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Pathology > Pharmacology Class 2020: Adrenergics > Flashcards

Pharmacology Class 2020: Adrenergics Flashcards

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
Q

what are the rest and digest response?

A 
lower heart rate
lower breathing or respiratory rate
pupil constrict
digestion stimulation
secretion
salivation increase
bronchi constrict
sexual arousal
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26
Q

What are adrenergic agonist?

A

drugs that mimic the effects of NE and Epi

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27
Q

What is the function alpha 1 receptor?

A

vascular constriction of smooth muscle

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28
Q

What is the function of beta 1 receptor?

A

increase heart ionotrophy and chronotrophy

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29
Q

What is the function of beta 2 receptor?

A

respiratory and uterine smooth muscle and skeletal muscle relaxation and vasodilation

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30
Q

inotrophy

A

strength of the muscle contraction of the heart

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31
Q

what are the effects of the alpha 1 receptor stimulation?

A

vasconstriction of the smooth muscle will result in the increase of BP due to perophreal vasoconstriction

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32
Q

What mechanism is activated upon stimulation of alpha 1 receptors?

A

Baroreflex compensatory mechanism to slow the heart rate

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33
Q

Which catecholamine has the greatest affinity for alpha 1 receptor?

A

Epi then NE then isoproterenol

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34
Q

What are the antagonist of the alpha 1 adrenergic receptor?

A

phentolamine and phenoxybenzamine

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35
Q

If it is harder for the heart to pump, what will the heart response be?

A

reduce HR

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36
Q

Where are alpha 2 receptors located ?

A 
postsynaptic CNS neurons
peripheral vasculature
Platelets
Adrenergic and Cholinergic nerve terminals
Fat Cells
Some vascular smooth muscle
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37
Q

What is the effect of stimulation of the alpha 2 receptors ?

A

activation of the receptors in the periphery causes vasoconstriction

activation of the receptors in the CNS decreases the release of NE from CNS neurons

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38
Q

What does the activation of the beta 1 receptors result?

A

higher cardiac output
higher heart rate
higher inotrophy
higher dromotrophy which is higher velocity of conduction

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39
Q

What are the effects of the beta 2 receptors stimulation?

A

vasodilation of skeletal blood vessels

bronchial smooth muscle dilation

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40
Q

What are the antagonist of the beta receptors?

A

Beta Blockers

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41
Q

Where are the beta 3 receptors located ?

A

Adipose tissue

Bladder

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42
Q

What does stimulation of the beta 3 receptors do?

A

Help patients breath better

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43
Q

Where are dopamine receptors located?

A

CNS and Renal Vasculature

Pulmonary artery and heart

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44
Q

The stimulation of the D1 receptor produces what effect?

A

Vasodilation of the Renal ,Splanchnic and
Coronary vessels

Renal natriuresis
Increased kidney perfusion

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45
Q

Changing what aspect of dopamine will affect its effect on organ systems?

A

Concentration

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46
Q

The selectivity of a drug is dependent upon what characteristics?

A

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

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47
Q

What drugs are the alpha agonist?

A

phenylephrine

clonidine

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48
Q

Which drug has higher affinity for alpha 2 receptor?

A

clonidine

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49
Q

which drug has a higher affinity for alpha 1 receptor among the alpha agonist?

A

phenylephrine

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50
Q

What are the mixed alpha and beta receptor agonist?

A

NE

EPI

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51
Q

Which catecholamine is completely non selective among all receptors?

A

EPI

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52
Q

Which beta receptor does NE prefer?

A

B1

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53
Q

What drugs are beta agonist?

A

Dobutamine

Isoproterenol

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54
Q

Which beta agonist is nonselective?

A

isoproterenol

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55
Q

which beta receptor does dobutamine prefer?

A

beta 1

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56
Q

what drugs are the dopamine agonist?

A

dopamine

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57
Q

Does dopamine have a higher affinity for alpha or beta receptors?

