Gonadal Hormones and Inhibitors Flashcards
Ovarian Hormone MOA
modulation of gene expression
Major ovarian estrogen in women
Estradiol
Mixtures of conjugated estrogens from biologic sources
Premarin
Used as HRT
Premarin
Used as Hormonal Contraceptive
Ethinyl Estradiol, Mestranol
Synthetic estrogens with high bioavailability
Ethinyl Estradiol, Mestranol
Used as Hormonal Contraceptive
Synthetic estrogens with high bioavailability
Used as HRT
Mixtures of conjugated estrogens from biologic sources
Synthetic estrogen MOA
Estrogen receptor activation
Estrogen used for contraception
Ethinyl estradiol, Mestranol, Estradiol cypionate
Estrogen used for hormone replacement
Ethinyl estradiol, Mestranol, Estradiol cypionate
Diethylstilbestrol
Atrophic vaginitis DOC
Diethylstilbestrol
Increases risk for Endometrial and Breast Ca
Synthetic Estrogen
Increases risk for Clear Cell Vaginal Adenocarcinoma in daughters with mothers who took what synthetic estrogen
Diethylstilbestrol
Progestins
Norgestrel (-gest, -nodiol, -nor)
Synthetic progesterone MOA
Progesterone receptor activation
Indications for Progestint
HRT
Contraception
Assisted reproduction
Anovulation induction
Progestins are combined with Estrogen for HRT to decrease risk of
Endometrial Ca
Progestin used as an appetite stimulant
Megestrol
Combination of estrogen-progestin tablets taken in constant dosage throughout the menstrual cycle
Monophasic
Combination of estrogen and progestin where drug dosage of either changes during the month
Biphasic
Type of OCP closely mimicking hormonal change in the menstrual cycle
Biphasic
Regimen for emergency contraception
Yuzpe regimen
Window period for administering emergency contraception
72 hours post-coitus
Primary action of combined hormonal contraceptive
inhibition of ovulation
T/F: Combined OCP does not change lifetime risk of breast cancer.
True
Anti-androgenic progestin
Drospirenone
Progestin-only OCP
Medroxyprogesterone acetate
Intramuscular progestin-only OCP
Depo-provera
T/F: Breakthrough bleeding occurs in between menstrual period
True
Yuzpe regimen
Levonorgestrel + Ethinyl Estradiol
Drugs that are mixed estrogen agonists: agonist in some tissues, partial agonist or antagonist in other tissues
Selective Estrogen Receptor Modulator (SERM)
SERM
Tamoxifen, Raloxifene, Clomiphene (-fen, -phene)
Tamoxifen SimD
Toremifene
Tamoxifen MOA
Estrogen antagonist in breast and CNS
Estrogen agonist in uterus, liver and bone
Tamoxifen side effect
Endometrial hyperplasia and Endometrial Ca
Protective effect of Tamoxifen
Osteoporosis and Atherosclerosis
Tamoxifen indication
Hormone-responsive Breast Ca
Raloxifene MOA
Estrogen antagonist in breast, CNS and UTERUS
Estrogen agonist in liver and bone
Raloxifene indication
breast cancer prevention
Partial estrogen agonist in pituitary
Reduce estradiol negative feedback cause increase in FSH and LSH output
Clomiphene
SERM used for induction of ovulation
Clomiphene
Clomiphene side effect
Multiple pregnancies
Ovarian enlargement
SERM with increased risk of Ovarian Ca with long term use
Clomiphene
Estrogen synthesis inhibitor
Anastrozole, Letrozole, Exemestane
Anastrozole MOA
Inhibits Aromatase
Breast Ca resistant to Tamoxifen DOC
Anastrozole
Ovarian inhibitor
Danazol
Partial progestin and androgen receptor agonist
Danazol
Endometriosis DOC
Danazol
Contraindication of Danazol
Pregnancy and breast feeding
GnRH antagonist that prevents premature LH surge
Ganirelix
Glucocorticoid receptor antagonist
Progesterone receptor antagonist
Mifepristone
Mifepristone
RU 486
Medical abortifacient
Mifepristone
Usually combined with Mifepristone for medical abortion
Misoprostol
Abortion cause sepsis due to which organism
Clostridium sordelli
Precursors of Testosterone
DHEA and progesterone
Converts Testosterone to DHT
5 alpha reductase
Clinical use of testosterone
hypogonadism
stimulate RBC production in anemia
weight gain
performance-enhancer
Male side effect of testosterone
Paradoxical feminization
Female side effect of testosteron
Virilization
Contraindication of testosterone
Pregnancy and Prostate Ca
Androgen receptor agonist used for illegal performance enhancement in athletes
Oxandrolone
Hepatic side effect of OCP
Hepatic adenoma
Hepatic side effect of Oxandrolone
Hepatocellular Ca and Cholestatic Jaundice
Flutamide MOA
Androgen receptor antagonist
Used for surgical castration
Nilutamide
Prevents acute flare up of prostate tumor in patients receiving Leuprolide
Flutamide
Does not cause acute flare up of prostate tumor
Ganirelix
Androgen receptor antagonist used for decreasing sexual drive in men
Cyproterone acetate (Orphan Drug status)
Inhibits 5 alpha reductase
Finasteride, Dutasteride
Benigh Prostatic Hyperplasia DOC
Finasteride
Male-pattern baldness DOC
Finasteride