Sympatholytics Flashcards

1
Q

What are the 3 classes of sympatholytics?

A

peripheral adrenergic receptor blocker
central α2 agonists
neurotransmitter depleters

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2
Q

What are the subclasses of the peripheral adrenergic receptor blockers?

A

α1 blockers
β blockers
mixed α + β blockers (vasodilating β blockers)

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3
Q

What are the α1 blocker agents?

A

Prazosin
Terazosin
Doxazosin

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4
Q

α1 receptor antagonists block what?

A

post-synaptic α1 receptor

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5
Q

α1 receptors naturally cause vaso________ on vascular smooth muscle.

A

vasoconstriction

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6
Q

Blocking the α1 receptor causes what?

A

vasodilation

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7
Q

The decrease in BP from α1 blockers initially causes ________ _________.

A

sympathetic stimulation or baroreceptor reflex

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8
Q

What are some results of sympathetic stimulation?

A

Increased HR and CO

Increase in plasma renin activity/release

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9
Q

In the use of α1 blockers renal blood flow is _______.

A

unchanged

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10
Q

α1 blockers can cause ______ _______, or what is known as the “first dose effect”.

A

postural hypotension

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11
Q

Inhibition of smooth muscle contraction with the use of α1 blockers occurs in what other areas of the body?

A

urinary bladder sphincter
prostate
seminal vesicles
uterus

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12
Q

What other conditions are α1 blockers indicated?

A

BPH

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13
Q

What are the adverse effects of α1 blockers?

A

Peripheral vasodilation: dizziness, postural hypotension, edema, palpitations, fatigue, nasal congestion
Anaphylaxis
Priapism

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14
Q

What are some drug interactions with α1 blockers?

A

combining with other antihypertensives can cause hypotension

Verampamil causes increased Terazosin levels

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15
Q

What is the ending for α1 blockers?

A

-zosin

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16
Q

What groups are α1 blockers contraindicated?

A

pregnancy

those with pheochromocytoma (adrenal tumor)

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17
Q

α1 blockers are/are not recommended for monotherapy?

A

are not

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18
Q

What populations may benefit from α1 blockers over other agents?

A

HTN diabetics
gout
BPH

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19
Q

What are the β blocker agents?

A

Propranolol
Metoprolol
Atenolol

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20
Q

What is the ending for β blockers?

A

-olol

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21
Q

What is the MOA for β blockers?

A

Blocking the β receptors reduces cardiac contractility and HR to reduce CO. β blockers also reduce the secretion of renin and lower plasma Ang II levels.

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22
Q

What is the most effective β blocker in treating HTN?

A

They are all equally effective.

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23
Q

How do β blockers effect the BP in normotensive patients?

A

no change

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24
Q

Pure β receptor antagonists _____ CO and cause and immediate reflex _______ in TPR.

A

reduce

increase

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25
Partial β receptor antagonists produce a ______ in CO but BP falls due to a _______ in TPR.
lesser decrease than pure β receptor antagonists | decrease
26
What are the vasodilating β blockers?
Labetolol Carvedilol Nebivolol
27
Vasodilating β blockers provide effective therapy in what stages of HTN?
all stages of HTN
28
In what cases are β blockers an appropriate first choice therapy?
post MI heart failure arrhythmias angina
29
Can you combine β blockers with ACEIs or ARBs?
no - its redundant
30
Are diuretics needed in combination with β blockers?
no
31
What are the adverse effects of β blockers?
bronchoconstriction bradycardia masks symptoms of hypoglycemia fatigue/dizziness/depression
32
Which subclass of sympatholytics are preferred in diabetics?
Vasodilating β blockers
33
What are the dosing considerations for β blockers?
start low, titrate up, titrate down
34
What drug interaction blunts the hypotensive effect of β blockers?
NSAIDS
35
What drug interaction can cause a hypertensive crisis?
epinephrine
36
What is the most concerning ADR with β blockers?
New onset diabetes
37
What conditions are the use of β blockers most supported in?
heart failure | post MI
38
What are the central α2 agonist agents?
α-methyldopa clonidine guanabenz guanfacine
39
What is the MOA of central α2 agonists?
By acting on the presynaptic α2 receptor, central NT release is decreased. Sympathetic outflow is reduced and BP is decreased.
40
Why are central α2 agonists not 1st line?
ADRs
41
Methyldopa is an analog of what?
DOPA
42
What is the MOA of methyldopa?
Acts in the brainstem to reduce sympathetic outflow
43
Is methyldopa degraded by monoamine oxidase?
no
44
Methyldopa has _____ effect on CO and HR except in _____.
little | elderly
45
In the use of α2 agonists the baroreceptor reflex is ____ ______.
turned down
46
In the use of α2 agonists, renal blood flow and function is ________.
unaffected
47
In the use of α2 agonists plasma renin levels ______.
decrease
48
α2 agonists should be combined with _______ to maintain efficacy.
diuretic
49
What medication is preferred for HTN in pregnant women?
Methyldopa
50
What are the adverse effects of Methyldopa?
CNS: sedation, depression, dry mouth, ↓ libido, Parkinsonian signs, hyperprolactinemia, bradycardia Hepatotoxicity Hemolytic anemia
51
α2 agonists _____ CO and ______ TPR.
decrease | decrease
52
Guanfacine is _____ selective for α2 receptors than clonidine and guanabenz.
more
53
Which α2 agonist is available in a patch?
clonidine
54
What are the adverse effects of α2 agonists?
CNS: sedation, dry mouth, sleep disturbances, bradycardia, sexual dysfunction
55
What is a main concern about discontinuing α2 agonists?
withdrawal syndrome
56
What does α2 agonist overdose look like?
opioid overdose
57
What are the minor sympatholytic agents?
Guanadrel | Reserpine
58
Guanadrel specifically targets what?
postganglionic adrenergic neurons
59
Guanadrel is taken up into ________ via the ___ _____.
presynaptic terminal | NE transporter
60
Guanadrel ______ NE in NT granuals.
replaces
61
Guanadrel has ______ agonist activity.
no
62
What drug interaction will blunt effectiveness of Guanadrel?
TCAs cocaine chlorpormazine
63
What population is Guanadrel contraindicated?
pheochromocytoma | CHF
64
Guanadrel causes vaso_____, __ TPR, minor __ in renal blood flow and GFR.
vasodilation decrease decrease
65
What are the adverse effects of Guanadrel?
orthostatic hypotension exercise intolerance volume expansion weakness, lassitude, sexual dysfunction, diarrhea
66
Guanadrel is not used as monotherapy due to what?
orthostatic hypotension
67
Reserpine binds to ___ ______ _____.
NT storage vesicles
68
Reserpine impairs ______, ________, ________ neurotransmission.
adrenergic dopaminergic serotonergic
69
Reserpine depletes NTs peripherally, centrally, or both?
both
70
Reserpine ___ TPR ___CO ___HR
decreases decreases decreases
71
In the use of Reserpine, orthostatic hypotension is/isn't a problem.
is not
72
In the use of Reserpine, plasma renin levels ______.
decrease
73
What are the adverse effects of Reserpine?
sedation, inattention, nasal congestion, sexual dysfunction, suicidal depression
74
Reserpine should/shouldn't be combined with a diuretic?
should