Term
| All steroid hormones interact with ___ receptors to ___ and thus ___ |
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Definition
Intracellular receptors
Alter gene transcription
Protein synthesis |
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Term
| Conjugated estrogens: composition |
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Definition
Salts of estrogen sulfates at pregnant mare levels
Conjugated with straight chain fatty acids to increase the activity and half-life |
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Term
| Physiological effects of estrogens (7) |
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Definition
Normal sexual maturation and development of secondary sexual characteristics
Fat goes to boobs and hips
Fluid goes from plasma to extracellular space = edema and compensatory salt/water retention
Accelerated growth and closure of epiphyseal plates
Skin, bone, mucosa, blood vessel maintenance
Increased synthesis of hepatic proteins including clotting factors (but free levels remain the same)
Increase HDL and TG, decrease LDL and total cholesterol |
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Term
| Ethinyl estradiol: pharmacokinetics |
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Definition
| Ethinyl substitution prevents first-pass metab = increases bioavailability, potency, and half-life |
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Term
| Since estrogens and their active metabolites recirculate through the liver... |
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Definition
| p.o. estrogens have a greater effect on the liver than on the periphery |
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Term
| Estrogens: indications (6) |
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Definition
Primary hypogonadism
Symptoms of menopause
Contraception
Dysmenorrhea or dysfunctional uterine bleeding
Hirsutism
Symptoms of benign breast disease (like painful fibrous tumors) |
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Term
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Definition
Decreased LDL-R, increased LDL = increased total cholesterol
HDL, VLDL, TG are unchanged |
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Term
| HRT, Tamoxifen, Raloxifene effects on lipid profile (2) |
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Definition
Decrease LDL
Increase HDL (not raloxifene), TGs
Doesn't always decrease CV risk, though! |
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Term
| OCPs are lipid ___ in pre-menopausal women |
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Definition
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Term
| The perfect HRT: properties |
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Definition
Agonist at skin, bone, mucous membranes, lipid profile, CNS
Antagonist or no effect at boobs, uterus, liver |
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Term
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Definition
| Large dose of estrogen within 72 hours (99% effective) |
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Term
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Definition
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Term
| Don't give estrogens to... (4, 4) |
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Definition
Absolutely never:
-Est. dependent breast/uterine cancer
-Undx abnoromal genital bleeding
-Hx thromboembolism
-Acute hepatic disease
Relatively never:
-Family hx breast/uterine cancer
-Severe varicose veins
-Hx hepatic disease
-HTN |
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Term
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Definition
n/v/d
Breast tenderness
Endometrial hyperplasia (avoid with co-admin of progestin)
Salt/water retention, HTN
Gallbladder disease and possible jaundice
Thromboembolus
Post-menopausal bleeding
Headache
Hyperpigmentation |
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Term
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Definition
Teratogenic!
-Females of moms that took it develop clear cell adenocarcinoma of the vagina in their 20s
-Males have undescended testes, epididymal cysts, azoospermia |
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Term
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Definition
Estradiol (17B-estradiol)
Conjugated estrogens
Ethinyl estradiol
Diethylstilbestrol |
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Term
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Definition
Clomiphene
Tamoxifen
Raloxifene
Never give to thromboembolic patients! Acts as est-R agonist in the liver = increased synthesis of clotting factors |
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Term
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Definition
Blocks est-R in HT = no feedback inhibition
Increased GnRH secretion and thus FSH/LH secretion
Stimulates estrogen, gametogenesis, and multiple ovulation |
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Term
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Definition
Ovarian enlargement
Multiple or still births
Visual scotoma (temporary)
Symptoms of menopause |
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Term
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Definition
| Induce ovulation in amenorrhea or anovulation |
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Term
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Definition
Blocks est-R
Pre-menopause: blockade in HT and pit causes increased GnRH and thus LH and thus estrogen = antagonizes the blockade effect (avoid with GnRH analog) |
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Term
| Tamoxifen: indications (2) |
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Definition
| Breast cancer and breast cancer prophylaxis |
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Term
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Definition
Venous thrombosis, pulmonary embolism
Endometrial hyperplasia
n/v (agonist)
Symptoms of menopause (antagonist)
Vaginal bleeding, menstrual irregularities
Increased PT in patients taking warfarin |
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Term
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Definition
Estrogen agonist:
-Bone resorption
-Lipid profile
-Hepatic protein synthesis
Estrogen antagonist:
-Uterus = not associated with endometrial hyperplasia or vaginal bleeding
-Breast = not associated with tenderness or cancer |
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Term
| Raloxifene: indications (3) |
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Definition
Decrease size of leiomyomas
Maintain bone density in post-menopausal women, decrease incidence of vertebral fracture (HRT with conjugated estrogens is better)
Breast cancer |
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Term
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Definition
Symptoms of menopause, insomnia
Flu-like syndrome, arthralgia
Antagonize beneficial effect of topical estrogen in atropic vaginitis |
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Term
| All SERMs: properties (2) |
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Definition
Cause symptoms of menopause
Increase hepatic protein synthesis = contraindicated in thromboembolic patients |
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Term
| Bone loss can be prevented by SERMs and ___, which... |
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Definition
Bisphosphonates (alendronate, ibandronate)
Which bind to remodeling bone surfaces and inhibit bone resorption |
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Term
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Definition
Esophagitis (empty stomach + 6-8 oz water + upright for 30 min.)
