Neuropharmacology Flashcards

1
Q

what are cholinergic drugs?

A

drugs that mimic the action of acetylcholine

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2
Q

what are adrenergic drugs?

A

drugs that mimic the action of epinephrine and norepinephrine

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3
Q

what are the general functions of the sympathetic and parasympathetic systems?

A

oppose each other
discrete vs diffuse action
both excitatory and inhibitory
maintain homeostasis
one may directly inhibit other

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4
Q

what are the events involved in a cholinergic response?

A

synthesis of acetylcholine
storage of acetylcholine in vesicles
arrival of impulse and calcium uptake
release of acetylcholine into synaptic cleft
interaction of acetylcholine with receptor
hydrolysis of acetylcholine by esterase
reuptake of choline

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5
Q

what are the agonist and antagonist of muscarinic receptors (subtype of cholinergic)?

A

muscarine is agonist
atropine is antagonist

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6
Q

what are the agonist and antagonist of nicotinic receptors (subtype of cholinergic)?

A

nicotine is agonist
curare is antagonist

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7
Q

nicotinic receptor is the _________________ and is activated by _____________________________________

A

sodium channel
2 acetylcholine binding to the 2 alpha subunits

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8
Q

what are the subclasses of muscarinic receptors?

A

M1
M2
M3

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9
Q

where are M2 receptors located?

A

heart

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10
Q

where are M3 receptors located?

A

smooth muscle
secretory glands

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11
Q

what is the receptor action of M1 and M3?

A

M1: close potassium channel
M3: increased contraction, increased secretion
depolarization

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12
Q

what is the M2 receptor action?

A

open potassium channels and decrease cAMP to decrease heart rate

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13
Q

if a cholinergic drug’s mechanism of action is at M1, what does it do?

A

excitatory
close potassium channel
activate phospholipase C

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14
Q

if a cholinergic drug’s mechanism of action is at M2, what does it do?

A

inhibitory
open potassium channel
inhibit adenylate cyclase

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15
Q

if a cholinergic drug’s mechanism of action is at M3, what does it do?

A

excitatory
activate phospholipase C
increase ionized calcium concentration

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16
Q

where are cholinergic actions in the body?

A

cardiovascular system
respiratory system
gastrointestinal system
urinary bladder
eye
skeletal and smooth muscles

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17
Q

what are cholinergic actions in the cardiovascular system?

A

decrease heart rate
decrease atrial contractility
decrease AV conduction
decrease blood pressure

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18
Q

what are cholinergic actions in the respiratory system?

A

bronchoconstriction
increase bronchial secretion

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19
Q

what are cholinergic actions in the gastrointestinal system?

A

increase motility
increase secretion
relax sphincters

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20
Q

what are cholinergic actions in the urinary bladder?

A

contract detrusor muscle
relax internal sphincter

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21
Q

what are cholinergic actions in the eye?

A

contract sphincter muscles and iris
contract ciliary muscle

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22
Q

what are cholinergic actions in skeletal and smooth muscles?

A

contraction: muscle spasms

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23
Q

what are some direct acting cholinomimetics?

A

natural alkaloids- muscarinic receptor
synthetic- choline esters

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24
Q

what are some natural alkaloids?

