Lecture 5 Flashcards

1
Q

Adrenergic Agonists are also called: (3)

A

Adrenoceptor Agonits
Sympathomimetics
Fight and flight

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2
Q

____ is the main SNS neurotransmitter.

A

Norepinephrine

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3
Q

Norepinephrine (noradrenaline), epinephrine (adrenaline), dopamine, and dobutamine are referred to as ________.

A

Catecholamines

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4
Q

____ is released from the adrenal medulla when stimulated by the SNS as a hormone.

A

Epinephrine

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5
Q

6 steps of norepinephrine:

A

1) Synthesis of norepi
2) Uptake into storage vesicles
3) Release of neurotransmitter
4) Binds to receptor
5) Removal of norepi
6) Metabolism

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6
Q

Norepinephrine is the main ___ neurotransmitter.

A

SNS

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7
Q

1) ____ is transported intracellularly and hydroxylated into dihydro-Phenoxyalanine (DOPA).

A

Tyrosine

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8
Q

Which step is the rate-limiting step of norepinephrine?

A

Synthesis (tyrosine to DOPA)

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9
Q

1) DOPA is then decarboxylated into ____.

A

Dopamine

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10
Q

2) Dopamine is transported into vesicles where some/most of it is converted into _____.

A

Norepinephrine

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11
Q

Epinephrine is released from the _____ when stimulated by the SNS as a hormone.

A

Adrenal medulla

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12
Q

3) The action potential reaches the neuron, ____ rushes into the cell, and the vesicles fuse with the cell at the synaptic junction releasing norepinephrine into the synapse.

A

Calcium

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13
Q

4) Norepinephrine diffuses into the synapse and binds to _____.

A

Either pre or post synaptic receptor.

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14
Q

4)The presynaptic receptors provide a ____.

A

Feedback loop

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15
Q

4) The postsynaptic receptors _____.

A

Trigger a response by the effector cell.

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16
Q

Tyrosine is transported intracellularly and hydroxylated into _______.

A

Dihydro-Phenoxyalanine (DOPA)

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17
Q

What 4 drugs are catecholamines?

A

Norepinephrine (Noradrenaline)
Epinephrine (Adrenaline)
Dopamine
Dobutamine

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18
Q

Epinephrine is released from the adrenal medulla when stimulated by the SNS as a _____.

A

Hormone

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19
Q

4) The __-synaptic receptors provide a feedback loop.

A

Pre

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20
Q

Epinephrine is released from the adrenal medulla when stimulated by the ____ as a hormone.

A

SNS

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21
Q

4) The __-synaptic receptors trigger a response by the effector cell.

A

Post

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22
Q

5) What are the 3 ways norepinephrine is removed?

A

Diffuses away
Metabolized by catechol-O-methyl transferase (COMT) on the postsynaptic membrane
Presynaptic membrane reabsorbs the norepinephrine

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23
Q

What is the most common way norepinephrine is removed?

A

Presynaptic membrane reabsorbs the norepinephrinet

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24
Q

6) What two ways can norepinephrine be metabolized?

A

Reused by presynaptic neuron

Degraded by monoamine oxidase (MOA)

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25
Q

___ receptors were identified because they have a relatively high affinity for norepinephrine.

A

Alpha 1

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26
Q

What are the 5 effects of Alpha 1 Agonists?

A
Increased vascular tone
Increased SVR which increases BP
Mydriasis (pupil dilation)
Increased bladder tone
Increased tension in prostate
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27
Q

____ are mainly located on pre junctional nerve terminals to create negative feedback loops.

A

Alpha 2 Agonists

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28
Q

What are the effects of Alpha 2 Agonists ?

A

Some GI and digestive effects

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29
Q

____ innervates smooth muscle of most non-cardiac origin.

A

Alpha 1 Agonists

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30
Q

Where are Alpha 2 Agonists being use increasingly more?

A

Human cardiovascular as a sedative

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31
Q

Alpha 2 Agonist example

A

Dexmedetomidine (Precedex)

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32
Q

___ receptors were found to have a high affinity for the anti-hypertensive drug Clonidine (Catapress).

A

Alpha 2

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33
Q

What 3 reasons make Alpha 2 Agonists good to use as a sedative for surgery?

A

Modulates DPB-induced inflammatory responses better than glucocorticoids.
Sympatholytic effects help ameliorate unwanted cardiovascular reflexes post-op
Significantly less respiratory depression post-op then other sedatives

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34
Q

___ receptors were found to have equal affinity for norepinephrine and epinephrine (but much less than isoproteronol).

A

Beta 1

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35
Q

Many tissues have some Beta 1, but it is mainly found in the ____.

A

Heart

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36
Q

___ receptors are involved in lipolysis.

A

Beta 3

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37
Q

Dexmedetomidine (Precedex) is a _____

A

Alpha 2 agonist

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38
Q

What does Alpha 1 Agonists innervate?

