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Pharmacology > BPH and ED > Flashcards

BPH and ED Flashcards

1
Q

Terazosin specificity

A

alpha1»»>alpha2

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2
Q

terazosin uroselectivity

A

No

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3
Q

Terazosin adverse effects

A

postural hypotension, dizziness, fatigue

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4
Q

Terazosin drug interactions

A

PDE-5 inhibitors (sildenafil, vardenafil–>used for ED)

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5
Q

Doxazosin specificity

A

alpha1»»>alpha2

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6
Q

Doxazosin uroselectivity

A

No

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7
Q

doxazosin adverse effects

A

postural hypotension, dizziness, fatigue

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8
Q

Doxazosin drug interactions

A

PDE-5 inhibitors

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9
Q

tamsulosin specificity

A

alpha1A = alpha1D > alpha1B

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10
Q

Where are alpha1A and alpha1D receptors located?

A

prostate and bladder

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11
Q

tamsulosin uroselectivity

A

yes, alpha1A = alpha1D

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12
Q

Tamsulosin adverse effects

A

reduced ejaculation, IFIS

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13
Q

Tamsulosin drug interactions

A

PDE-5 inhibitors (sildenafil, vardenafil); increase concentrations of CYP 34A substrates

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14
Q

What is the best mono therapy for prompt relief of symptoms (days)?

A

alpha1 adrenergic receptor antagonists

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15
Q

What is the benefit of alfuzosin?

A

has functional uroselectivity

distributes into the prostate > serum

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16
Q

When do you take alfuzosin?

A

immediately after the same meal every day

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17
Q

When do you avoid using alfuzosin?

A

hepatic impairment

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18
Q

Steroid 5alpha reductase inhibitors

A

finasteride, dutasteride

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19
Q

What do steroid 5alpha reductase inhibitors do and how long does it take for them to work?

A

prevents enlargement and shrinks prostate

shrinkage and symptom relief takes 3-6 months

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20
Q

Why does the prostate enlarge?

A

aging + dihydrotestosterone

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21
Q

What enable prostate epithelium survival and growth?

A

testosterone and dihydrotestosterone \

androgenic steroids

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22
Q

What do steroid 5alpha-reductase (SAR) type 1 and 2 do?

A

convert serum T to DHT in cells

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23
Q

What does a prostate that has undergone hyperplasia have an excess in?

A

SAR-2

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24
Q

DHT “starvation” causes what?

A

epithelial atrophy, shrinkage, and gradual relief of LUTS

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25
Q

Direct effects of SARs

A

T accumulation

DHT depletion

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26
Q

Indirect effects of SARs

A

androgen receptor less occupied

no gene transcription

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27
Q

Finasteride selectivity

A

specific inhibitor to SAR-2

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28
Q

Dutasteride selectivity

A

dual inhibitor of SAR-1 and SAR-2

29
Q

SAR in BPH

A

SAR 2&raquo_space; SAR 1

30
Q

Prostate DHT with finasteride and dutasteride

A

90% decreased

31
Q

Prostate serum Ag with finasteride and dutasteride

A

50% decreased

32
Q

Serum T with finasteride and dutasteride

A

15-20% increased

33
Q

Serum DHT with finasteride

A

70% decreased

34
Q

Serum DHT with dutasteride

A

90% decreased

35
Q

Why is there a larger decrease in serum DHT with dutasteride?

A

SAR-1 is in the serum and that is what dutasteride acts on

36
Q

Adverse effects of finasteride and dutasteride

A

ED
gynecomastia
depressed libido
ejaculation disturbances

37
Q

Are dosage adjustments necessary with finasteride and dutasteride?

A

No, not for age or renal insufficiency

38
Q

What are the significant drug interactions with finasteride and dutasteride?

A

None

39
Q

When should you use caution with finasteride and dutasteride?

A

liver abnormalities because it is metabolized by hepatic CYP3A

40
Q

When do you use combination therapy with alpha1 adrenergic antagonists and 5alpha reductase inhibitors?

A

severe symptoms of BPH, known to have large prostate, no response to monotherapy

41
Q

What is a positive of combo therapy?

A

long-term significantly improves pt symptoms (66%) vs either drug alone

42
Q

Tadalafil

A

PDE-5 inhibitor
treats BPH
used for pts with

43
Q

Erectile dysfunction

A

consistent or recurrent inability to acquire or sustain an erection of sufficient rigidity and duration for sexual intercourse

44
Q

What are the risk factors for acquiring ED?

A

obesity
smoking
stress

45
Q

What facilitates smooth muscle relaxation to get an erection?

A

Nitric oxide–>maximizes blood flow—>penile engorgement

46
Q

Where does blood flow to get an erection?

A

corpora cavernosa and corpus spongiosum

47
Q

What does sildenafil (Viagra) do?

A

keeps the erection one already has; it does NOT cause an erection

48
Q

How does sildenafil work?

A

Competitively inhibits PDE-5–>cGMP cannot bind –>maintained erection

49
Q

Sildenafil onset, duration of action, stomach contents required, half life, and clearance

A 
60
4
empty
4
Hepatic CYP34A
50
Q

Vardenafil onset, duration of action, stomach contents required, half life, and clearance

A 
60
4-5
empty
4
hepatic CYP34A
51
Q

Tadalafil (Cialis) onset, duration of action, stomach contents required, half life, and clearance

A 
60
36
doesn't matter
18
Hepatic CYP 34A
52
Q

Avanafil (Stendra) onset, duration of action, stomach contents required, half life, and clearance

A 
15 (high dose); 30 (normal dose)
4
doesn't matter
4
Hepatic CYP34A
53
Q

Where is PDE-5 located in the body?

A

corpus cavernosum; also in and around heart

54
Q

Side effects of PDE-5 inhibitors

A

headache (15%), dyspepsia (5-10%), nasal congestion (5-10%)

55
Q

Where is PDE-6 located in the body?

A

Retina

56
Q

PDE6-related side effects

A

blue/blurred vision

57
Q

What drugs are PDE-6 related

A

sildenafil
vardenafil
avanafil

58
Q

What side effects are specific to tadalafil

A

back pain, myalgia, limb pain

59
Q

Contraindications of PDE-5 inhibitors

A

ORGANIC NITRATES–>EXTREME AND DANGEROUS HYPOTENSION
Organic nitrates stimulate NO to be present already, so if you take these, there will be too much NO–>too much smooth muscle relaxation

60
Q

Contraindications to vardenafil

A

hemodynamically unstable

61
Q

Contraindications to tadalafil

A

when used for BPH, concurrent alpha1-blockers not recommended

62
Q

Contraindications to sildenafil

A

concurrent alpha-blockers initiated at lowest recommended dose

63
Q

Second-line ED therapies

A

vacuum erection devices

penile injections with alprostadil–>prostaglandin E1

64
Q

Another name for alprostadil

A

caverject

65
Q

How does alprostadil work?

A

increased cAMP and erection

stimulates the beginning of the process to get an erection

66
Q

Adverse effects of alprostadil

A

prolonged erection (priapism)

67
Q

How do you treat priapism?

A

sympathomimetic (phenylephrine) and aspiration

68
Q

MOA of alprostadil

A

Prostaglandin E-1 agonist

Pharmacology (3 decks)

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