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Pathology > Pharmacology Class 2020: Adrenergics > Flashcards

Pharmacology Class 2020: Adrenergics Flashcards

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1
Q

Where does the preganglionic neuron originate within the autonomic nervous system?

A

CNS Adrenal Medulla

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2
Q

what two neurons are required to reach a target organ within the autonomic nervous system?

A

preganglionic

postganglionic

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3
Q

What part of the body is the sympathetic nervous system originate?

A

thoracolumbar

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4
Q

Does the sympathetic nervous system have long or short postganglionic fibers?

A

Long

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5
Q

Is the sympathetic nervous system anabolic or catabolic?

A

catabolic

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6
Q

The parasympathetic nervous system is a catabolic system.

True or False

A

False

Anabolic

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7
Q

What part of the body does the parasympathetic nervous system originate from?

A

craniosacral

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8
Q

Are the fibers within the parasympathetic nervous system long or short?

A

short fibers

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9
Q

Where does NE originate from within the CNS?

A

adrenergic nerve endings in the brain

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10
Q

Where is Epi released from within the body?

A

Adrenal Medulla and acts as a hormone

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11
Q

Drugs that mimic the actions of Epi and NE

A

Sympathomimetic

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12
Q

What is the immediate precursor to NE

A

Dopamine

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13
Q

What are Epi and NE classified as

A

Catecholamines

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14
Q

What molecule are catacholamines derived from?

A

Tyrosine AA

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15
Q

What is the mechanism of tyrosine conversion to dopamine?

A

Tyrosine is converted to dopamine through the rate limiting step of hydroxylation of tyrosine and its transport into a vesicle.

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16
Q

The transportation of tyrosine into the vesicle to create dopamine is inhibited by what drug?

A

Reserpine

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17
Q

What is required for the release of NE within the vesicle at the adrenergic receptor?

A

The influx of Calcium to cause the infusion of the vesicle with the membrane in a process called exocytosis.

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18
Q

What is the process of the fusion of the vesicle with the membrane?

A

exocytosis mediated by influx of calcium

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19
Q

What blocks the release of the NE from the vesicle?

A

Guanethidine and Bretylium

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20
Q

What prevents reuptake of NE into the neuron?

A

Cocaine and imipramine

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21
Q

What molecule methylates NE in the metabolism process?

A

COMT

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22
Q

What molecule oxidizes NE in metabolism process?

A

MAO

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23
Q

What mediated the effects of Epi, NE and Dopamine?

A

G protein coupled receptors

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24
Q

What are the fight or flight responses?

