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PT&X > adrenergic pharmacology > Flashcards

adrenergic pharmacology Flashcards

1
Q

what are the major neurotransmitters in adrenergic pharmacology?

A

epi
norepi

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1
Q

which nervous division is adrenergic primarily focused on?

A

sympathetic

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2
Q

which cell makes epi?

A

chromaffin cells

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3
Q

true or false
sympathetic post ganglionic uses norepi

A

true

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4
Q

where did chromaffin cell originate from?

A

neural crest

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5
Q

sympathetic postganglionic neurons make and use what?

A

norepi

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6
Q

what are chromaffin cells?

A

cells in the adrenal glands that the sympathetic preganglionic neuron project to

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7
Q

where is norepi stored?

A

in the synaptic vesicle

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8
Q

where is epi stored?

A

in the chromaffin cell vesicle

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9
Q

what kind of effect is norepi?

A

local site and circulation (a little)
primarily at the local site because sympathetic postganglionic neurons are far from effector cells

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10
Q

what kind of effect is epi?

A

circulation because chromaffin cells are far away from effector cells

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11
Q

what can induce chromaffin cell to make more epi?

A

Ach
because sympathetic preganglionic neurons use Ach

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12
Q

what does Metyrosine do?

A

block the conversion of Tyrosine to L-dopa

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13
Q

what does Reserpine do?

A

block the packaging of norepi into vesicles

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14
Q

what does Bretylium do?

A

block the release to norepi

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15
Q

what does Guanethidine do?

A

block the release of norepi

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16
Q

which transporter reuptake and recycle norepi?

A

NET

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17
Q

which transporter take in norepi for vesicle packaging?

A

VMAT

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18
Q

which drugs target and block NET transporter?

A

cocaine
TCA - tricyclic antidepressants like imipramine

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19
Q

what happens when NET is blocked?

A

inhibit the reuptake/recycle of norepi
thereby increasing the conc of norepi at the synaptic cleft

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20
Q

which drugs target COMT?

A

drugs ending in -capone

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21
Q

what are the five receptors in adrenergic system?

A

alpha 1, 2
beta 1, 2, 3
all GPCR

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22
Q

which type of GPCR is alpha 1?

A

Gq

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23
Q

what type of GPCR is alpha 2?

A

Gi/0

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24
Q

what type of GPCR are the beta receptors?

A

Gs

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25
Q

where can alpha 1 receptors be found?

A

arterioles(coronary, visceral, cutaneous) PREDOMINANTLY
veins
internal sphincters
iris dilator muscle

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26
Q

where can alpha 2 receptors be found?

A

presynaptic membrane
pancreas
veins
adipose tissue
GI tract sphincter
salivary glands

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27
Q

where can beta 1 receptors be found?

A

heart - SA node, atrial muscle, AV node, ventricles
kidney - JG apparatus
adipose tissue

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28
Q

where can beta 2 receptors be found?

A

blood vessels
arterioles muscular
veins
bronchi
liver
pancreas
uterus
iris constrictor muscle

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29
Q

where can beta 3 receptors be found?

A

adipose tissues
urinary bladder

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30
Q

what is the function of autoreceptors?

A

inhibit the release of norepi
these are a group of alpha 2 receptors

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31
Q

true or false
epi acts very strong on alpha subtype receptors ie. 1 and 2

A

TRUE

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32
Q

true or false
epi has strong effect on beta receptors (1, 2)

A

TRUE

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33
Q

what is Isoproterenol?

A

a non-selective beta-adrenoreceptor agonist
an analog of epi
synthetic drug
pure beta agonist
no alpha effect

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34
Q

does epi have any effect on beta3 receptor?

A

weak or no effect at all

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35
Q

does norepi have any effect on beta2 receptor?

A

none at all

36
Q

what is the function of alpha 1 receptor?

A

cause the constriction of blood vessels (arterioles)
causing HYPERtension

37
Q

what does activation of beta 2 receptor do?

A

blood vessel dilation
can cause HYPOtension

38
Q

which beta receptors are most abundant in the heart?

A

beta 1 receptors

39
Q

what happens to the heart when beta 1 is activated?

A

increase heart rate which can cause tachycardia
increase contractility of the cardiomyocytes
overall effect is increased cardiac output

40
Q

which nerves does the adrenergic system control the heart from?

A

T1-T3

41
Q

true or false
norepi is release from adrenergic nerves

A

true

42
Q

how is blood pressure decreased?

A

thru M3 receptor of parasympathetic system
M3 activation dilate blood vessels

43
Q

what is the overall effect of the adrenergic sympathetic system on the heart?

A

to increase BP

44
Q

what happens when beta2 receptor is activated by epi?

