Drugs for GU Disorders Flashcards

1
Q

2 manifestations of benign prostatic hyperplasia

A
  • Painful/difficult urination (compression of urethra)

- Frequent urination (compression of bladder)

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2
Q

Dynamic pathogenic cause of BPH

A

Excessive alpha-adrenergics

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3
Q

Static pathogenic causes of BPH

A
  • Epithelial hyperplasia via androgens

- Stromal hyperplasia via estrogens

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4
Q

Which causes of BPH can be treated clinically?

A
  • Alpha-adrenergic excess

- Epithelial hyperplasia via androgens

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5
Q

FIRST CHOICE for treating BPH?

Why? (5)

A

Alpha-1 antagonists

Faster acting, more effective, does not affect PSA level, does not reduce prostate size, has less sexual dysfunction

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6
Q

Terazosin

A

Second-generation alpha-1 antagonist
Treatment of BPH
Side effects = orthostatic hypotension, syncope, dizziness
Requires does titration

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7
Q

Doxazosin

A

Second-generation alpha-1 antagonist
Treatment of BPH
Side effects = orthostatic hypotension, syncope, dizziness
Requires dose titration

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8
Q

Alfuzosin

A

Second-generation alpha-1 antagonist
Treatment of BPH
UROSELECTIVE - no systemic side effects
Does NOT require dose titration

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9
Q

Alpha-1 receptors involved in BPH

A
1A = prostatic smooth muscle
1B = vasculature
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10
Q

Tamsulosin

A

Third-generation alpha-1 antagonist
Treatment of BPH
Alpha-1A > Alpha-1B

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11
Q

Silodosin

A

Third-generation alpha-1 antagonist
Treatment of BPH
ALPHA-1A (HIGHLY SELECTIVE)
NO orthostatic hypotension

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12
Q

Side effects of second-generation alpha-1 antagonists

A

Syncope, dizziness, hypotension

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13
Q

Side effect of third-generation alpha-1 antagonists

A

Ejaculatory dysfunction

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14
Q

Drug interactions?????

A

h

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15
Q

5-alpha reductase

Types?

A

Converts testosterone to DHT

Type 1 = skin, hair, liver
Type 2 = prostate, genitals, scalp

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16
Q

Important 5-alpha reductase for BPH?

A

Type 2 - causes epithelial portion enlargement in prostate

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17
Q

Maximal size decrease of prostate by 5-alpha reductase inhibitor?

A

20% - portion due to epithelial tissue

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18
Q

When are 5-alpha reductase inhibitors preferred?

A
  • SEVERELY enlarged prostate (>40g)

- Contraindications to adrenergic antagonists

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19
Q

Patient with large prostate and high PSA is treated how?

A

Combo therapy of reductase inhibitors + alpha-1 antagonist

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20
Q

Adverse effects of reductase inhibitors

A

Sexual dysfunction (multiple)
Teratogenesis (pregnancy)
Increased risk of INVASIVE prostate cancer
Gynecomastia, muscle weakness, abdominal pain

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21
Q

Patient has BPH. What do you NOT give him? (3)

A
  • Testosterone
  • Alpha agonists (decongestant - phenylephrine, ephedrine)
  • Antimuscarinics (antihistamine, antidepressant, atropine, anti-Parkinson’s drugs)
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22
Q

Finasteride

A

SELECTIVE type 2 5-alpha reductase inhibitor

Treats BPH

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23
Q

Dutasteride

A

NON-selective (types 1 and 2) 5-alpha reductase inhibitor

Treats BPH

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24
Q

Patient has hypogonadism. Treat with what?

A

Testosterone replacement

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25
Q

Patient has erectile dysfunction due to non-gonadal cause. Treat with hat?

A

Agent to RELAX corpus cavernosum smooth muscle

26
Q

2 major groups for treatment of ED

A
  • Phosphodiesterase type 5 inhibitors

- Prostaglandins

27
Q

Phosphodiesterase type 5 inhibitor drugs for ED

A

Sildenafil (Viagra)
Vardenafil
Tadalafil (Cialis)

28
Q

Prostaglandin drug for ED (what is is?)

A

Alprostadil (PGE1 analog)

29
Q

A patient is treated with a phosphodiesterase type 5 inhibitor for ED. What is the primary MOA?

