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13 Cards in this Set
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Antiandrogens
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Testosterone --> DHT (more potent) via 5alpha-reductase
Finasteride - 5alpha red inhib (dec conversion of test to DHT); useful in BPH and promotes hair growth (male-pattern baldness) Flutamide - nonsteroidal compet inhib of androgens @ test R; prostate CA PCOS tx: (prev hirsutism) Ketoconazole - inhib steroid synth Spironolactone - inhib steroid binding S/E: gynecomastia, amenorrhea |
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Leuprolide
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MOA: GnRH analog w/ agonist properties when used in PULSATILE fashion; antagonist when used in CONTINOUS fashion
Use in infertility (pulstaile), prostate CA (contin + flutamide), uterine fibroids Tox: antiandrogen, N/V |
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Sildenafil, Vardenafil
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MOA: Inhibit cGMP phosphodiesterase causing inc cGMP, smooth m relax in corpus cavernosum, inc blood flow, penile erection
Use in erectile dysfxn Tox: headache, flushing, dyspepsia, impaired blue-green color vision, risk of life-threatening hypoTN in pts taking nitrates |
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Mifepristone (RU-486)
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MOA: compet inhib of progestins @ progesterone receptor
Use in termin of PG; admin w/ misoprostol (PGE1) Tox: heavy bleeding, GI, abd pain |
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Oral contraception
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Prevent estrogen surge, no LH surge --> no ovulation
Adv: reliable, dec risk of endometrial/ovarian CA, dec risk ectopic PG, dec pelvic infec's, regular menses Disadv: taken daily, no STD protection, inc TG's, depression, wt gain, nausea, HTN, hypercoag |
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Hormone replacement therapy (HRT)
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Relief/prevention of menopausal sx's and osteoporosis
Unopposed estrogen replacement therapy increases risk of endometrial CA (so use w/ progesterone); possible inc CV risk |
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Dinoprostone
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PGE2 analog, cervical dilation and uterine contraction, inducing labor
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Ritodrine/Terbutaline
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B2-agonists that relax the uterus, reduce premature uterine contractions
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Anastroazole, exemestane
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Aromatase inhibitors used in postmen women w/ breast CA
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Testosterone (methyltestosterone)
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MOA: agonist at androgen receptors
Treat hypogonadism and promote dev of 2* sex charc's, stim anabolism to promote recovery after burn/injury, treat ER(+) BC Tox: masculinization in females, reduce intratesticular test supply in males by inhib Leydig cells, leads to gonadal atrophy; premature closeure of epiphyseal plates, inc LDL, dec HDL |
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Estrogen (ethinyl estradiol, DES, mestranol)
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Bind estrogen receptor
Used in hypogonadism or ovarian failure, men abnormalities, HRT In postmen females, men w/ androgen-dep prostate cancer Inc risk of endometrial cancer, bleeding in postmen women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, inc risk of thrombi; CI in ER(+) BC |
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Progestins
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Bind progesterone receptors, reduce grwoth, and incrrease vasculinization of endometrium
Use in OC, and tx of endometrial CA and abn uterine bleeding |
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Estrogen partial agonists (SERMs)
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Clomiphene - partial agonist at ER in pit gland; prev normal feedback inhib and increase release of LH/FSH from pit which stim ovulation; used to treat infertility and PCOS; Tox: hot flashes, ovarian enalrgement, multiple simultaneous pregnanices and visual disturb's
Tamoxifen - antagonist on breast tissue, to treat and prevent ER pos BC recurrence Raloxifene - agonist on bone, reduce resorption of bone, treats osteoporosis |