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Pharmacology 1 > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

what produces a physiological response as that of endogenous mediators

A

adrenergic agonist

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2
Q

which adrenergic agonist acts through stimulation of adrenergic receptors

A

direct action

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3
Q

which adrenergic agonist produces a response through the release of catecholamines from adrenergic neurons

A

indirect action

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4
Q

what are the 3 receptors of the adrenergic neurotransmission pathway

A

alpha
beta
alpha-2

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5
Q

what is the purpose of the alpha-2 adrenergic receptors in the adrenergic neurotransmission pathway

A

provide negative feedback to control the release of norepinephrine

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6
Q

what neurotransmitter is released in the adrenergic neurotransmission pathway

A

norepinephrine

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7
Q

what does the norepinephrine of the adrenergic neurotransmission pathway originate from (think neurotransmitter)

A

dopamine

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8
Q

what process is used to change dopamine into norepinephrine

A

hydrolyzation

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9
Q

what triggers the release of the norepinephrine from the neuron in the adrenergic neurotransmission pathway

A

change in cell membrane potential (action potentials) / influx of Ca++

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10
Q

which neurotransmitters are involved with adrenergic receptors

A

norepinephrine & epinephrine

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11
Q

what types of receptors are associated with adrenergic receptors

A

alpha & beta

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12
Q

which adrenergic receptors have a slightly higher affinity for epinephrine over norepinephrine

A

beta 2 and alpha receptors

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13
Q

which adrenergic receptor has an equal affinity for epinephrine and norepinephrine

A

beta 1

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14
Q

where are alpha-1 receptors found

A

post synaptic membrane of effector organs

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15
Q

where can alpha-2 receptors be found

A
  1. pre-synaptic
  2. post synaptic in beta cells of pancreas and blood vessels
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16
Q

what G protein is associated with alpha 1 receptors

A

Gq

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17
Q

what G protein is associated with alpha-2 receptors

A

Gi

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18
Q

which G protein is associated with beta receptors

A

Gs

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19
Q

what enzyme is used in addition to G protein Gq

A

Phospholipase C

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20
Q

what is the result of Gq acting on an alpha-1 receptor

A

smooth muscle contraction

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21
Q

what is the result of the activation of Phospholipase C

A

IP3 –> Ca++ release

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22
Q

what is the result of Gi acting on the Alpha-2 receptor

A

decrease adenylyl cyclase
decrease cAMP

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23
Q

if there is an inhibitory effect on alpha-2 receptor, what is the outcome

A

smooth muscle contraction / vasoconstriction

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24
Q

what is the result of the activation of beta receptor with Gs

A

heart muscle contraction
smooth muscle contraction
glycogenolysis

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25
Q

what stops the functions of the alpha-2 receptor

A

dephosphorylation

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26
Q

what adrenergic receptor is critical in controlling blood pressure

A

Beta-1

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27
Q

which beta receptor has a higher affinity for epinephrine

A

beta-2

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28
Q

where are beta-1 receptors often found

A

heart
kidney
fat cells

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29
Q

True or False:

Beta-1 receptors have an equal affinity for epinephrine and norepinephrine

A

true

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30
Q

where are Beta-2 receptors mostly found

A

blood vessels of skeletal muscle
liver
smooth muscles of bronchus
IG tract
uterus

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31
Q

what tissue/ organ does B1 receptors affect

A

cardiac

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32
Q

if there is an increase of epinephrine on a B1 receptor in the cardiac tissue, what is the result

A

increased HR
increased contractibility
increased cardiac output

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33
Q

what is the effect of norepinephrine on a B1 receptor in cardiac tissue

A

increased HR followed by a decrease in HR caused by vagal stimulation

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34
Q

True or False:

There will be an increase in heart contractibility in the presence of norepinephrine in the cardiac tissue

A

true

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35
Q

what receptor is mainly in charge of blood pressure

A

B1

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36
Q

why does diastolic pressure see little to no change in the presence of epinephrine on B1 receptors in cardiac tissue

A

B2 receptors = relaxation
norepinephrine has a greater affinity on B2 receptors

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36
Q

why does diastolic pressure see little to no change in the presence of epinephrine on B1 receptors in cardiac tissue

