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
Q

Drugs that work on B1 receptors

A
Epi
NE
isoproterenol
dopamine
dobutamine
epinephrine
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26
Q

Therapeutic applications of B1 application

A

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

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27
Q

Adverse Effects B1 Activation

A

tachycardia
dysrhythmias
angina

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28
Q

B2 activation is limited to

A

lungs and uterus

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29
Q

Drugs used for B2 activating

A

Epi
isoproterenol
albuterol

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30
Q

therapeutic B2 Activation

A

Asthma - for bronchoconstriction and inflammation

Delay of preterm labor

31
Q

Adverse effects of B2 activation

A

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
Q

Activation of peripheral dopamine receptors causes

A

dilation of the renal vasculature

33
Q

When is activation of dopamine receptor employed

A

in the treatment of shock - dilating renal blood vessels, we can improve renal perfusion and reduce risk for renal failure

34
Q

What drug is the only one that can activate dopamine recetors

A

dopamine

35
Q

When dopamine is given to treat shock, the drug also enhances

A

cardiac performance bc activates B1 receptors in heart

36
Q

Anaphylactic shock manifestations

A

hypotension from widespread vasodilation

bronchoconstriction and edema of glottis from release of other mediators such as leukotrienes

37
Q

Why are antihistamines not very useful in anaphalaxis

A

histamine contributes but symptoms are mostly due to release of other mediators such as leukotrienes

38
Q

Receptors Epi work on

A

A1, A2, B1, B2

39
Q

Epi and diabetics

A

Can cause hyperglycemia

40
Q

Epi and BP

A

Can cause hypertensive crisis which can lead to cerebral hemorrhage

41
Q

receptors NE work on

A

A1, A2, B1

42
Q

what drug is NE

A

Levophed

43
Q

NE and diabetics

A

does not promote hyperglycemia

44
Q

clinical indications for NE

A

hypotensive state

cardiac arrest

45
Q

Receptors for isoproterenol

A

B1 B2

46
Q

Therapeutic uses for isoproterenol for heart

A

manage AV block
improve outcomes in cardiac arrest
increase cardiac output during shock

47
Q

adverse effects isoproterenol

A

tachydysrhythmias
angina
hyperglycemia in diabetics

48
Q

Effects of isoproterenol are _____ by MAO inhibitors and tricyclic antidepressants and _____ by B adrenergic blocking agents

A

enhanced

reduced

49
Q

Dopamine receptors

A

dopamine
B1
at high doses - A1

50
Q

at low therapeutic doses, dopamine acts on

A

dopamine receptors only

51
Q

at moderate therapeutic doses, dopamine acts on

A

dopamine and B1

52
Q

at very high doses, dopamine acts on

A

dopamine, B1, A1

53
Q

major indication for dopamine is

A

shock

heart failure - increases myocardial contractility and increases cardiac output

54
Q

by activating b1 receptors in the the heart, dopamine can

A

increase cardiac output, improving tissue perfusion

55
Q

by activating dopamine receptors in the kidney, dopamine can

A

dilate renal blood vessels - improves renal perfusion

56
Q

most common adverse effects of dopamine

A

tachycardia, dysrhythmias, anginal pain, extravasation may cause necrosis

57
Q

MAO inhibitors and Dopamine

A

if a pt is receiving a MAO inhibitor the dose of dopamine will need to be reduced by at least 90%

58
Q

Drug interactions with dopamine

A

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
Q

dobutamine receptor

A

B1

60
Q

The only indication for dobutamine is

A

heart failure

61
Q

major adverse effect of dobutamine is

A

tachycardia

62
Q

Drug interactions dobutamine

A

MAO inhibitors - reduce dobutamine by at least 90%

tricyclic antidepressants

certain general anestetics increase risk of dysrhythmias

63
Q

receptor for phenylephrine

A

A1

64
Q

use for phenylephrine

A

reduce nasal congestion
IV for elevating BP
eye drops to dilate pupil
coadministered with local anestetics to delay absorbtion

65
Q

receptor for albuterol

A

B2

66
Q

Adverse effects albuterol

A

tremors

tachycardia - by activating B1 receptors in heart

67
Q

receptor for ephedrine

A

A1
A2
B1
B2

68
Q

chemical class of ephedrine

A

non-catecholamine

69
Q

use of ephedrine

A

bronchodilation - asthma
improve hemodynamic status in shock
manage anesthesia induced hypotension

70
Q

Adverse effects of ephedrine

A
HTN
dysrhythmias
angina
hyperglycemia
insomnia
71
Q

MAOI s

A

isocarboxazid (Marplan)
phenelzine (Nardil)
tranylcypromine (Parnate)
Selegiline (Emsam) - patch

72
Q

drug interactions for epi

A

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
Q

tricyclic antidepressants

A
Amitriptyline
Clomipramine (Anafranil)
Desipramine (Norpramin)
Doxepin (Sinequan)
Imipramine (Tofranil)
Trimipramine (Surmontil)
74
Q

what class of anti-hypertensives can reduce adverse caused by epi and other B1 agonists

A

B Blockers (ie) metoprolol)