Block 10 > pharm: adrenergic agonists > Flashcards

pharm: adrenergic agonists Flashcards

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1
Q

What are the 6 steps of neurotransmission at Adrenergic Neurons?

A
  1. Synthesis of norepinephrine
  2. Storage of norepinephrine
  3. Release of norepinephrine
  4. Binding to receptor
  5. Removal of norepinephrine
  6. Potential fates of recaptured norepinephrine
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2
Q

How is norepinephrine released into the synapse?

A

AP at nerve junction triggers influx of calcium ions. Increased calcium causes the vesicles to fuse with the cell membrane and expel contents into the synapse.

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3
Q

What is the rate limiting step in the synthesis of NE?

A

Hydroxylation of tyrosine.

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4
Q

What is the function of the vesicular monoamine transporter (VMAT)?

A

Uptakes catecholamines into vesicles.

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5
Q

What drug inhibits the transport of dopamine into vesicles where it becomes NE?

A

Reserpine.

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6
Q

To what receptors does NE bind?

A

Adrenergic receptors.

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7
Q

Where is NE synthesized?

A

Within the vesicle.

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8
Q

What does COMT do?

A

Degrades catecholamines.

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9
Q

If NE is not broken down by COMT, where can it go?

A

It can be brought back into the nerve terminal by NET.

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10
Q

What drug blocks the reuptake of NE into the nerve terminal?

A

Cocaine.

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11
Q

How does activation of the Alpha 2 receptor impact NE release?

A

Activation of alpha 2 receptor decreases production of cAMP and Ca2+ influx which leads to an inhibition of further release of NE from the neuron.

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12
Q

What is MAO?

A

Monoamine oxidase.

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13
Q

What does MAO do?

A

Breaks down dopamine and NE.

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14
Q

How does an Alpha 2 agonist impact levels of NE in the synapse?

A

Decreases levels.

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15
Q

How does an Alpha 2 antagonist impact levels of NE in the synapse?

A

Increases.

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16
Q

How does a COMT inhibitor impact levels of NE in the synapse?

A

Increases.

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17
Q

How does an MAOI impact levels of NE in the synapse?

A

Increases.

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18
Q

How do amphetamines impact levels of NE in the synapse?

A

Increases.

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19
Q

How does cocaine impact levels of NE in the synapse?

A

Increases.

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20
Q

How do tricyclic antidepressants impact levels of NE in the synapse?

A

Increases.

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21
Q

How do serotonin NE reuptake inhibitors impact levels of NE in the synapse?

A

Increases.

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22
Q

How does an Alpha 2 agonist impact HR/BP?

A

Decreases.

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23
Q

How does an Alpha 2 antagonist impact HR/BP?

A

Increases.

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24
Q

How does a COMT inhibitor impact HR/BP?

A

Increases.

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25
How does an MAOI impact HR/BP?
Increases.
26
How do amphetamines impact HR/BP?
Increases.
27
How does cocaine impact HR/BP?
Increases.
28
How do tricyclic antidepressants impact HR/BP?
Increases.
29
How do serotonin NE reuptake inhibitors impact HR/BP?
Increases.
30
Where does an Alpha 2 agonist work?
Pre-synaptically.
31
Where does an Alpha 2 antagonist work?
Pre-synaptically.
32
Where does a COMT inhibitor work?
In the synapse.
33
Where does an MAOI work?
In nerve - pre-synaptic.
34
Where do amphetamines work?
Pre-synaptically.
35
Where does cocaine work?
Pre-synaptic.
36
Where do tricyclic antidepressants work?
Pre-synaptically.
37
Where do serotonin NE reuptake inhibitors work?
Pre-synaptically.
38
How does an Alpha 1 agonist impact blood vessels and BP?
- Vasoconstriction - Increased BP
39
How does an alpha 1 antagonist impact blood vessels and BP?
Vasodilation and decreases BP.
40
BP = _____ x _____
CO x PVR.
41
How does a Beta 2 agonist impact blood vessels and BP?
Vasodilation and decreases BP.
42
What G-protein is associated with Alpha 1 receptors?
Gq.
43
What G-protein is associated with Alpha 2 receptors?
Gi.
44
What G-protein is associated with Beta 1 receptors?
Gs.
45
What G-protein is associated with Beta 2 receptors?
Gs.
46
What G-protein is associated with M1 and M3 receptors?
Gq.
47
What G-protein is associated with M2 receptors?
Gi.
48
What are the primary effects of Alpha 1 receptors?
- Vasoconstriction - Increased BP - Urethral constriction - Pupil dilation
49
How does activation of the alpha 2 receptor impact NE release?
Inhibits NE release.
50
What are the primary effects of Beta-1 receptors?
- Increased contraction and HR - Increased renin release
51
What are the primary effects of Beta-2 receptors?
- Vasodilation - Decreased PVR - Bronchodilation
52
What is the urinary tract effect of beta-3 receptors?
Relaxes detrusor muscle - mirabegron.
53
What are the primary effects of M2 receptors?
- Decreased contraction and HR
54
What are the primary effects of M3 receptors?
- Bronchoconstriction - Bladder contraction - Pupillary constriction - Peripheral vasodilation and decreased BP
55
NE is methylated to ___________: both are stored in _______________ cells.
Epinephrine ## Footnote Chromaffin
56
What activates Beta-2 receptors?
Epinephrine released from the adrenal medulla.
57
Voiding urine = ___________ detrusor, ___________ trigone and sphincter.
Contract detrusor (M3) ## Footnote Relax trigone and sphincter (M3)
58
Inhibiting urination = __________ detrusor, ____________ sphincter.
Relax detrusor (B3) ## Footnote Contract sphincter (a1)
59
Drugs that change TPR will change BP causing an ANS reflex change on the heart in the ___________ direction of the BP change.
Opposite.
60
What receptors predominate on the heart and what effects do they cause?
B1 ## Footnote Increased conduction velocity and cardiac force.
61
Norepinephrine acts on what receptors?
a1, a2, b1.
62
What is the main action of NE?
Increase TPR and BP.
63
When is NE used?
Septic shock to increase BP.
64
Epinephrine acts on what receptors?
alpha 1, alpha 2, beta 1, beta 2.
65
At low doses, epinephrine activates ___________ receptors.
Beta.
66
At high doses, epinephrine activates ___________ receptors.
Alpha.
67
At low doses, epinephrine _________ BP and __________ HR.
Decreases BP and Increases HR.
68
At high doses, epinephrine ________ BP.
Increases.
69
What is epinephrine used for?
Drug of choice for type 1 hypersensitivity anaphylaxis reactions and local anesthetic administration.
70
Isoproterenol acts on what receptors?
beta 1 and beta 2.
71
How does Isoproterenol impact BP and HR?
Lowers BP and increases HR.
72
Phenylephrine acts on what receptors?
alpha 1.
73
How does Phenylephrine impact BP?
Increases BP but causes reflex bradycardia.
74
What are the uses of Phenylephrine?
Treat hypotension, nasal decongestant, MYDRIASIS in ocular exam.
75
Albuterol acts on what receptors?
beta 2.
76
What are the effects of Albuterol?
Bronchodilation.
77
Mirabegron acts on what receptor?
B3.
78
What is Mirabegron used to treat?
Urinary incontinence/OAB.
79
At low epinephrine concentrations, what effect does this lead to?
Relaxation.
80
At high epinephrine concentrations, what effect does this lead to?
Vascular smooth muscle contraction.
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