A

B2 receptors = relaxation
norepinephrine has a greater affinity on B2 receptors

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37
Q

what receptors create constriction of the blood vessels in the presence of epinephrine

A

alpha 1
alpha 2

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38
Q

what receptors cause dilatation of the blood vessels in splanchic and skeletal muscles in the presence of epinephrine

A

alpha 1
alpha 2
beta 2

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39
Q

what is the response of alpha 1 & 2 receptors of the blood vessels in the presence of norepinephrine

A

constriction

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40
Q

what receptor is caused bronchial dilation / relaxation in the presence of epinephrine

A

beta 2

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41
Q

how does beta 2 receptors in the respiratory tract response to norepinephrine

A

no response

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42
Q

what is the function of alpha 1, alpha 2, and beta 2 receptors in the GIT with epinephrine

A

relaxation

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43
Q

with the GI tract, what receptor is responsible for contraction of the sphincter muscle with epinephrine

A

alpha 1

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44
Q

True or False:

both epinephrine and norepinephrine cause constriction of the sphincter muscles of the GI tract with an A1 receptor present

A

true

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45
Q

what receptors are found in the urinary bladder

A

Beta 2
Alpha 1

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46
Q

where is the beta 2 receptor found in the urinary bladder

A

detrusor muscle

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47
Q

where is the alpha 1 receptor found in the urinary bladder

48
Q

what is the result of epinephrine acting on the detrusor muscle

A

relaxation via beta 2 receptor

49
Q

what receptors are found in the uterus

A

alpha 1
alpha 2
beta 2

50
Q

what is the result of the presence of epinephrine on the uterus

A

relaxation and contraction due to the mix of receptors

51
Q

which receptor is most used for relaxation of smooth muscles

52
Q

what receptor is found within the male sex organs

A

alpha 1
(constriction functions)

53
Q

what receptor’s primary job is constriction

54
Q

what receptor is found in relation to “goose bumps”

55
Q

what receptors are found within the eye structures

A

alpha 1
beta 2

56
Q

what receptor is found within the iris/ radial muscle of the eye

57
Q

what is the result of alpha 1 receptors under epinephrine and norepinephrine in the eye

A

contraction for pupil dilation

58
Q

what is the result of epinephrine acting on the beta 2 receptor in the eye

A

relaxation for far vision

59
Q

where in the eye are the beta 2 receptors found

A

ciliary muscle

60
Q

what receptors are used for metabolic effects

A

alpha 2
alpha 1
beta 1
beta 2

61
Q

what receptors are found in the liver

A

alpha 1
beta 2

62
Q

what process is triggered by the increase of epinephrine or norepinephrine in the liver

A

glycogenolysis

63
Q

what receptors are found associated with fat cells/ tissue

A

alpha 2
beta 1

64
Q

what process is associated with the increase of epinephrine or norepinephrine in the fat cells/ tissue

65
Q

what receptors are found in associated with the pancreas

A

alpha 2
beta 2

66
Q

what is the function of the alpha 2 receptor in the pancreas in the presence of epinephrine

A

decreased insulin secretion

67
Q

what is the function of the beta 2 receptor in the pancreas in the presence of epinephrine

A

increased insulin secretion

68
Q

True or False:

the pancreas receptors respond to both epinephrine and norepinephrine

A

FALSE
they respond the most to epinephrine increases

69
Q

what receptor has mostly inhibitory effects because of its presynaptic location

70
Q

what is the biotransformation route of catecholamines in the oral route

A

metabolism by conjugation and oxidation

71
Q

which administration route is not effective with catecholamines

A

oral route

72
Q

why is the SubQ administration not a great route for catecholamines

A

needs good perfusion / slow absorption

73
Q

how are catecholamines metabolized

A

COMT & MAO

74
Q

how are catecholamines excreted from the system

A

in urine
(renal system)

75
Q

how should an epinephrine solution be administered

76
Q

what kind of epinephrine is used as an aerosol and ophthalmic solution

A

epinephrine bitartrate

77
Q

what route / mix of epinephrine can give a slow consistent release from 2 mg/ml

A

epinephrine suspension

78
Q

if using epinephrine to relieve respiratory distress due to bronchospasm, what receptor would be affected

