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Pharm 1 > Lecture 5 > Flashcards

Lecture 5 Flashcards

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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
___ receptors were identified because they have a relatively high affinity for norepinephrine.
Alpha 1
26
What are the 5 effects of Alpha 1 Agonists?
``` Increased vascular tone Increased SVR which increases BP Mydriasis (pupil dilation) Increased bladder tone Increased tension in prostate ```
27
____ are mainly located on pre junctional nerve terminals to create negative feedback loops.
Alpha 2 Agonists
28
What are the effects of Alpha 2 Agonists ?
Some GI and digestive effects
29
____ innervates smooth muscle of most non-cardiac origin.
Alpha 1 Agonists
30
Where are Alpha 2 Agonists being use increasingly more?
Human cardiovascular as a sedative
31
Alpha 2 Agonist example
Dexmedetomidine (Precedex)
32
___ receptors were found to have a high affinity for the anti-hypertensive drug Clonidine (Catapress).
Alpha 2
33
What 3 reasons make Alpha 2 Agonists good to use as a sedative for surgery?
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
34
___ receptors were found to have equal affinity for norepinephrine and epinephrine (but much less than isoproteronol).
Beta 1
35
Many tissues have some Beta 1, but it is mainly found in the ____.
Heart
36
___ receptors are involved in lipolysis.
Beta 3
37
Dexmedetomidine (Precedex) is a _____
Alpha 2 agonist
38
What does Alpha 1 Agonists innervate?
Smooth muscle of most non-cardiac origin
39
___ receptors have more affinity for epinephrine than norepinephrine (but less than isoproteronol)
Beta 2
40
Alpha 2 receptors were found to have a high affinity for the anti-hypertensive drug _____.
Clonidine (Catapress)
41
4 effects of Beta 1 Agonists
Positive chronotrope Positive inotrope Increased lipolysis Kidneys release more renin
42
Favorite food for the heart during increased cardiac demand
Triglycerides
43
Beta 2 is mostly found in the ____.
Lungs
44
4 effects of Beta 2:
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
45
___ mostly affects the vasculature.
Alpha 1
46
___ mostly affects the heart.
Beta 1
47
___ mostly affects CNS feedback loops to treat HTN ad provide sedation.
Alpha 2
48
___ mostly affects the lungs.
Beta 2
49
____ essentially has an effect on all the other adrenergic receptors.
Dopamine
50
3 characteristics of dopaminergic receptors:
Positive Chronotrope Positive Inotrope Vasoconstriction at high dose
51
Beta 2 mostly affects the ____.
Lungs
52
Alpha 1 mostly affects the _____.
Vasculature
53
Beta 1 mostly affects the ____.
Heart
54
Alpha 2 mostly affects ____.
CNS feedback loops to treat HTN and provide sedation.
55
____ acts as both a hormone and neurotransmitter.
Adrenaline
56
____ is the archetypical adrenergic response.
Adrenaline
57
Cardiovascular effects of epinephrine.
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
What is the overall effect on blood pressure by epinephrine?
Increased SBP | Decreased DBP
59
Epinephrine respiratory effects
Profound bronchodilation by Beta 2
60
Epinephrine metabolic effects
Profound hyperglycemia | Liberates fat energy stores
61
What causes the profound hyperglycemia effect of epinephrine?
B2 causes the pancreas to release glucagon and stimulates the liver both increasing gluconeogenesis.
62
How can epinephrine be administered?
IV, IM, SQ, ET | NOT PO
63
How is epinephrine degraded?
MAO | COMT
64
How is epinephrine excrete?
Urine
65
What is the relevance of epinephrine to perfusion?
``` Code Hypotension and shock Anaphylactic reactions/shock Asthma/bronchoconstriction In conjunction with local anesthetics (like lidocaine) ```
66
What is the dose of epinephrine given during a code?
1 mg IV/IO every 3-5 minutes
67
Which type of hypersensitivities could epinephrine be used for?
Type 1 (Anaphylactic reactions/shock)
68
Typical adult epinephrine dose
2 to 10 mcg bolus PRN to effect | 1 to 10 mcg/min titrated to effect
69
Typical pediatric epinephrine dose
0. 05 to 10 mcg/kg bolus | 0. 05 to 0.5 mcg/kg/min infusion
70
Norepinephrine is also known as:
Noradrenaline Levophed Levarternol
71
Norepinephrine is an ____ transmitter.
endogenous
72
What receptor effects does norepinephrine have?
Alpha and Beta 1 but little Beta 2
73
Cardiovascular effects of norepinephrine
