Cholinergic Drugs Flashcards

1
Q

what is the main neurotransmitter of cholinergic drugs

A

acetylcholine

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2
Q

what are the precursors of acetylcholine

A

acetyl coenzyme A
choline

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3
Q

where is acetyl coenzyme A derived and synthesized from

A

derived: pyruvate
Synthesized: mitochondria

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4
Q

True or False:
choline uptake is a rate limiting step

A

true

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5
Q

what are the choline transport systems

A

high affinity transport system
synaptic vesicles by vesicular transporters

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6
Q

what is the inhibitor of the high affinity transport system of choline

A

hemicholinium

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7
Q

what is the inhibitor of the synaptic vesicles of ACh transport

A

vesamicol

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8
Q

how is acetylcholine released

A

exocytosis

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9
Q

what can inhibit the release of acetylcholine

A

botulinum toxins

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10
Q

what can bind to the receptors of cholinergic nerve terminals to interupt the SNARE complex components

A

clostridium toxins

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11
Q

which animal uses clostridium toxins to their advantage to kill

A

black widow spiders

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12
Q

what enzyme is used to hydrolyze ACh

A

acetylcholinesterase

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13
Q

what is the purpose of AChE

A

recycling of choline to increase ACh synthesis

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14
Q

where is AChE synthesized

A

autonomic ganglia
neuromuscular motor endplates
visceral neuroeffector junctions

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15
Q

what is the pseudo chE

A

butyrylcholinesterase

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16
Q

where is butyrylcholinesterase synthesized

A

liver

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17
Q

what is the purpose of butyrylcholinesterase

A

metabolism of certain drugs

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18
Q

what occurs if there is an inhibition of AChE

A

accumulation of ACh in nerve terminal

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19
Q

which receptors are involved with cholinergic receptors

A

nicotinic and muscarinic receptors

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20
Q

what type of receptor are nicotinic receptors

A

ligand gated ion channel

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21
Q

what is the main result of activating a nicotinic receptor

A

skeletal muscle contraction

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22
Q

where are nicotinic receptors found

A

autonomic ganglion
adrenal medulla
CNS

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23
Q

what type of receptors are muscarinic receptors

A

GPCR

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24
Q

what are the responses of activating muscarinic receptors

A

excitatory
inhibitory

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25
Q

where are non-innervated muscarinic receptors found

A

vascular endothelium

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26
Q

which muscarinic receptor is normally found as non-innervated in blood vessels

A

M3

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27
Q

where are M1 receptors found

A

ganglia
secretory glands

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28
Q

where are M2 receptors found

A

myocardium
smooth muscle

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29
Q

where are M3 & M4 receptors found

A

smooth muscle and secretory glands

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30
Q

where are M5 receptors found

A

CNS

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31
Q

what is the most common muscarinic receptor

A

M5

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32
Q

which muscarinic receptors activate Gq proteins

A

M1
M3
M5
(odd receptors)

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33
Q

what type of responses are expected with the activation of M1, M3 or M5 receptors

A

excitatory

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34
Q

what muscarinic receptors are responsible for “relaxation”

A

M2
M4

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35
Q

which muscarinic receptors act on Gi protein

A

M2
M4

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36
Q

what is the result of M2 receptor activation of the heart muscle

A

decreased HR
decrease impulse conduction / contraction

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37
Q

what is the effect of activating M3 receptors of smooth muscle

A

increase in contraction (GI system)

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38
Q

what is the effect of activating M3 receptors of secretory glands

A

increased secretion

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39
Q

how do M3 receptors in vascular endothelium cause vasodilation

A

release of NO

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40
Q

what are the 2 types of cholinergic agonists

A

direct and indirect

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41
Q

how do indirect cholinergic agonists work

A

inhibit cholinesterase to cause accumulation of ACh

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42
Q

what are the direct acting agonists

A

carbachol
bethanechol
pilocarine

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43
Q

what are the reversible indirect cholinergic agonists

A

physostigmine
neostigmine
edrophonium
pyridostigmine

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44
Q

what is the irreversible indirect agonist

A

organophosphate

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45
Q

how do low doses of acetylcholine impact the cardio vascular system

A

rapid fall in pressure –> reflex tachycardia
muscarinic receptors of vascular endothelium are activated (M3 creates vasodilation)

