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Renal II Quizam #2 > Lecture 2: Male GU Pharm > Flashcards

Lecture 2: Male GU Pharm Flashcards

1
Q

Which α receptor is on the detrusor m. and when stimulated by NE can lead to detrusor instability?

A

α1D

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2
Q

Which α receptor subtype is found on prostate smooth muscle and is resposnsible for contraction when stimulated by NE?

A

α1A

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3
Q

Which two α1 receptor antagonists used in BPH are selective for the α1 >>>> α2 receptor?

A
  1. Terazosin
  2. Doxazosin
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4
Q

What are the AE’s associated w/ terazosin and doxazosin used to treat BPH?

A

Postural hypotension, dizziness, fatigue –> α1 receptor antagonists

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5
Q

Which two α1 receptor antagonists used for BPH are uroselective and bind α1A = α1D?

A

1) Tamsulosin
2) Silodosin

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6
Q

What are the AE’s associated with tamsulosin and silodosin used for BPH?

A
  • Reduced ejaculation
  • IFIS = intraoperative floppy iris syndrome
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7
Q

Which α1 receptor antagonist has functional uroselectivity and is used to treat BPH?

A

Alfuzosin

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8
Q

What is a serious AE associated with Alfuzosin used in treatment of BPH?

A

QT prolongation

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9
Q

Which three α1 receptor antagonists used in BPH increase the concentration of CYP3A4 substrates?

A
  • Tamsulosin
  • Silodosin
  • Alfuzosin
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10
Q

What is the best monotherapy for prompt relief of BPH symptoms (days)?

A

α1 receptor antagonists

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11
Q

Alfuzosin should not be given to tx BPH in patients with what impairment?

A

Hepatic impairment

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12
Q

What are the two steroid 5α-reductase inhibitors used for BPH?

How quickly do they work?

A
  • Finasteride and Dutasteride
  • Delayed action –> shrinkage and sx relief in 3-6 months
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13
Q

What are the direct effects (MOA) of steroid 5α reductase inhibitors?

A
  • Directly inhibit production of DHT in prostate epithelial cells
  • Cause TestosteroneaccumulationandDHT depletion
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14
Q

Which steroid 5α reductase inhibitor is specific for SAR-2?

A

Finasteride = SpeciFIc inhibitor of SAR-2

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15
Q

Which steroid 5α-reductase inhibitor is a dual inhibitor of both SAR-1 and 2?

A

Dunasteride = DUal inhibitor

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16
Q

Which steroid 5α-reductase (SAR) is most implicated in BPH and is seen in excess in a hyperplastic prostate?

A

SAR-2

17
Q

Which steroid 5α-reductase inhibitor causes the greatest (90%) decrease in serum DHT?

A

Dutasteride

18
Q

What are 4 AE’s associated with the steroid 5α-reductase inhibitors used for BPH?

A
  1. Erectile dysfunction
  2. Gynecomastia
  3. Depressed libido
  4. Ejaculation dysfunction
19
Q

Caution should be taken when using 5α-reductase inhibitors in pts with what?

A

Liver abnormalities –> metabolized by hepatic CYP3A

20
Q

Which PDE-5 inhibitor is now approved by the FDA to treat BPH as well as erectile dysfunction?

A

Tadalafil

21
Q

Which PDE-5 inhibitor can be taken 15 mins prior (high dose) or 30 mins prior (normal dose) for ED?

A

Avanafil

22
Q

What are 2 AE’s of the PDE-5 inhibitors sildenafil, vardenafil, and avanafil due to binding PDE-6 in the retina at high doses?

A
  • Blue vision
  • Blurred vision
23
Q

What are 3 less common AE’s specific to tadalafil?

A
  • Back pain
  • Myalgia
  • Limb pain
24
Q

What is a major contraindication for PDE-5 inhibitors?

Why?

A
  • Organic nitrates
  • Extreme and dangerous hypotension
25
Q

If using tadalafil for BPH, what should not be used at the same time?

A

Concurrent α1-blockers

26
Q

Patients need to be what before starting vardenafil?

A

Hemodynamically stable

27
Q

What are 2 second-line ED therapies?

A
  • Vacuum erection devices
  • Penile injections w/ alprostadil –> PGE 1 agonist
28
Q

What is the MOA of Alprostadil?

A
  • Leads to increases in cAMP
  • Decreases in iCa2+
  • Smooth muscle relaxation
  • Erection
29
Q

What is a serious AE of Alprostadil used as an alternative ED tx?

How does it need to be dealt with or can progress to what?

A
  • Prolonged erection (priapism)
  • Medical emergency! Need to evacuate clogged blood
  • Can result in permanent corporal fibrosis and ED
30
Q

What is the pharmacological treatment for prolonged erection (priapism)?

A

Sympathomimetic (phenylephrine) + aspiration

31
Q

What is recommended for using Sildenafil for ED and a concurrent α1-blocker for BPH?

A

Concurrent α-blockers initiated at lowest recommended dose

Renal II Quizam #2 (12 decks)

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