A

Smooth muscle of most non-cardiac origin

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39
Q

___ receptors have more affinity for epinephrine than norepinephrine (but less than isoproteronol)

A

Beta 2

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40
Q

Alpha 2 receptors were found to have a high affinity for the anti-hypertensive drug _____.

A

Clonidine (Catapress)

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41
Q

4 effects of Beta 1 Agonists

A

Positive chronotrope
Positive inotrope
Increased lipolysis
Kidneys release more renin

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42
Q

Favorite food for the heart during increased cardiac demand

A

Triglycerides

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43
Q

Beta 2 is mostly found in the ____.

A

Lungs

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44
Q

4 effects of Beta 2:

A

Mostly relaxation in skeletal muscles and liver and some organs
ALSO
Vasodilation in skeletal muscles and liver and some organs
Insulin release
Uterine muscle relaxation

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45
Q

___ mostly affects the vasculature.

A

Alpha 1

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46
Q

___ mostly affects the heart.

A

Beta 1

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47
Q

___ mostly affects CNS feedback loops to treat HTN ad provide sedation.

A

Alpha 2

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48
Q

___ mostly affects the lungs.

A

Beta 2

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49
Q

____ essentially has an effect on all the other adrenergic receptors.

A

Dopamine

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50
Q

3 characteristics of dopaminergic receptors:

A

Positive Chronotrope
Positive Inotrope
Vasoconstriction at high dose

51
Q

Beta 2 mostly affects the ____.

A

Lungs

52
Q

Alpha 1 mostly affects the _____.

A

Vasculature

53
Q

Beta 1 mostly affects the ____.

A

Heart

54
Q

Alpha 2 mostly affects ____.

A

CNS feedback loops to treat HTN and provide sedation.

55
Q

____ acts as both a hormone and neurotransmitter.

A

Adrenaline

56
Q

____ is the archetypical adrenergic response.

A

Adrenaline

57
Q

Cardiovascular effects of epinephrine.

A

Powerful positive inotrope and chronotrope (B1)
Increase CO, Increased myocardial O2 consumption
Constricts arterioles to mucous membranes, viscera, and skin (Alpha 1) and dilates arterioles to the liver and skeletal muscles (B2)
Causes kidneys to release renin (B1) –> profound vasoconstriction

58
Q

What is the overall effect on blood pressure by epinephrine?

A

Increased SBP

Decreased DBP

59
Q

Epinephrine respiratory effects

A

Profound bronchodilation by Beta 2

60
Q

Epinephrine metabolic effects

A

Profound hyperglycemia

Liberates fat energy stores

61
Q

What causes the profound hyperglycemia effect of epinephrine?

A

B2 causes the pancreas to release glucagon and stimulates the liver both increasing gluconeogenesis.

62
Q

How can epinephrine be administered?

A

IV, IM, SQ, ET

NOT PO

63
Q

How is epinephrine degraded?

A

MAO

COMT

64
Q

How is epinephrine excrete?

A

Urine

65
Q

What is the relevance of epinephrine to perfusion?

A
Code
Hypotension and shock
Anaphylactic reactions/shock
Asthma/bronchoconstriction
In conjunction with local anesthetics (like lidocaine)
66
Q

What is the dose of epinephrine given during a code?

A

1 mg IV/IO every 3-5 minutes

67
Q

Which type of hypersensitivities could epinephrine be used for?

A

Type 1 (Anaphylactic reactions/shock)

68
Q

Typical adult epinephrine dose

A

2 to 10 mcg bolus PRN to effect

1 to 10 mcg/min titrated to effect

69
Q

Typical pediatric epinephrine dose

A
  1. 05 to 10 mcg/kg bolus

0. 05 to 0.5 mcg/kg/min infusion

70
Q

Norepinephrine is also known as:

A

Noradrenaline
Levophed
Levarternol

71
Q

Norepinephrine is an ____ transmitter.

A

endogenous

72
Q

What receptor effects does norepinephrine have?

A

Alpha and Beta 1 but little Beta 2

73
Q

Cardiovascular effects of norepinephrine

A

Profound vasoconstriction due to alpha but without the vasodilator effects of Beta 2
Increased SBP and DBP
Increased SVR
Positive inotrope (B1) but little chronotropic change

74
Q

What does norepinephrine cause little chronotropic change?

A

Baroreceptor refex arcs

75
Q

Dose, half-life, route of norepinephrine

A

0.5 to 12 mcg/min titrated to effect in adult
short half-life
given by bolus or infusion
Not given SQ

76
Q

Dopamine has ___ receptors at higher doses.

A

Alpha

77
Q

Dopamine has ___ receptors at lower doses.

