Gonadal Hormones and Inhibitors Flashcards
Androgen Receptor Antagonist
Flutamide, Bicalutamide, Nilutamide
Cyproterone, Cyproterone Acetate
Androgen Synthesis Inhibitor/5-Alpha Reductase Inhibitor
Finasteride
Dutasteride
MOA: FINASTERIDE
inhibits 5 alpha reductase enzyme that converts testosterone to DHT (most potent form)
Anabolic Steroids
Oxandrolone, Nandrolone Decanoate
Used in male hypogonadism
Androgens - Testosterone, Methyltestosterone, Testosterone Cypionate, Oxymetholone, Mesterolone
Used in illegal performance enhancement by athletes
Anabolic Steroids
oxandrolone, nandrolone decanoate
Used in Prostate CA
Flutamide, Bicalutamide, Nilutamide
Used in hirsutism
Cyproterone, Cyproterone acetate
Used in BPH
Finasteride, Dutasteride
SERM
Tamoxifen
Toremifene
Raloxifene
Clomiphene
Aromatase Inhibitors
Anstrozole
Letrozole
Exemestane
Ovarian Inhibitor (Anti-Androgen)
Danazol
GNRH AGONISTS
Leuprolide Gonadorelin Goserelin Histrelin Nafarelin Triptorelin
GNRH ANTAGONISTS
Ganirelix
Cetrorelix
Abarelix
Degarelix
Glucocorticoid and Progesterone Receptor Antagonist
Mifepristone
Use: Tamoxifen, Toremifene
Hormone-responsive Breast Cancer
ER+ PR+
Use: Raloxifene
Osteoporosis
preferred
increases bone mineral density without estrogenic effects on endometrial tissue
Use: Clomiphene
Induction of ovulation
antagonizes estrogen receptors in the pituitary thus inhibiting the negative feedback by estrogen = increase LH and FSH
Enzyme that converts Testosterone to Estrogen (Estradiol)
Aromatase
Irreversible aromatase inhibitor
Exemestane
Pharmacologic antagonist of glucocorticoid and progesterone receptors used in medical abortion
Mifepristone
AE of Tamoxifen
Increased risk for endometrial hyperplasia, endometrial CA, DVT
AE of Raloxifene
Increased risk for DVT
Side effect of Clomiphene
Multiple pregnancies (10%)
Increased risk of low-grade ovarian cancer with long term use
Full Estrogen receptor antagonist
FLUVESTRANT
Intermittent GnRH agonists will result to
increased FSH AND LH secretion
Prolonged continuous administration of GnRH Agonists will result to
reduced LH and FSH secretion due to downregulation of GnRH receptors
What should be given with GnRH agonists to prevent temporary exacerbation in treating prostate CA?
Flutamide
Uses: GnRH Agonists
Ovarian Suppression
Controlled ovarian hyperstimulation
Advanced Prostate CA
MOA: Danazol
Weak CYP450 inhibitor
Partial agonists of progestin and androgen receptors
Use: Danazol
Endometriosis
Fibrocystic Disease
Hemophilia
Angioneurotic edema
Emergency contraception
Levonorgestrel
Ethinyl Estradiol + Levonorgestrel
Emergency contraception must be taken within ?
72 hours
Progestin-only Contraceptive
Medroxy-Progesterone Acetate
Absolute Contraindications to OCPs
>35y who smokes >15 sticks per day with IHD or multiple CVD risk factors with previous stroke hx complicated VHD complicated solid organ transplantation HTN SLE Cirrhosis, hepatic adenoma or hepatoma Pregnancy and early postpartum (<12d) undiagnosed AUB
Relative Risk to OCP
Hypertension controlled
Taking anticonvulsants
Post bariatic surgery
PROGESTINS
norgestrel norethindrone ethynodiol megestrol desogestrel norelgestromin norgestimate etonogestrel progesterone LEVONORGESTREL dydrogesterone ulipristal tibolone norethisterone dienogest
Progestin used as an appetite stimulant
Megestrol
a synthetic steroid with weak estrogrenic, progestogenic and androgenic effect used in menopausal hormone therapy, postmenopausal osteoporosis and endometriosis
TIBOLONE
Use: Progestins
HRT, contraception, assisted reproduction, anovulation induction
Synthetic estrogen associated with Clear Cell vaginal adenocarcinoma
DES or Diethylstilbestrol
ESTROGENS
Ethinyl Estradiol Mestranol Estradiol Cypionate Premarin Estriol