MHT and SERMs & TSECs (Segars) Flashcards
the primary therapy for menopausal symptoms is ___
estrogen…w/without the addition of progestin
what should women with an intact uterus taking estrogen as primary therapy for menopausal symptoms must take in addition to the estrogen?
progestin –> endometrial hyperplasia and carcinoma possible d/t unopposed proliferation for prolonged duration
list some available Estrogens for menopausal HT:
estradiol
conjugated estrogens
esterified estrogens
estropipate
list some available Progestinic components available for menopausal HT:
medroxyprogesterone
methyltestosterone
progesterone
progestins oppose estrogens effects
what happens to cholesterol, anti-thrombin III, and osteoclastic activity with the use of Estrogen-only HT?
they all decrease
what happens to TG’s & HDL-C, clotting factors, platelet aggregation, Na/fluid retention, and TBG with the use of Estrogen-only HT?
they all increase
benefits with the use of oral estrogen and progestin in postmenopausal women compared with no tx?
decrease in total fractures/hip fractures
harms associated with use of oral estrogen and progestin in postmenopausal women compared with no tx?
- stroke
- DVT
- PE
- invasive breast cancer
- GB disease
- Dementia
- self-reported urinary incontinence
benefits with the use of unopposed oral estrogen in postmenopausal women without a uterus compared with no tx?
- decrease in invasive breast cancer incidence
- decrease in breast cancer deaths
- decrease in total/hip fractures
harms associated with the use of unopposed oral estrogen in postmenopausal women without a uterus compared with no tx?
- stroke
- DVT
- GB disease
- self-reported urinary incontinence
what is the summary message from the findings of the WHI regarding MHT?
MHT very effectively minimizes/treats vasomotor symptoms and vaginal changes (and their associated complications)
-MHT should NOT be used to prevent CVD or dementia
take home messages for MHT use if therapy is needed for moderate-severe vasomotor symptoms?
- use lowest dose possible to control symptoms
- tx for shortest duration possible and instinctively re-evaluate at least yearly for ongoing therapy need
name a SERM drug that we need to know:
Ospemifene
name a TSEC drug that we need to know:
Bazedoxifene
indications for Ospemifene (SERM)?
tx of moderate-to-severe DYSPAREUNIA (painful intercourse) –> a symptom of vulvar and vaginal atrophy of menopause
MOA of Ospemifene?
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
contraindications for Ospemifene?
- unusual/abnormal vag bleeding
- thromboembolic diseases
- estrogen-related neoplasias
Bazedoxifene indications?
- 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
MOA of Bazedoxifene?
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)
side effects of Bazedoxifene?
- all estrogen-related effects (d/t CE component)
- Bazedoxifene specific: potential of worsening hot flashes/sweating
contraindications of Bazedoxifene?
in all situations estrogens are contraindicated (d/t CE component)
