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Pharm - Repro

Reproductive Pharmacology from First Aid 2013

QuestionAnswer
Leuprolide: MOA, Use, Tox MOA: GnRH analogue Use: Agonist when pulsatile (fertility) Antagonist when continuous(fibroids, precocious puberty, prostate cancer) Tox: anti-androgenic, N/V
Testosterone/methyltestosterone: MOA, Use, Tox MOA: agonist at androgen receptors Use: hypogonadism, 2' sex characteristics, stimulation of anabolism after burn Tox: masculinization, gonadal atrophy, closure of epiphyseal plates (with estrogen), inc LDL, dec HDL
Finasteride: MOA, Use, Tox MOA: 5a-reductase inhibitor (test -> DHT) Use: BPH, baldness Tox: feminization
Flutamide: MOA, Use MOA: inhibitor of androgen receptor Use: prostate carcinoma
Ketoconazole: MOA, Use, Tox MOA: inhibit steroid synthesis (desmolase) Use: PCOS Tox: Amenorrhea
Spironolactone: MOA, Use MOA: inhibits steroid binding Use: Treat hirsutism in PCOS Gynecomastia may be desirable SFX.
Estrogens: naming, MOA, Use, Tox Nom: estradiol, DES, mestranol MOA: bind estrogen receptors Use: hypogonadism, ovarian failure, post-menopausal HRT, androgen-dep prostate cancer Tox: risk endometrial cancer, DES in utero -> clear cell adenocarc., thrombi/DVT, ER+ breast cancer
Name three SERMs. Clomiphene Tamoxifen Raloxifene
Clomiphene: MOA, Use, Tox MOA: partial agonist estrogen rec in hypothal prevents feedback inhib on pituitary -> stimulates FSH/LH, ovulation Use: infertility, PCOS Tox: hot flashes, ovarian enlargement, vision disturbances, multiple pregnancies
Tamoxifen: MOA, Use, Tox Antagonist at breast: ER+ breast cancer Agonist at uterus: risk of endometrial cancer
What is the MOA and use of raloxifene? Agonist at bone: osteoporosis
What are the indications and risks of HRT? Relief of menopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (inhibit OAF/IL-1). Risk of endometrial cancer (add progesterone) and CV risk.
What is the mechanism and use of anastrozole/exemestane? They are aromatase inhibitors used in postmenopausal women with breast cancer.
Progestins: MOA, Use MOA: bind progesterone receptors, reducing the growth and vascularity of the endometrium Use: active ingredient in OCPs, treating/preventing endometrial cancer
Mifepristone (RU-486): MOA, Use, Tox MOA: competitive inhibitor of progesterone Use: termination of pregnancy Use with misoprostol (PGE1) Tox: heavy bleeding, GI upset, abdominal pain
How do OCPs work? What are their contraindications? Inhibit FSH/LH, preventing the estrogen / luteal surges, and thus, ovulation. Progestins thicken the cervical mucus. Progestins inhibit endometrial proliferation. C/I: smokers >35y, risk of thromboembolism, or estrogen-dep tumors
Terbutaline: MOA, Use MOA: b2 agonist that relaxes the uterus Use: reduce premature uterine contractions
Tamsulosin: MOA, Use MOA: a1 antagonist used to treat BPH, selective for a1(A/D) receptors on the prostate over a1B receptors in vasculature
Sildenafil, vardenafil: MOA, Use, Tox MOA: PDE inhibitor, increasing cAMP -> smooth muscle relaxation in corpus cavernosum Use: erectile dysfunction Tox: Hot and sweaty, headache, heartburn, Hypotension
Danazol: MOA, Use, Tox MOA: synthetic partial androgen agonist Use: endometriosis, hereditary angioedema Tox: weight gain, edema, acne, hirsutism, dec HDL, masculinization, hepatotox
Created by: wmwebb89