Menopausal Hormone Therapy (MHT) and Selective Estrogen Receptor Modulators (SERMS) Flashcards
Define menopausal transition and post menopause time intervals
- Menopausal transition (peri) - 2 skipped cycles progressing to 60+ days of amenorrhea
- Post menopause - 12 mo of complete amenorrhea
What is the primary therapy of menopausal symptoms
Estrogen
When do you give estrogen only v. E/P?
Intact uterus = must give E/P
Six available forms of estrogenic therapy
Estradiol, Conjugated estrogens (CEE), Synthetic conjugated estrogens-A, synthetic conjugated estrogens-B, esterified estrogens (EE), estroPIPate (piperazine)
**Three main forms of progestinic components for MHT
- Medroxyprogesterone (MPA), Methyltestosterone –> E/P
- Progesterone - P ONLY
Estrogen only Hormone therapy - MOA
MOA - bind to endogenous estrogen receptors in various tissues throughout body
Effect - endometrial proliferation
***Effects of estrogen-only hormone therapy
Endometrial proliferation.
- **Decreased production/activity - cholesterol, anti-thrombin 3, osteoclastic activity (bone turnover).
- **Increased production/activity - TG, clotting factors, platelet aggregation, Na/Fluid retention, TBG
Menopausal Hormone Therapy should NOT be used in people with what? Should NOT be used to prevent what?
- CVD or dementia
- Do not use to prevent: bone loss, or colon cancer
Goal of SERMs
Beneficial E-agonist actions in select tissue with anti-E antagonist action sin other tissues - bone, brain, breast, endometrium
Two main SERMs
Ospemifene, Bazedoxifene
When do you use Ospemifene?
ORAL therapy for dyspaerunia - sx of vulvar/vaginal atrophy of menopause.
MOA ospemifene
E-agonist in vagina, E-antagonist in breast
SE of ospemifene
Increase in menopause sx - hot flashes/sweating, vaginal discharge, E-effects on coagulation, endometrial hyperplasia.
CI of ospemifene
Vaginal bleeding, thromboembolic dz, estrogen-related neoplasia
Tx use for Bazedoxifene (w/CEE). Only use in what types of females.
For women with intact uterus.
Tx of moderate to severe vasomotor sx associated with menopause. Prevention of post-menopausal osteoperosis.