Reproductive/Endocrine Flashcards
GnRH analog with agonist properties when used in pulsatile fashion; antagonist
properties when used in continuous fashion
(downregulates GnRH receptor in pituitary
that decreases FSH/LH).
Leuprolide
What drug causes transient increase in pituitary LH secretion; which leads to a rise in testosterone levesl; continuous use will suppress LH release and leads to a decrease in testosterone levels
Leuprolide
Antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and
increases release of LH and FSH from pituitary, which stimulates ovulation
clomiphene
Antagonist at breast; agonist at bone, uterus; increased risk of thromboembolic events and endometrial
cancer.
tamoxifen
Antagonist at breast, uterus; agonist at bone; increased risk of thromboembolic events but no increased risk
of endometrial cancer (
raloxifene
Anastrozole, letrozole, exemestane are examples of:
aromatase inhibitors
Inhibit peripheral conversion of androgens to estrogen.
aromatase inhibitors
Used for relief or prevention of menopausal symptoms (eg, hot flashes, vaginal atrophy),
osteoporosis ( increased estrogen, decreased osteoclast activity).
Unopposed estrogen replacement therapy ; increased risk of endometrial cancer, so progesterone is added.
Possible increased cardiovascular risk.
hormone replacement therapy
Agonists at androgen receptors
testosterone, methyltestosterone
5α-reductase inhibitor (decreases conversion of
testosterone to DHT).
Used for BPH and malepattern
baldness.
Finasteride
Inhibits steroid binding, 17α-hydroxylase, and
17,20-desmolase.
Spironolactone
Inhibits steroid synthesis (inhibits
17,20-desmolase).
Ketoconazole
Nonsteroidal competitive inhibitor at androgen
receptors. Used for prostate carcinoma.
Flutamide
α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1A,D receptors (found on prostate) vs vascular α1B receptors.
tamsulosin
Direct arteriolar vasodilator.
minoxidil
used to treat androgenic alopecia
minoxidil
Sildenafil, vardenafil, tadalafil are examples of:
phosphodiesterase type 5 inhibitors
Inhibit PDE-5 which increases cGMP and causes prolonged
smooth muscle relaxation in response to NO which increases blood flow in corpus cavernosum of penis,
and decreases pulmonary vascular resistance.
phosphodiesterase type 5 inhibitors
Risk of life threatening hypotension in patients taking nitrates
phosphodiesterase type 5 inhibitors
Synthetic androgen that acts as partial agonist at androgen receptors.
danazol
MC SE of danazol
decreased HDL levels and hepatoxicity
β2-agonists that relax the uterus; used to decrease contraction frequency in women during labor.
terbutaline, and ritodrine
Produces local inflammatory reaction toxic to sperm and ova, preventing fertilization and implantation; hormone free.
copper IUD
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge no
LH surge no ovulation.
Combined contraception
Competitive inhibitors of progestins at progesterone receptors.
Mifepristone, ulipristal
**Termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal)
Bind progesterone receptors, decreased growth and increased vascularization of endometrium, thicken cervical
mucus.
progestins (Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol, and many others
when combined with estrogen)
MOA: work by suppressing pituitary LH secretion and subsequently decreasing ovarian androgen production.
Oral contraceptives