A

beta more than alpha

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58
Q

dopamine prefer D1 over D2 receptor

True or False

A

False

Nonselective D receptor agonist

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59
Q

What is the function of the alpha 1 receptor?

A

Vascular smooth muscle contraction

Increase inotrophy of heart

Contract prostate

Contract pilomotor smooth muscle for erecting hair

Dilate pupils through pupillary dilator muscle

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60
Q

What are the alpha 2 receptor functions?

A

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

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61
Q

What are the beta 1 receptor functions?

A

Increase force and rate of contraction of the heart

Increase the release of renin from juxtaglomerular cells to promote vasoconstricton

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62
Q

What are the functions of the beta 2 receptors?

A

respiratory, uterine and vascular smooth muscle relaxation

promote potassium uptake in skeletal muscle

Activates glycogenolysis and glucagon release

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63
Q

What is the function of the D1 receptor of the smooth muscle?

A

Dilates renal blood vessel

64
Q

What is the function of the D2 receptor?

A

Modulates transmitter release at nerve endings

65
Q

What are the selective direct acting adrenergic agents?

A

alpha 1 = phenylephrine
alpha 2= clonidine
beta 1= dobutamine

66
Q

What are the nonselective acting adrenergic agents?

A 
isoproterenol = beta receptors
Epi= all receptors
NE= alpha and beta receptors but prefer beta 1
67
Q

What are the mixed acting adrenergic agents?

A

NE

Epi

68
Q

What is the role of indirect acting adrenergic agents?

A

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
Q

What is a releasing agents of the adrenergic agonist?

A

amphetamine

Tyramine

70
Q

What is an uptake inhibitor of adrenergic agents?

A

Cocaine

71
Q

What molecule is a MAO inhibitor?

A

Selegine

72
Q

What molecule is a COMT inhibitor?

A

Entacapone

73
Q

What is the main effect of Epi?

A

Vasoconstriction and Cardiac Stimulant

74
Q

When Epi stimulates Beta 1 receptor what is the effect?

A

Increased BP due to inotrophic and chronotrophic effects which increase cardiac output

75
Q

What is the effects of the alpha 1 receptor stimulation by Epi?

A

vasoconstriction which increases peripheral resistance

76
Q

What is the effect of the beta 2 stimulation by Epi?

A

vasodilation of the skeletal smooth muscle blood vessels and relieves bronchospasm.

77
Q

What are the adverse effects of Epi?

A

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
Q

Is Epi the first line of choice in treating shock?

A

No, it is second

79
Q

What are the symptoms of shock?

A

oliguria which is an abnormal amount of urine being produced

hypotension

metabolic acidosis

altered mental status

80
Q

Major forms of shock

A

hypovolemic
septic
cardiogenic

81
Q

What are the main methods of treating shock?

A

vasopressors and fluid

82
Q

Why is Epi not the first line of choice for treating shock?

A

arrythmia and lactic acidosis

83
Q

Where is it best to administer a vasopressor?

A

Central line

84
Q

What is Epi best used for?

A

Treatment of anaphylaxis and hypersensitivity reactions

Cardiac arrest and asystole

Bradycardia

Local anesthetic
Hemostatic
Dental

85
Q

What are the adverse effects of Epi?

A 
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
Q

What happens in vasopressor extravasation?

A

Peripheral extravasation of vasopressors into surrounding tissue can cause excessive vasoconstriction resulting in tissue necrosis.

87
Q

What is the antidote to vasopressor extravasation?

A

phentolamine

88
Q

NE other name

A

levophed

89
Q

Which receptor does NE act upon the most?

A

alpha 1

90
Q

What is the effect of NE on alpha 1 receptor?

A

Periphreal vasoconstriction and increases systemic vascular resistance and thus mean arterial pressure.This leads to a decrease in renal mesenteric blood flow

91
Q

What kind of effects does NE have upon beta 1 receptor ?

A

minimal effects with cardiac output and contractility due to baroreflex mechanism

92
Q

Which is better used to treat shock Epi or NE?

