ANS Cholinergic Flashcards

1
Q

prototype that acts directly at both muscarinic and nicotinic receptors

A

Ach

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2
Q

prototype for the indirect acting cholinesterase inhibitors

A

neostigmine

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3
Q

Muscarinic mechanism of action

A

g protein and releases second messengers DAG and IP3. IP3 causes release of calcium from storage sites and causes smooth muscle contraction

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4
Q

Nicotinic mechanism of action

A

Ach receptor is located on channel protein that is selective for sodium and potassium. Receptor activation causes depolarization with influx of Na+ causes EPSP

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5
Q

drug that blocks synthesis of Ach

A

hemicholinium

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6
Q

drug that blocks storage of Ach

A

vesamicol

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7
Q

drug that blocks release of Ach

A

botulinum toxin

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8
Q

drug that block NE synthesis

A

metyrosine

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9
Q

drug that blocks catecholamine storage

A

reserpine

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10
Q

drug that blocks catecholamine release

A

guanethidine

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11
Q

drug that facilitates release of catecholamine

A

amphetamine

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12
Q

drug that impairs reuptake of catecholamines

A

cocaine

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13
Q

causes relaxation of skeletal muscle and systemic blood vessels

A

beta 2

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14
Q

causes contraction of skeletal muscle and systemic blood vessels

A

alpha 1

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15
Q

causes increase in heart rate

A

beta 1

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16
Q

causes relaxation of lungs and tracheal and bronchial smooth muscle

A

beta 2

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17
Q

short duration of action, quaternary structure , susceptible to pseudocholinesterase

A

direct acting cholinergic agonists

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18
Q

pilocarpine, bethanachol, methacholine

A

direct acting muscarinic agonists

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19
Q

Methacholine has the greatest muscarinic action on which system?

A

cardiac

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20
Q

2 drugs with very high selectivity to nicotinic receptors

A

Ach and pilocarpine

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21
Q

How do you reverse the effect of methacholine?

A

beta agonist

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22
Q

first cause depolarization at nicotinic receptor but then become antagonist

A

nicotinic receptor agonists

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23
Q

nicotine, succinylcholine varenicline

A

nicotinic receptor agonists

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24
Q

Effect of large dose of nicotine on NMJ

A

depolarization and depression of transmission, receptor desensitization

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25
partial agonist of nicotinic receptors and receptor is mesolimbic nicotinic
varenicline
26
what is varenicline selective for?
alpha4 beta 2 neuronal nicotinic receptor
27
adverse effects of varenicline (4)
1. nausea 2. sleep disturbances 3. GI 4. nicotine withdrawal
28
block acetylcholinesterase from degrading Ach
indirect acting cholinergic agonists
29
edrophonium, neostigmine, physostigmine, and malathion examples of ?
reversible acetylcholinesterase inhibitors (indirect acting agonists)
30
example of irreversible indirect acting agonists
organophosphates
31
Cholinesterase regenerator; reverse organophosphates
pralidoxime (2 PAM) | diacetylmonoxime (DAM)
32
tertiary NH and antidote for antimuscarinic CNS toxicity, tx of glaucoma, tx of MG
physostigmine
33
antibodies to alpha 1 subunit of nicotinic receptor channel complex
myasthenia gravis
34
Which cholinesterase inhibitor has the shortest duration of action?
edrophonium
35
prototype of antimuscarinic drugs
atropine
36
use for mydriasis and cycloplegia
antimuscarinic drugs
37
muscarinic antagonists
glycopyrrolate atropine tolterodine ipratropium
38
Which antimuscarinic has a quarternary structure and will limit distribution in the CNS?
trospium
39
primary uses of muscarinic antagonists (5)
1. bronchodilation 2. treat bradyarrhythmia 3. urinary incontinence 4. decreased GI motility 5. dry secretions
40
large doses of this drug make it an antagonist
nicotine
41
Small dose of nicotine increase ___ and ___.
BP and HR
42
Hypotension caused by larger doses of ___.
nicotine
43
nicotinic antagonist ganglionic blocker
trimethaphan
44
nicotinic antagonist neuromuscular blockers
atracurium pancuronium rocuronium
45
Which nicotinic antagonist neuromuscular blocker has the longest duration of action?
pancuronium
46
membrane depolarizes resulting in an initial which produces fasciculations then flaccid paralysis
phase I block of depolarizing NMB
47
membrane repolarizes but receptor is desensitized to effect of acetylcholine
phase II block of depolarizing NMB
48
compete with Ach to bind with nicotinic receptor of motor end plate; blockade inhibit Ach from binding
Non depolarizing, competitive NMB
49
Histamine release is a direct effect of ___
NMB nicotinic antagonists
50
Phase II can be antagonized by
antiChE agent
51
3 effects of depolarizing agents
1. ) muscle fasciculation 2. ) hyperkalemia 3. ) masseter muscle rigidity
52
can be reversed by acetylcholinesterase inhibitor agents
non depolarizing agents
53
indirect acting cholinergic receptor antagonist
botulinum toxin
54
adverse effects of nicotinic and muscarinic
1. anaphylaxis 2. associated with site of injection and dose (local effects, dry mouth, dysphagia, ptosis, vision effects)
55
most likely cause of death from cholinesterase inhibitor toxicity
respiratory failure
56
neostigmine and pyridostigmine causes ___
diarrhea; cholinesterase inhibitors increase bowl movement
57
parasympathetic innervation and bethanechol will cause ___
increase bronchial smooth muscle tone
58
what do muscarinic cholinergic agonists treat
miosis (tx of narrow angle glaucoma)
59
drug with little to none vascular effect and CNS effect and duration of action of 2-4 hours
neostigmine
60
both ganglion blockers and muscarinic blockers cause ____
mydriasis
61
therapeutic indication for antimuscarinic drugs?
COPD
62
which drug causes vasodilation and can be blocked by atropine
bethanechol
63
beta 2 stimulants cause ___
tremors