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PMCOL 343 > 3- autonomic > Flashcards

3- autonomic Flashcards

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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
what are the CNS effects of nicotine
mild stimulation, can cause emesis, coma at high doses
26
how does nicotine act as an insecticide?
overstimulates the neuromuscular junction, leading to paralysis
27
does nAChR stimulate the sympathetic or the parasympathetic branch
both of them (found in the ganglia of both)
28
what does nicotine do to the cardiovascular system
hypertension, sympathetic effects on heart
29
what is nicotine's effect on the GI tract
parasympathetic increase secretion and motility
30
what are the skeletal muscle effects of nicotine
depolarization and excitation | -it can cause a small disorganized twitch or even a strong contraction o
31
what do anticholinesterases do to nicotinic and muscarinic receptors
indirectly stimulate by preventing hydrolysis of ACh, causing ACh to bind to the nicotinic/muscarinic receptors
32
name 4 acetylcholinesterases
edrophonium neostigmine malathion soman
33
what is edrophonium
a simple alcohol anticholinesterase
34
what is neostigmine
carbamic esters of alcohols with quaternary or tertiary ammonium group -an anticholinesterases
35
what is malathion
insecticide anticholinesterase | organophosphate
36
what is soman
nerve gas anticholinesterase organophosphate
37
are anticholinesterases well absorbed in the body
yes, via skin gut lung and conjuctiva
38
what effects are anticholinesterases similar to
direct acting cholinergic agonists
39
what would anticholinesterases do to respiration
constrict bronchiole, increase secretion (they are like cholinergic agonists which are like parasympathetic agonists)
40
what would anticholinesterases do to gut
increase motility | they are like cholinergic agonists which are like parasympathetic agonists
41
what would anticholinesterases do to heart
slow heart rate, decreased cardiac output | they are like cholinergic agonists which are like parasympathetic agonists
42
what do anticholinesterases do to neuromuscular transmission
increase strength of contraction -can lead to depolarizing neuromuscular blockade
43
what do acetylcholinesterases do to the vascular systen
little overall change in BP since an increase in upstream SNS activity cancels out parasympathomimetic effects
44
what is depolarizing neuromuscular blockade
when neurons are chronically stimulated and depolarized to the point that they cannot make AP
45
what happens to the body in nerve gas / insecticide poisoning
cardiac arrest, fluid in lungs, bronchioconstriction, blockage of respiratory muscle contraction
46
what drug can be used to limit the effects of nerve gas? what class of drug is it?
atropine, a muscarinic antagonist
47
what are 4 conditions that cholinomimetics work well for
glaucoma urinary retention postoperative ileus (low GI motility) myasthenia gravis (decreased nAChR at the NM junction)
48
what are cholinomimetics
muscarinic agonist or anticholinesterases
49
what causes myasthenia gravis
autoimmune disease with decreased nAChR expression at neuromuscular junction
50
what are the symptoms of myasthenia gravis
weakness, fatigue, difficulty opening eyes, respiration
51
how would you treat myasthenia gravis
anticholinesterases (work better than cholingeric agonists for some reason)
52
what are 3 neuromuscular blockers (nicotinic antagonists)
succinylcholine D-tubocurarine α-bungarotoxin
53
what is succinylcholine
nicotinic antagonist/neuromuscular blocker, used for paralysis during surgery
54
what is D-tubocurarine
nicotinic antagonist poison in blow darts, curari
55
what is α-bungarotoxin
nicotinic antagonist protein in snake venom which causes paralysis
56
list 3 muscarinic antagonists
atropine scopolamine ipratropium
57
what is atropine
muscarinic antagonist
58
what causes parkinsons
excess cholinergic activity, lack of dopaminergic activity | lack of dopamine activity
59
how can atropine help with parkinsons
antimuscarinics can help control with parkinsons tremors (lessens ACH cause parkinsons has excess)
60
what is scopolamine (drug class)
muscarinic antagonist
61
what can scopolamine treat
vestibular disturbances (motion sickness) -muscarinic antagonist
62
what do muscarinic antagonists do to cardiovascular system and why
drug like atropine would stop the parasympathetic breaks-increases HR, force of contraction
63
what do muscarinic antagonists do to respiratory system and why
slight bronchodilation and decreased secretion (block of parasympathetic tone)
64
what is ipratropium and what is it used for
muscarinic antagonist | COPD (chronic obstructive pulmonary disease)
65
what are directly acting sympathomimetics (definition)
α or β adrenoceptor agonists
66
what are 3 examples of directly acting sympathomimetics
adrenaline noradrenaline isoproterenol
67
what are indirectly acting sympathomimetics (definition+examples)
displace stored catecholamines from vesicles (amphetamines and tyramine, cocaine and) inhibit catecholamine reuptake (cocaine + TCAs)
68
what do alpha receptors have highest and lowest affinity for
A>=N>>I adrenaline stronger than noradrenaline than isoproterenol
69
what do beta receptors have highest and lowest affinity for
I>A>=N isoproterenol then adrenaline than noradrenaline
70
how to remember beta and alpha affinities
``` aggressive ANI (alpha) beaten IAN (beta) ```
71
what is vasomotor reversal
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
what affinity do β1 receptors have for A vs NA
equal
73
what affinity do β2 receptors have for A vs NA
higher affinity for A than NA
74
what does prazosin do
blocks α1 adrenoceptors
75
what does yohibine do
blocks α2 adrenoceptors
76
are α or β receptors more sensitive to agonists
β are more sensitive to agonists
77
what is phenylephrine
α1 agonist (nasal decongestion)
78
what is clonidine
α2 agonist
79
what is isoproterenol (INA)
all β agonist
80
what is dobutamine
β1 agonist
81
what is salbutamol
β2 agonist (asthma puffer)
82
what is phentolamine
all α antagonist
83
what is prazosin
α1 antagonist
84
what is yohimbine
α2 antagonist
85
what is propanolol
allβ antagonist
86
what is metoprolol
β1 antagonist
87
what g protein pathway for α1 receptors
Gq
88
if α1 and M3 are both Gq, why do they have opposing effects on vascular smooth muscle?
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
what G pathway for α2 receptors
Gi
90
what G pathway for β receptors
Gs
91
what does α1 do to blood vessels
vasoconstrict
92
what does α2 do to blood vessels
vasoconstrict
93
what does β do to blood vessels
vasodilate

PMCOL 343 (31 decks)

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