Pharmacology Flashcards
GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion (downregulates GnRH-R)
Leuprolide
Pulsatile Leuprolide use
Infertility
Continuous use of Leuprolide with Flutamide
prostate cancer
Continuous use of Leuprolide
uterine fibrinoids; precocious puberty
Toxicity of leuprolide
Antiandrogen, N/V
Bind estorgen receptors
ethinyl estradiol, DES, mestranol
Cause clear cell adenocarcinoma is exposed to in utero
DES
antagonist at estrogen receptors in hypothalamus to increase LH and FSH and therefore stimulate ovulation
Clomiphene (SERM)
Used to treat infertility due to PCOS
Clomiphene (SERM)
S/E of Clomiphene
Hot flashes; ovarian enlargement; multiple simultaneous pregnancies and visual disturbances
Antagonist on breast tissue; agonist on uterus and bone’ primarily used to treat and prevent estrogen receptor positive breast cancer
Tamoxifen (SERM)
S/E of tamoxifen
Thromboembolic events and endometrial cancer
Estorgen agonist on bone; antagonist on uterus; used to treat osteoporosis of bone
Raloxifene (SERM)
Aromatase inhibitors used in postmenopausal women with breast cancer
Anastrozole/exemestane
Binds progesterone receptors to decrease endometrial growth but increase vascularization
Progestins
Used as OCP and in the tx of endometrial cancer and abnormal uterine bleeding
Progestins
Competitive inhibitor of progestins at progesterone receptors; terminates pregnancy
Mifepristone (PGE1)
C/I of OCP
smokers >35 years old, hx f thromboembolism and stroke of history of estrogen-dependent tumor
Beta-2 agonist that relaxes the uterus; used to decrease contraction frequency in women during labor
Terbutaline
Synthetic androgen that acts as a partial agonist for endometriosis and hereditary angioedema
Danazol
Toxicity on Danazol
Weight gain, edema, acne, hirsutism, masculinization, decrease HDL, hepatotoxicity
5alpha-reductase inhibitor used for male pattern balding and BPH
Finasteride
Nonsteroidal competitive inhibitor of androgens at testosterone receptor used in prostate carcinoma
Flutamide
Inhibits steroid synthesis; inhibits 17,20 desmolase
ketoconazole
Inhibits steroid binding, 17alpha-hydroxylase, and 17,20-desmolase
Spironolactone
Used in treatment of PCOS to prevent hirsutism; both cause gynecomastia and amenorrhea
Ketoconazole and Spironolactone`
An alpha1A &1D antagonist used to tx BPH by inhibiting smooth muscle contraction
Tamosulosin
Don’t take with nitrates
sildenafil and vardenafil
MoA of sildenafil and vardenafil
Inhibits phosphodiesterase 5 causing increase in cGMP, smooth muscle relaxation of corpus cavernosum and increase blood flow to penis to get penile erection