79
Q

what receptors would be affected in cases of inducing bronchodilation with epinephrine

80
Q

in cases of hypotension, what receptors would be affected

A

alpha 1
beta 1

81
Q

in a case of cardiac arrest, what receptors are acted on with epinephrine

A

all of them

82
Q

why are all receptors activated in a case of hypersensitivity reactions

A

multiple systems are failing and there are several correcting factors

83
Q

what neurotransmitter can be used to prolong the action of local anaesthetic drugs

A

epinephrine

84
Q

how can epinephrine be used as a topical haemostatic agent

A

alpha 1 receptors constrict peripheral vessels

85
Q

what are the adverse effects of epinephrine uses

A
  • fear, anxiety, weakness, dizziness, tremors and respiratory difficulty and palpitations
86
Q

what are some adverse effects of using epinephrine in a hypertensive patient

A
  • cerebral vascular haemorrhage
    -ruptured aneurysms
87
Q

what pre-existing conditions could possibly lead to an increase of myocardial toxicity if given epinephrine

A
  1. hyperthyroid
  2. halogenated hydrocarbon anaesthetics
  3. hypertensive
88
Q

what are some major adverse effects to look out for in the case of administering epinephrine

A

cardiac arrhythmia & necrosis/ sloughing tissue at injection site

89
Q

why is epinephrine considered contraindicated in pregnancies

A

induces contraction of the uterus

90
Q

what is the immediate metabolic precursor of norepinephrine and epinephrine

91
Q

what does dopamine effect

A

motor activity

92
Q

what is dopamine (class)

A

central neurotransmitter

93
Q

how is dopamine metabolized

94
Q

at low concentrations, what receptor is involved with dopamine

95
Q

what is the result of a low dopamine dosage

A

increased renal blood flow and urine production

96
Q

in what cases could epinephrine be used but should be used with caution

A

cardiogenic
hypovolemic shock

97
Q

at higher doses of dopamine, what receptors are affected

A

B1 receptors

98
Q

what type of reaction is caused from a high dosage of dopamine

A

positive inotropic action

99
Q

what is the physiological result of the high doses of dopamine

A

releases NE from nerve terminals

100
Q

at maximal concentrations of dopamine, what receptor is being affected

101
Q

what is the physiological result of a maximal dose of dopamine

A

vasoconstriction

102
Q

how would you administer dopamine hydrochloride

A

IV route
administered @ 2-5 ug/kg/min

gradually increase to 20-50 ug/kg/min

103
Q

how does the use of dopamine affect cats

A

delayed diuresis in cats

104
Q

how is delayed diuresis caused in cats from the administration of dopamine

A

reduced number of dopaminergic receptors

105
Q

what is the synthetic analogue of dopamine

A

dopexamine

106
Q

how does dopexamine affect cardiac output

A

activates B-receptors to increase cardiac output

107
Q

what is the effect of neuronal reuptake from the administration of dopexamine

A

inhibits neuronal reuptake (inotropic effect)

108
Q

what is the D1 selective agonist derivative of dopamine

A

fenoldopam

109
Q

what is fenoldopam used to treat

A

hypertensive crisis

110
Q

what G protein in affected by Fenoldopam

A

Gs proteins

111
Q

what precaution should be used when treating hypovolemic shock with dopamine

A

fluids should be administered first
(hypovolemia corrected first)

112
Q

what is the possible adverse reactions caused by dopamine

A
  1. extravasation of dopamine
  2. ischaemic necrosis and sloughing
113
Q

when should dopamine administration be avoided

A

patients receiving MAO inhibitors or taking tricyclic antidepressants

114
Q

what are the direct-acting agonists

A

-epinephrine
-norepinephrine
-dopamine
-phenylephrine
-clonidine

115
Q

what is the impact of using indirect acting agonists on the body

A

release NE from the storage vesicles

116
Q

what are the indirect-acting agonists

A

amphetamine
tyramine

117
Q

what is an example of a mixed-action agonist

Pharmacology 1 (10 decks)

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