Osteonecrosis of the jaw (IV + 1st generation + previous insult) |
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Term
| Tamoxifen, raloxifene: properties (3) |
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Definition
Blockade of est-R in breast tissue, skin, mucous membranes
Maintain bone density post-menopause
Improve lipid profile |
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Term
| Breast cancer drug classes (2) |
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Definition
SERMs (tamoxifen, raloxifene)
Aromatase inhibitors |
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Term
| Aromatase inhibitors: MOA |
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Definition
Prevents conversion of testosterone to estradiol, DHEA to estrone = block synthesis of all estrogens in the body
Pre-menopausal: (androstenedione) testosterone conversion happens granulosa cells
Post-menopausal: DHEA conversion happens in fat cells |
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Term
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Definition
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Term
| Aromatase inhibitors: indications |
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Definition
Post-menopausal women:
-with est-R positive cancer
-with advanced/metastatic breast cancer
-who haven't responded to tamoxifen
-who've been taking tamoxifen for 5 years |
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Term
| Aromatase inhibitors: S/E (2) |
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Definition
Symptoms of menopause
MSK issues |
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Term
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Definition
Drospirenone
Medroxyprogesterone
Norelgestromin
Norethindrone
Norgestimate |
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Term
| Norethindrone: properties (2) |
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Definition
Androgenic effects
No anti-mineralocorticoid activity |
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Term
| Ortho Tri-cyclen: composition, properties |
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Definition
Norgestimate (active metabolite = norelgestromin)
Doesn't stimulate androgenR = no antagonist effect of estrogen on lipid profile
Combined with ethinyl estradiol: increase in SHBG causing a fall in free testosterone |
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Term
| Drospirenone (spironolactone derivative): MOA (2) |
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Definition
Stimulates progesteroneR
Blocks androgen and mineralocorticoidR = no acne or CV risks (actually CV benefit) |
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Term
| Post-menopausal HRT estrogen with (cyclic or intermittent) progestin preparations (4) |
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Definition
Ethinyl estradiol + norethindrone
17B-estradiol + norgestimate
Estradiol + norethindrone
Ethinyl estradiol + drospirenone (Yasmin) |
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Term
| OCPs all contain ___ and ___ |
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Definition
Ethinyl estradiol
Progestin (norethindrone, norgestimate) |
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Term
| Yaz: composition, physiologic effects (3) |
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Definition
Ethinyl estradiol + drospirenone
No acne or hirsutism
Less water retention and negative affect
Decreased BP and LDL |
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Term
| Ortho-evra patch: composition, benefits, risks |
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Definition
Ethinyl estradiol + norelgestromin
Better compliance than daily p.o. OCPs
Exposure to increased levels of estrogen (than typical OCP) due to the fact that the constant levels of the patch are much greater than the OCP-spikes |
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Term
| Progestins: indications () |
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Definition
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Term
| Depo-provera: composition, benefits (4) |
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Definition
IM depot of medroxyprogestrone
Benefits
-Lasts 3 mo
-Complete amenorrhea (perhaps unpredictable bleeding)
-Very small risk of pregnancy
-No increased risk of thromboembolism or endometrial hyperplasia |
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Term
| How estrogen works on acne (3) |
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Definition
Suppresses release of LH via HT and pit = decreased ovarian synthesis of testosterone
Increased hepatic synthesis of SHBG = decreased free testosterone
Decreased free testosterone = decreased sebum production |
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Term
| Mifepristone: indication, MOA, physiologic effects (3) |
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Definition
Outpatient abortion of fetus <49 days
Progesterone-R antagonist
Prevent implantation of fertlized egg
Alleviate symptoms of endometriosis
Treat leiomyomas, Cushings syndrome (glucocorticoid-R antagonist), and un-resectable meningiomas |
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