A

muscarine
pilocarpine
arecoline

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25
what are some synthetic cholinomimetics?
choline esters: carbachol bethanechol methacholine
26
how do indirect acting cholinomimetics work?
inhibit acetylcholinesterase
27
what are some reversible indirect acting cholinomimetics?
physostigmine neostigmine pyridostigmine edrophonium
28
what are some irreversible indirect acting cholinomimetics?
echothiophate malathion
29
what can organophosphate poisoning be treated with and why?
atropine antagonist: blocks acetylcholine until can make more acetylcholinesterase proteins
30
what are the clinical applications of cholinomimetics?
glaucoma ileus and urinary bladder atony myasthenia gravis edrophonium test and atropine curareform toxicity anticholinergic toxicity alzheimer's disease
31
what blocks choline uptake and acetylcholine synthesis?
hemicholinium
32
what blocks release of acetylcholine?
low calcium excess magnesium botulinum toxicity aminoglycosides local anesthetics
33
what inhibits acetylcholine-receptor interaction?
curare atropine hexamethonium
34
what inhibits acetylcholine hydrolysis by esterase?
neostigmine organophosphate
35
what is atropine's mechanism of action?
prevents acetylcholine from binding and inducing its effects by interacting with muscarinic acetylcholine receptors attenuates parasympathetic nerve impulses
36
what are the actions of muscarinic antagonists on the cardiovascular system?
increase heart rate increase intranodal conduction slight increase or no change in blood pressure (dose dependent decrease in heart rate and second degree AV block can occur)
37
what are the actions of muscarinic antagonists on the respiratory system?
produce bronchodilation decrease bronchial secretion
38
what are the actions of muscarinic antagonists on the gastrointestinal system?
relaxation of GI smooth muscle decreased secretions decreased salivation
39
what are the actions of muscarinic antagonists on the urinary bladder?
relaxes smooth muscle of urinary tract urinary retention
40
what are the actions of muscarinic antagonists on the eye?
relax sphincter muscle and iris, dilated pupil
41
what are some antimuscarinic drugs?
atropine glycopyrrolate homatropine propantheline ipratropium
42
what is one autonomic ganglion blocker?
hexamethonium
43
what are some neuromuscular blockers?
curure succinylcholine
44
what are some clinical applications of anticholinergics in the GI?
spasmolytic peptic ulcer colic in horses
45
what are some results of cholinergic drug toxicity?
severe colic and diarrhea increased exocrine secretion dyspnea hypotension, cardiac slowing death if not treated
46
when should you be careful while using anti-cholinesterases?
liver disease respiratory disease late pregnancy
47
when should you avoid using anti-cholinesterases?
other anti-cholinesterase drugs metabolized by cholinesterase phenothiozines
48
when should you be careful with anti-muscarinic drugs?
glaucoma gastric ulcer
49
what are some competitive non-depolarizing blockers?
D-tubocurarine gallamine pancuronium
50
what are some depolarizing blockers?
succinyl choline decamethonium
51
what is the mechanism of action for competitive/non-depolarizing blockers?
bind to receptors no depolarization block access of agonist to receptors action can be reversed
52
what is the mechanism of action for non-competive/depolarizing blockers?
bind to receptors cause depolarization membrane remains depolarized cannot be reversed with acetylcholinesterase inhibitor
53
how are D-tubocurarine and pancuronium metabolizd?
liver excreted in bile and urine
54
how are gallamine and decamethonium metabolized?
excreted unchanged in urine minimal tissue distribution
55
how is succinylcholine metabolized?
hydrolyzed by serum psuedo cholinesterase
56
what is the order for muscles being relaxed?
toes, ears, eyes head and neck limbs respiratory muscles
57
what are some pharmacological actions of blockers?
central autonomic effect contracture of ocular muscles hypotension cardiac arrhythmia
58
what are the clinical applications of blockers?
major and minor surgery chemical restraint strychnine poisoning muscle disorders
59
how do you treat blocker toxicosis?
artificial respiration anticholinesterase and atropine
60
what are some ways that the junctional events in cholinergic junctions can be blocked?
choline uptake and acetylcholine synthesis release of acetylcholine inhibition of acetylcholine-receptor interaction acetylcholine hydrolysis by esterase
61
what are some clinical applications of anticholinergics in ophthalmology?
mydriasis cycloplegia
62
what is a clinical application of anticholinergics in respiratory?
bronchodilator
63
what is a clinical application of anticholinergics in the cardiovascular system?
sinus bradycardia
64
what is a clinical application of anticholinergics using no system in particular?
pre-anesthetic anti-cholinesterase toxicity
65
what do anti-nicotinic drugs do?
muscle relaxants neuromuscular blocking agents
66
how do anti-nicotinic drugs cause hypotension?
blockade of ganglion histamine release
67
which anti-nicotinic drug can cause cardiac arrhythmia at high doses?
succinylcholine