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PMCOL 343 > 3- autonomic > Flashcards

3- autonomic Flashcards

1
Q

what are 4 choline esters

A

acetylcholine
carbachol
bethanechol
methacholine

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2
Q

how are choline esters absorbed in the GI tract

A

poorly

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3
Q

what is the main effect of muscarinic agonists

A

parasympathomimetic (stimulates the parasympathetic system)

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4
Q

what is the main effect of nicotinic agonists

A

parasympathetic and sympathetic effects in autonomic ganglia and skeletal muscle

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5
Q

is ACh nicotinic or muscarinic

A

both

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6
Q

is carbachol nicotinic or muscarinic

A

both

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7
Q

is bethanecol nicotinic or muscarinic

A

muscarinic

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8
Q

what makes carbachol and bethanecol different from ACh

A

they are not hydrolyzed by acetylcholinesterase

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9
Q

what is the methacholine challenge for asthma

A

Methacholine is a non-selective muscarinic receptor agonist that acts directly on airway smooth muscle receptors to induce bronchoconstriction. It is administered to test how sensitive lungs are to the PSNS

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10
Q

what are 3 muscarinic agonists

A

muscarine
oxotremorine
pilocarpine

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11
Q

what is acetylcholine

A

a choline ester

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12
Q

what is carbachol

A

a choline ester

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13
Q

what is bethanechol

A

a choline ester

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14
Q

what is muscarine

A

muscarinic agonist

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15
Q

what is oxotremorine

A

muscarinic agonist

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16
Q

what is pilocarpine

A

muscarinic agonist

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17
Q

what are the main effects of muscarinic agonist

A

parasympathomimetic

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18
Q

what do muscarinic agonists do to the cardiovascular system

A

slow HR, decrease force&rate of contraction

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19
Q

what do muscarinic agonists do to endothelium

A

the muscarinic receptors in the endothelium that cause release of NO that causes relaxation

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20
Q

when does ACh not cause relaxation in the endothelium

A

when the endothelium is not intact
muscarinic receptors are no longer present and endothelial cells can no longer release NO

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21
Q

what do muscarinic agonists do to the respiratory system

A

contraction of bronchiole smooth muscle, increased secretion of mucous

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22
Q

why can muscarinic agonists be bad for asthmatics

A

lots of mucous and bronchiole contraction makes respiration less efficient

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23
Q

what do muscarinic agonists do to the GI tract? what messenging system would this require?

A

increases saliva and stomach acid secretion, motility and peristalsis

likely Gq (M1, M3) system since effects are stimilatory which would require Ca2+ release

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24
Q

what does muscarinic agonists do to the bladder

A

stimulates detrusor muscle, relaxes trigone and internal sphincter (promotes voiding)

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25
Q

what are the CNS effects of nicotine

A

mild stimulation, can cause emesis, coma at high doses

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26
Q

how does nicotine act as an insecticide?

A

overstimulates the neuromuscular junction, leading to paralysis

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27
Q

does nAChR stimulate the sympathetic or the parasympathetic branch

A

both of them (found in the ganglia of both)

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28
Q

what does nicotine do to the cardiovascular system

A

hypertension, sympathetic effects on heart

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29
Q

what is nicotine’s effect on the GI tract

A

parasympathetic
increase secretion and motility

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30
Q

what are the skeletal muscle effects of nicotine

A

depolarization and excitation

-it can cause a small disorganized twitch or even a strong contraction o

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31
Q

what do anticholinesterases do to nicotinic and muscarinic receptors

A

indirectly stimulate by preventing hydrolysis of ACh, causing ACh to bind to the nicotinic/muscarinic receptors

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32
Q

name 4 acetylcholinesterases

A

edrophonium
neostigmine
malathion
soman

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33
Q

what is edrophonium

A

a simple alcohol anticholinesterase

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34
Q

what is neostigmine

A

carbamic esters of alcohols with quaternary or tertiary ammonium group
-an anticholinesterases

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35
Q

what is malathion

A

insecticide anticholinesterase

organophosphate

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36
Q

what is soman

A

nerve gas
anticholinesterase
organophosphate

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37
Q

are anticholinesterases well absorbed in the body

A

yes, via skin gut lung and conjuctiva

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38
Q

what effects are anticholinesterases similar to

A

direct acting cholinergic agonists

39
Q

what would anticholinesterases do to respiration

A

constrict bronchiole, increase secretion (they are like cholinergic agonists which are like parasympathetic agonists)

40
Q

what would anticholinesterases do to gut

A

increase motility

they are like cholinergic agonists which are like parasympathetic agonists

41
Q

what would anticholinesterases do to heart

A

slow heart rate, decreased cardiac output

they are like cholinergic agonists which are like parasympathetic agonists

42
Q

what do anticholinesterases do to neuromuscular transmission

A

increase strength of contraction -can lead to depolarizing neuromuscular blockade

43
Q

what do acetylcholinesterases do to the vascular systen

A

little overall change in BP since an increase in upstream SNS activity cancels out parasympathomimetic effects

44
Q

what is depolarizing neuromuscular blockade

A

when neurons are chronically stimulated and depolarized to the point that they cannot make AP

45
Q

what happens to the body in nerve gas / insecticide poisoning

A

cardiac arrest, fluid in lungs, bronchioconstriction, blockage of respiratory muscle contraction

46
Q

what drug can be used to limit the effects of nerve gas? what class of drug is it?