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46
Q

what are the effects of high doses of acetylcholine

A

vasodilation –> decreased peripheral resistance and BP
slow HR (- chronotropic effect)
- inotropic effect
slow SA and AV node conduction
decreased cardiac output

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47
Q

how does acetylcholine impact smooth muscle

A

increase motility
increase GIT secretion
increase bronchial muscle contraction
increase urinary bladder contraction

48
Q

how does acetylcholine effect exocrine glands

A

increase secretion

49
Q

how does acetylcholine impact the eye

A

reduces intraocular pressure
contraction of iris muscle

50
Q

what can be induced in the eye with acetylcholine

A

miosis

51
Q

what are the choline ester direct-acting parasympathomimetic agonists

A

carbachol
bethanechol

52
Q

what are the natural alkaloid direct-acting parasympathomimetic agonists

A

pilocarine

53
Q

which direct-acting agonist is a very potent nicotinic and muscarinic agonist that is resistant to hydrolysis by AChE

A

carbachol

54
Q

True or False:

Carbachol has a longer duration of action

A

true

55
Q

what is the pathway of carbachol

A

stimulate autonomic ganglia = acetylcholine release

56
Q

when should one administer carbachol

A

impaction colic in horses
glaucoma in dogs
rumen atony and impaction in cattle

57
Q

when should you NOT administer carbachol

A

in cases of maybe solid impactions - can cause bowel ruptures

58
Q

which direct-acting agonist is very potent and selective for muscarinic receptors and resistant to hydrolysis to AChE

A

bethanechol

59
Q

when would you administer bethanechol

A

GI paralytic ileus
urinary retention associated with bladder muscle atony

60
Q

what should you be aware of when thinking about using bethanechol

A

only use when there is no mechanical obstruction in GIT

61
Q

what receptor does Pilocarine act on

A

M3

62
Q

what is the effects of using M3

A

contraction of iris sphincter and ciliary muscle of the lens

63
Q

what can pilocarine be used to treat

A

acute glaucoma
keratoconjunctivitis sicca

64
Q

what are the therapeutic uses of parasympathomimetic

A

GI atony / impaction
urinary bladder muscle atony
glaucoma

65
Q

how do reversible cholinesterase inhibitors work

A

inhibit ACh binding to AChE

66
Q

how is physostigmine administered

A

orally

67
Q

what is physostigmine used for

A

glaucoma
atropine toxicity

68
Q

how is neostigmine administered

A

orally

69
Q

what receptors does neostigmine work on

A

selective for nicotinic receptors at the Nm junction

70
Q

when is neostigmine used (therapeutic)

A

myasthenia gravis
reverse neuromuscular blockade (non-depolarizing)

71
Q

what type of inhibitor is edrophonium

A

competitive reversible inhibitor

72
Q

when is edrophonium used (therapeutic)

A

anti-curare
myasthenia gravis

73
Q

what is a longer acting drug used for myasthenia gravis

A

pridostigmine

74
Q

what are the digestive pharmacologic effects of reversible cholinesterase inhibitors

A

increase GIT motility
increase frequency / strength of peristaltic waves

75
Q

what should you be aware of (warnings) before using reversible cholinesterase inhibitors

A

intestinal spasm
colic

76
Q

what are the ocular effects of using reversible cholinesterase inhibitors

A

pupillary constriction
loss of accommodation

77
Q

when are pharmacologic effects more pronounced in skeletal muscle

A

low doses

78
Q

how do reversible cholinesterase inhibitors affect cardiac tissue

A

hypotension
bradycardia
arrhythmia

79
Q

how do reversible cholinesterase inhibitors affect the bladder and lungs

A

bronchoconstriction
contraction of the urinary bladder (detrusor muscle)

