MHT and SERMs - Segars Flashcards
In Menopause, you simply must resupply _____
The hormones that she is now deficient in
Menopause symptoms
Hot flashes, night sweats, vaginal dryness, painful intercourse, sexual dysfunction, sleep disturbances, mood/cognition issues, urinary incontinence, reduced quality of life
Menopause causes increased prevalence of what diseases/issues?
Osteopenia/osteoporosis/fractures
ACS/MI/CVD
Primary therapy for menopause symptoms
***When must Progestin ALSO be given w/ estrogen? Why?
Estrogen
IF intact uterus – estrogen alone will cause endometrial hyperplasia and cancer
6 forms of post-menopause estrogens
Estradiol (+/- acetate, etc.) Conjugated estrogens (CEE) Synthetic conjugated estrogens - A Synthetic conjugated estrogens - B Esterified estrogens (EE) Estropipate (w/ piperazine)
3 forms of post-menopause progesterone (ONLY FOR THIS)
Medroxyprogesterone
Methyltestosterone
Progesterone
Which post-menopause progesterone can come with estrogen? Which one?
Medroxyprogesterone + CEE
Methyltestosterone + EE
Can progestins from HCs also be used in post-menopause?
YES - some of them
Are there non-oral forms of estrogen-only therapy?
Can they be used in all post-menopausal women?
YES - many
NO - only if uterus has been removed
***Estrogen-only therapy will DECREASE what lab values or physiologic processes?
These are the SAME as what?
Cholesterol (TC, LDL)
AT3
Osteoclastic activity
HC estrogens
***Estrogen-only therapy will INCREASE what lab values or physiologic processes?
These are the SAME as what?
TGs, HDL Clotting factors Platelet aggregation Na/H20 retention (wt gain) TBG levels
HC estrogens
***ANY women on estrogen-only therapy (HC or HRT) have increased risk of what serious side effects?
Estrogen-only therapy in ANY woman (HC or HRT) is contraindicated in who?
DVT/PE/MI etc.
PMHx of vascular disease or event
A woman has a FHx of osteoporosis and wants to take HRT to prevent it. She has a Hx of a previous MI. Should you prescribe the HRT?
NO
Should MHT be used to prevent CVD and dementia in post-menopausal women?
Should MHT be used to prevent/treat osteoporosis or colon cancer?
NO - worsens risk
NO - CV risks outweigh benefits
***When can MHT be used to treat moderate/severe menopausal symptoms (more than just vaginal symptoms)?
Younger than 60 or within 10 years of menopause start
***How can MHTs be used to treat vaginal symptoms ONLY post-menopause?
Topical
***Describe breast cancer risk with MHT
Increases w/ 3-5 years of continuous treatment, but returns to normal over time after stopping treatment
A post-menopausal woman free of breast/uterine cancers or CV disease has been taking HRT for hot flashes, night sweats, vaginal issues, etc. She has been taking it for 3-5 years now. What should be discussed?
Potentially cutting dose or trying to stop therapy and re-assess symptoms. SHOULD NOT BE TAKEN INDEFINITELY
MHT should ONLY be used for what?
Should NOT be used primarily for what?
Reducing hot flashes/night sweats/vaginal issues in post-menopausal women
NOT for bone disease, heart disease, or w/ concurrent cancers
Goal of SERMs
Estrogenic (agonist) effects in some tissues w/ anti-estrogenic effects (antagonist) in other tissues
Raloxifene, Tamoxifen, and Toremifene can be used for what? (NOT FOR HIS QUESTIONS)
Treating ER+ breast cancers, and potentially for osteoporosis too
Ospemifene - what is it used for (ONLY)?
What is this caused by?
SERM - used for ORAL therapy for moderate to severe dyspareunia (painful intercourse)
Vulvar/vaginal atrophy and dryness
Ospemifene - MoA
Specifically does what to the vagina?
ER agonist in vagina, ER antagonist in breast
Increases vagiinal superficial cell growth, increases vaginal secretions, decreases vaginal pH, and reduces vaginal pain/discomfort
Ospemifene - side effects
Increased hot flashes/sweating, vaginal discharge, pro-coagulation, endometrial hyperplasia
Ospemifene - contraindications
Vaginal bleeding, thromboembolic diseases, estrogen-related neoplasia (SAME AS ALL ESTROGENS)
Bazedoxifene - ingredients
Has what effect?
SERM w/ CEE (estrogen)
PROGESTIN replacement (without being
Bazedoxifine - MoA
Antagonist in endometrium (like progesterone) + estrogen agonist in bone (b/c CEE)
Bazedoxifene - uses
- Treat moderate/severe vasomotor symptoms of menopause (WITH UTERUS)
- Prevent post-menopausal osteoporosis
How does Bazedoxifene differ from other SERMs in terms of side effects?
How does Bazedoxifene differ than CEE + progestin?
No endometrial proliferation or worsened vasomotor symptoms
Less vaginal bleeding/spotting
Bazedoxifene - side effects
Estrogen-related effects:
- Hot flashes, sweating, etc.
Bazedoxifene - contraindications
Anything where estrogen is contraindicated