A

Nitric oxide release from NANC neurons –> cGMP –> smooth muscle relaxation –> increased blood flow to penis

30
Q

Compare/contrast the 3 PDE5 inhibitors

A

Sil, Vard = 1 hour onset, 5-6 hour duration

Tad = 2 hour onset, 36 hour duration

31
Q

First line treatment of ED?

Administered how?

A

PDE5 inhibitors

Oral

32
Q

Adverse effects of all PDE5 inhibitors

A

Hypotension, headache, dizzy, flushing, PRIAPISM

33
Q

Adverse effect of Sil and Vard

A

Impaired blue-green vision, vision loss (PDE6 inhibition)

34
Q

Adverse effect of Tad

A

Lower back and limb pain (PDE11 inhibition)

35
Q

Drug interactions?????

A

/

36
Q

Alprostadil administration

MOA?

A

Intra-cavernosal injection

EP2 receptor agonism –> cAMP –> smooth muscle relaxation –> increased blood flow to penis

37
Q

When is alprostadil used?

Why?

A

IF PDE5 inhibitors are not effective

Pain/burning at injection, fibrotic plaques at injection site, hematomas/bruising at injection, priapism

38
Q

If intra-cavernosal injection of alprostadil is ineffective, next option?

A

Intra-urethral alprostadil

39
Q

Flibanserin

A

CNS 5HT1-A receptor agonist, 5HT1-2 antagonist

Treatment of HYPOACTIVE SEXUAL DESIRE DISORDER (women)

40
Q

Contraindications of Flibanserin use

A

Alcohol, liver damage, CYP3A4 inhibitors

41
Q

CYP 3A4 inhibitors to avoid with Flibanserin

A

Protease inhibitors, macrolide antibiotics, antifungal azoles

42
Q

Adverse effects of Flibanserin

A

Dizziness, nausea, sleepiness, fainting

43
Q

3 sites of control of micturition (w/ control type)

A
Detrusor muscle (cholinergic M3)
Intrinsic sphincter (alpha-1)
External sphincter (voluntary)
44
Q

Stress urinary incontinence

A

Urethral underactivity via physical exertion

45
Q

Urge urinary incontinence

A

Bladder (detrusor) overactivity

46
Q

Drugs to avoid w/ urinary incontinence (6)

A

Diuretics, cholinesterase inhibitors, muscarinic agonists, alpha-1 antagonists, alpha-2 agonists, ACE inhibitors

47
Q

How to treat urge urinary incontinence

A
  • Relax detrusor (muscarinic antagonist, anticholinergic)
48
Q

How to treat stress urinary incontinence

A
  • Improve intrinsic sphincter (alpha-1 agonist, antidepressants, estrogen (women))
49
Q

Oxybutynin

A

Non-selective muscarinic antagonist

Tx of urinary incontinence

50
Q

Trospium

A

Same as oxybutynin

51
Q

4 M3 selective antagonists

Function?

A
  • Tolterodine (PREFERRED)
  • Darifenacin
  • Solifenacin
  • Fesoterodine (NEWEST)

Relax detrusor

52
Q

Benefit of Fesoterodine

A

Hydrolyzed to same active metabolite as Tolterodine, and MORE CONSISTENT levels of it

53
Q

Adverse actions of muscarinic antagonists

A

Typical sympathetic symptoms

54
Q

Other way to relax detrusor besides M3 antagonism?

A

BOTOX - indirect anticholinergic (local injection)

55
Q

Alpha-1 agonists for treating stress urinary incontinence

Function?

A

Ephedrine (NE release increased)
Midodrine (alpha-1 agonist)

Improve intrinsic sphincter via alpha-1

56
Q

Adverse effects of alpha-1 agonists

A

Insomnia, HTN, worsened MI, arrhythmias

57
Q

Other ways to increase internal sphincter besides alpha-1 agonists?

A

Antidepressants (Imipramine, Duloxetine)

Estradiol

58
Q

Imipramine

A

Tri-cyclic antidepressant
SUI treatment
Blocks re-uptake of NE
Increases sympathetics on sphincter

59
Q

Duloxetine

A

SSRI antidepressant
SUI treatment
Blocks re-uptake of NE and serotonin
Increases sympathetics on sphincter

60
Q

Estradiol

Administration?

A

SUI treatment
Increases urethral epithelium
Enhances local blood circulation
Increases expression of urogenital alpha-1 receptors

TOPICAL only

61
Q

When is estradiol particularly indicated for SUI?

A

Women with vaginitis or urethritis + SUI