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Flashcards in Pharm 1 Deck (15)
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Leuprolide (mechanism, use, toxicity)

GnRH analog that acts as an agonist in pulsatile doses and an antagonist in continuous doses (down regulates GnRH receptor in pituitary thus decreases FSH/LH); used as an agonist for infertility and an antagonist for prostate cancer, fibroids, and precocious puberty; antiandrogenic


Clomiphene (mechanism, use, toxicity)

Partial estrogen agonist in the hypothalamus (antagonist at estrogen receptor in hypothalamus), increases release of LH and FSH, stimulating ovulation; used for infertility and PCOS; visual disturbances, multiple pregnancies, ovarian enlargement, hot flashes


Finasteride (mechanism, use, toxicity)

5-alpha reductase inhibitor; used for BPH and male-pattern baldness


Flutamide (mechanism, use, toxicity)

Testosterone receptor antagonist; used in prostate cancer


Ketoconazole (mechanism, use, toxicity)

Inhibits 17,20-desmolase, stopping sex steroid synthesis; used to treat polycystic ovarian syndrome; gynecomastia and amenorrhea


Tamoxifen (mechanism, use, toxicity)

Estrogen receptor antagonist at the breast, agonist at uterus and bone; used for breast cancer; can cause endometrial hyperplasia


Raloxifene (mechanism, use, toxicity)

Estrogen receptor agonist at bone, antagonist at uterus, inhibits osteoclast activity and stimulates osteoblast activity; used to treat osteoporosis; can cause thromolytic events


Anastrozole, exemestane (mechanism, use, toxicity)

Aromatase inhibitors; used in breast cancer with post menopausal women


Mifepristone (mechanism, use, toxicity)

Progesterone receptor antagonist, given with misoprostol for abortion; abortifacient; bleeding, abdominal pain


Terbutaline (mechanism, use, toxicity)

Beta-2 agonist that relaxes the uterus, inhibits uterine contractions during labor


Tamsulosin (mechanism, use, toxicity)

Alpha-1 antagonist by inhibiting smooth muscle contractions (selective for prostrate Alpha-1-A,D vs Vascular 1-B) ; used to treat BPH


Sildenafil, vardenafil (mechanism, use, toxicity)

Phosphodiesterase 5 inhibitors, causing inc. cGMP levels and smooth muscle relaxation; used in erectile dysfunction; impaired blue-green vision, contradindicated with nitrates (causes hypotension)


Danazol (mechanism, use, toxicity)

Partial androgen receptor agonist; used to treat endometriosis and hereditary angioedema; weight gain, acne, hirsutism, low HDL, hepatoxicity


Progestins (mechanism, use)

Bind progesterone receptors, decrease growth and increase vascularization of endometrium; oral contraceptives, endometrial CA and abnormal uterine bleeding.


Estrogens: ethinyl estrodial, DES, mestanol (mech, use, toxicity)

Bind estrogen receptors; hypogonasism/ovarian failure, menstral abnormalities, Hormone Replacement Therapy (postmenapausal), Men with androgen-dependent prostate cancer; increase risk of endometrial cancer, bleeding, clear cell adenocarcinoma (exposure to DES in utero), THROMBUS, contraindicated: breast cancer, DVT's