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
What does norepinephrine cause little chronotropic change?
Baroreceptor refex arcs
75
Dose, half-life, route of norepinephrine
0.5 to 12 mcg/min titrated to effect in adult short half-life given by bolus or infusion Not given SQ
76
Dopamine has ___ receptors at higher doses.
Alpha
77
Dopamine has ___ receptors at lower doses.
Beta
78
Cardiovascular effects of dopamine
Positive inotrope and chronotrope via Beta 1 | Vasoconstriction at high doses (Alpha 1)
79
Renal and visceral effects of Dopamine
Increased renal blood flow and visceral perfusion via D receptors
80
Rate and effects of low dose dopamine
1 to 2 mcg/kg/min | Vasodilation to kidneys, brain, and viserca
81
Rate and effects of medium dose dopamine
2 to 10 mcg/kg/min | Increased cardiac output
82
Rate and effects of high dose dopamine
> 10 mcg/kg/min | Alpha activity predominates with profound arterial and venous vasoconstriction
83
4 instances that dopamine will be used
``` Cardiogenic or septic shock Renal failure Hypotension* CHF* *particularly in patients with low-outpu renal failure ```
84
___ is the synthetic an along of dopamine
Dobutamine (Dobutrex)
85
What receptor does dobutamine work on?
Beta 1 selective agonist
86
What are the effects of Dobutamine (Dobutrex) compared to Dopamine?
Greater inotropic | Less chronotropic
87
Dobutamine half life with IV infusion
about 10 minutes
88
Adult dobutamine dose
2 to 20 mcg/kg/min titrated to effect with heart rate not increasing > 10% above baseline
89
Drug-of-choice for cardiogenic or septic shock
Dopamine
90
Dobutamine is the ____ analog of dopamine.
Synthetic
91
Pediatric dobutamine dose
2.5 to 10 mcg/kg/min
92
How dose dobutamine cause increase CO?
It increases SV
93
Dobutamine causes ____ increase in myocardial O2 demand than the other catecholamines.
Less
94
What is a good short term example to use Dobutamine?
Short-term support for patients with CHF like patients struggling to come off CPB
95
What receptor does Prenalterol work on?
Partial Beta 1 selective agonist
96
How can Prenalterol be administered?
PO or IV
97
____ is a strong positive chronotrope and positive inoptrope and potent vasodilator (B2 effects)
Isoproterenol (Isuprel)
98
Isoproterenol (Isuprel) is a ____ catecholamine B1 and B2 selective agonist.
synthetic
99
What are the cardiovascular effects of isoproterenol (Isuprel)?
Increase CO | Decrease after load
100
What receptors are involved with Phenylephrine (Neo-Synephrine)?
Relatively alpa-1 selective agonist
101
Is Neo a catecholamine derivative?
No
102
Cardiovascular effects of Neo
Potent vasoconstrictor Increases SBP and DBP Has little effect on the heart, but causes reflex tachycardia
103
____ is mostly used as a cardiac stimulant in emergency situations (usually as a 2nd line drug).
Isoproterenol (Isuprel)
104
Is Neo inactivated by COMT?
No and because it isn't it has a longer duration.
105
When is phenylephrine commonly used in perfusion?
in adult perfusion to increase SVR/arterial pressure
106
What receptors are involved with Isoproterenol (Isuprel)?
B1 and B2 selective agonist
107
____ is commonly used as a nasal spray for decongestant.
Neo
108
Typical phenylephrine bolus dose and frequency in adult CPB.
50 to 200 mcg until desired effect
109
Typical pedi neo dose
0.05 to 0.5 mcg/kg
110
Phenylephrine is mostly ___.
Alpha
111
Epinephrine is _____.
Non-selective
112
Isoproterenol is mostly _____.
Beta
113
____ is also used to treat SVT.
Neo
114
Examples of mixed-action adrenergic agonists
Ephedrine | Pseudoephedrine
115
Ephedrine and pseudoephedrine are sort of ______.
Broad spectrum sympathomimetics
116
Effects of ephedrine and pseudoephedrine: (4)
Cardiac stimulation Elevated SBP and DBP CNS stimulation Bronchodilation
117
Ephedrine is still used clinically as a _____, but rarely.
Vasopressor
118
6 side effects of adrenergic agonists:
``` Arrhythmias Insomnia HA Nausea Hyperactivity Tremors ```
119
____ is metabolized into dopamine in the brain.
Levodopa
120
Does Levodopa cross the blood-brain barrier?
No
121
Levodopa is useful treatment for ______.
Parkinson's Disease
122
What causes Parkinson's Disease?
Degeneration of dopamine-producing cells in the brain.
123
_____ is useful treatment for Parkinson's Disease.
Levodopa

Pharm 1 (6 decks)

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