BPH And ED Pharmacology Flashcards

1
Q

What Adrenergic Receptor is important for stimulating Prostatic Smooth Muscle Contraction?

A

a1A

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2
Q

What Adrenergic Receptor is most important for Vascular Resistance Maintenance?

A

a1B&raquo_space; a1A

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3
Q

What Adrenergic Receptor when activated will stimulate Detrusor Muscle instability?

A

a1D > a1A

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4
Q

What adrenergic receptor functions when stimulated in the spinal cord control over urinary function?

A

a1D

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5
Q

What is the Adrenergic receptor Specificity for Doxazosin and Terazosin?

A

Doxazosin and Terazosin are Selective a1 Receptor Antagonists, However they are not selective for any particular a1 subtype

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6
Q

What is the Adrenergic receptor Specificity of Tamsulosin and Silodosin?

A

Tamsulosin and Silodosin are equally Specifically a1A & a1D Receptor Selective Antagonists, but less so for a1B

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7
Q

What Adrenergic Receptors is Alfuzosin specific for?

A

Alfuzosin is a Selective a1 Receptor Antagonist; HOWEVER, even though it is not specific for any particular a1 Subtypes, it is Uroselective and works mostly on just the Prostate and Bladder.

It should be avoided in Pt’s with Hepatic impairment though

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8
Q

What side effects might a patient experience if they take Doxazosin or Terazosin? Why?

A

Postural Hypotension
Dizziness
Fatigue

Because they are Non-Specific a1 Antagonists

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9
Q

What side effects might a patient taking Silodosin or Tamsulosin experience?

A

Reduced Ejaculation

IFIS

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10
Q

What side effects might a patient taking Alfuzosin experience?

A

QT Prolongation

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11
Q

What Drug Interactions should you be concerned about if a patient is taking Doxazosin, Terazosin, Tamsulosin, Silodosin, or Alfuzosin?

A

If a patient is taking Doxazosin, Terazosin, Tamsulosin, Silodosin, or Alfuzosin you need to be concerned about the potential interaction of these drugs with PDE-5 Inhibitors (Sildenafil/Vardenafil) for Erectile dysfunction

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12
Q

What class of drug are Finasteride and Dutasteride? What do they function to treat and how?

A

Finasteride and Dutasteride are Steroid 5a-Reductase Inhibitors

They help to relieve the symptoms of BPH by preventing prostate enlargement and causing it to shrink some

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13
Q

What is the drawback of using Steroid 5a-Reductase Inhibitors (Finasteride, Dutasteride) to treat the symptoms of BPH?

A

Steroid 5a-Reductase Inhibitors take 3-6 months of regular dosing before symptom relief will begin

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14
Q

What two hormones influence Prostatic epithelial growth and survival? Which one of them is more potent?

A

Testosterone (T) and Dihydrotestosterone (DHT)

DHT is 10x as potent

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15
Q

What enzyme converts Testosterone into DHT? In a Prostate that is undergoing Hyperplasia a such as in BPH, what subtype of this enzyme is aberrantly acting excessively?

A

Steroid 5a-Reductase (SAR)

SAR-2 acts excessively in BPH

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16
Q

What is the difference between Finasteride and Dutasteride?

A

Finasteride Targets specifically SAR-2

Dutasteride targets both SAR-1 and SAR-2

17
Q

How much do Finasteride and Dutasteride decrease DHT in individuals with BPH? How much do they decrease PSA?

A

Finasteride and Dutasteride decrease DHT by 90%, they also decrease PSA by 50%

18
Q

What is the one clinical consideration that should be kept in mind when giving a Pt Finasteride or Dutasteride?

A

Caution should be used in Pt’s with Liver abnormalities

19
Q

What is unique about the drug Tadalafil?

A

Tadalafil is a PDE-5 Inhibitor that has been approved to treat both BPH AND Erectile Dysfunction

20
Q

What are the 4 PDE-5 Inhibitors we discussed for treatment of ED?

A

Sildenafil
Vardenafil
Tadalafil
Avanail

21
Q

Which PDE-5 Inhibitor has the shortest time to onset of action?

A

Avanafil has the shortest time to onset of action at 15min (for a high dose) and 30min (for a normal dose)

22
Q

Which of the PDE-5 Inhibitors has the longest Duration of action and the longest Half-life?

A

Tadalafil is the PDE-5 Inhibitor with the Longest duration of action, and also has the longest half-life

23
Q

What side effects common to all PDE-5 Inhibitors might a Patient experience?

A

HA
Dyspepsia
Nasal Congestion

24
Q

What side effects are unique to Tadalafil?

A

Back Pain
Myalgia
Limb Pain

25
Q

What are the PDE-6 Inhibtor (Sildenafil, Vardenafil, Avanafil) unique side effects?

A

Blue/Blurred Vision

26
Q

What Contraindications are there for Vardenafil?

A

NITRATES

Pt must be Hemodynamically stable

27
Q

What are the Contraindications for Tadalafil?

A

NITRATES

When Used to treat BPH, concurrent a1 blockers are not recommended

28
Q

What Contraindications are there for Sildenafil?

A

NITRATES

Concurrent a-Blockers initiated at lowest possible dose

29
Q

What are second-line treatments for ED?

A

Vacuum Erection Devices

Penile Injections with Alprostadil (PGE1)

30
Q

What is Alprostadil?

A

Alprostadil is an injectable treatment for ED. Alprostadil (PGE1) leads to activation of Adenylate Cyclase and increased levels of cAMP leading to Erection

31
Q

What are some of the adverse effects of Alprostadil (PGE1)?

A

Prolong Erection (Priapism)

32
Q

Why is Priapism (Prolonged Erection) a medical emergency?

A

Priapism causes an emergent need to evacuate clogged blood. It can result in corporal fibrosis and ED. While Alprostadil is most often responsible, PDE-5 INhibitors can cause this as well, however it is far less common.

33
Q

What is the treatment for Priapism (Prolonged Erection)?

A

To treat Priapism you’ll administer a Sympathomimetic (Phenylephrine) and Aspiration of the Blood

34
Q

When should you consider combination a1 Antagonist and 5a-Reductase Inhibitor Therapy for BPH?

A

You’d only use combination therapy of an a1 Antagonist and 5a-Reductase Inhibitor when a Patient:
- Has severe BPH symptoms
- Is known to have a large Prostate
- Has no response to monotherapy
(Long term combo therapy can improve Sx up to 66%)

35
Q

How long does it take to see Symptom relief with a1 Antagonists?

A

A1 Antagonists may relief BPH Sx in 1-3 Days

36
Q

How long does it take to get symptom relief from BPH when starting a 5a-Reductase Inhibitor?

A

5a-reductase Inhibitors take 3-6 months before symptom relief may begin

37
Q

What’s the difference between Finasteride and Dutasteride in their effect on Serum DHT?

A

Dutasteride has a 90% reduction in Serum DHT as it effects both SAR1 and SAR2. Finasteride only has a 70% reduction in Serum DHT as it only effects SAR2

38
Q

What are some of the adverse effects of 5a-Reductase Inhibitors?

A
  • ED
  • Gynecomastia
  • Depressed Libido
  • Ejaculatory Disturbances