Ch 15 Flashcards

1
Q

Class of drugs who produce their effects by activating adrenergic receptors

A

Adrenergic Agonists aka sympathomimetics

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2
Q

Drugs can activate adrenergic receptors by what 4 basic mechanisms

A

1) direct receptor binding!!!!!
2) promotion of Norepinephrine (NE)
3) blockade of NE reuptake
4) inhibition of NE inactivation

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3
Q

what are the two major classes of adrenergic agonists

A

catecholamines

noncatecholamines

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4
Q

What 3 things do catecholamines have in common

A

cannot be used orally

brief duration of action

cannot cross BBB

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5
Q

what are the two enzymes responsible for the brief duration of action and not being able to take catecholamines orally

A

MAO

COMT

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6
Q

Where does MAO and COMT (enzymes) live

A

liver and intestinal wall

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7
Q

Can you give catacholamines orally? why/why not

A

no, because MAO and COMT inactivate them before reaching systemic circulation

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8
Q

Which catecholamines are only effective if given by continuous infusion

A

NE
dopamine
dobutamine

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9
Q

NE or dopamine that has turned from colorless to pink or brown. Is this normal?

A

no, the pigmentation is caused by oxidation and should be discarded

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10
Q

Dobutamine that has turned pink or brown. Is this normal?

A

Dobutamine can be used up to 24 hours after solution was made even if discoloration appears

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11
Q

ephedrine
albuterol
phenylephrine

are what?

A

noncatecholamines

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12
Q

3 differences of noncatechlamines

A

longer half-lives
can be given orally
more able to cross the BBB

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13
Q

what receptors does albuterol activate

A

highly selective for B2

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14
Q

what receptors for isoproterenol

A

less selective, B1, B2

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15
Q

What receptors for Epinephrine

A

even less selective, A1, A2, B1, B2

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16
Q

At low doses, selectivity is

A

maximal

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17
Q

as doses increased, selectivity

A

declines

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18
Q

What drugs are capable of activating A1 receptors

A
epinephrine
NE
phenylephrine
ephedrine
dopamine
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19
Q

Theraeputic application of A1 activation

A

vasoconstriction -blood vessels of skin, viscera, mucous membranes

mydriasis

uses
hemostasis (Epi)
nasal decongestants
adjunct to local anesthetics (lido with epi)
Elevation of BP
Mydriasis (dilate pupil for eye exams or surgery)

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20
Q

adverse effects of A1 activation

A

Hypertension (widespread vasoconstriction)

Necrosis (IV extravates - surrounding tissue tissue)

Bradycardia (A1 agonists can cause reflex slowing of the heart. Vasoconstriction elevates BP which triggers baroreceptor reflex which leads to bradycardia

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21
Q

if extravation of a A1 agonists, what should the area be infiltrated with?

A

A1 blocking agent

phentolamine

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22
Q

2 effects of Central A2 agonists

A

1) reduction of sympathetic outflow to heart and blood vessels
2) relief of severe pain

