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-Antiestrogen (blocks feedback on LSH) Tx: Ovarian failure (fertility drug) *Used if infertility is the result of excessive estrogenic inhibition Sfx: Can overstimulate |
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-Replacement FSH and LH for women who don't make it (causes follicular stimulation) *Used to simulate FSH, followed (14 days later) by a single injection of hCG to simulate LH |
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-Mimics LH surge to induce ovulation |
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GnRH analog Tx: Infertility resulting from hypothalamic amenorrhea. A pulsatile dosing (IV infusion) causes release of LH and FSH Contraceptive: when given often desensitizes GnRH receptors (suppression of LH and FSH). |
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Syntheitic GnRH Used as contraceptive or fertility drug (depending on how given) |
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-GnRH superagonist Tx: Androgen dependent Prostate CA Desensitizes GnRH receptors , reducing Testosterone (medical castration) |
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GnRH Antagonist -Instead of desensitizing/just blocks Tx: management of infertility, prevents premature LH surge |
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-Estradiol that is active orally |
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Orally effective pro-drug -demethylated to ethinyl estradiol |
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Watersoluble with charge sulfate -Slowly absorbed in the gut |
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Non-steroidal plant derivatives w/ estrogen like activity |
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oral active nonsteroidal estrogen -Increase risk of clear cell CA and cervical adenoma |
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Functional competitive Estrogen receptor antagonist (SERM) -Prevent breast cancer (lowers LDL too) ^ bone density Sfx: ^ risk of endometrial CA |
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Fxnal competitive Estrogen receptor antag -Better than Tamoxifen on uterine tissue |
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Steroidal Aromatase Inhibitor (lowers production of E2) -adjuvant with tamoxifen |
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Non-steroidal aromatase inhibitor -Postmenopausal women w/ BrCA who are in risk of recurrence |
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-Less thromboembolic events -Higher incidence of cardiac events and hot flashes |
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Non-steroidal aromatase inhibitor |
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Added to conjugated E2 for HRT to blunt E2 effect on uterine tissue |
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19-nor progestin, has oral activity, but also active at androgen receptors |
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19-nor derivative that is less active at androgen (hirsuitism) |
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Competitive Antagonist at Progesterone and glucocorticoid receptors *abortion pill (break down endometrium) - |
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-Promotes weight gain after surgery Sfx: ^LDL and decrease HDL |
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Non-steroidal anti-androgen Tx: prostatic CA Can be used to w/ leuprolide to block effects of adrenal androgens |
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non-steroidal anti-androgen -less hepatotoxic than flutamide |
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5-alpha reductase inhibitor Prevents testosterone from becoming dihydrotestosterone Tx: BPH and male pattern baldness |
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Progestin-only contraceptive (subdermal implant)
-can get infertility upon withdrawal |
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Post-Coital Emergency Contraception
-Prevents ovulation, fertilization, and possibly implantation |
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Steroidal anti-androgen (Prostate CA)
Weak Partial agonist at testoterone androgen receptor
Sfx: Inhibit libido and spermatogenesis |
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