13. BPH and Erectile Dysfunction Pharmacology Flashcards

1
Q

Benign prostatic hyperplasia BPH is caused by enlarged prostate. What are the common lower urinary tract symptoms LUTS?

A
frequency
interrupted steam
hesitation
dribbling
fullness
urgency
weak stream
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2
Q
The following are what?
Terzosin
doxazosin
tamsulosin
sildosin
alfuzosin
A

alpha 1 adrenergic receptor antagonists

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3
Q

The -osins a1 receptor antagonists relax muscle tone and provide rapid releif of symptoms in days. What does a1A receptors + NE result in? 2

A

muscle contraction

bladder outlet obstruction

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4
Q

What does alpha1D receptors + NE result in? 1

A

Detrusor instability

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5
Q

With alpha1 antagonists to compete with NE, what are the positive results? 3

A

reduce spasm
promote muscle relaxation
improve urine flow

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6
Q

terazosin and doxazosin
have alpha1 specificity
adverse effects of postural hypotension, dizziness and fatigue
are they uroselective?

A

no

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7
Q
Tamsulosin and silodosin
Are uroselective for alpha1A/D
have alpha1A/D specifcity
and increases concentration of CYP3a4 substrates
What are the two adverse effects?
A

Reduced ejaculation

IFIS

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8
Q
Alfuzosin
is a nonspecific alpha1 selective
it is uroselective
inc. conc. of CYP3A4 substrates
adverse effects?
A

QT prolongation

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9
Q

What do all the a1 adrenergic receptor antagonists have a drug interaction with?

A

PDE5 inhibitors (sildenafil/vardenafil)

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10
Q

Alfuzosin has function uroselectivity meaning it distributes into the prostate more than serum. Why is this good?

A

to avoid hepatic impairment

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11
Q

What are the two 5alpha reductase inhibitors that prevent enlargement and shrinks prostate in 3-6 months?

A

Finasteride

Dutasteride

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12
Q

Androgenic steroids, testosterone and dihydrotestosterone DHT enable prostate epi to grow. DHT is 10x more potent than T. What does steroid 5a reductase do?

A

types 1 and 2, convert serum T to DHT

hypertrophic prostate has excess SAR2

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13
Q

SAR inhibitors bind SAR2 and inhibit T to DHT, resulting in?

A

Excess T, lack of DHT, and no gene transcription for the prostate

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14
Q

What is the enzyme selectivity for finasteride?

A

FInasteride

speciFIc inhibitor of only SAR2

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15
Q

What is the enzyme selectivity for DUtasteride?

A

DUtasteride

DUal inhibitor of both SAR1/2

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16
Q

Why is there a difference in the serum DHT when comparing finasterid and dutasteride’s effects?

A

because dutasteride inhibits both SARs = has a great decrease in the serum DHT than finsteride

17
Q

When can one use a combination therapy of a1 receptor antagonist and 5a reductase inhibitor? 3

A

when there are severe symptoms of BPH
known to have large prostate
**no response to monotherapy

18
Q

What are 3 risk factors of erectile dysfunction ED?

A

obesity
smoking
stress

19
Q

Larginine from sexual stimulation causes increase in NO leading to inc cGMP, releasing Ca2+ causing smooth muscle relaxation leading to?

A

erection

20
Q

What is used by the body to rid a erection?

A

PDE-5 takes cGMP and makes 5’GMP, ending the erection

21
Q

What allows for a sustained erection?

A

Increase NO
sustained levels of cGMP
(dec Ca2+?)

22
Q

What are the 4 different types of PDE5 inhibitors for ED? and how are they cleared through the body?

A
Sildenafil
Vardenafil
Tadalafil
Avanafil
Hepatic CYP3A4
23
Q

What are the two things that makes tadalafil (Cialis) different from the rest?

A

lasts for 36 hours

half life of 18 (much longer than other PDE5 inhibitors)

24
Q

What is unique about avanafil PDE5 inhib?

A

it has a high dose and a normal dose

25
Q

What are some side effects of PDE5 inhibs?

A

Headache
dyspepsia
nasal congestion
(back pain, myalgia, limb pain tadalafil)

26
Q

What is an extremely important contraindictation to remember with PDE5 inhibitors?

A

DONT combine with organic nitrates (NO) can cause extreme and dangerous hypotension

27
Q

A few secondline ED therapies include vacuum erection devices, and penile injections with?

A

(caverject) alprostadil, a prostaglandin E1 agonist leading to increase in cAMP

28
Q

Adverse effects of alprostadil include prolonged erection (priapism) which is a medical emergency that can result in?

A

permanent corporal fibrosis and ED

29
Q

NOTE: what is special about tadalafil?

A

It is a PDE5 inhibitor that can treat both BPH AND ED