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42 Cards in this Set
- Front
- Back
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Which component of estrogen is required for high affinity binding with the estrogen receptor?
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Phenolic A ring
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Most abundant, naturally occurring estrogen?
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17 beta estradiol
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Which is more biologically active, estrone or estradiol?
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Estradiol is 10x more active
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Where is estriol (E3) made?
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The placenta. Elevated levels during pregancy.
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What enzyme is responsible for the conversion of androstenedione to estrogen in premenopausal women?
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Aromatase in ovaries (premenopausal women)
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What enzyme is responsible for the conversion of dehydroepiandrosterone to estrogen in post menopausal women?
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Aromatase in adipose tissue
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What converts androstenedione to estrogen males? Where? Where else does estrogen come from?
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Aromatase in adipose tissue.
Some estrogen also synth in testes. |
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Is estrogen very bioavailable?
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Yes. Very lipophilic, readily absorbed through passive diffusion in GI, akin, mucus membranes.
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Is oral estrogen effective? Is there an alternative?
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Estrogen has extensive first pass effect. Oral C17 synthetic derivatives bypass first pass and prolong half life (don't bind SHBG --> freely available).
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Describe estrogen metabolism
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Hepatic metabolites are then really eliminated, may undergo enterohepatic recirculating.
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Adverse effects of estrogen
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Postmenopausal bleeding, endometrial hyperplasia (avoid with progestin), nausea, breast tenderness, hyper pigmentation, migraines, cholestasia, hypertension, endometrial cancer, breast cancer, CV problems (DVT)
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Should not use estrogen if
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History of endometrial cancer, breast cancer, uterine cancer, thromboembolic disorder, pregnant, liver disease
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Progesterone. Produced by? During? Levels are maintained by?
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Corpus luteum, luteal phase in response to LF surge
HCG (made by trophoblast) maintains corpus luteum Eventually (8 weeks) progesterone and estrogen are secreted by the placenta |
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Progesterone is extremely important for what phase of the menstrual cycle?
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The development of the secretory endometrium. Abrupt decline leads to the onset of menstruation.
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What is the role of progesterone during pregnancy?
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Leads to proliferation of mammary gland acini and elevation of body temperature
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Describe progesterone metabolism?
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Readily absorbed orally, first pass hepatic metabolism and inactivation (much like estrogen)
Effective oral derivates have been developed |
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Hormone replacement therapy for Postmenopausal women?
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Estrogen (should be combined with progesterone to prevent endometrial hyperplasia)
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What is the role of the previous drug in Postmenopausal women?
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Hormone replacement therapy- Decrease menopausal symptoms (hot flashes, sweating, atrophic vaginitis), reduce bone resorption/osteoporosis prevention, also lowers LDL and increases HDL
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Notable drugs which can interfere with HRT?
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Acetaminophen, rifampin, antibiotics, anticonvulsants
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HRT can cause increased efficacy of:
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Benzodiazepines, caffeine, corticosteroids, alcohol, beta blockers
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HRT can cause decreased effects of:
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Benzodiazepines, warfarin, thyroid agents, methyldopa
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Other uses for estrogen:
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Primary hypogonadism- stimulate secondary sex characteristics
Dysmenorrhea- inhibit ovulation with estrogen due to uterine prostaglandins, so use NSAIDs Prostate cancer- inhibition of androgen secretion |
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Other uses for progestin
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Endometriosis- dysmenorrhea, painful masses and infertility, continuous treatment
Metastatic endometrial carcinoma- palliative |
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Other estrogenic compounds
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Phytoestrogens- over the counter supplements
Diethylstilbesterol- pot |
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Health factors which must be considered when treating polycystic ovary syndrome?
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Obesity, insulin levels, fertility/desire for pregnancy
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Eflornithine
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For hair removal- must be taken indefinitely
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Norethindrone, norgestimate, desogestrel
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Oral contraceptives (progestins) which are used for hirsuitism and acne
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MOA of estrogens in hirsuitism
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Increased estrogen --> increased inhibition of LH/FSH --> decreased ovarian androgen production --> increased sex hormone binding globulin --> decreased free androgens
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If treatment with estrogen/progesterone for hirsuitism/acen is ineffective, what is a good add on drug?
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Spironolactone (anti-androgen effects)- reduce dose over time
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Concerns for oral contraceptives
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Insulin resistance, glucose intolerance, vascular reactivity/coagulability
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Spironolactone- MOA in hirsuitism/male pattern baldness
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Inhibits androgen biosynthesis and competitive inhibitor at androgen receptor (large doses)
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Spironolactone- SEs
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May prevent external genitalia development in MALE fetus
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Hirsuitism + oligomenorrhea- treatment
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Estrogen, progestin, contraceptive + metformin & low dose flutamide
Metformin + flutamide Estrogen progestin contraceptive + flutamide |
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Endometrial complication of PCOS? How do we treat this?
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Hyperplasia (due to chronic anovulation). Give medroxyprogesterone daily to induce withdrawal bleed`
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Drugs for inducing ovulation?
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Clomiphene- increases FSH/LH
Metformin- alone or with clomiphene (not consistent) Thiazolinedione Gonadotropin therapy |
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Effects of weight & insulin on ovulation?
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Weight loss may restore normal ovulation and reduce insulin levels
Insulin lowering (metformin) may reduce ovarian androgen production and free testosterone concentrations and restore menstrual cyclicity |
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Initial treatment in PCOS
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Metformin (especially if overweight/obese)
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Clomiphene- MOA
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Increases FSH, used for infertility in anovulatory women
Competitive antagonist of ER in hypothalamus --> increased GnRH --> increased FSH |
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Clomiphene- adverse effects
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antiestrogen effects (think menopause)- hot flashes, inhibition of endometrial proliferation, multiple gestation, maybe ovarian cancer
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Aromatase inhibitors
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Increase FSH by decreasing formation of estrogen --> increase GnRH --> increase FSH
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Injectable gonadotropins
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FSH or FSH+ LH. Administered subcutaneously for duration of follicular phase. May inhibit LH surge. Will Administer HCG subQ or intramuscularly
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To monitor maturing follicles
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Use transvaginal ultrasound. If too many, stop FSH, don't give HCG and cancel cycle.
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