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36 Cards in this Set
- Front
- Back
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biological effects of estrogens?
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- growth of genital structures and secondary sexual characteristics
- modifies serum protein levels - dec bone resorption - inc coagulability - inc trig & dec LDL - inhibits secretion of LH/FSH |
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risks associated with ERT?
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- premature closure of epiphyses
- endometrial CA - breast CA - MI, stroke - nausea, br tenderness, migraines, thromboses, gallbladder dz, hypertriglyceridemia, HTN |
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which synthetic hormone is assocd w infertility, ectopic pregnancy, and vaginal adenocarcinoma in daughters of women treated with it?
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diethylsilbestrol (DES)
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what was the clinical use of DES?
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prevent recurrent spontaneous abortion
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what reduces the risk of endometrial cancer in ERT?
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combining it with progestin
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biological effects of progestins?
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- induces secretory chgs in endometrium and maintains pregnancy
- affect CHO metab - inc fat deposition - high doses suppress LH/FSH -> anovulation |
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adverse effects of progestins?
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increase BP, dec HDLs
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composition of hormonal contraceptives?
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either combo estrogen and progestin, or a progestin alone
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post-coital contraceptives?
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pro alone (L-norgestrel, fewer side effects), est alone, or combo est and pro
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MOA of hormonal contraceptives?
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est/pro combos inhibit ovulation and affect cervical mucus, uterine tubes, and endometrium, decreasing likelihood of fertilization and implantation
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beneficial side effects of hormonal contraceptives?
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dec risk of ovarian cysts, ovarian and endometrial CA, benign breast dz and PID; dec incidence of ectopic pregnancy, iron deficiency anemia and RA
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what factors increase the risk of thromboembolic events with hormonal contraceptives/ERT?
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smoking, older age, personal/fam hx of problems, and genetic defects affecting production/fxn of clotting factors
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estrogen antagonist used to treat ER/PR + breast cancer
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tamoxifen
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side effects of tamoxifen?
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agonist of endometrial receptors -> inc risk of endometrial CA
hot flushes inc risk of venous thrombosis dec risk of osteoporosis |
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estrogen partial agonist used for prevention and tx of osteoporosis in postmenopausal women?
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raloxifene
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difference between raloxifene and tamoxifen?
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raloxifene has no effects on endometrial tissue
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nonsteroidal pituitary estrogen receptor blocker used to stimulate ovulation?
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clomiphene
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pure estrogen receptor antagonist used to treat tamoxifen-resistant breast cancer?
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fulvestrant
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what are anastrozole, letrozole and exemestane used for/MOA?
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tx of breast cancer by inhibiting aromatase (dec est synthesis)
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inhibitor of p450 enzyme gonadal steroid synthesis and weak partial agonist of progestin, androgen and glucocorticoid receptors; used to tx endometriosis and fibrocystic dz of the breast?
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danazol
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GnRH agonist used to inhibit est/pro synthesis and, combined with other drugs for ovarian hyperstimulation?
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Leuprolide
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tx with leuprolide > 6 mo in premenopausal women can cause what?
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dec bone density
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orally active steroid antagonist of progesterone and glucocorticoids?
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mifepristone
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combination of what two drugs produces complete abortion in 95% of early pregnancies?
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mifepristone (pro antagonist) and misoprostol (PGE analog)
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from what is testosterone synthesized in the body?
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progesterone and DHEA
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synthetic androgens that increase the ratio of anabolic-androgenic action?
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oxandrolone and stanozolol
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effects of androgens by females?
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hirsutism, enlarged clitoris, deepend voice, menstrual irregularity
can cause virilization of fetus |
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effect of large doses of androgens in males?
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paradoxical feminization (feedback inhibition of pituitary and conversion of androgens to estrogens)
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effect of large dose androgens in either sex?
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cholestatic jaundice, elevated LFTs, possible hepatocellular carcinoma
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uses of antiandrogens?
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benign and malignant prostate dz, precocious puberty, hair loss, and hirsutism
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androgen receptor inhibitors?
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flutamide, spironolactone, cyproterone
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what converts testosterone to DHT?
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5-alpha-reductase
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5-alpha-reductase inhibitor used for BPH and prevention of hair loss?
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finasteride
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MOA of leuprolide?
clinical uses? |
suppresses gonadotropin secretion (esp LH), reducing the production of testosterone
used in prostatic carcinoma |
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what must be administered with leuprolide for the first week of therapy against prostatic carcinoma?
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androgen receptor antagonist (flutamide)
prevents tumor flare d/t initial surge in testosterone synthesis |
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antifungal that also inhibits gonadal and adrenal steroid synthesis for tx of steroid-responsive metastatic prostate cancer?
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Ketoconazole
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