Drugs for GU Disorders - Konorev Flashcards

1
Q

Cause of epithelial tissue hyperplasia

A

androgens

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2
Q

Cause of stromal tissue hyperplasia

A

estrogens

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3
Q

aromatase

A

converts androgens to estrogens

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4
Q

Tx: dynamic prostatic pathogenic factors

A

selective alpha-1 andrenergic antagonists

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5
Q

Tx: static prostatic pathogenic factors

A

5alpha-reductase inhibitors

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6
Q

second generation alpha-1 andrenergic antagonists

A
  • terazosin
  • doxazosin
  • alfuzosin
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7
Q

third generation alpha-1 andrenergic antagonists

A
  • tamulosin

- silodosin

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8
Q

5alpha-reductase inhibitors

A
  • finasteride

- dutasteride

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9
Q

benefits of using alpha-1 and antagonisis over 5alpha-reductase inhibitors

A
  • faster acting
  • effective reduction of LUTS
  • ass’d w/ less sexual dysfxn
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10
Q

alfuzosin

A
  • second generation alpha-1 and antagonist
  • more uroselective (d/t PK not selectivity)
  • doesn’t need titration
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11
Q

AE: doxazosin

A
  • may cause orthostatic hypotension
  • first does syncope
  • dizziness
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12
Q

AE: terazosin

A
  • may cause orthostatic hypotension
  • first does syncope
  • dizziness
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13
Q

tamsulosin

A
  • alpha-1A selective (prostatic sm), some 1B activation (vasculature)
  • used in BPH pts who have significant orthostatic hypotension
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14
Q

silodosin

A
  • highly alpha-1A selective
  • no orthostatic hypotension
  • severe ejaculatory dysfxn
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15
Q

AE: alpha-1 antagonists

A
  • syncope, dizziness, hypotension (2nd gen)
  • ejaculatory dysfxn (3rd gen)
  • nasal congestion
  • flu-like s/s
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16
Q

DI: alpha-1 antagonists + PDE5 inhibitor

A

marked systemic hypotension

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17
Q

DI: alpha-1 antagonists + cimetidine, diltiazem

A

decreased alpha-1 antagonists metabolism

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18
Q

DI: alpha-1 antagonists + carbamazepine, phenytoin

A

increased metabolism

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19
Q

MOA: finasteride

A
  • selective type II reductase inhibitor

- inhibits DHT synthesis from T

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20
Q

MOA: Dutasteride

A
  • non-selective ( type I and II) reductase inhibitor

- inhibits DHT synthesis from T

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21
Q

Type I enzyme reductase locations

A

skin, hair follicles, liver

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22
Q

Type II enzyme reductase locations

A

prostate, genital tissue, scalp

-responsible for epithelial tissue enlargement in prostate

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23
Q

MOA: 5alpha-reductase inhibitors

A
  • reduce DHT formation
  • prevent AR activation
  • shrink prostate
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24
Q

negative aspects of 5alpha-reductase inhibitors

A
  • need 6-12 m to develop effect
  • more pronounced sexual dysfunction
  • “second-line” agent
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25
Q

when to use 5ARi over A1AAs

A
  • severe prostatic enlargement (40g or >)
  • andrenergic ant contraindications
  • pts with high PSA (>1.4 ng/ml)
26
Q

drug classes that exacerbate BPH

A
  • T replacement therapy
  • alpha-and agonists
  • antimuscarininc drugs
27
Q

types of organic ED

A
  • hormonal
  • neurologic
  • vascular
28
Q

Oral phosphodiesterase type 5 inhibitors

A
  • sildenafil
  • vardenafil
  • tadalafil
29
Q

injectable or intraurethral prostaglandins

A

alprostadil

30
Q

unapproved ED tx agents

A
  • phentolamine
  • papaverine
  • trazodone
31
Q

MOA: PDE-5 inhibitor

A
  • stops degredation of cGMP
  • cGMP used to decreased the intracellular Ca2+
  • decreased intracellular Ca2+ = smooth mm relaxation = erection!
32
Q

