RPM Pharm Quiz Flashcards

1
Q

List SERMs (2)

A

tamoxifen, raloxifene

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2
Q

MOA and use of SERMs

A

competes with estrogen for receptor binding (competitive antagonist)
for breast cancer treatment

(tamoxifen, raloxifene)

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3
Q

Toxicity of Tamoxifen

A

increased risk of VTE (inhibits anti-thrombin while increasing fibrinogen VII and X)

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4
Q

List Aromatase inhibitors (3)

A

letrozole, anastrozole, exemestane

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5
Q

aromatase inhibitor MOA and use

A

inhibit conversion of androgens into estrogens
(prevents androstenedione to estrone and testosterone to estradiol)
for breast cancer treatment

(letrozole, anastrozole, exemestane)

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6
Q

What population is aromatase inhibitors effective in? which is it not?

A

effective in post-menopausal women
not effective in pre-menopausal

(letrozole, anastrozole, exemestane)

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7
Q

What types of drugs can be used in overactive voiding dysfunction?

A

M3 antagonist and B3 agonist

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8
Q

What types of drugs can be used in urinary retention or incomplete voiding?

A

M3 agonists and alpha 1 antagonist

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9
Q

M3 agonist and MOA

A

bethanechol

contraction of detrusor muscle

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10
Q

M3 antagonist and MOA

A

oxybutynin

relaxation of detrusor muscle

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11
Q

B3 agonist and MOA

A

mirabegron

relaxation of detrusor muscle

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12
Q

alpha antagonist and MOA

A

tamsulosin

relaxation of urethral smooth muscle

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13
Q

Oxybutynin has what type of side effects?

A

anti-cholinergic
blurred vision, pupil dilation, constipation, xerostomia, sedation

(M3 antagonist)

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14
Q

Mirabegron side effects

A

constipation, xerostomia, hypertension

B3 agonist

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15
Q

tamsulosin side effect

A

hypotension (vasorelaxation), somnolence

alpha 1 antagonist

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16
Q

What medication can cause ED?

A

beta blockers due to decreased BP

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17
Q

List PDE5 inhibitors (4)

A

Avanafil, tadalafil, sildenafil, vardenafil

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18
Q

What is unique about Tadalafil?

A

Very long half-life (17 hrs)

PDE5 inhibitor

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19
Q

What side effect is specific to vardenafil?

A

prolonged QT

PDE5 inhibitor

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20
Q

What is a side effect specific to PDE5 inhibitors?

A

cyanopsia

Avanafil, tadalafil, sildenafil, vardenafil

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21
Q

What drug interaction must be avoided with PDE5 inhibitors?

A

nitrates-huge risk for hypotension

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22
Q

Can you mix PDE5 inhibitors and alpha 1 antagonists?

A

yes, but use 3rd generation alpha 1 antagonists that are selective for alpha1a receptors (tamsulosin and silodosin)

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23
Q

What drugs can also be used to treat pulmonary arterial hypertenstion?

A

tadalafil and sildenafil

PDE5 inhibitors

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24
Q

What is the opium derived PDE5 inhibitor?