A 
increased heart rate
increased breathing or respiratory rate
decreased secretion
muscle tension
pupil dilation
digestion slows
inhibit bladder contraction
bronchi dilate
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25
what are the rest and digest response?
``` lower heart rate lower breathing or respiratory rate pupil constrict digestion stimulation secretion salivation increase bronchi constrict sexual arousal ```
26
What are adrenergic agonist?
drugs that mimic the effects of NE and Epi
27
What is the function alpha 1 receptor?
vascular constriction of smooth muscle
28
What is the function of beta 1 receptor?
increase heart ionotrophy and chronotrophy
29
What is the function of beta 2 receptor?
respiratory and uterine smooth muscle and skeletal muscle relaxation and vasodilation
30
inotrophy
strength of the muscle contraction of the heart
31
what are the effects of the alpha 1 receptor stimulation?
vasconstriction of the smooth muscle will result in the increase of BP due to perophreal vasoconstriction
32
What mechanism is activated upon stimulation of alpha 1 receptors?
Baroreflex compensatory mechanism to slow the heart rate
33
Which catecholamine has the greatest affinity for alpha 1 receptor?
Epi then NE then isoproterenol
34
What are the antagonist of the alpha 1 adrenergic receptor?
phentolamine and phenoxybenzamine
35
If it is harder for the heart to pump, what will the heart response be?
reduce HR
36
Where are alpha 2 receptors located ?
``` postsynaptic CNS neurons peripheral vasculature Platelets Adrenergic and Cholinergic nerve terminals Fat Cells Some vascular smooth muscle ```
37
What is the effect of stimulation of the alpha 2 receptors ?
activation of the receptors in the periphery causes vasoconstriction activation of the receptors in the CNS decreases the release of NE from CNS neurons
38
What does the activation of the beta 1 receptors result?
higher cardiac output higher heart rate higher inotrophy higher dromotrophy which is higher velocity of conduction
39
What are the effects of the beta 2 receptors stimulation?
vasodilation of skeletal blood vessels bronchial smooth muscle dilation
40
What are the antagonist of the beta receptors?
Beta Blockers
41
Where are the beta 3 receptors located ?
Adipose tissue | Bladder
42
What does stimulation of the beta 3 receptors do?
Help patients breath better
43
Where are dopamine receptors located?
CNS and Renal Vasculature | Pulmonary artery and heart
44
The stimulation of the D1 receptor produces what effect?
Vasodilation of the Renal ,Splanchnic and Coronary vessels Renal natriuresis Increased kidney perfusion
45
Changing what aspect of dopamine will affect its effect on organ systems?
Concentration
46
The selectivity of a drug is dependent upon what characteristics?
Receptor regulation which is the number and function is regulated by other drugs and catecholamines , hormone changes, age and disease states. Dominant receptor located on the tissue Concentration of the drug
47
What drugs are the alpha agonist?
phenylephrine | clonidine
48
Which drug has higher affinity for alpha 2 receptor?
clonidine
49
which drug has a higher affinity for alpha 1 receptor among the alpha agonist?
phenylephrine
50
What are the mixed alpha and beta receptor agonist?
NE | EPI
51
Which catecholamine is completely non selective among all receptors?
EPI
52
Which beta receptor does NE prefer?
B1
53
What drugs are beta agonist?
Dobutamine | Isoproterenol
54
Which beta agonist is nonselective?
isoproterenol
55
which beta receptor does dobutamine prefer?
beta 1
56
what drugs are the dopamine agonist?
dopamine
57
Does dopamine have a higher affinity for alpha or beta receptors?
beta more than alpha
58
dopamine prefer D1 over D2 receptor True or False
False Nonselective D receptor agonist
59
What is the function of the alpha 1 receptor?
Vascular smooth muscle contraction Increase inotrophy of heart Contract prostate Contract pilomotor smooth muscle for erecting hair Dilate pupils through pupillary dilator muscle
60
What are the alpha 2 receptor functions?
Postsynaptic neurons=Decrease the release of NE from postsynaptic neurons Platelets =Promote platelet aggregation Adrenergic and Cholinergic=Inhibit transmitter release from adrenergic and cholinergic nerve terminals Vascular smooth muscle=Contract some vascular smooth muscle Fat Cells=Inhibit lypolysis of fat cells
61
What are the beta 1 receptor functions?
Increase force and rate of contraction of the heart Increase the release of renin from juxtaglomerular cells to promote vasoconstricton
62
What are the functions of the beta 2 receptors?
respiratory, uterine and vascular smooth muscle relaxation promote potassium uptake in skeletal muscle Activates glycogenolysis and glucagon release
63
What is the function of the D1 receptor of the smooth muscle?
Dilates renal blood vessel
64
What is the function of the D2 receptor?
Modulates transmitter release at nerve endings
65
What are the selective direct acting adrenergic agents?
alpha 1 = phenylephrine alpha 2= clonidine beta 1= dobutamine
66
What are the nonselective acting adrenergic agents?
``` isoproterenol = beta receptors Epi= all receptors NE= alpha and beta receptors but prefer beta 1 ```
67
What are the mixed acting adrenergic agents?
NE | Epi
68
What is the role of indirect acting adrenergic agents?