80
Q

what is physostigmine used to treat

A

glaucoma
impaction in cattle

81
Q

what drug combination is used to prevent or breakdown of synechia formed between lens and iris

A

physostigmine + atropine

82
Q

which reversible cholinesterase inhibitors are used to treat myasthenia gravis and anticurare

A

neostigmine
pyridostigmine

83
Q

which reversible cholinesterase inhibitor is used to differentiate myasthenia gravis from cholinergic crisis

A

edrophonium

84
Q

when should reversible cholinesterase inhibitors use be avoided

A

impaction with possible mechanical obstruction
pregnancy

85
Q

which reversible cholinesterase inhibitor depresses the CNS at large doses and causes convulsions at massive doses

A

physostigmine

86
Q

which reversible cholinesterase inhibitor can cause skeletal muscle weakness in cases of overdose

A

neostigmine

87
Q

what are some possible respiratory repercussions of reversible cholinesterase inhibitors

A

respiratory paralysis
increased bronchiolar secretion

88
Q

what is the antagonist to reversible cholinesterase inhibitors

A

atropine

89
Q

what is the irreversible cholinesterase inhibitor

A

organophosphourous compounds

90
Q

True or False:
organophosphourous compounds can cross the brain blood barrier

A

true

91
Q

what is the antidote used for organophosphorus poisoning

A

atropine

92
Q

which organophosphorus compound is used to reactivate ChE

A

pralidoximine

93
Q

True or False:

Use of pralidoxime and atropine is a time-sensitive treatment for organophosphate poisoning

A

true

94
Q

for what type of poisoning should pralidoxime not be used

A

carbamate poisoning

95
Q

what are some precautions that should be taken before administering pralidoxime or atropine

A

-no exposure to other cholinesterase inhibitor drugs
-history of respiratory illness or hepatic disease
-pregnant patients

96
Q

how do cholinergic antagonists work

A

inhibit actions of acetyl choline by blocking cholinergic receptors

97
Q

what receptors do cholinergic antagonists act on

A

muscarinic
Nm receptors

98
Q

what is the response of using a cholinergic antagonist on a muscarinic receptor

A

muscle relaxation

99
Q

how do antimuscarinic agents work

A

inhibit muscarinic actions of acetylcholine and related cholinergic agonists

100
Q

what is the affect of atropine on the cardio vascular system

A

tachycardia
increased cardiac output
increased blood pressure

101
Q

what is the response of atropine in the GIT

A

relaxation of GIT
decrease in motility
decrease in secretions

102
Q

what is the affect of atropine on the urinary system

A

relaxes smooth muscle of bladder
urinary retention

103
Q

what is the affect of atropine on the respiratory system

A

decreased secretions
bronchodilation

104
Q

what is the affect of atropine on the ocular system

A

increased intraocular pressure

105
Q

True or False:

atropine has minimal effect on the CNS

A

true

106
Q

which species is resistant to atropine

A

rabbits

107
Q

what atropine derivative causes slight sedation and antiemetic effects

A

scopolamine

108
Q

how is atropine poisoning tested for

A

drop of urine
mydriasis in cat eyes

109
Q

what is the treatment of atropine poisoning

A

neostigmine
physostigmine

110
Q

which antimuscarinic drug can be used to reduce gastric acid secretion

A

pirenzepine

111
Q

which antimuscarinic drug can be used for ophthalmic purposes

A

tropicamide

112
Q

what is tropicamide used to treat

A

adhesion between iris and lens

113
Q

what is the antidote for cholinergic agonists

A

atropine

114
Q

what antimuscarinic drug can be used to prevent motion sickness

A

scopolamine

115
Q

which antimuscarinic drug can be used as a preanaesthetic in veterinary medicine

A

glycopyrrolate