A

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
Q

What parameters we be monitoring when administering NE in shock?

A

BP
Extravasation
Volume Status
HR

94
Q

What are the adverse effects if NE?

A

Arrhythmia

Palpitations

Bradyardia

HTN

Chest pain

Anxiety

Headache

Extravasation which could lead to necrosis of tissue

95
Q

Isoproterenol

A

beta agonist that is nonselective and is structurally related to Epi

96
Q

What is the effect of isoproterenol upon beta receptors?

A

Positive chronotrope and inotrope
Increase CO
Potent Vasodilator due to activation of Beta 2 receptor which leads to reflex tachycardia

97
Q

What does isoproterenol treat?

A

Bronchospasm
Shock
Cardiac arrest
AV block

98
Q

What are the adverse effects of isoproterenol?

A

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
Q

Which neural pathway does dopamine regulate?

A

nigrostriatal pathway

100
Q

What is the effect of a low dose of dopamine upon the D1 receptor?

A

Mesentery vasodilation
Dilation of renal vasculature
Increase Urine output and sodium excretion
Increase GFR

101
Q

What are the effects of medium dose of dopamine upon the D1 receptor?

A

Cardiac stimulant
positive inotrophic and chronotrope
Increase blood pressure
More alpha stimulation at 10 mcg

102
Q

What are the effects of high dose of dopamine?

A

increase blood pressure

more vasoconstriction

103
Q

At what dose of dopamine does the alpha andrenergic receptors become stimulated?

A

greater than 20 mcg

104
Q

When dopamine high concentration stimulates alpha receptors what is the adverse effect?

A

Vasoconstriction that compromise the circulation of limbs

105
Q

Is dopamine a useful treatment in shock?

A

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
Q

What are the adverse cardiac effects of dopamine?

A 
Ectopic beats
Tachycardia
Cardiac Conduction
Vasoconstriction
HTN
Ventricular arrhythmia
Angina
Palpitations
107
Q

What are the adverse effects of dopamine on the CNS?

A

anxiety

headache

108
Q

What are other adverse effects of dopamine?

A

Dilated pupils

Piloerection

Dyspnea

109
Q

What receptor does dobutamine activate?

A

Beta 1

110
Q

What are the effects of dobutamine on beta 1 receptor?

A

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
Q

What is dobutamine used to treat?

A

refractory heart failure
Cardiogenic shock

May be effective in low cardiac output state

112
Q

What are the adverse effects of dobutamine?

A 
tachycardia
premature ventricular contractions
increased systolic pressure
angina pectoris
dyspnea
headache 
nausea
113
Q

What receptor does phenylephrine act upon?

A

Alpha 1

114
Q

What is the advantage of phenylephrine acting like a catecholamine?

A

cannot be hydrolyzed by COMT

115
Q

What is phenylephrine used to treat?

A

Hypotension/ shock
anesthesia induced Hypotension
Mydriasis
Nasal Decongestant

116
Q

What are phenylephrine adverse effects?

A 
Reflex bradycardia
HTN
Anxiety
Headache and nausea
Rebound Congestion
Pulmonary Edema
Decreased renal perfusion/ reduced urine output
Extravasation can cause tissue necrosis
117
Q

What does midodrine treat?

A

orthostatic hypotension by being a selective alpha 1 agonist

118
Q

Ephedrine

A

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
Q

What does ephedrine treat?

A

hypotension during anesthesia
OTC weight loss products
OTC asthma symptoms

120
Q

What adverse effects are from ephedrine?

A 
Cardiac tachycardia
Palpitations
HTN
Ectopy
Arrhythmia
Bradycardia

CNS: Moderate ability to cross into CNS

121
Q

What is the enatiomer of ephedrine?

A

Pseudoephedrine

122
Q

What receptors do pseudoepedrine work upon?

A

alpha and beta adrenergic receptors

123
Q

What is pseudoephedrine made to treat?

