Intro to NMJ Pharmacology Flashcards by Matt Stanton | Brainscape

Q

cisatracurium

A

nondepolarizing isoquinoline derivative

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Q

tubocurarine

A

nondepolarizing isoquinoline derivative

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Q

pancuronium

A

steroid derivative nondepolarizing agent

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Q

rocuronium

A

steroid derivative nondepolarizing agent

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Q

vecuronium

A

steroid derivative nondepolarizing agent

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Q

succinylcholine

A

depolarizing neuromuscular blocking agent

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Q

dantrolene

A

spasmolytic - muscle relaxant

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Q

echothiophate

A

acetylcholinesterase inhibitor

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Q

edrophonium

A

acetylcholinesterase inhibitor

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Q

neostigmine

A

acetylcholinesterase inhibitor

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Q

physostigmine

A

acetylcholinesterase inhibitor

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Q

pyridostigmine

A

acetylcholinesterase inhibitor

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Q

atropine

A

antimuscarinic

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Q

pralidoxime

A

cholinesterase reactivator

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Q

spasmolytics

A

centrally acting

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Q

nondepolarizing neuromuscular blocking agent

A

agonist at nAChR

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Q

depolarizing neuromuscular blocking agent

A

excess of depolarizing agonist

ex. succinylcholine

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Q

all neuromuscular blocking agents

A

highly polar and inactive orally

must be given parenterally**

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Q

quaternary nitrogen

A

make poorly lipid soluble - limit CNS entry

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Q

kidney excretion

A

longer half life

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Q

liver excretion

A

shorter half life

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Q

rocuronium

A

fast onset and short duration of action

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Q

diaphragm

A

last muscle to be paralyzed and quickest to recover

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Q

reversal of neuromuscular blockade

A

reversed with ACh or succinylcholine

also - may give cholinesterase inhibitor

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Q

edrophonium

A

pure cholinesterase inhibitor

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Q

neostigmine and pyridostigmine

A

cholinesterase inhibitor AND increase release of ACh at motor nerve terminal

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Q

large dose of neuromuscular blockade

A

enter pore of nAChR - more intense blockade - diminish ability of acetylcholinesterase inhibitor to antagonize effect

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Q

adverse of nondepolarizing agents

A

histamine release

-wheals, bronchospasm, hypotension

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Q

tubocuraine

A

declined use

because of histamine release
and very long duration of action

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Q

inhaled anesthetic

A

potentiate neuromuscular blockade

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Q

aging and neuromuscular response

A

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

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Q

myasthenia gravis

A

enhanced effect of neuromuscular blockade

Q

severe burn and upper motor neuron disease

A

resistant to nondepolarizing agents

need higher dose

Q

laudanosine

A

breadown product of atracurium and cisatracurium

high concentration in brain - seizures

Q

long acting steroid relaxant

A

pancuronium

high potency

Q

intermediate acting steroid relaxant

A

vecuronium and rocuronium

Q

steroid nondepolarizing agent for several days in ICU

A

3 hydroxy metabolite can cause prolonged paralysis

Q

least tendency for histamine release

A

steroid neuromuscular blocking agents

Q

paralysis for >1 hour

A

pancuronium

Q

rapid time of onset, intermediate duration, low potency

A

rocuronium

Q

rapid onset anesthesia

A

rocuronium

Q

2-4 minute onset (slower), intermediate duration, high potency

A

vecuronium

Q

succinycholine pharmacokinetics

A

ultra short duration of action

Q

phase 1 succinylcholine block

A

depolarizing

depolarized membrane remains depolarized
-flaccid paralysis occurs

augmented by cholinesterase inhibitors

Q

phase 2 succinylcholine block

A

desensitizing

initial end plate depolarization decreases and membrane repolarized

membrane unable to depolarize again - bc desensitized

reversed by AChE inhibitors

Q

rapid sequence induction

A

succinylcholine

Q

adverse effects of succinylcholine

A

cardiac arrhythmia
negative inotropic and chronotropic effect

larger dose - positive effects above

intraocular pressure
intragastric pressure
muscle pain
histamine release

Q

CI for succinylcholine

A

fam hx of malignant hyperthermia
myopathies
major burn, multi trauma, denervation

Q

black box warning succinylcholine

A

cardiac arrest risk
-health children with undiagnosed skeletal m myopathy

acute rhabdomyolysis, hyperK, ventricular dysrhythmia, cardiac arrest, and even death

Q

tx of malignant hyperthermia

A

caused by abnormal release of Ca from stores in skeletal m

tx - dantrolene

Q

first choice for rapid sequence intubation

A

succinylcholine

Q

MOA dantrolene

A

inhibit RyR calcium channel

blocks release of Ca from SR

Q

CI for dantrolene

A

no oral if hepatitis

Q

MOA botulinum

A

cleave SNARE complex and block release of ACh

Q

cholinesterase inhibitors

A

indirect acting

causes increase in ACh at synapse

Q

butyrylcholinesterase

A

pseudocholinesterase

plasma and liver

Q

acetylcholinesterase

A

in NMJ

Q

edrophonium

A

alcohol AChE inhibitor

binding noncovalent and reversible

Q

neostigmine

A

carbamic acid ester AChE inhibitor

noncovalent and reversible binding to AChE

Q

pyridostigmine

A

carbamic acid ester AChE inhibitor

noncovalent and reversible binding to AChE

Q

physostigmine

A

carbamic acid ester AChE inhibitor

noncovalent and reversible binding to AChE

Q

echothiophate

A

organophosphate AChE inhibitor

Q

tertiary and uncharged AChE inhibitors

A

CNS distribution

physostigmine

Q

quaternary and charged AChE inhibitors

A

no CNS distribution

neostigmine, pyridostigmine, echothiophate

Q

alcohol AChE inhibitors

A

short duration of action 2 - 10 mins

Q

carbamic acid ester AChE inhibitors

A

30min to 6 hour action

Q

organophosphate AChE inhibitors

A

hundreds of hours of action

Q

aging

A

breaking of one O-P bonds of inhibitor
-further strengthens interaction

difficulty to break

Q

organophosphate and tertiary AChE inhibitors

A

central and peripheral activity

Q

tx of myasthenia gravis

A

pyridostigmine
neostigmine
ambenonium

do not cross BBB

dosing based on titrations

Q

diagnosis of myasthenia gravis

A

edrophonium test

has been phased out

now - ice pack test - to fix ptosis temoprarily

Q

myasthenic vs. cholinergic crisis

A

myasthenic - severe enough for intubation
cholinergic - side effect of excessive AChE inhibitors

differentiate two - edrophonium test

myasthenic - symptoms improve
cholinergic - symptoms unchanged or worsen

Q

paralytic ileus tx

A

AChE inhibitors

Q

tx of dementia

A

alzheimer type and parkinson association benefit from AChE inhibitor

Q

physostigmine

A

crosses BBB

used as antimuscarinic antidote for intoxication

sx - vasodilation, anhidrosis, mydriasis, delirium, hallucinations

Q

homicide and suicide

A

organophosphate and carbamate AChE inhibitors

sx - miosis, salivation, sweating, bronchial constriction, vomiting, diarrhea

route of admin - determines the sx

antidote - atropine - mAChR agonist

Q

miosis

A

contraction of pupil

Q

cholinesterase regenerator

A

pralidoxime

regenerate active enzyme from organophosphorous cholinesterase complex

give before aging
don’t reverse central effects - doesn’t enter CNS

Q

prophylactic pyridostigmine

A

reduce incapacitation and mortality of nerve agent poisoning

for combat use military personnel