very effectively minimizes/treates _ symptoms and _ changes

Answer 26

vasomotor symptoms and vaginal changes

Question 27

MHT should not be used to prevent _ or _

Answer 27

CVD or dementia

Question 28

MHT benefit on bone and colon cancer are outweighed by _

Answer 28

all the other risks

Question 29

for younger women with menopausal symptoms can you give them MHT?

Answer 29

yes, it can treat troubling menopausal symptoms in the relatively young and within 10 years of menopause you can individualize this to your patients they dont have to be on it forevere start with patch over oral therapy

Question 30

for women with vaginal symptoms only the preffered treatment is?

Answer 30

low dose vaginal estrogen topicals

Question 31

both estrogen alone therapy and estrogen with progestin increases risk of _

Answer 31

blood clots ## Footnote counsel your patients

Question 32

alhtough risks of blood clots and stroke increase with either MHT, risk is less in _ year old age group

Answer 32

50-59 year old

Question 33

there is an increased risk of _ cancer seen within 2-4 uears of continuous estrogen with progestin therapy

Answer 33

breast ## Footnote for women at risk for breast cancer, maybe shouldnt give them this

Question 34

MHT take home messages use the _ (lowest/highest) dose possible to control symptoms treat for the _ (shortest/longest) duration possible and re-evaluate at least yearly )

Answer 34

lowest shortest | make sure you document everything ## Footnote risks and benefits of MHT are essentially eliminated several years after MHT is stopped

Question 35

what are SERMS

Answer 35

selective estrogen receptor modulators

Question 36

what is the goal of a SERM

Answer 36

to be proestrogenic at select tissues like the bone, vagina, and hotflashes but to be anti estrogenic at other sites like the breast or the endometrium

Question 37

whar are TSECS

Answer 37

tissue selective estrogen complexes

Question 38

what is the goal of TSECs

Answer 38

to combine the unique elements of a SERM with an estrogen compound

Question 39

SERMs are replacing progestin actions of traditional progestin- inclusive

Answer 39

MHT

Question 40

what are the SERMs we need to know?

Answer 40

ospemifene clomiphene

Question 41

what is a TSEC we need to know about?

Answer 41

Bazedoxifene this is a combo with conjugated estrogen and selective receptor modulator ## Footnote not available in a single ingredient compound

Question 42

OSpemifene indications (serm)

Answer 42

dypareunia (symptom of menopause due to vaginal atropy) vaginal dryness ## Footnote if vaginal dryness is the only issue maybe just topical

Question 43

MOA of ospemifene (SERM)

Answer 43

functions as an estrogen agonist by binding to ER in the vagina but anti- estrogenic at the breast increases vaginal secretions, decreases vaginal pH, reduces pain during intercourse, increase superifical cell growth

Question 44

side effects of ospemifene

Answer 44

hot flashes, estrogenic effects of coagulation/endometrial thickening and hyperplasia

Question 45

contrainications of ospemifene

Answer 45

AUB, thromboembolic events, estrogen related neoplasia

Question 46

bazedoxifen is used in women with a _ uterus

Answer 46

intact

Question 47

bazedoxifence with a conjugate estrogen is used for?

Answer 47

menopausal symptoms in women with a uterus prevention of post menopausal osteoporosis in women with a uterus

Question 48

MOA of bazedoxifene (TSEC)

Answer 48

antagonistic affect in the endometrium (prelaces the progestin concept in tradiational MHT) and in breast tissue agonist/estrogenic physioloigcal effect in bone does not stimulate endometrial proliferation destroys HER2 malignant cells

Question 49

TSECS with Conjugated estrogen have replaced what

Answer 49

traditional MHT therapy with progestin this is because they are anti-estrogenic at the places where unapposed estrogen could create problems ## Footnote less vaginal bleeding compared to progestin therapy

Question 50

side effects of bazedoxifene

Answer 50

all estrogen related side effects: DVT, dementia, stoke, gall bladder disease, urinary incontinence specific: worsening of hot flashes contraindicated in all estrogen situations

Question 51

what is clomiphene

Answer 51

an anti estrogen SERM that is used in infertility and anovulatory women, irregular ovulation, luteal phase defects, PCOS used in infertility !

Question 52

MOA of clomiphene

Answer 52

blocks inhibitory/negative feedback actions of estrogen oon the hypothalamus preventing estrogen from lowering GNRH on the pituitary gonadotropin release (LH and FSH) increases gonadotropin (LH and FSH) secretion to help stimulate ovaries to develop oocyte follicles ## Footnote given orally between cycle days 5 and 9

Question 53

side effects of clomiphene used in infertility

Answer 53

1. multiple gestations 2. ovarian cysts 3. hot flashes 4. luteal-phase dysfunction (inadequate progesterone production)