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
Patient has erectile dysfunction due to non-gonadal cause. Treat with hat?
Agent to RELAX corpus cavernosum smooth muscle
26
2 major groups for treatment of ED
- Phosphodiesterase type 5 inhibitors | - Prostaglandins
27
Phosphodiesterase type 5 inhibitor drugs for ED
Sildenafil (Viagra) Vardenafil Tadalafil (Cialis)
28
Prostaglandin drug for ED (what is is?)
Alprostadil (PGE1 analog)
29
A patient is treated with a phosphodiesterase type 5 inhibitor for ED. What is the primary MOA?
Nitric oxide release from NANC neurons --> cGMP --> smooth muscle relaxation --> increased blood flow to penis
30
Compare/contrast the 3 PDE5 inhibitors
Sil, Vard = 1 hour onset, 5-6 hour duration | Tad = 2 hour onset, 36 hour duration
31
First line treatment of ED? Administered how?
PDE5 inhibitors Oral
32
Adverse effects of all PDE5 inhibitors
Hypotension, headache, dizzy, flushing, PRIAPISM
33
Adverse effect of Sil and Vard
Impaired blue-green vision, vision loss (PDE6 inhibition)
34
Adverse effect of Tad
Lower back and limb pain (PDE11 inhibition)
35
Drug interactions?????
/
36
Alprostadil administration MOA?
Intra-cavernosal injection EP2 receptor agonism --> cAMP --> smooth muscle relaxation --> increased blood flow to penis
37
When is alprostadil used? Why?
IF PDE5 inhibitors are not effective Pain/burning at injection, fibrotic plaques at injection site, hematomas/bruising at injection, priapism
38
If intra-cavernosal injection of alprostadil is ineffective, next option?
Intra-urethral alprostadil
39
Flibanserin
CNS 5HT1-A receptor agonist, 5HT1-2 antagonist | Treatment of HYPOACTIVE SEXUAL DESIRE DISORDER (women)
40
Contraindications of Flibanserin use
Alcohol, liver damage, CYP3A4 inhibitors
41
CYP 3A4 inhibitors to avoid with Flibanserin
Protease inhibitors, macrolide antibiotics, antifungal azoles
42
Adverse effects of Flibanserin
Dizziness, nausea, sleepiness, fainting
43
3 sites of control of micturition (w/ control type)
``` Detrusor muscle (cholinergic M3) Intrinsic sphincter (alpha-1) External sphincter (voluntary) ```
44
Stress urinary incontinence
Urethral underactivity via physical exertion
45
Urge urinary incontinence
Bladder (detrusor) overactivity
46
Drugs to avoid w/ urinary incontinence (6)
Diuretics, cholinesterase inhibitors, muscarinic agonists, alpha-1 antagonists, alpha-2 agonists, ACE inhibitors
47
How to treat urge urinary incontinence
- Relax detrusor (muscarinic antagonist, anticholinergic)
48
How to treat stress urinary incontinence
- Improve intrinsic sphincter (alpha-1 agonist, antidepressants, estrogen (women))
49
Oxybutynin
Non-selective muscarinic antagonist | Tx of urinary incontinence
50
Trospium
Same as oxybutynin
51
4 M3 selective antagonists Function?
- Tolterodine (PREFERRED) - Darifenacin - Solifenacin - Fesoterodine (NEWEST) Relax detrusor
52
Benefit of Fesoterodine
Hydrolyzed to same active metabolite as Tolterodine, and MORE CONSISTENT levels of it
53
Adverse actions of muscarinic antagonists
Typical sympathetic symptoms
54
Other way to relax detrusor besides M3 antagonism?
BOTOX - indirect anticholinergic (local injection)
55
Alpha-1 agonists for treating stress urinary incontinence Function?
Ephedrine (NE release increased) Midodrine (alpha-1 agonist) Improve intrinsic sphincter via alpha-1
56
Adverse effects of alpha-1 agonists
Insomnia, HTN, worsened MI, arrhythmias
57
Other ways to increase internal sphincter besides alpha-1 agonists?
Antidepressants (Imipramine, Duloxetine) | Estradiol
58
Imipramine
Tri-cyclic antidepressant SUI treatment Blocks re-uptake of NE Increases sympathetics on sphincter
59
Duloxetine
SSRI antidepressant SUI treatment Blocks re-uptake of NE and serotonin Increases sympathetics on sphincter
60
Estradiol Administration?
SUI treatment Increases urethral epithelium Enhances local blood circulation Increases expression of urogenital alpha-1 receptors TOPICAL only
61
When is estradiol particularly indicated for SUI?
Women with vaginitis or urethritis + SUI