3- autonomic Flashcards

1
Q

what are 3 choline esters

A

acetylcholine
carbachol
bethanechol

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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 are 3 muscarinic agonists

A

muscarine
oxotremorine
pilocarpine

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10
Q

what is acetylcholine

A

a choline ester

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11
Q

what is carbachol

A

a choline ester

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12
Q

what is bethanechol

A

a choline ester

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13
Q

what is muscarine

A

muscarinic agonist

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14
Q

what is oxotremorine

A

muscarinic agonist

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15
Q

what is pilocarpine

A

muscarinic agonist

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16
Q

what are the main effects of muscarinic agonist

A

parasympathomimetic

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17
Q

what do muscarinic agonists do to the cardiovascular system

A

slow HR, decrease force&rate of contraction

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18
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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19
Q

when does ACh not cause relaxation in the endothelium

A

when the endothelium is not intact

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20
Q

what do muscarinic agonists do to the respiratory system

A

contraction of bronchiole smooth muscle, increased secretion of mucous

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21
Q

why can muscarinic agonists be bad for asthmatics

A

lots of mucous and bronchiole contraction makes respiration less efficient

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22
Q

what do muscarinic agonists do to the GI tract

A

increases saliva and stomach acid secretion, motility and peristalsis

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23
Q

what does muscarinic agonists do to the bladder

A

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

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24
Q

what are the CNS effects of nicotine

A

mild stimulation, can cause emesis, coma at high doses

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25
Q

does nAChR stimulate the sympathetic or the parasympathetic branch

A

both of them

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26
Q

what does nicotine do to the cardiovascular system

A

hypertension

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27
Q

is nicotines cardio effect parasympathetic or sympathetic

A

sympathetic

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28
Q

is nicotines GI effect parasympathetic or sympathetic

A

parasympathetic

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29
Q

what does nicotine do to the GI system

A

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 twitch or even a strong contraction of a whole muscle

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31
Q

what do anticholinesterases do to nicotinic and muscarinic receptors

A

indirectly stimulate by preventing hydrolysis of ACh

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32
Q

what is edrophonium

A

a simple alcohol anticholinesterase

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33
Q

what is neostigmine

A

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

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34
Q

what is malathion

A

insecticide anticholinesterase

organophosphate

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35
Q

what is soman

A

nerve gas
anticholinesterase
organophosphate

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36
Q

are anticholinesterases well absorbed in the body

A

yes, via skin gut lung and conjuctiva

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37
Q

what effects are anticholinesterases similar to

A

direct acting cholinergic agonists

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38
Q

what would anticholinesterases do to respiration

A

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

39
Q

what would anticholinesterases do to gut

A

increase motility

they are like cholinergic agonists which are like parasympathetic agonists

40
Q

what would anticholinesterases do to heart

A

slow heart rate, decreased cardiac output

they are like cholinergic agonists which are like parasympathetic agonists

41
Q

what do anticholinesterases do to neuromuscular transmission

A

increase strength of contraction -can lead to depolarizing neuromuscular blockade

42
Q

what is depolarizing neuromuscular blockade

A

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

43
Q

what happens to the body in nerve gas / insecticide poisoning

A

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

44
Q

what drug can be used to limit the effects of nerve gas

A

atropine

45
Q

what are 4 conditions that cholinomimetics work well for

A

glaucoma
urinary retention
postoperative ileus
myasthenia gravis

46
Q

what are cholinomimetics

A

muscarinic agonist or anticholinesterases

47
Q

what causes myasthenia gravis

A

autoimmune disease with decreased nAChR expression at neuromuscular junction

48
Q

what are the symptoms of myasthenia gravis

A

weakness, fatigue, difficulty opening eyes, respiration

49
Q

how would you treat myasthenia gravis

A

anticholinesterases

50
Q

what are 3 neuromuscular blockers (nicotinic antagonists)

A

succinylcholine
D-tubocurarine
α-bungarotoxin

51
Q

what is succinylcholine

A

nicotinic antagonist/neuromuscular blocker, used for paralysis during surgery

52
Q

what is D-tubocurarine

A

poison in blow darts, curari

53
Q

what is α-bungarotoxin

A

protein in snake venom which causes paralysis

54
Q

what is atropine

A

muscarinic antagonist

55
Q

what causes parkinsons

A

excess cholinergic activity

lack of dopamine activity

56
Q

how can atropine help with parkinsons

A

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

57
Q

what is scopolamine (drug class)

A

muscarinic antagonist

58
Q

what can scopolamine treat

A

vestibular disturbances (motion sickness) -muscarinic antagonist

59
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

60
Q

what do muscarinic antagonists do to respiratory system and why

A

slight bronchodilation and decreased secretion (block of parasympathetic tone)

61
Q

what is ipratropium and what is it used for

A

muscarinic antagonist

COPD (chronic obstructive pulmonary disease)

62
Q

what are directly acting sympathomimetics (definition)

A

α or β adrenoceptor agonists

63
Q

what are directly acting sympathomimetics (examples)

A

adrenaline
noradrenaline
isoproterenol

64
Q

what are indirectly acting sympathomimetics (definition+examples)

A

displace stored catecholamines from vesicles (amphetamines)

inhibit catecholamine reuptake (cocaine + TCAs)

65
Q

what do alpha receptors have highest and lowest affinity for

A

A>=N»I

adrenaline stronger than noradrenaline thaaan isoproterenol

66
Q

what do beta receptors have highest and lowest affinity for

A

I>A>=N

isoproterenol then adrenaline than noradrenaline

67
Q

how to remember beta and alpha affinities

A
aggressive ANI (alpha)
beaten IAN (beta)
68
Q

what is vasomotor reversal

A

given adrenaline, BP goes up

given adrenaline with antagonist , BP goes down :0

69
Q

what affinity do β1 receptors have for A vs NA

A

equal

70
Q

what affinity do β2 receptors have for A vs NA

A

higher affinity for A than NA

71
Q

what does prazosin do

A

blocks α1 adrenoceptors

72
Q

what does yohibine do

A

blocks α2 adrenoceptors

73
Q

are α or β receptors more sensitive to agonists

A

β are more sensitive to agonists

74
Q

what is phenylephrine

A

α1 agonist (nasal decongestion)

75
Q

what is clonidine

A

α2 agonist

76
Q

what is isoproterenol (INA)

A

all β agonist

77
Q

what is dobutamine

A

β1 agonist

78
Q

what is salbutamol

A

β2 agonist (asthma puffer)

79
Q

what is phentolamine

A

all α antagonist

80
Q

what is prazosin

A

α1 antagonist

81
Q

what is yohimbine

A

α2 antagonist

82
Q

what is propanolol

A

allβ antagonist

83
Q

what is metoprolol

A

β1 antagonist

84
Q

what g protein pathway for α1 receptors

A

Gq

85
Q

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

A

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

86
Q

what G pathway for α2 receptors

A

Gi

87
Q

what G pathway for β receptors

A

Gs

88
Q

what happens in Gq

A

PLC increase IP3 and DAG

89
Q

what happens in Gi

A

adenylyl cyclase is inhibited so less cAMP is made

90
Q

what happens in Gs

A

adenylyl cyclase is activated so more cAMP is made

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

94
Q

how to remember G protein types for α1, α2, β

and blood vessel effect

A

goes q,i,s
like “kiss”
nervous nervous relaaaxed
vasoconstrict, vasoconstrict, vasodilate