The agent does not directly bind to the receptor but it increases the effect of the catecholamine by being a releasing agent of the adrenergic uptake inhibitor of the adrenergic MAO inhibitor COMT inhibitor
69
What is a releasing agents of the adrenergic agonist?
amphetamine | Tyramine
70
What is an uptake inhibitor of adrenergic agents?
Cocaine
71
What molecule is a MAO inhibitor?
Selegine
72
What molecule is a COMT inhibitor?
Entacapone
73
What is the main effect of Epi?
Vasoconstriction and Cardiac Stimulant
74
When Epi stimulates Beta 1 receptor what is the effect?
Increased BP due to inotrophic and chronotrophic effects which increase cardiac output
75
What is the effects of the alpha 1 receptor stimulation by Epi?
vasoconstriction which increases peripheral resistance
76
What is the effect of the beta 2 stimulation by Epi?
vasodilation of the skeletal smooth muscle blood vessels and relieves bronchospasm.
77
What are the adverse effects of Epi?
tachycardia due to over inotrophy and chronotrphy HTN due to over vasoconstriction Increased myocardial oxygen demand arthymias which is abnormal rhythm of the heart decreased renal blood flow due to vasconstriction reduced splanchnic blood flow due to vasoconstriction
78
Is Epi the first line of choice in treating shock?
No, it is second
79
What are the symptoms of shock?
oliguria which is an abnormal amount of urine being produced hypotension metabolic acidosis altered mental status
80
Major forms of shock
hypovolemic septic cardiogenic
81
What are the main methods of treating shock?
vasopressors and fluid
82
Why is Epi not the first line of choice for treating shock?
arrythmia and lactic acidosis
83
Where is it best to administer a vasopressor?
Central line
84
What is Epi best used for?
Treatment of anaphylaxis and hypersensitivity reactions Cardiac arrest and asystole Bradycardia Local anesthetic Hemostatic Dental
85
What are the adverse effects of Epi?
``` Tachycardia HTN Arrythmia anxiety headache increased myocardial oxygen demand weakness tremor decreased renal blood flow urinary retention decreased splanchnic flow sudden death ``` Epi is a powerful vasoconstrictor and cardiac stimulant
86
What happens in vasopressor extravasation?
Peripheral extravasation of vasopressors into surrounding tissue can cause excessive vasoconstriction resulting in tissue necrosis.
87
What is the antidote to vasopressor extravasation?
phentolamine
88
NE other name
levophed
89
Which receptor does NE act upon the most?
alpha 1
90
What is the effect of NE on alpha 1 receptor?
Periphreal vasoconstriction and increases systemic vascular resistance and thus mean arterial pressure.This leads to a decrease in renal mesenteric blood flow
91
What kind of effects does NE have upon beta 1 receptor ?
minimal effects with cardiac output and contractility due to baroreflex mechanism
92
Which is better used to treat shock Epi or NE?
NE because it has minimal impact on beta 1 receptor NE increases vascular resistance due to stimulation of alpha 1 receptor NE is effective circulating blood volume and venous return and preload However, Epi can be added if NE does not be effective
93
What parameters we be monitoring when administering NE in shock?
BP Extravasation Volume Status HR
94
What are the adverse effects if NE?
Arrhythmia Palpitations Bradyardia HTN Chest pain Anxiety Headache Extravasation which could lead to necrosis of tissue
95
Isoproterenol
beta agonist that is nonselective and is structurally related to Epi
96
What is the effect of isoproterenol upon beta receptors?
Positive chronotrope and inotrope Increase CO Potent Vasodilator due to activation of Beta 2 receptor which leads to reflex tachycardia
97
What does isoproterenol treat?
Bronchospasm Shock Cardiac arrest AV block
98
What are the adverse effects of isoproterenol?
Cardiac HTN Cardiac arrhythmia Premature ventricular contractions chest pain ``` CNS: nervousness restlessness anxiety insomia tremor vertigo ``` GI: Nausea and vomit Endocrine: Hyperglycemia Cough and dyspnea Skin flushing and sweating
99
Which neural pathway does dopamine regulate?
nigrostriatal pathway
100
What is the effect of a low dose of dopamine upon the D1 receptor?
Mesentery vasodilation Dilation of renal vasculature Increase Urine output and sodium excretion Increase GFR
101
What are the effects of medium dose of dopamine upon the D1 receptor?
Cardiac stimulant positive inotrophic and chronotrope Increase blood pressure More alpha stimulation at 10 mcg
102
What are the effects of high dose of dopamine?
increase blood pressure | more vasoconstriction
103
At what dose of dopamine does the alpha andrenergic receptors become stimulated?
greater than 20 mcg
104
When dopamine high concentration stimulates alpha receptors what is the adverse effect?
Vasoconstriction that compromise the circulation of limbs
105
Is dopamine a useful treatment in shock?
Yes , it is second line to NE It is preferred to be used in shock that is caused by bradycardia and aortic regurgitation, however, dopamine can cause arrythmia in shock treatment
106
What are the adverse cardiac effects of dopamine?
``` Ectopic beats Tachycardia Cardiac Conduction Vasoconstriction HTN Ventricular arrhythmia Angina Palpitations ```
107
What are the adverse effects of dopamine on the CNS?
anxiety | headache
108
What are other adverse effects of dopamine?
Dilated pupils Piloerection Dyspnea
109
What receptor does dobutamine activate?
Beta 1