DOA: sildenafil and vardenafil

A
  • onset = 1 hr

- DOA = 5-6 hr

33
Q

DOA: tadalafil

A
  • onset = 2 hr

- DOA = 36 hr

34
Q

AE: PDEi

A
  • hypotension
  • HA
  • dizziness
  • flushing
  • priapism
35
Q

unique AE: sildenafil & vardenafil

A

-visual defects: impaired blue-green discrimination d/t PDE6

36
Q

unique AE: tadalafil

A

-lower back mm & limb pain d/t PDE11 inhibition

37
Q

DI: PDEi

A
  • nitrates: severe hypotension
  • alpha1-adrenergic ants
  • EtOH: orthostatic hypertension
38
Q

MOA: Alprostadil

A

-acts via EP2 receptor to cause smooth mm relaxation

39
Q

AE: Alprostadil

A
  • pain and burning at injection site
  • fibrotic plaque formation
  • hematomas & brusin
  • priaprasm
40
Q

Use of flibanserin

A

enhance sexual desire in women

41
Q

MOA: flibanserin

A
  • postsynaptic 5HT1A receptor agonist

- 5HT2A receptor antagonist

42
Q

AE: flibanserin

A
  • dizziness
  • nausea
  • sleepiness
  • syncope (espt w/ etoh use)
43
Q

CI:flibanserin

A
  • etoh use
  • liver damage
  • concomitant use of CYP3A4i
44
Q

detrusor mm receptor

A

cholinergic M3 (ANS)

45
Q

intrinsic sphincter mm receptor

A

alpha-1 AR (ANS)

46
Q

external sphincter mm receptor

A

nicotinic (voluntary control)

47
Q

stress urinary incontinence

A

occurs as a result of physical exertion - anything that increases intrabdominal pressure - urethral underactivity

48
Q

urge urinary incontinence

A

detrusor mm overactivation, contracts during filling phase - bladder overactivity

49
Q

drugs that aggrevate UI manifestation

A
  • diuretics
  • AChEi
  • mAChR agonists
  • alpha1- adrenergic antagonistis
  • alpha2-adrenergic agonists
  • ACEi
50
Q

nonselective mAChR antagonists used in UI

A
  • oxybutynin (MC)

- trospium

51
Q

M3 R selective mAChR antagonists used in UI

A
  • darifenacin
  • solifenacin
  • tolerodine: drug of choice
  • festoerodine: same active metabolite as toler-
52
Q

MOA: mAChR antagonists in UI

A
  • relax detrusor muscle
  • increase bladder capacity
  • prevent urgency
53
Q

AE: mAChR antagonists in UI

A
  • dry mouth
  • constipation
  • dry eyes
  • tachy
  • cognitive impairment, confusion, memory loss
  • vision impairment
54
Q

indirect anticholinergic drug

A

botox

55
Q

clinical use of botox in UI

A
  • local injection into detrusor mm

- mm paralysis lasst from 3-9 mos

56
Q

andrenergic agonists used to tx UI

A
  • ephedrine

- midodrine

57
Q

MOA: midorine

A
  • alpha-1AR selective agonist

- improve intrinsic sphincter

58
Q

AE: midodrine

A
  • isomnia
  • elevated BP
  • myocardial ischemia exacerbation
  • cardiac arrhythmias
59
Q

MOA: impramine

A

tricyclic antidepressant used to tx UI

  • blocks NE reuptake
  • antimuscarinic effect
  • increases intrinsic sphincter tone
60
Q

MOA: dulozetine

A

antidepressant used to tx UI

  • block NE and 5HT reuptake
  • increases intrinsic sphincter tone
61
Q

MOA: estrogens

A
  • increase urethral epi prolif
  • enhance local blood circulaiton
  • increase urogenital alpha1-andrenergic receptors
  • only topical use!