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16 Cards in this Set
- Front
- Back
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What is menopause
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- primary loss of ovarian function due to loss of response to FSH and LH
- Symptoms result from lack of estradiol |
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Why not take estrogen alone?
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- can cause uterine endometrial cancer
- this can be blocked by taking estrogen with progestin - and can cause breast cancer I believe |
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WHI
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- womens health initiative study
- showed more breast CA, heart attacks, strokes, and lund embolism |
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SERMS
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- selective estrogen receptor modulators
- tissue specidive estrogen receptor agaonists and antagonists - |
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Raloxifene
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- SERM
- approved to prevent osteoporosis - agonist - increases intestinal calcium absorption - no uterine stimulation - will decrease risk of breast CA - women still have hot flashes*** |
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SERM Mechanism
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- agosist= bind ER, recruidts other proteins that active DNA binding and gene expression
- antagonist= binds ER, BUT DOES NOT recruit ofther proteins necessary to activate DNA binding and gene expression |
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Raloxifine mechanisms
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- Agonist= increase Ca++ absorption, decrease osteoclast and bone absorption
- Antagonist= decrease breast tissue growth, and uterine growth, increase hot flashes |
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Osteoporosis is
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- a condition of skeletal fragility characterized by reduced bone mass and microarchitectural deterioration
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Disease related Osteroporosis
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- hypogonadism
- hyperparathyroidism - hyperthyroidism |
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Drug induced osteoporosis
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- corticosteroids
- thyroid replacements - CnRH agonist suppression of gonadal steroid synthesis - aromatase inhibitors (breast cancer) |
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what are bisphosphonates
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- most widely prescribed osteoporosis agents
- small organic polyphosphate compounds that potently inactivate bone resorption by osteoclasts - integrate into bone, thicken and stabilize structure |
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Name the bispohosphonates (3)
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- Aledronate- daily
- Risedronate- weekly - Ibandronate- monthly = cause few bone problems and are effective for 5 years - used for osteoporosis- both postmenopausal and glucocoritcoid induced |
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Bioavailablity of bisphosphonates
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- oral bioavailabiltiy is low and food impairs absorption
- esophageal ulceration may occur - must be taken with large quantities of water and pts shoudl remain upright - strict instructions to be followed for Alendronate |
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What two have additive effects to increase BMD in postmenopausal wome??
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- alendronate and raloxifene
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Progestins to know for course
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- Medroxy profesterone
- Progesterone - Synthetic Progestins: Norethindrone, norgestrel, desogestrel, norgestimate, drospireneone |
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Estrogens to know for course
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- conjugated estrogens
- 17B-estradiol - ethinyl estradiol - Raloxifene |
