Alpha and Beta Adrenergic Blockers - LeBlanc Flashcards

(77 cards)

1
Q

Catecholamines causes peripheral (inhibition/excitation) on gut, bronchial, blood vessles supplying skeletal muscle SM

A

inhibitory

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the effects on the heart of catecholamines?

A

increase in frequency and contractile force, increase conduction velocity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Regarding metabolism, what are the effects of catecholamines on fats and sugars?

A

glycogenolysis from liver and skeletal muscles

release of free fatty acids from adipose tissue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Which endocrine hormones do catecholamines regulate?

A

insulin
renin
pituitary hormones

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the CNS effects of catecholamines?

A

wakefulness
appetite
resp. stim
psychomotor activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the PREjunctional actions of catecholamines?

A

inhibition or facilitation of neurotransmitter release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

describe the strength of Epi, NorEpi, and Iso on a1 receptors

A

Epi > NE&raquo_space; Iso

phenylephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

describe the strength of Epi, NorEpi, and Iso on a2 receptors

A

Epi > NE»Iso

clonidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

describe the strength of Epi, NorEpi, and Iso on B1 receptors

A

Iso > Epi =NE

dobutamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

describe the strength of Epi, NorEpi, and Iso on B2 receptors

A

Iso > Epi&raquo_space; NE

terbutaline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

describe the strength of Epi, NorEpi, and Iso on B3 receptors?

A

Iso = NE > epi

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Wat is the a1 antagonist?

A

prazosin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the a2 antagonist?

A

yohimbine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the B1 antagonist?

A

metoprolol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

which two receptors are found on smooth muscle?

A

a1

B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

which receptor is found on nerve terminals?

A

a2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Which receptor is found on cardiac muscle?

A

b1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

which receptor is found on adipose tissue?

A

B3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the effect of stimulating a1 receptors?

A

contraction of SM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what is the effect of stimulating a2 receptors?

A

decreased transmitter release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

wha is the effect of stimulating B1 receptors?

A

increase:
chronotropic
inotropic
dromotropic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is the effect of stimulating b2 receptors?

A

SM relaxation (think albuterol inhalers)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what is the effect of stimulating b3 receptors?

A

lipolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is the G protein assc’d with a1?

A

Gq

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
what is the G protein assc'd with a2?
Gi/o
26
what is the G protein assc'd with B receptors?
Gs
27
a1 directly stimulates (blank), which activates (blank) which converts PIP2 to IP3 and DAG
phospholipase | Protein kinase C
28
IP3 production allows for (blank) release from intracelllular stores which causes SM contraction
Ca
29
a2 stimulation blocks (blank) release from intracellular stores which blocks neurotransmitter release
Ca
30
A2 activation blocks (blank) activity which converts ATP to cAMP
adenylyl cyclase
31
cAMP production post A2 signaling has what effect on SM?
contraction
32
B receptors activate adenylyl cyclase to produce cAMP which does what?
increase cardiac contractility SM relaxation glycogenolysis
33
How does calcium release from intracellular stores actually get the cell to do things?
activates Ca dependent protein kinase
34
which two receptors have competing action on adenylate cyclase?
a2 and B receptors
35
Except for Phenoxybenzamine (PBZ) and related compounds, all α receptor antagonists are (blank) inhibitors
competitive
36
where do we find the greatest affect of a-1 blockers?
smooth muscle; while present in CNS the effect is extremely small
37
a2 receptors (inc/dec) intracellular calcium by decreasing cAMP levels
incerease intracell calcium
38
a2 receptors (enhance/limit) sympathetic outflow
limit
39
a2 receptors increase (blank) tone and therefore parasympathetic outflow
vagal tone
40
what type of receptor increases PLT aggregation in the periphery?
a2
41
a2 receptors decrease the release of which two neurotransmitters in the periphery?
NE and ACh
42
What is the effect of a2 stimulation on insulin release and lipolysis?
decreases both
43
T/F: a2 stimulation decreases lipolysis indirectly
false; directly acts on fat cells
44
what receptor class increases insulin release?
b
45
what do we use a1 blockers for?
decrease blood pressure
46
is the decrease in BP from a1 blockers more noticeable when standing or lying down?
standing
47
what can exacerbate the lowering of the BP after giving an a1 blocker?
hypovolemia
48
what mechanism compensates for the lowering in BP from a1 blockers?
baroreflex: | increase HR and CO
49
If an a1 blocker is mixed with a (blank) blocker, it can exaggerate the baroreflex by leading to the release of NE which activates B1 receptors
a2 receptors on a peripheral nerve ending
50
a1 blockers will inhibit the effects of (blank) drugs adminstered externally
sympathomimetics; can use to reverse an adverse effect
51
what is the pure a1 agonist and blocker?
agon: phenylephrine blocker: prazosin
52
what is the pure a2 agonist and blocker?
agon: clonidine blocker: yohimbine
53
what is the pure b1 agonist and blocker?
agon: dobutamine blocker: metoprolol
54
what is the pure b2 agonist and blocker?
agonist: terbutaline | no blocker
55
t/f: a2 blockers target both the CNS and the periphery
true
56
what are the effects of a2 blockers on the periphery?
increase release of NE from nerve endings
57
what is the effect of a2 blockers on the CNS?
increase sympathetic outflow; increase BP
58
which a1 and 2 blocker binds irreversibly via covalent modification?
PBZ/phenoxybenzamine
59
what are the effects of phenoxybenzamine in the periphery?
block a receptor in SMC leads to decrease in peripheral resistance enhanced baroreflex
60
what are the effects of phenoxybenzamine in the CNS?
increase sympathetic outflow | tachycardia due to a2 block
61
why would epi produce severe hypotension if given alongside phenoxybenzamine
PBZ blocks epi a action, therefore unapposed b2 action, therefore loooots of SMC relaxation
62
why do you get hypotension when standing when taking PBZ?
lack of vasomotor reflex from baroreflex
63
at high doses PBZ irreversibly binds to what three other neurotransmitters?
Serotonin histamine ACH
64
what is the half life of PBZ?
less than 24 hours
65
what is the use of PBZ?
pheochromocytoma: lots of catecholamines means HTN; PBZ lowers the BP by blocking cat. action
66
what is the non-serious use for PBZ?
benign prostatic hypertrophy in men
67
Besides postural hypotension, what are the other side effects of PBZ?
nasal stuffiness; miosis | sexual dysfunction in men
68
which drug blocks a1 and a2 similarly via reversible competitive inhibition?
phentolamine; PTL
69
what are the two "classic" a blockers?
phenoxybenzamine and phentolamine
70
Beside the cardio effects of PTL (which are similar to PBZ), what are the other effects of PTL on other organ systems?
stimulates GI smooth muscle and enhances gastric acid secretion
71
(phentolamine/phenoxybenzine) can be used to rapidly alleviate a hypertensive episode
phentolamine
72
what happens when you get extravasation of phenyelephrine?
necrosis
73
do you use PBZ or PTL for Raynaud's?
PTL
74
which a blocker do you give during rapid clonidine withdrawal or tyramine rich foods during MAOI Tx?
phentolamine
75
what are the cardiac SE of phentolamine?
``` hypotension reflex tachycardia arrhythmia ischemic events MI ```
76
what are the GI SE of phentolamine?
abdominal pain nauseua PUD exacerbation
77
what two conditions contraindicate the use of phentolamine?
PUD and CAD