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Maddy - CPR I - some pharm > BPH and ED Drugs > Flashcards

BPH and ED Drugs Flashcards

1
Q

list the alpha 1 adrenergic receptor antagonists

A
  • terazosin
  • doxazosin
  • tamsulosin
  • silodosin
  • alfuzosin
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2
Q

MOA of alpha 1 adrenergic receptor antagonists

A

relax muscle tone

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3
Q

what receptors on the prostate control smooth muscle contraction

A

alpha1A

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4
Q

what receptors on the detrusor muscle control instability

A

alpha1D

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5
Q

what receptors in the spinal cord control urinary function

A

alpha1D

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6
Q

how to alpha 1 antagonists mediate lower urinary tract symptoms

A

they compete with NE to:

  • reduce spasm
  • promote muscle relaxation
  • improve urine flow
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7
Q

terazosin and doxazosin are specific for what receptor

A

alpha 1

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8
Q

tamsulosin and silodosin are specific for what receptor

A

alpha1A and alpha1D

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9
Q

alfuzosin is specific for what receptor

A

non-specific alpha1 selective

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10
Q

what alpha 1 antagonists are uroselective (selective for prostate and bladder)

A 
tamsulosin
silodosin
alfuzosin (functional)
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11
Q

adverse effects terazosin and doxazosin

A

postural hypotension (have pt take before bed)
dizziness
fatigue

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12
Q

adverse effects tamsulosin and silodosin

A

reduced ejaculation

IFIS

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13
Q

adverse effects alfuzosin

A

QT prolongation

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14
Q

what do finasteride and dutasteride do

A

prevent enlargement and shrink the prostate

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15
Q

compare relief of symptoms between alpha 1 antagonists and steroid 5a reductase inhibitors

A

alpha 1 antagonists: rapid relief (days)

steroid 5a reductase inhibitors: delayed action, 3-6 months

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16
Q

function of steroid 5a reductase

A

convert serum testosterone to DHT in cells

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17
Q

excess SAR2 (steroid 5a reductase) leads to

A

BPH

18
Q

what does finasteride target

A

SAR2 only

19
Q

what does dutasteride target

A

dual inhibitor: SAR1 and SAR2

20
Q

what SAR is more prevalent in BPH

A

SAR2

21
Q

what is the effect of finasteride and dutasteride on prostate DHT, prostate serum antigen, and serum testosterone

A

90% decrease in DHT
50% decrease in PSA
15-20% increase in T

22
Q

compare the effect of finasteride and dutasteride on serum DHT

A

finasteride: 70% decreased DHT
dutasteride: 90% decreased DHT

23
Q

adverse effects of finasteride and dutasteride

A

ED
gynecomastia
depressed libido
ejaculation disturbances

24
Q

why do you have to use caution when prescribing finasteride and dutasteride to pts with liver abnormalities

A

these drugs are metabolized by CYP3A4

25
Q

describe the pathway to an erection

A

sexual stimulation –> L-arginine stimulates NOS to release NO –> increase in cGMP –> decrease in Ca2+ –> smooth muscle relaxation –> erection

26
Q

molecular mechanism behind PDE-5 inhibition

A

PDE-5 normally degrades cGMP to 5’GMP which stops the pathway towards erection, and PDE-5 inhibitors block this to maintain the erection

27
Q

why is sildenafil an effective PDE-5 inhibitor

A

it is structurally similar to cGMP and competitively inhibits PDE-5

28
Q

compare onset between the PDE-5 inhibitors

A

all are 60mins except avanafil with is 15 min for the high dose and 30 for normal dose

29
Q

compare duration of action between the PDE-5 inhibitors

A

sildenafil: 4 hrs
vardenafil: 4-5 hrs
tadalafil: 36 hrs
avanafil: 4 hrs

30
Q

stomach contents requirements for PDE-5 inhibitors

A

sildenafil and verdenafil: empty

tadalafil and avanafil: doesn’t matter

31
Q

clearance of PDE-5 inhibitors

A

hepatic CYP3A4

32
Q

side effects PDE5 inhibitors

A

HA
dyspepsia (indigestion)
nasal congestion

33
Q

side effects of PDE6-related inhibitors

A

blue/blurred vision

34
Q

specific tadalafil side effects

A

back pain
myalgia
limb pain

35
Q

why can’t you prescribe PDE-5 inhibitors to pts on organic nitrates

A

with PDE-5 inhibitors, you’re preventing the breakdown of cGMP which forms from NO, if you prescribe nitrates you’re going to have too much NO which will cause dangerous hypotension

36
Q

contraindications to vardenafil

A

pts needs to be hemodynamically stable

37
Q

contraindications to tadalafil

A

concurrent alpha1-blockers not recommended

38
Q

contraindications to sildenafil

A

concurrent alpha blockers initiated at lower recommended dose

39
Q

describe the mechanism for how alprostadil works

A

alprostadil stimulates PGE1 –> stimulates adenylate cyclase to increase camp –> decreases Ca2+ –> smooth muscle relaxation –> erection

40
Q

adverse effects alprostadil

A

prolonged erection

Maddy - CPR I - some pharm (25 decks)

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