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13 Cards in this Set

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Antiandrogens
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
Leuprolide
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
Sildenafil, Vardenafil
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
Mifepristone (RU-486)
MOA: compet inhib of progestins @ progesterone receptor

Use in termin of PG; admin w/ misoprostol (PGE1)

Tox: heavy bleeding, GI, abd pain
Oral contraception
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
Hormone replacement therapy (HRT)
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
Dinoprostone
PGE2 analog, cervical dilation and uterine contraction, inducing labor
Ritodrine/Terbutaline
B2-agonists that relax the uterus, reduce premature uterine contractions
Anastroazole, exemestane
Aromatase inhibitors used in postmen women w/ breast CA
Testosterone (methyltestosterone)
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
Estrogen (ethinyl estradiol, DES, mestranol)
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
Progestins
Bind progesterone receptors, reduce grwoth, and incrrease vasculinization of endometrium

Use in OC, and tx of endometrial CA and abn uterine bleeding
Estrogen partial agonists (SERMs)
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