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23
Q

catecholamines that work on A2

A

epinephrine

norepinephrine

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24
Q

noncatecholamine that works on A2

A

Ephedrine

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25
Drugs that work on B1 receptors
``` Epi NE isoproterenol dopamine dobutamine epinephrine ```
26
Therapeutic applications of B1 application
Heart failure - positive inotropic effects Shock - increase HR and force of contraction - which increases Cardiac output and tissue perfusion AV heart block - enhance impulse conduction Cardiac arrest
27
Adverse Effects B1 Activation
tachycardia dysrhythmias angina
28
B2 activation is limited to
lungs and uterus
29
Drugs used for B2 activating
Epi isoproterenol albuterol
30
therapeutic B2 Activation
Asthma - for bronchoconstriction and inflammation Delay of preterm labor
31
Adverse effects of B2 activation
Hyperglycemia in Diabetics Tremors - activation of B2 receptors in skeletal muscle enhances contraction This can be a problem in diabetics bc a symptom of hypoglycemia is tremors but it may be accompanied by hyperglycemia
32
Activation of peripheral dopamine receptors causes
dilation of the renal vasculature
33
When is activation of dopamine receptor employed
in the treatment of shock - dilating renal blood vessels, we can improve renal perfusion and reduce risk for renal failure
34
What drug is the only one that can activate dopamine recetors
dopamine
35
When dopamine is given to treat shock, the drug also enhances
cardiac performance bc activates B1 receptors in heart
36
Anaphylactic shock manifestations
hypotension from widespread vasodilation bronchoconstriction and edema of glottis from release of other mediators such as leukotrienes
37
Why are antihistamines not very useful in anaphalaxis
histamine contributes but symptoms are mostly due to release of other mediators such as leukotrienes
38
Receptors Epi work on
A1, A2, B1, B2
39
Epi and diabetics
Can cause hyperglycemia
40
Epi and BP
Can cause hypertensive crisis which can lead to cerebral hemorrhage
41
receptors NE work on
A1, A2, B1
42
what drug is NE
Levophed
43
NE and diabetics
does not promote hyperglycemia
44
clinical indications for NE
hypotensive state | cardiac arrest
45
Receptors for isoproterenol
B1 B2
46
Therapeutic uses for isoproterenol for heart
manage AV block improve outcomes in cardiac arrest increase cardiac output during shock
47
adverse effects isoproterenol
tachydysrhythmias angina hyperglycemia in diabetics
48
Effects of isoproterenol are _____ by MAO inhibitors and tricyclic antidepressants and _____ by B adrenergic blocking agents
enhanced | reduced
49
Dopamine receptors
dopamine B1 at high doses - A1
50
at low therapeutic doses, dopamine acts on
dopamine receptors only
51
at moderate therapeutic doses, dopamine acts on
dopamine and B1
52
at very high doses, dopamine acts on
dopamine, B1, A1
53
major indication for dopamine is
shock heart failure - increases myocardial contractility and increases cardiac output
54
by activating b1 receptors in the the heart, dopamine can
increase cardiac output, improving tissue perfusion
55
by activating dopamine receptors in the kidney, dopamine can
dilate renal blood vessels - improves renal perfusion
56
most common adverse effects of dopamine
tachycardia, dysrhythmias, anginal pain, extravasation may cause necrosis
57
MAO inhibitors and Dopamine
if a pt is receiving a MAO inhibitor the dose of dopamine will need to be reduced by at least 90%
58
Drug interactions with dopamine
MAO inhibitor - large dose decrease needed Tricyclic antidepressants can also intensify dopamines actions Certain general anesthetics can increase risk for dysrhythmias diuretics can complement the beneficial effects of dopamine on kidneys
59
dobutamine receptor
B1
60
The only indication for dobutamine is
heart failure
61
major adverse effect of dobutamine is
tachycardia
62
Drug interactions dobutamine
MAO inhibitors - reduce dobutamine by at least 90% tricyclic antidepressants certain general anestetics increase risk of dysrhythmias
63
receptor for phenylephrine
A1
64
use for phenylephrine
reduce nasal congestion IV for elevating BP eye drops to dilate pupil coadministered with local anestetics to delay absorbtion
65
receptor for albuterol
B2
66
Adverse effects albuterol
tremors | tachycardia - by activating B1 receptors in heart
67
receptor for ephedrine
A1 A2 B1 B2
68
chemical class of ephedrine
non-catecholamine
69
use of ephedrine
bronchodilation - asthma improve hemodynamic status in shock manage anesthesia induced hypotension
70
Adverse effects of ephedrine
``` HTN dysrhythmias angina hyperglycemia insomnia ```
71
MAOI s
isocarboxazid (Marplan) phenelzine (Nardil) tranylcypromine (Parnate) Selegiline (Emsam) - patch
72
drug interactions for epi
MAOIs - will prolong and intensify effects of epi. should not receive epi in most cases Tricyclic antidepressants - blocking reuptake of catecholamines - can intensify and prolong epis effects. May need a lower dose of epi general anesthetics - several inhalation anesthetics make the heart hypersensitive exposure to epi can cause tachydysrhythmias
73
tricyclic antidepressants
``` Amitriptyline Clomipramine (Anafranil) Desipramine (Norpramin) Doxepin (Sinequan) Imipramine (Tofranil) Trimipramine (Surmontil) ```
74
what class of anti-hypertensives can reduce adverse caused by epi and other B1 agonists
B Blockers (ie) metoprolol)