BPH and ED Pharmacology Flashcards

1
Q

What are the 3 different MOA classes used to treat BPH?

A

a1-adrenergic receptor antagonists

Steroid 5a-reductase inhibitors

PDE-5 inhibitors

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2
Q

What are the 2 different MOA classes used to treat ED?

A

PDE-5 inhibitors

PGE1 agonists

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3
Q

5 a1-adrenergic receptor antagonist drug names

A
Terazosin
Doxazosin
Tamsulosin
Silodosin
Alfuzosin

-zosin

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4
Q

What is the goal of a1-adrenergic receptor antagonists?

When does relief occur?

A

Relax muscle tone

Rapid relief (days)

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5
Q

What a1 subtypes do a1-adrenergic receptor antagonists act on?

Prostate
Detrusor m.
SC

A

Prostate - a1A
Detrusor m. - a1D>a1A
SC - a1D

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6
Q

What happens when a1A receptors in the bladder are activated by NE?

A

Muscle contracts -> bladder outlet obstruction

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7
Q

What happens when a1D receptors in the bladder are activated by NE?

A

Destrusor instability -> start and stop feeling

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8
Q

What happens when a1 antagonists compete with NE? (3)

A

Reduce spasm
Promote muscle relaxation
Improve urine flow

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9
Q

Which 2 a1-adrenergic receptor antagonist drugs have a greater specificity for a1»>a2?

A

Terazosin

Doxazosin

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10
Q

Which 2 a1-adrenergic receptor antagonist drugs have a1A=a1D specificity?

A

Tamsulosin

Silodosin

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11
Q

Which a1-adrenergic receptor antagonist drug is non-specific a1 selective?

A

Alfuzosin

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12
Q

What are the adverse effects of terazosin and doxazosin?

A

Postural HypoTN
DIzziness
Fatigue

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13
Q

What are the adverse effects of tamsulosin and silodosin?

A

Reduced ejaculate

IFIS

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14
Q

What is an adverse effect of alfuzosin?

A

QT prolongation

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15
Q

What drug interaction is common to all a1-adrenergic receptor antagonists?

A

PDE-5 inhibitors (sildenafil, vardenafil)

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16
Q

Increased concentration of CYP 34A substrates is a common drug interaction with which 3 BPH meds?

A

Tamsulosin
Silodosin
Alfuzosin

17
Q

Which a1-adrenergic receptor antagonist has an approved generic?

A

Tamsulosin

18
Q

2 steroid 5a reductase inhibitors

A

Finasteride

Dutasteride

19
Q

What is the overall MOA for 5a reductase inhibitors?

A

To decrease prostate size and inhibit enlargement

20
Q

How long does it take 5a reductase inhibitos to work?

A

3-6 mo. It is a delayed action.

21
Q

What causes the prostate to enlarge?

What is a SARs role in this?

A

T and DHT (DHT is 10x more potent than its T precursor).

SARs inhibit T’c conversion to DHT.

22
Q

What type of SAR does a prostate that has undergone hyperplasia have?

A

SAR-2

23
Q

2 direct effects of SAR inhibitors

2 indirect effects

A

Direct: T accumulation, DHT depletion

Indirect: androgen receptor is less occupied, no gene transcription occurs

24
Q

Finasteride targets which SAR?

Dutasteride?

A

Finasteride: SAR-2

Dutasteride: SAR-1,2 (dual inhibitor, thus will lead to less serum DHT (70% reduction for Fin. and 90% reduction for Dut.))

25
Q

Possible S/E for pts. on SAR inhibitors

A

ED
Gynecomastia
Dec. libido
Ejaculation disturbances

26
Q

SAR inhibitors do not require _______ for age or renal problems.

Are there significant drug interactions?

Which pts. should be cautioned to use it?

A

Dosage adjustments

No

Pts. w/ liver disease -> metabolized by CYP3A

27
Q

When should combo Tx of SAR inhibitors and a1 adrenergic antagonists be used?

A

Severe sx of BPH
Known large prostate
No response to monotherapy

28
Q

What drug is the lone PDE-5 inhibitor to treat BPH?

Why should it be given?

A

Tadalafil

If pt. has BPH and ED.

29
Q

Risk factors for ED

A

Obesity
Smoking
Stress

30
Q

What is the normal physiologic pathway to an achieve an erection?

Where does PDE-5 come into play?

A

L-Arg (via NOS) -> NO -> cGMP -> + Ca2+ -> SM relaxes -> erection.

PDE-5 turns cGMP into 5’-GMP and slows the process.

31
Q

What kind of inhibition do PDE-5 inhibitors use to inhibit PDE-5?

A

Competitive

32
Q

4 PDE-5 inhibitors to know

A

Sildefanil (Viagra)
Vardenafil (Levitra)
Tadalafil (Cialis)
Avanafil (Stendra)

33
Q

Which PDE-5 inhibitor has the fastest onset?

A

Avanafil

34
Q

Which PDE-5 inhibitor has the longest duration of action?

A

Tadalafil

35
Q

S/E of PDE-5 inhibitors

A

Mild.

HA, dyspepsia, nasal congestion.
Blurred vision (Sildenafil, vardenafil, avanafil)
Back pain, myalgia (Tadalafil)

36
Q

Most major contraindication to a patient taking a PDE-5 inhibitor:

A

Organic nitrates

37
Q

How does Alprostadil treat ED?

A

It is PGE1 and is injected in an effect to increase cAMP levels to achieve an erection.

*PGE1 agonist

38
Q

Why is an erection > 4 hrs. an issue?

Tx?

A

Blood may be clogged in penis and lead to corporal fibrosis and permanent ED (more common to Alprostadil).

Phenylephrine (a sympathomimetic) and aspiration