What 2 antiandrogens are used to prevent hirsutism in PCOS?
Spironolactone and Ketoconazole
What is the controversy with DES?
Causes clear cell adenocarcinoma of vagina in females exposed in utero
What is the MOA of progestins?
Reduce growth and increase vascularization of the endometrium by binding progesterone receptors
What is the MOA of flutamide? What drug is it co-administered with to treat prostatic cancer?
Competitive antagonist for testosterone at the androgen receptor; administered with CONTINUOUS leuprolide
What are the 3 estrogen drugs?
Ethinyl estradiol, mestranol, and DES = Diethylstilbestrol
Which SERM increases the risk for cervical cancer? Which has no effect?
What is the MOA and use of Mifepristone? What is it given with?
A competitive inhibitor of progestins at the endometrium? Used to terminate pregnancy. Given with misoprostol (PGE1)
Which SERM is used to induce ovulation?
Which SERM is used for breast cancer and in preventing recurrences of Estrogen-Receptor positive breast cancer?
This drug inhibits the alpha 1 a, d receptor
Tamsulosin for BPH
In whom are OCP's contraindicated?
Smokers over 35 and ppl with Hx of thromboembolism
What is another name for RU-486?
Mifepristone--competitive inhibitor of progestins
This is a beta-2 agonist that relaxes the uterus and prevents premature contractions
Which SERM is used mostly for osteoporosis?
What is the use of tamsulosin? Receptor?
Treats BPH by inhibiting smooth muscle contraction? alpha 1a,d
Which OCP's cause thickening of the cervical mucus making sperm motility more difficult?
What is the MOA and use of terbutaline?
Beta-2 agonist that relaxes uterus and prevents premature contractions
MOA of testosterone and methyltestosterone
Agonist at androgen receptors
What is testosterone and methyltestosterone used for clinically?
Hypogonadism and forming secondary sex characteristics
AE of PDE-5 inhibitors (4)
Headache, flushing, dyspepsia (heart burn), and risk of hypotension with nitrates
How are ketoconazole and spironolactone anti-androgenics? What AE do they share?
Ketoconazole inhibits 17, 20 desmolase so inhibits steroid synthesis, Spironolactone prevents steroid binding? Both cause gynecomastia and amenorrhea
What kind of drug are anastrozole and exemestane?
4 uses of leuprolide
Infertility = pulsatile, prostate CA = continuous and with flutamide, Uterine Fibroids (continuous) and Precocious puberty (continuous)
Which drugs inhibit phosphodiesterase 5? Phosphodiesterase 3?
Sildenafil, vardenafil etc.; Cilostazol and Dipyridamole
MOA of finasteride? Uses?
5-alpha reductase inhibitor (no DHT formed)? Tx of BPH and Male Pattern Baldness
How do synthetic estrogens and progestins act as oral contraceptives?
They inhibit LH and FSH via negative feedback and therefore prevent ovulation; also, progestins thicken cervical mucus which makes it difficult for sperm to get through
Name 2 aromatase inhibitors
Anastrozole and Exemestane
What are the 2 contraindications of estrogen therapy in women?
Hx of DVT's or ER (estrogen receptor) positive breast CA
What antiandrogen is used to treat prostate cancer?
This GnRH analog is an agonist when used pulsatile and antagonist when continuous
In the context of the reproductive system, what are spironolactone and ketoconazole used for?
Preventing hirsuitism in polycystic ovarian syndrome
Which drug can be used to shrink uterine fibroids?
Continuous leuprolide (GnRH analog)
What kind of drug is danozol?
Synthetic androgen acting as a partial agonist at androgen receptors
This is a synthetic partial agonist androgen used in endometriosus and hereditary angioedema
Which repro system drugs can cause blue-green vision?
PDE-5 inhibitors-- sildenafil and vardenafil
What kind of drug is mestranol?
What 2 drugs are used in conjunction for prostate cancer?
Leuprolide (GnRH analog used CONTINUOUSLY) and Flutamide (nonsteroidal competitive inhibitor of androgens at testosterone receptor)
When are estrogens used in men?
Androgen dependent prostate CA
What are the lipid effects of testosterone?
Increase LDL and decrease HDL
Which antiandrogenic drug inhibits 17, 20 desmolase?
List the 4 antiandrogens
Finasteride, Flutamide, Spironolactone, and Ketoconazole
What is the MOA of clomiphene to induce ovulation?
Partial agonist of estrogen receptors in hypothalamus causes release of LH and FSH (induces LH surge)