Intro to NMJ Pharmacology Flashcards
1
Q
cisatracurium
A
nondepolarizing isoquinoline derivative
2
Q
tubocurarine
A
nondepolarizing isoquinoline derivative
3
Q
pancuronium
A
steroid derivative nondepolarizing agent
4
Q
rocuronium
A
steroid derivative nondepolarizing agent
5
Q
vecuronium
A
steroid derivative nondepolarizing agent
6
Q
succinylcholine
A
depolarizing neuromuscular blocking agent
7
Q
dantrolene
A
spasmolytic - muscle relaxant
8
Q
echothiophate
A
acetylcholinesterase inhibitor
9
Q
edrophonium
A
acetylcholinesterase inhibitor
10
Q
neostigmine
A
acetylcholinesterase inhibitor
11
Q
physostigmine
A
acetylcholinesterase inhibitor
12
Q
pyridostigmine
A
acetylcholinesterase inhibitor
13
Q
atropine
A
antimuscarinic
14
Q
pralidoxime
A
cholinesterase reactivator
15
Q
spasmolytics
A
centrally acting
16
Q
nondepolarizing neuromuscular blocking agent
A
agonist at nAChR
17
Q
depolarizing neuromuscular blocking agent
A
excess of depolarizing agonist
ex. succinylcholine
18
Q
all neuromuscular blocking agents
A
highly polar and inactive orally
must be given parenterally**
19
Q
quaternary nitrogen
A
make poorly lipid soluble - limit CNS entry
20
Q
kidney excretion
A
longer half life
21
Q
liver excretion
A
shorter half life
22
Q
rocuronium
A
fast onset and short duration of action
23
Q
diaphragm
A
last muscle to be paralyzed and quickest to recover
24
Q
reversal of neuromuscular blockade
A
reversed with ACh or succinylcholine
also - may give cholinesterase inhibitor
25
edrophonium
pure cholinesterase inhibitor
26
neostigmine and pyridostigmine
cholinesterase inhibitor AND increase release of ACh at motor nerve terminal
27
large dose of neuromuscular blockade
enter pore of nAChR - more intense blockade - diminish ability of acetylcholinesterase inhibitor to antagonize effect
28
adverse of nondepolarizing agents
histamine release
| -wheals, bronchospasm, hypotension
29
tubocuraine
declined use
- because of histamine release
- and very long duration of action
30
inhaled anesthetic
potentiate neuromuscular blockade
31
aging and neuromuscular response
longer duration of action with nondepolarizing agents in older patient - bc of reduced hepatic and renal function
so need to decrease dose**
usually age >70yo
32
myasthenia gravis
enhanced effect of neuromuscular blockade
33
severe burn and upper motor neuron disease
resistant to nondepolarizing agents
need higher dose
34
laudanosine
breadown product of atracurium and cisatracurium
high concentration in brain - seizures
35
long acting steroid relaxant
pancuronium
high potency
36
intermediate acting steroid relaxant
vecuronium and rocuronium
37
steroid nondepolarizing agent for several days in ICU
3 hydroxy metabolite can cause prolonged paralysis
38
least tendency for histamine release
steroid neuromuscular blocking agents
39
paralysis for >1 hour
pancuronium
40
rapid time of onset, intermediate duration, low potency
rocuronium
41
rapid onset anesthesia
rocuronium
42
2-4 minute onset (slower), intermediate duration, high potency
vecuronium
43
succinycholine pharmacokinetics
ultra short duration of action
44
phase 1 succinylcholine block
depolarizing
depolarized membrane remains depolarized
-flaccid paralysis occurs
augmented by cholinesterase inhibitors
45
phase 2 succinylcholine block
desensitizing
initial end plate depolarization decreases and membrane repolarized
membrane unable to depolarize again - bc desensitized
reversed by AChE inhibitors
46
rapid sequence induction
succinylcholine
47
adverse effects of succinylcholine
cardiac arrhythmia
negative inotropic and chronotropic effect
larger dose - positive effects above
intraocular pressure
intragastric pressure
muscle pain
histamine release
48
CI for succinylcholine
fam hx of malignant hyperthermia
myopathies
major burn, multi trauma, denervation
49
black box warning succinylcholine
cardiac arrest risk
-health children with undiagnosed skeletal m myopathy
acute rhabdomyolysis, hyperK, ventricular dysrhythmia, cardiac arrest, and even death
50
tx of malignant hyperthermia
caused by abnormal release of Ca from stores in skeletal m
tx - dantrolene
51
first choice for rapid sequence intubation
succinylcholine
52
MOA dantrolene
inhibit RyR calcium channel
blocks release of Ca from SR
53
CI for dantrolene
no oral if hepatitis
54
MOA botulinum
cleave SNARE complex and block release of ACh
55
cholinesterase inhibitors
indirect acting
causes increase in ACh at synapse
56
butyrylcholinesterase
pseudocholinesterase
plasma and liver
57
acetylcholinesterase
in NMJ
58
edrophonium
alcohol AChE inhibitor
binding noncovalent and reversible
59
neostigmine
carbamic acid ester AChE inhibitor
noncovalent and reversible binding to AChE
60
pyridostigmine
carbamic acid ester AChE inhibitor
noncovalent and reversible binding to AChE
61
physostigmine
carbamic acid ester AChE inhibitor
noncovalent and reversible binding to AChE
62
echothiophate
organophosphate AChE inhibitor
63
tertiary and uncharged AChE inhibitors
CNS distribution
physostigmine
64
quaternary and charged AChE inhibitors
no CNS distribution
neostigmine, pyridostigmine, echothiophate
65
alcohol AChE inhibitors
short duration of action 2 - 10 mins
66
carbamic acid ester AChE inhibitors
30min to 6 hour action
67
organophosphate AChE inhibitors
hundreds of hours of action
68
aging
breaking of one O-P bonds of inhibitor
-further strengthens interaction
difficulty to break
69
organophosphate and tertiary AChE inhibitors
central and peripheral activity
70
tx of myasthenia gravis
pyridostigmine
neostigmine
ambenonium
do not cross BBB
dosing based on titrations
71
diagnosis of myasthenia gravis
edrophonium test
has been phased out
now - ice pack test - to fix ptosis temoprarily
72
myasthenic vs. cholinergic crisis
myasthenic - severe enough for intubation
cholinergic - side effect of excessive AChE inhibitors
differentiate two - edrophonium test
- myasthenic - symptoms improve
- cholinergic - symptoms unchanged or worsen
73
paralytic ileus tx
AChE inhibitors
74
tx of dementia
alzheimer type and parkinson association benefit from AChE inhibitor
75
physostigmine
crosses BBB
used as antimuscarinic antidote for intoxication
sx - vasodilation, anhidrosis, mydriasis, delirium, hallucinations
76
homicide and suicide
organophosphate and carbamate AChE inhibitors
sx - miosis, salivation, sweating, bronchial constriction, vomiting, diarrhea
route of admin - determines the sx
antidote - atropine - mAChR agonist
77
miosis
contraction of pupil
78
cholinesterase regenerator
pralidoxime
regenerate active enzyme from organophosphorous cholinesterase complex
give before aging
don't reverse central effects - doesn't enter CNS
79
prophylactic pyridostigmine
reduce incapacitation and mortality of nerve agent poisoning
for combat use military personnel
