Androgens, Estrogens, and Progestins Flashcards
Testosterone
main androgenic hormone
made by Leydig cells of testes
Hydroxylase in Leydig Cells
CYP17
5a-Reductase
converts testosterone to dihydrotestosterone
P450 Aromatase
converts testosterone to estradiol
Effects of Androgen
penile/ scrotal growth
changes in skin and vocal cords
prostate growth
increases lean body mass and stim body hair growth
Examples of Androgens
testosterone
oxandrolone
nandrolone decanoate
Uses of Androgens
replacement therapy in Male Hypogonadism
enhance athletics- DHEA
SE of Androgens
Conversion to estrogens- gynecomastia
virilization of women and children
GnRH Antagonists
inhibit production of LH
Tx for Enlarged Prostate
alpha-1 blockers
5-a reductase inhibitors
Flutamide
androgen receptor blocker
for prostate cancer
for hirsutism in women
Finasteride
5-a Reductase Inhibitors
for benign prostatic hyperplasia
male pattern baldness
PDE5 Inhibitor Examples
sildenafil
vardenafil
tadalafil
MOA of PDE5 Inhibitors
blocks metabolism of cGMP by inhibiting PDE5
relaxes smooth muscle in corpora cavernosum and increased blood flow and erectile response
SE of Sildenaafil and Vardenafil
blurred vision
loss of blue green color vision
SE of Tadalafil
greatest inhibitory effect on PDE 11
lower back and limb pain
Don’t mix PDE5 Inhibitors with…..
nitrates
Estradiol
main ovarian estrogen in women
Ethynyl Estradiol
synthetic estrogen
hormonal contraceptives
Effects of Estrogen
essential for normal female reproductive development
Continuous Estrogen
inhibits gonadotropin secretion
Use of Estrogen
treating hypogonadism in females
preventing bone loss and osteoporosis
Estrogen Toxicity
when used as HRT- increased risk of endometrial cancer
Examples of SERMS
Tamoxifen
Raloxifene
Use of SERMS
estrogen receptor (+) breast cancer raloxifene for osteoporosis as well
SE of Tamoxifen
increased risk of endometrial cancer
SE of Raloxifene
hot flushes and increase risk of venous thrombosis
Fulvestrant
pure estrogen receptor antagonist
MOA of Fulvestrant
inhibits binding of estrogen
alters receptor structure so that the estrogen receptor is targeted for degradation
Use of Fulvestrant
estrogen receptor + breast cancer
Tamoxifen resistant breast cancer
MOA of Clomiphene
blocks inhibitory action of estrogen on gonadotropin release
Use of Clomiphene
first line treatment for infertility in polycystic ovarian syndrome
SE of Clomiphene
hot flashes
multiple pregnancies
ovarian enlargement
Progestin Effects
progesterone induces secretory changes in endometrium and is needed for pregnancy
Use of Progestins
contraceptives
combo w/ estrogen for replacement therapy to prevent estrogen induced endometrial cancer
Mifepristone Use
combo with prostaglandins to terminate pregnancy
increase contractions and ensure expulsion of detached blastocyst
Ulipristal Use
emergency contraceptive
w/in 72 hours
lasts 5 days
