Lecture 8: ANS Neuromuscular Blockers Flashcards
each somatic neuron of the neuromuscular junction has many presynaptic boutons that create localized regions where ___ is released in close proximity to the ____ receptors on the other side of the synapse
Ach, Nm Ach
Nm Ach receptors are a specific nictonic subtype receptor only. found at the ____
neuromuscular jucntion
activation of Nm Ach receptors causes membrane ___ leading to ___
depolarization, muscle contraction
in the case of muscles, breakdown of ach causes ___
muscle relaxation
when ach binds to the Nm receptor there is an influx of ___ ions
Na
____ breaks down Ach, which allows channels to close, causing membrane to be ___
ache; repolarize
prolonged activation of Nm receptors leasd to ___
muscle paralysis
what 3 things can cause muscle paralysis at Nm receptors?
- organophospahte
- nerve gas
- nicotine overdose
if Nm channels are not activated it can have a ___ effect
paralytic
_____ are used in conjunction with anesthesia in surgery to prevent muscle contraction and achieve temporary paralysis
neuromuscualr blockers
wha are the 2 main types of neuromuscular blockers?
- depolarizing
2. non-depolarizing
what is the role of Nm antagonsits?
prevent passing of ions through the channel, preventing muscle contractio
what is the classic exampleof non-depolarizing neuromuscualr blocker?
tubocuranine
what is tubocurarine the derivative of?
a natural product used by hunters of native tribes to paralyze prey
what happens to Ach binding in the presence of tubocurarine?
unable to bind to Nm receptor and channel remains closed
tubocurarine is a ___ of the Nm receptor
competitive antagonsist
the paralytic effects of tubocurarine can be reversed by increasing ___ . Thsi can be done by adding ____ inhibitor
adding more Ach to the synaptic cleft ; ache
what is an example of a depolarizing neuromuscular blocker?
succinylcholine
succinylcholine binds to ion channels once they have alredy ___
opened
succinylcholine is a ___ of the Nm receptor
competitive antagonist
what is the effect of succinylcholine binding to channels once they are already open?
preliminary depolarization and muscle contraction
describe the “depolarization block” caused by succinylcholine
becease cells cannot rapidly repolarize, they are held in a refractory state that will not respond to furthe stimuli
as long as succinylcholine is bound to the receptor, the cells may slowly ___ over several minutes, but ___ will be delayed
repolarize, reactivation and contraction
is succinylcholine reversible or irreversible
reversible
because the blocking effect of succinylcholine is acheived by holding the channel open, the block cannot be ___ inhibited using ache inhibitors
competively
botulinum toxin binds to the ___ complex, preventing the release of ___
SNAP; Ach
botulinum toxin is a ____ toxin that interferes with the process of ___
bacterial; exocytosis of Ach vessicles
systemic exposure of botulinum toxin causes ____ and ___ but local administration is used to treat ___ and ___
paralysis and death; wrinkles, migraine pain
does botox interact with cholinergic receptors directly? What type of antagonist does this make botox?
No; indirect