Gonadal Hormones And Inhibitors Flashcards
GnRH pulses
Inc LH and FSH
Continuous stimulation of gonadotrope inhibits LH/FSH release
GnRH analogs
Leuprolide and Leuprolide acetate
Short activity for ovulation stimulation
Hot flashes, gynecomastia, osteoporosis, dec libido, VTE
Gonadal steroids
Ketoconazole inhibits at 17,20 desmolase and 17alpha-hydrolase
Spironolactone inhibits at 17alpha-hydrolase and 17,20 desmolase
Full Agonist estrogen products
Oral (estr)
Estradiol (E2) > estrone (E1) > estriol (E3)
Synthetic/nonidentical (estr)
Effects of estrogen: prothrombotic
AE: thromboembolism, category X in pregnancy, endometrial/uterine neoplasia
Clomiphene
SERM
Inc GnRH secretion
Raloxifene
SERM
Partial agonist in bone, Agonist in liver, antagonist in breast and uterus
CI in pregnancy
Tamoxifen
SERM Antagonists in breasts Breast cancer SE: hot flashes, inc risk DVT, inc risk endometrial cancer, vaginal bleeding Drugs that inhibit 2D6 dec efficacy
Aromatase inhibitors
Anastrazole
AE: fatigue, arthralgia, inc risk of fracture
No risk of uterine cancer or venous thromboembolism
Progestogens
-gest, Norethindrone, Drospirenone
Effects of progesterone: dec endometrial proliferation, progestin withdrawal causes menstruation
Ulipristal
SPRM
Partial Agonist
Prevents follicular rupture pre ovulation and implantation post ovulation
Efficacy dec 3A4 inducers
Mifepristone
Weak partial agonist, glucocorticosteroid antagonist, estrogen antagonist
Emergency contraception
Decreasing androgen
Leuprolide: sustained release GnRH agonists
Degaralix: GnRH antagonists and depletes testosterone without initial surge
Bicalutamide: testosterone receptor antagonist
5-alpha-reductase inhibitors (5-ARIs)
Finasteride
Blocks formation of dihydrotestosterone
Pregnant women should not handle these
Inc hair growth, dec libido, gynecomastia, erectile dysfunction
Progestin only pills
Norethindrone and Norgestrel
Oral contraception
Contraceptive DI
Abx
CDC refutes Abx dec efficacy of oral contraceptives
Except Rifampin (drug inducer)
