RPM Pharm Quiz Flashcards
List SERMs (2)
tamoxifen, raloxifene
MOA and use of SERMs
competes with estrogen for receptor binding (competitive antagonist)
for breast cancer treatment
(tamoxifen, raloxifene)
Toxicity of Tamoxifen
increased risk of VTE (inhibits anti-thrombin while increasing fibrinogen VII and X)
List Aromatase inhibitors (3)
letrozole, anastrozole, exemestane
aromatase inhibitor MOA and use
inhibit conversion of androgens into estrogens
(prevents androstenedione to estrone and testosterone to estradiol)
for breast cancer treatment
(letrozole, anastrozole, exemestane)
What population is aromatase inhibitors effective in? which is it not?
effective in post-menopausal women
not effective in pre-menopausal
(letrozole, anastrozole, exemestane)
What types of drugs can be used in overactive voiding dysfunction?
M3 antagonist and B3 agonist
What types of drugs can be used in urinary retention or incomplete voiding?
M3 agonists and alpha 1 antagonist
M3 agonist and MOA
bethanechol
contraction of detrusor muscle
M3 antagonist and MOA
oxybutynin
relaxation of detrusor muscle
B3 agonist and MOA
mirabegron
relaxation of detrusor muscle
alpha antagonist and MOA
tamsulosin
relaxation of urethral smooth muscle
Oxybutynin has what type of side effects?
anti-cholinergic
blurred vision, pupil dilation, constipation, xerostomia, sedation
(M3 antagonist)
Mirabegron side effects
constipation, xerostomia, hypertension
B3 agonist
tamsulosin side effect
hypotension (vasorelaxation), somnolence
alpha 1 antagonist
What medication can cause ED?
beta blockers due to decreased BP
List PDE5 inhibitors (4)
Avanafil, tadalafil, sildenafil, vardenafil
What is unique about Tadalafil?
Very long half-life (17 hrs)
PDE5 inhibitor
What side effect is specific to vardenafil?
prolonged QT
PDE5 inhibitor
What is a side effect specific to PDE5 inhibitors?
cyanopsia
Avanafil, tadalafil, sildenafil, vardenafil
What drug interaction must be avoided with PDE5 inhibitors?
nitrates-huge risk for hypotension
Can you mix PDE5 inhibitors and alpha 1 antagonists?
yes, but use 3rd generation alpha 1 antagonists that are selective for alpha1a receptors (tamsulosin and silodosin)
What drugs can also be used to treat pulmonary arterial hypertenstion?
tadalafil and sildenafil
PDE5 inhibitors
What is the opium derived PDE5 inhibitor?
papaverine (delivered IC) for ED
What alpha 1 antagonist can be used alone to treat ED?
phentolamine-vasorelaxation, increased penile blood flow
PGE1 analog and what it treats
alprostadil to cause vasodilation for ED treatment
What enzyme converts testosterone to dihyrotestosterone
5 alpha reductase
5 alpha reductase inhibitor? what does it treat?
finasteride for BPH
Other uses for finasteride
decrease risk for prostate cancer, prevent/reverse androgenic alopecia
(5 alpha reductase inhibitor)
Tadalafil is a possible treatment for? (although unconfirmed)
BPH
PDE5 inhibitor
Ketoconazole MOA and use
inhibits androgen synthesis
part of androgen deprivation therapy (ADT) in prostate cancer
Leuprolide MOA and use
downregulates GnRH receptor and inhibits testosterone synthesis as part of ADT for prostate cancer
androgen receptor antagonists (2)
flutamide and spironolactone
PDE5 inhibitor MOA and use
inhibit the breakdown of cGMP, leading to vasodilation/vascular smooth muscle relaxation
for ED
androgen receptor antagonist MOA
antagonize the binding of DHT to androgen receptor
flutamide, spironolactone
List natural estrogens (3)
estradiol (E2), estrone (E1), estriol (E3)
List synthetic estrogens (3)
ethinyl estradiol, diethylsilbestrol, mestranol
List synthetic progestins (3)
etonogestrel, levonorgestrel, norethindrone
What is the MOA of combine OCPs?
maintain high levels of estrogen and progestin, “mimicking pregnancy”
-inhibit maturation, ovulation, fertilization and implantation
What are progestin’s effects on endometrial development and cervical mucus?
inhibits endometrial development-inhibiting implantation
increases cervical mucus-blocking sperm from fertilization
What does the progestin mini pill prevent?
