MHT and SERMs & TSECs (Segars)

Question 1

the primary therapy for menopausal symptoms is ___

Answer 1

estrogen…w/without the addition of progestin

Question 2

what should women with an intact uterus taking estrogen as primary therapy for menopausal symptoms must take in addition to the estrogen?

Answer 2

progestin –> endometrial hyperplasia and carcinoma possible d/t unopposed proliferation for prolonged duration

Question 3

list some available Estrogens for menopausal HT:

Answer 3

estradiol
conjugated estrogens
esterified estrogens
estropipate

Question 4

list some available Progestinic components available for menopausal HT:

Answer 4

medroxyprogesterone
methyltestosterone
progesterone

progestins oppose estrogens effects

Question 5

what happens to cholesterol, anti-thrombin III, and osteoclastic activity with the use of Estrogen-only HT?

Answer 5

they all decrease

Question 6

what happens to TG’s & HDL-C, clotting factors, platelet aggregation, Na/fluid retention, and TBG with the use of Estrogen-only HT?

Answer 6

they all increase

Question 7

benefits with the use of oral estrogen and progestin in postmenopausal women compared with no tx?

Answer 7

decrease in total fractures/hip fractures

Question 8

harms associated with use of oral estrogen and progestin in postmenopausal women compared with no tx?

Answer 8

• stroke
• DVT
• PE
• invasive breast cancer
• GB disease
• Dementia
• self-reported urinary incontinence

Question 9

benefits with the use of unopposed oral estrogen in postmenopausal women without a uterus compared with no tx?

Answer 9

• decrease in invasive breast cancer incidence
• decrease in breast cancer deaths
• decrease in total/hip fractures

Question 10

harms associated with the use of unopposed oral estrogen in postmenopausal women without a uterus compared with no tx?

Answer 10

• stroke
• DVT
• GB disease
• self-reported urinary incontinence

Question 11

what is the summary message from the findings of the WHI regarding MHT?

Answer 11

MHT very effectively minimizes/treats vasomotor symptoms and vaginal changes (and their associated complications)

-MHT should NOT be used to prevent CVD or dementia

Question 12

take home messages for MHT use if therapy is needed for moderate-severe vasomotor symptoms?

Answer 12

• use lowest dose possible to control symptoms

- tx for shortest duration possible and instinctively re-evaluate at least yearly for ongoing therapy need

Question 13

name a SERM drug that we need to know:

Answer 13

Ospemifene

Question 14

name a TSEC drug that we need to know:

Answer 14

Bazedoxifene

Question 15

indications for Ospemifene (SERM)?

Answer 15

tx of moderate-to-severe DYSPAREUNIA (painful intercourse) –> a symptom of vulvar and vaginal atrophy of menopause

Question 16

MOA of Ospemifene?

Answer 16

functions as an estrogen agonist by binding to ERs in vagina, but also anti-estrogenic on breast

increases superficial cell growth, increases vag secretions, decrease vag pH, reduces pain/discomfort during sex

Question 17

contraindications for Ospemifene?

Answer 17

• unusual/abnormal vag bleeding
• thromboembolic diseases
• estrogen-related neoplasias

Question 18

Bazedoxifene indications?

Answer 18

• 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

-For women with intact uterus

Question 19

MOA of Bazedoxifene?

Answer 19

antagonistic activity in endometrium (replaces progestin-concept in women with an intact uterus) and in breast tissue; but also estrogenic (agonist) physioogical effects, esp in bone (d/t CE component)

Question 20

side effects of Bazedoxifene?

Answer 20

• all estrogen-related effects (d/t CE component)

- Bazedoxifene specific: potential of worsening hot flashes/sweating

Question 21

contraindications of Bazedoxifene?

Answer 21

in all situations estrogens are contraindicated (d/t CE component)