(10.1) BPH and ED pharmacology (Sheehy) Flashcards

1
Q

Describe what benign prostatic hypertrophy (BPH) is:

A

BPH causes bladder outlet obstruction

Prostate gets enlarged and blocks urethra, urine gets blocked

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2
Q

What are the lower urinary tract symptoms (LUTS) asociated with BPH?

A

Interrupted stream

Frequency

Hesitation

Fullness

Dribbling

Urgency

Weak stream

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3
Q

What class of drugs are used to treat BPH?

A

Alpha1 adrenergic receptor antagonists

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4
Q

What drugs are used to treat BPH?

A

-OSIN

Terazosin

Doxazosin

Tamsulosin

Sildosin

Alfuzosin

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5
Q

What is the main goal of alpha1 adrenergic receptor antagonists in treating BPH?

A

Relax muscle tone

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6
Q

Describe the receptor specificity of

Terazosin

Doxazosin

Tamsulosin

Sildosin

Alfuzosin

A
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7
Q

Which of the following alpha 1 adrenergic receptor antagonists is uroselective

Terazosin

Doxazosin

Tamsulosin

Sildosin

Alfuzosin

A

Tamsulosin

Silodosin

Alfuzosin

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8
Q

What are the adverse effects of these drugs?

Terazosin

Doxazosin

Tamsulosin

Sildosin

Alfuzosin

A
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9
Q

What are the drug interactions of

Terazosin

Doxazosin

Tamsulosin

Sildosin

Alfuzosin

A
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10
Q

What are the structural remedy drugs for BPH?

A

Steroid 5alpha reductase inhibitors

Finasteride

Dutasteride

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11
Q

How do steroid 5alpha reductase inhbitors act as a structural remedy for BPH?

A

Prevent enlargement and shrink the prostate

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12
Q

What are the downsides to taking finasteride or dutasteride?

A

DELAYED ACTION

Shrinkage and symptom relief takes 3-6 months

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13
Q

Why does the prostate enlarge?

A

Aging

+

Dihydrotestosterone

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14
Q

Physiologically, how do steroid 5alpha reductase inhibitors work?

A

DHT is 10 times more potent than T

SAR type 1 and 2 convert serum T to DHT in cells

A prostate that has undergone hyperplasia has excess SAR2

DHT “starvation” causes epithelial atrophy, shrinkage and gradual relief of LUTS

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15
Q

Descibe the enzyme selectivity of Finasteride

A

Finasteride

is a….

SpeciFIc inhibitor

SAR-2

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16
Q

Descibe the enzyme selectivity of Dutasteride

A

Dutasteride

is a…

DUal inhibitor

SAR-1 and SAR-2

17
Q

Which SAR is more prevalent in BPH?

A

SAR-2

18
Q

Explain why the serum DHT levels are:

70% decreased with finasteride

90% decreased with dutasteride

A

Finasteride is SPECIFIC to SAR-2, which is primarily in the prostate

Dutasteride is DUAL acting on SAR-1 and SAR-2 and will have a greater systemic influence on serum DHT

19
Q

What are the adverse effects of finasteride and dutasteride?

A

Erectile dysfunction

Gynecomastia

Depressed libido

Ejaculation disturbances

20
Q

Is it possible to administer a combo therapy for BPH?

A

YES!

Use combo therapy when pt. has no response to monotherapy

21
Q

Define:

Erectile dysfunction (ED)

A

Consistent or recurrent inability to acquire or sustain an erection of sufficient rigidity and duration for sexual intercourse

22
Q

What are some risk factors for ED?

A

Obesity

Smoking

Stress

23
Q

How do PDE-5 inhibitors work to sustain an erection?

A
24
Q

What PDE-5 inhibitor has the longest half life?

A

Tadalafil

25
Q

What is the fastest acting PDE-5 inhibitor?

A

Avanafil

26
Q

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

A

Tadalafil

27
Q

What are some side effects of PDE-5 inhibitors?

A

Reasonably well tolerated

PDE-5 related = headache, dyspepsia, nasal decongestion

PDE-6 related = blue/blurred vision

Specific to tadalafil = Back pain, myalgia, limb pain

28
Q

What is a MAJOR contraindication of PDE-5 inhibitors?

A

ORGANIC NITRATES

–> Extreme and dangerous hypotension

29
Q

What are second-line ED therapies?

A

Vacuum erection devices

Penile injections w/ alprostadil

30
Q

What is a major side effect of alprostadil?

A

Priapism

31
Q
A

C. Nitrovasodilator (i.e. nitroglycerin)