A

blood vessel dilation

45
Q

what happens to bronchial when beta2 receptor is activated?

A

bronchial dilation thru airway smooth muscle relaxation
increased size of the airway

46
Q

which receptor is predominantly in the airway?

A

beta2

47
Q

what is mostly use for management of astha?

A

beta2 agonist

48
Q

activation of alpha 1 does what to the pupil?

A

pupil dilation

49
Q

activation of alpha 1b does what to the irish?

A

arteriole contraction = decreased aqueous humor production

50
Q

what happens when alpha receptors in GI tract activate?

A

decrease GI tract motility

51
Q

what happens when beta2 receptors activated in GI tract?

A

causes relaxation of smooth muscle which further decrease GI motility

52
Q

what happens to RAAS system when beta 1 is activated?

A

renin release from juxtaglomerular kidney cells activate angiotensin to increase BP

53
Q

which sweat gland is controlled by alpha receptor?

A

apocrine

54
Q

which swear gland is controlled by Ach?

A

eccrine

55
Q

what does activation of adrenergic system do to glucose?

A

promote glucose availability

56
Q

what receptor is activated for release of glucose?

A

beta 2 receptors in the alpha cells of the pancreas

57
Q

what hormone is released from pancreas alpha cells to increase blood glucose?

A

glucagon

58
Q

what happens when alpha2 receptor in pancreas is avctivated?

A

decrease production and secretion of insulin
increase glycolysis to give energy

59
Q

what happens to fatty acid when beta 1. 2, 3 are activated?

A

promote metabolism of fatty acid to gives energy

60
Q

how to rescue someone with low blood sugar in a coma?

A

give sugar and glucagon
or give epi to activate beta2 which will increase glucagon

61
Q

what are direct acting sympathomimetics?

A

act directly on alpha or beta receptors
act like epi or norepi

62
Q

what are in-direct acting sympathomimetics?

A

act by providing more norepi to act on alpha or beta receptors
either by inhibiting the breakdown of epi/norepi or inhibit the reuptake of norepi

63
Q

what are the 7 classes of adrenergic drugs?

A

pressor agents
cardiac stimulants
bronchodilators
nasal decongestants
CNS stimulants
anorectics
uterine relaxant and vasodilators

64
Q

what are pressor agents?

A

agents which regulate blood pressure
by increasing blood pressure
target agent is alpha1 agonist

65
Q

what are cardiac stimulant?

A

stimulates the heart
target agent is beta1 agonist

66
Q

what are bronchodilators?

A

agents to dilate/open airway
target beta2

67
Q

what is the net effect of norepi in the circulatory system?

A

increase BP because of alpha 1 activation

68
Q

what is the mechanism of Dopamine?

A

weak alpha adrenergic agonist
also acts indirectly by releasing endogenous norepi

69
Q

what happens when Dopamine indirectly release norepi?

A

increases cardiac output and systolic and diastolic pressures
therefore increase BP

70
Q

what is the clinical use of Dopamine?

A

use to increase BP in patients with hypotension

71
Q

what are the direct sympathomimetics?

A

alpha agonist
selective alpha1 agonist
selective alpha2 agonist
beta agonist
selective beta subtype agonist

72
Q

how to know with drugs are non-selective alpha agonist?

A

drugs ending in -zoline

73
Q

what is Oxymetazoline and its mechanism?

A

a non-selective alpha agonist

74
Q

how does Oxymetazoline works?

A

by stimulating alpha receptors to constrict smaller arterioles of the nasal passages and conjunctiva

75
Q

what is Oxymetazoline used for?

A

temporary relief of nasal congestion caused by allergies or common cold

76
Q

what are the selective alpha 1 agonists?

A

phenylephrine
methoxamine

77
Q

what is the mechanism of phenylephrine?

A

alpha 1 adrenergic receptor agonist

78
Q

how does phenylephrine works?

A

causes vasoconstriction, increases BP very quickly and dilates pupils

79
Q

what is phenylephrine used for?

A

injections to treat hypotension caused by shock or anesthesia
intranasal to treat congestion

80
Q

what is the mechanism of Methoxamine?

A

a pure alpha 1 adrenergic receptor agonist

81
Q

what is methoxamine used for?

A

tx and management of hypotension

82
Q

what is the selective alpha 2 agonist?

A

tizanidine

83
Q

what is the mechanism of tizanidine?

A

alpha 2 adrenergic receptor agonist

84
Q

what does tizanidine do?

A

relax skeletal muscle cells

85
Q

what is tizanidine indicated for?

A

short acting muscle relaxant

86
Q

how to know which drugs are selective alpha2 agonist?

A

drugs ending in -nidine

87
Q
A

PT&X (13 decks)

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