110
What are the effects of dobutamine on beta 1 receptor?
inotrophic agent that is not a vasopressor insiginificant stimulation of beta 1 and alpha 1 positive cardiac effects increased cardiac output increases inotrophy increases chronotrophy produce peripheral vasodilation
111
What is dobutamine used to treat?
refractory heart failure Cardiogenic shock May be effective in low cardiac output state
112
What are the adverse effects of dobutamine?
``` tachycardia premature ventricular contractions increased systolic pressure angina pectoris dyspnea headache nausea ```
113
What receptor does phenylephrine act upon?
Alpha 1
114
What is the advantage of phenylephrine acting like a catecholamine?
cannot be hydrolyzed by COMT
115
What is phenylephrine used to treat?
Hypotension/ shock anesthesia induced Hypotension Mydriasis Nasal Decongestant
116
What are phenylephrine adverse effects?
``` Reflex bradycardia HTN Anxiety Headache and nausea Rebound Congestion Pulmonary Edema Decreased renal perfusion/ reduced urine output Extravasation can cause tissue necrosis ```
117
What does midodrine treat?
orthostatic hypotension by being a selective alpha 1 agonist
118
Ephedrine
Non selective and mixed acting, indirect stimulation of adrenergic receptor through increased activity NE of postsynaptic alpha and beta receptors and causes the release of NE from tissues stores
119
What does ephedrine treat?
hypotension during anesthesia OTC weight loss products OTC asthma symptoms
120
What adverse effects are from ephedrine?
``` Cardiac tachycardia Palpitations HTN Ectopy Arrhythmia Bradycardia ``` CNS: Moderate ability to cross into CNS
121
What is the enatiomer of ephedrine?
Pseudoephedrine
122
What receptors do pseudoepedrine work upon?
alpha and beta adrenergic receptors
123
What is pseudoephedrine made to treat?
nasal decongestion such as Sudafed
124
Pseudoephedrine is the precursor to what agent?
methamphetamine
125
What are the adverse effects of pseudoephedrine?
``` Cardiac Tachycardia Cardiac Palpitatons HTN Ectopy Arrhythmia ```
126
Amphetamines
Indirect acting on alpha and beta receptors to stimulate DA and NE and blocks reuptake
127
What is used as a treatment of ADHD?
Amphetamine
128
What are the effects of amphetamines?
``` Wakefullness Alertness Elevated mood Euphoria Increased motor or speech activites ```
129
Which has greater CNS effects metamphetamine or amphetamine?
methamphetamine
130
What is used to treat narcolepsy?
Amphetamine | Methylphenidate
131
What are the adverse effects of amphetamines?
``` Cardiovascular tachycardia HTN CNS psychological episodes Dizziness insomnia euphoria tremor headache Tourette Syndrome ``` ``` GI: Dry Mouth Diarrg=hea Constipation Anorexia ```
132
The adverse effect of Tourette Syndrome is given by which adrenergic indirect stimulant?
Amphetamine
133
Tyramine
Indirect Sympathomimetic that induces the release of catecholamines by displacing them from adrenergic nerve endings.
134
What inactivates Tyramine?
Monoamine oxidase in the liver
135
What is the effect of increased catecholamine release?
HTN
136
Which adrenergic molecule induces the release of catecholamine?
Tyramine
137
What are the catecholamine reuptake inhibitors?
COMT Antidepressants and drugs used from ADHD
138
What medical condition uses COMT inhibitors?
Parkinsons
139
What are the two nonselective alpha receptor antagonist?
Phenoxybenzamine Phentolamine
140
Reserpine
Reserpine inhibits the uptake of NE into storage vesicles resulting in depletion of catecholamines and serotonin from central peripheral axons.
141
Why is Reserpine no longer used in the United States?
Too many side effects
142
Pheochromocytoma
Tumor of the adrenal medulla that causes secretion of enormous quantities of Epi and NE.
143
What are the symptoms of pheochromoctoma?
HTN Headaches Palpitations Sweating
144
What is the treatment of pheochromocytoma?
Phentolamine or phenoxybenzamine
145
What are the effects of nonselective alpha antagonist?
Decrease peripheral resistance
146
Phentolamine
Competitive Antagonist that is used to treat alpha agonist extravasation.
147
Phenoxybenzamine
Irreversible antagonist used before surgery
148
What are the adverse effects of nonselective alpha agonist?
Hypotension Reflex tachycardia Arrhythmia
149
What are the effects of selective alpha 1 antagonist?
lead to vasodilation which will decrease BP which makes it an option for treating HTN. Relax smooth muscle in bladder neck and prostate BPH which is benign prostatic hyperplasia
150
Which alpha 1 antagonist treat both BPH and HTN?
Prazosin Terazosin Doxazosin
151
Which alpha 1 antagonist treat BPH only?
Alfuzosin Tamasulosin Silodosin
152
What are the adverse effects of alpha antagonist?
Palpitations Orthostatic hypertension syncope tachycardia CNS: drowsiness,dizziness,depression, vertigo GI:Nausea Neuromuscular: Weakness
153
Clonidine
Alpha 2 receptor agonist that promotes vasoconstriction and within the CNS suppress sympathetic outflow from the CNS. Decreases periphreal resistance, renal vascular resistance, heart rate, BP
154
Clonidine
HTN Withdrawal Migraine
155
Adverse effects of clonidine?
Bradycardia Hypotenision CNS depression Xerostomia
156
What are the clonidine derivatives ?
Apraconidine and Brimonidine eye drops Reduces intraocular pressure Bromonidine crosses BBB

Pathology (10 decks)

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