A

nasal decongestion such as Sudafed

124
Q

Pseudoephedrine is the precursor to what agent?

A

methamphetamine

125
Q

What are the adverse effects of pseudoephedrine?

A 
Cardiac Tachycardia
Cardiac Palpitatons
HTN
Ectopy
Arrhythmia
126
Q

Amphetamines

A

Indirect acting on alpha and beta receptors to stimulate DA and NE and blocks reuptake

127
Q

What is used as a treatment of ADHD?

A

Amphetamine

128
Q

What are the effects of amphetamines?

A 
Wakefullness
Alertness
Elevated mood
Euphoria
Increased motor or speech activites
129
Q

Which has greater CNS effects metamphetamine or amphetamine?

A

methamphetamine

130
Q

What is used to treat narcolepsy?

A

Amphetamine

Methylphenidate

131
Q

What are the adverse effects of amphetamines?

A 
Cardiovascular tachycardia
HTN
CNS psychological episodes
Dizziness
insomnia
euphoria
tremor 
headache
Tourette Syndrome
GI:
Dry Mouth
Diarrg=hea
Constipation
Anorexia
132
Q

The adverse effect of Tourette Syndrome is given by which adrenergic indirect stimulant?

A

Amphetamine

133
Q

Tyramine

A

Indirect Sympathomimetic that induces the release of catecholamines by displacing them from adrenergic nerve endings.

134
Q

What inactivates Tyramine?

A

Monoamine oxidase in the liver

135
Q

What is the effect of increased catecholamine release?

A

HTN

136
Q

Which adrenergic molecule induces the release of catecholamine?

A

Tyramine

137
Q

What are the catecholamine reuptake inhibitors?

A

COMT

Antidepressants and drugs used from ADHD

138
Q

What medical condition uses COMT inhibitors?

A

Parkinsons

139
Q

What are the two nonselective alpha receptor antagonist?

A

Phenoxybenzamine

Phentolamine

140
Q

Reserpine

A

Reserpine inhibits the uptake of NE into storage vesicles resulting in depletion of catecholamines and serotonin from central peripheral axons.

141
Q

Why is Reserpine no longer used in the United States?

A

Too many side effects

142
Q

Pheochromocytoma

A

Tumor of the adrenal medulla that causes secretion of enormous quantities of Epi and NE.

143
Q

What are the symptoms of pheochromoctoma?

A

HTN
Headaches
Palpitations
Sweating

144
Q

What is the treatment of pheochromocytoma?

A

Phentolamine or phenoxybenzamine

145
Q

What are the effects of nonselective alpha antagonist?

A

Decrease peripheral resistance

146
Q

Phentolamine

A

Competitive Antagonist that is used to treat alpha agonist extravasation.

147
Q

Phenoxybenzamine

A

Irreversible antagonist used before surgery

148
Q

What are the adverse effects of nonselective alpha agonist?

A

Hypotension
Reflex tachycardia
Arrhythmia

149
Q

What are the effects of selective alpha 1 antagonist?

A

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
Q

Which alpha 1 antagonist treat both BPH and HTN?

A

Prazosin
Terazosin
Doxazosin

151
Q

Which alpha 1 antagonist treat BPH only?

A

Alfuzosin
Tamasulosin
Silodosin

152
Q

What are the adverse effects of alpha antagonist?

A

Palpitations
Orthostatic hypertension
syncope
tachycardia

CNS: drowsiness,dizziness,depression, vertigo

GI:Nausea

Neuromuscular: Weakness

153
Q

Clonidine

A

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
Q

Clonidine

A

HTN
Withdrawal
Migraine

155
Q

Adverse effects of clonidine?

A

Bradycardia
Hypotenision
CNS depression
Xerostomia

156
Q

What are the clonidine derivatives ?

A

Apraconidine and Brimonidine eye drops
Reduces intraocular pressure
Bromonidine crosses BBB

Pathology (10 decks)

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