A

papaverine (delivered IC) for ED

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25
What alpha 1 antagonist can be used alone to treat ED?
phentolamine-vasorelaxation, increased penile blood flow
26
PGE1 analog and what it treats
alprostadil to cause vasodilation for ED treatment
27
What enzyme converts testosterone to dihyrotestosterone
5 alpha reductase
28
5 alpha reductase inhibitor? what does it treat?
finasteride for BPH
29
Other uses for finasteride
decrease risk for prostate cancer, prevent/reverse androgenic alopecia (5 alpha reductase inhibitor)
30
Tadalafil is a possible treatment for? (although unconfirmed)
BPH | PDE5 inhibitor
31
Ketoconazole MOA and use
inhibits androgen synthesis | part of androgen deprivation therapy (ADT) in prostate cancer
32
Leuprolide MOA and use
downregulates GnRH receptor and inhibits testosterone synthesis as part of ADT for prostate cancer
33
androgen receptor antagonists (2)
flutamide and spironolactone
34
PDE5 inhibitor MOA and use
inhibit the breakdown of cGMP, leading to vasodilation/vascular smooth muscle relaxation for ED
35
androgen receptor antagonist MOA
antagonize the binding of DHT to androgen receptor | flutamide, spironolactone
36
List natural estrogens (3)
estradiol (E2), estrone (E1), estriol (E3)
37
List synthetic estrogens (3)
ethinyl estradiol, diethylsilbestrol, mestranol
38
List synthetic progestins (3)
etonogestrel, levonorgestrel, norethindrone
39
What is the MOA of combine OCPs?
maintain high levels of estrogen and progestin, "mimicking pregnancy" -inhibit maturation, ovulation, fertilization and implantation
40
What are progestin's effects on endometrial development and cervical mucus?
inhibits endometrial development-inhibiting implantation increases cervical mucus-blocking sperm from fertilization
41
What does the progestin mini pill prevent?
implantation and fertilization
42
What are the 3 combined OCP formulations
cyclic, extended cycle and continuous cycle
43
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
44
Other benefits of OCPs
decreased bleeding, lighter periods, decreased dysmenorrhea, decreased acne, increased bone density
45
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
46
OCPs are conraindicaetd in wha populaion
those with cardiovascular risk can at time use mini pill instead
47
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)
48
List emergency contraception and their mechanism of action
- levonorgestrel, ulipristal - take within 24-72 hours of intercourse MOA: inhibit LH surge and ovulation
49
What medication is used for medical abortion? MOA?
Mifepristone (RU-486) | -disrupts the endometrium (by inhibiting progesterone effect on endometrial development), terminating the pregnancy
50
What is mifepristone often paired with? why?
misoprostol | -induces uterine contraction
51
What is estrogens effects on LDL levels?
estrogens reduce serum LDL levels by regulating lipid metabolism in the liver
52
What is estrogens effects on bones?
estrogens inhibit bone resorption by inhibiting osteoclasts and stimulating osteoblasts
53
Main 2 steps in treating ovulatory infertility
1. downregulate GnRH receptors and inhibit gonadotropin release 2. administer hormones that stimulate maturation and ovulation
54
What drug down regulate GnRH receptors and can be used to treat ovulatory infertility?
leuprolide
55
What hormones are administered to stimulate maturation and ovulation? and what does each do?
1. rFSH- stimulates estradiol production and follicle maturation 2. hCG- mimics LH surge and stimulates ovulation
56
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)
57
When is clomiphene administered?
on days 3-7 to promote FSH and LH release midcycle to induce ovulation
58
Clomiphene toxicities
superovulation effects: abdominal pain/bloating, ectopic pregnancy, fraternal twins menopause like symptoms: mood swings, hot flashes increased risk of VTE
59
What drug disinhibits the HPG axis and can promote spermatogenesis?
clomiphene
60
What can directly stimulate spermatogenesis?
rFSH and LH/hCG
61
What drug inhibits the conversion of testosterone to estradiol in obesity associated hypogonadism?
anastrozole (aromatase inhibitor)
62
What causes PMS/PMDD?
sensitivity to monthly estrogen/progesterone fluctuations
63
What can be used to prevent monthly fluctuation of estrogen/progesterone?
OCPs and leuprolide
64
What can be used during menopause to mediate symptoms?
estradiol, progesterone and medroxyprogesterone | -to maintain non-fertility benefits
65
What are non-fertility benefits of estrogen?
reduction of hot flashes, increase in bone mineralization
66
estrogen toxicities
estrogen-dependent endometrial hyperplasia
67
What drugs can be used to treat PCOS?
clomiphene, OCPs, spironolactone, flutamide, and finasteride
68
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!!)
69
What is OCPs MOA in PCOS?
stimulate expression of SHBG reducing free testosterone
70
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
71
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
72
What is a GnRH receptor antagonist used to treat endometriosis?
elagolix | -blocks the receptors
73
what is a GnRH receptor agonist that treats endometriosis?
leuprolide | -decreases number of receptors
74
What role does progestin treatment play in menopause?
prevents estradiol induced endometrial hyperplasia therefore not needed in individuals who have had a hysterectomy
75
What is the cause of increased risk of VTE w/ SERMs?
estrogenic effect on liver cells that produce clotting factors