A

Beta

78
Q

Cardiovascular effects of dopamine

A

Positive inotrope and chronotrope via Beta 1

Vasoconstriction at high doses (Alpha 1)

79
Q

Renal and visceral effects of Dopamine

A

Increased renal blood flow and visceral perfusion via D receptors

80
Q

Rate and effects of low dose dopamine

A

1 to 2 mcg/kg/min

Vasodilation to kidneys, brain, and viserca

81
Q

Rate and effects of medium dose dopamine

A

2 to 10 mcg/kg/min

Increased cardiac output

82
Q

Rate and effects of high dose dopamine

A

> 10 mcg/kg/min

Alpha activity predominates with profound arterial and venous vasoconstriction

83
Q

4 instances that dopamine will be used

A
Cardiogenic or septic shock
Renal failure
Hypotension*
CHF*
*particularly in patients with low-outpu renal failure
84
Q

___ is the synthetic an along of dopamine

A

Dobutamine (Dobutrex)

85
Q

What receptor does dobutamine work on?

A

Beta 1 selective agonist

86
Q

What are the effects of Dobutamine (Dobutrex) compared to Dopamine?

A

Greater inotropic

Less chronotropic

87
Q

Dobutamine half life with IV infusion

A

about 10 minutes

88
Q

Adult dobutamine dose

A

2 to 20 mcg/kg/min titrated to effect with heart rate not increasing > 10% above baseline

89
Q

Drug-of-choice for cardiogenic or septic shock

A

Dopamine

90
Q

Dobutamine is the ____ analog of dopamine.

A

Synthetic

91
Q

Pediatric dobutamine dose

A

2.5 to 10 mcg/kg/min

92
Q

How dose dobutamine cause increase CO?

A

It increases SV

93
Q

Dobutamine causes ____ increase in myocardial O2 demand than the other catecholamines.

A

Less

94
Q

What is a good short term example to use Dobutamine?

A

Short-term support for patients with CHF like patients struggling to come off CPB

95
Q

What receptor does Prenalterol work on?

A

Partial Beta 1 selective agonist

96
Q

How can Prenalterol be administered?

A

PO or IV

97
Q

____ is a strong positive chronotrope and positive inoptrope and potent vasodilator (B2 effects)

A

Isoproterenol (Isuprel)

98
Q

Isoproterenol (Isuprel) is a ____ catecholamine B1 and B2 selective agonist.

A

synthetic

99
Q

What are the cardiovascular effects of isoproterenol (Isuprel)?

A

Increase CO

Decrease after load

100
Q

What receptors are involved with Phenylephrine (Neo-Synephrine)?

A

Relatively alpa-1 selective agonist

101
Q

Is Neo a catecholamine derivative?

A

No

102
Q

Cardiovascular effects of Neo

A

Potent vasoconstrictor
Increases SBP and DBP
Has little effect on the heart, but causes reflex tachycardia

103
Q

____ is mostly used as a cardiac stimulant in emergency situations (usually as a 2nd line drug).

A

Isoproterenol (Isuprel)

104
Q

Is Neo inactivated by COMT?

A

No and because it isn’t it has a longer duration.

105
Q

When is phenylephrine commonly used in perfusion?

A

in adult perfusion to increase SVR/arterial pressure

106
Q

What receptors are involved with Isoproterenol (Isuprel)?

A

B1 and B2 selective agonist

107
Q

____ is commonly used as a nasal spray for decongestant.

A

Neo

108
Q

Typical phenylephrine bolus dose and frequency in adult CPB.

A

50 to 200 mcg until desired effect

109
Q

Typical pedi neo dose

A

0.05 to 0.5 mcg/kg

110
Q

Phenylephrine is mostly ___.

A

Alpha

111
Q

Epinephrine is _____.

A

Non-selective

112
Q

Isoproterenol is mostly _____.

A

Beta

113
Q

____ is also used to treat SVT.

A

Neo

114
Q

Examples of mixed-action adrenergic agonists

A

Ephedrine

Pseudoephedrine

115
Q

Ephedrine and pseudoephedrine are sort of ______.

A

Broad spectrum sympathomimetics

116
Q

Effects of ephedrine and pseudoephedrine: (4)

A

Cardiac stimulation
Elevated SBP and DBP
CNS stimulation
Bronchodilation

117
Q

Ephedrine is still used clinically as a _____, but rarely.

A

Vasopressor

118
Q

6 side effects of adrenergic agonists:

A
Arrhythmias
Insomnia
HA
Nausea
Hyperactivity
Tremors
119
Q

____ is metabolized into dopamine in the brain.

A

Levodopa

120
Q

Does Levodopa cross the blood-brain barrier?

A

No

121
Q

Levodopa is useful treatment for ______.

A

Parkinson’s Disease

122
Q

What causes Parkinson’s Disease?

A

Degeneration of dopamine-producing cells in the brain.

123
Q

_____ is useful treatment for Parkinson’s Disease.

A

Levodopa