implantation and fertilization
What are the 3 combined OCP formulations
cyclic, extended cycle and continuous cycle
define monophasic v. bi/triphasic OCPs
monophasic-every pill contains the same doses of estrogen and progestin
bi/triphasic-pills vary in dosses of estrogen and/or progestin
Other benefits of OCPs
decreased bleeding, lighter periods, decreased dysmenorrhea, decreased acne, increased bone density
OCPs effects on cancer risk
increased risk in breast (ER+/PR+), cervical and liver (estrogen dependent) cancer
decreased risk in ovarian endometrial and colorectal cancer
OCPs are conraindicaetd in wha populaion
those with cardiovascular risk
can at time use mini pill instead
What type of drugs can decrease effectiveness of OCPs?
anti-epileptic drugs by inducing metabolism
anti-bacterial drugs by reducing enterohepatic circulation (not recycled by bacteria)
List emergency contraception and their mechanism of action
- levonorgestrel, ulipristal
- take within 24-72 hours of intercourse
MOA: inhibit LH surge and ovulation
What medication is used for medical abortion? MOA?
Mifepristone (RU-486)
-disrupts the endometrium (by inhibiting progesterone effect on endometrial development), terminating the pregnancy
What is mifepristone often paired with? why?
misoprostol
-induces uterine contraction
What is estrogens effects on LDL levels?
estrogens reduce serum LDL levels by regulating lipid metabolism in the liver
What is estrogens effects on bones?
estrogens inhibit bone resorption by inhibiting osteoclasts and stimulating osteoblasts
Main 2 steps in treating ovulatory infertility
- downregulate GnRH receptors and inhibit gonadotropin release
- administer hormones that stimulate maturation and ovulation
What drug down regulate GnRH receptors and can be used to treat ovulatory infertility?
leuprolide
What hormones are administered to stimulate maturation and ovulation? and what does each do?
- rFSH- stimulates estradiol production and follicle maturation
- hCG- mimics LH surge and stimulates ovulation
What drug with a different MOA may promote maturation and ovulation? how?
clomiphene (SERM)
disinhibits HPG axis and promotes maturation and ovulation (anti-estrogenic effect: inhibits estrogens negative feedback on axis)
When is clomiphene administered?
on days 3-7 to promote FSH and LH release midcycle to induce ovulation
Clomiphene toxicities
superovulation effects: abdominal pain/bloating, ectopic pregnancy, fraternal twins
menopause like symptoms: mood swings, hot flashes
increased risk of VTE
What drug disinhibits the HPG axis and can promote spermatogenesis?
clomiphene
What can directly stimulate spermatogenesis?
rFSH and LH/hCG
What drug inhibits the conversion of testosterone to estradiol in obesity associated hypogonadism?
anastrozole (aromatase inhibitor)
What causes PMS/PMDD?
sensitivity to monthly estrogen/progesterone fluctuations
What can be used to prevent monthly fluctuation of estrogen/progesterone?
OCPs and leuprolide
What can be used during menopause to mediate symptoms?
estradiol, progesterone and medroxyprogesterone
-to maintain non-fertility benefits
What are non-fertility benefits of estrogen?
reduction of hot flashes, increase in bone mineralization
estrogen toxicities
estrogen-dependent endometrial hyperplasia
What drugs can be used to treat PCOS?
clomiphene, OCPs, spironolactone, flutamide, and finasteride
anti-androgenic drugs serve what purpose in PCOS?
inhibit activity of androgens that can cause hirsutism
clomiphene, OCPs, spironolactone, flutamide, and finasteride (also think about how each of these would do so!!)
What is OCPs MOA in PCOS?
stimulate expression of SHBG reducing free testosterone
How do OCPs help in endometriosis?
inhibit the HPG axis and interrupt the growth/shrinkage cycle
this includes OCPs, levonorgestrel, and medroxyprogesterone
progestin-only pills may also be effective
What is Danazol’s MoA
androgenic effects that inhibit the HPG axis, also increases levels of free testosterone in plasma by binding SHBG and kicking testosterone off (in endometriosis)
-has a lot of side effects so not really used anymore
What is a GnRH receptor antagonist used to treat endometriosis?
elagolix
-blocks the receptors
what is a GnRH receptor agonist that treats endometriosis?
leuprolide
-decreases number of receptors
What role does progestin treatment play in menopause?
prevents estradiol induced endometrial hyperplasia
therefore not needed in individuals who have had a hysterectomy
What is the cause of increased risk of VTE w/ SERMs?
estrogenic effect on liver cells that produce clotting factors