A

atropine, a muscarinic antagonist

47
Q

what are 4 conditions that cholinomimetics work well for

A

glaucoma
urinary retention
postoperative ileus (low GI motility)
myasthenia gravis (decreased nAChR at the NM junction)

48
Q

what are cholinomimetics

A

muscarinic agonist or anticholinesterases

49
Q

what causes myasthenia gravis

A

autoimmune disease with decreased nAChR expression at neuromuscular junction

50
Q

what are the symptoms of myasthenia gravis

A

weakness, fatigue, difficulty opening eyes, respiration

51
Q

how would you treat myasthenia gravis

A

anticholinesterases (work better than cholingeric agonists for some reason)

52
Q

what are 3 neuromuscular blockers (nicotinic antagonists)

A

succinylcholine
D-tubocurarine
α-bungarotoxin

53
Q

what is succinylcholine

A

nicotinic antagonist/neuromuscular blocker, used for paralysis during surgery

54
Q

what is D-tubocurarine

A

nicotinic antagonist
poison in blow darts, curari

55
Q

what is α-bungarotoxin

A

nicotinic antagonist
protein in snake venom which causes paralysis

56
Q

list 3 muscarinic antagonists

A

atropine
scopolamine
ipratropium

57
Q

what is atropine

A

muscarinic antagonist

58
Q

what causes parkinsons

A

excess cholinergic activity, lack of dopaminergic activity

lack of dopamine activity

59
Q

how can atropine help with parkinsons

A

antimuscarinics can help control with parkinsons tremors (lessens ACH cause parkinsons has excess)

60
Q

what is scopolamine (drug class)

A

muscarinic antagonist

61
Q

what can scopolamine treat

A

vestibular disturbances (motion sickness) -muscarinic antagonist

62
Q

what do muscarinic antagonists do to cardiovascular system and why

A

drug like atropine would stop the parasympathetic breaks-increases HR, force of contraction

63
Q

what do muscarinic antagonists do to respiratory system and why

A

slight bronchodilation and decreased secretion (block of parasympathetic tone)

64
Q

what is ipratropium and what is it used for

A

muscarinic antagonist

COPD (chronic obstructive pulmonary disease)

65
Q

what are directly acting sympathomimetics (definition)

A

α or β adrenoceptor agonists

66
Q

what are 3 examples of directly acting sympathomimetics

A

adrenaline
noradrenaline
isoproterenol

67
Q

what are indirectly acting sympathomimetics (definition+examples)

A

displace stored catecholamines from vesicles (amphetamines and tyramine, cocaine and)

inhibit catecholamine reuptake (cocaine + TCAs)

68
Q

what do alpha receptors have highest and lowest affinity for

A

A>=N»I
adrenaline stronger than noradrenaline than isoproterenol

69
Q

what do beta receptors have highest and lowest affinity for

A

I>A>=N
isoproterenol then adrenaline than noradrenaline

70
Q

how to remember beta and alpha affinities

A 
aggressive ANI (alpha)
beaten IAN (beta)
71
Q

what is vasomotor reversal

A

given adrenaline, BP goes up due to alpha contraction
as NE decreases, the vessel dilates due to beta activity

whic givving NE with an alpha antagonist, an initial drop in BP is observed

72
Q

what affinity do β1 receptors have for A vs NA

A

equal

73
Q

what affinity do β2 receptors have for A vs NA

A

higher affinity for A than NA

74
Q

what does prazosin do

A

blocks α1 adrenoceptors

75
Q

what does yohibine do

A

blocks α2 adrenoceptors

76
Q

are α or β receptors more sensitive to agonists

A

β are more sensitive to agonists

77
Q

what is phenylephrine

A

α1 agonist (nasal decongestion)

78
Q

what is clonidine

A

α2 agonist

79
Q

what is isoproterenol (INA)

A

all β agonist

80
Q

what is dobutamine

A

β1 agonist

81
Q

what is salbutamol

A

β2 agonist (asthma puffer)

82
Q

what is phentolamine

A

all α antagonist

83
Q

what is prazosin

A

α1 antagonist

84
Q

what is yohimbine

A

α2 antagonist

85
Q

what is propanolol

A

allβ antagonist

86
Q

what is metoprolol

A

β1 antagonist

87
Q

what g protein pathway for α1 receptors

A

Gq

88
Q

if α1 and M3 are both Gq, why do they have opposing effects on vascular smooth muscle?

A

CELL SPECIFIC EXPRESSION

M3 relax via receptors on endothelial cells that cause eventual NO release
α1 receptors are directly smooth muscle and cause it to contract

89
Q

what G pathway for α2 receptors

A

Gi

90
Q

what G pathway for β receptors

A

Gs

91
Q

what does α1 do to blood vessels

A

vasoconstrict

92
Q

what does α2 do to blood vessels

A

vasoconstrict

93
Q

what does β do to blood vessels

A

vasodilate

PMCOL 343 (31 decks)

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