Neuromuscular blockers Flashcards
Which subunits MUST be occupied to open the nicotinic receptor at the motor endplate?
a. alpha and alpha
b. alpha and gamma
c. alpha and delta
d. alpha and epsilon
a. alpha and alpha
The neuromuscular junction is the synaptic connection between a
motor nerve and skeletal muscle
When the presynaptic nerve terminal depolarizes, it releases ___________ into the synaptic cleft
acetylcholine
__________________ is a pentameric ligand-gated ion channel located in the motor endplate at the neuromuscular junction
The postsynaptic nicotinic receptor
_______________ is an enzyme that terminates the effect of Ach
acetylcholinesterase
When acetylcholine binds to the _____________ on the postsynaptic nicotinic receptor, it allows _______ to enter the skeletal muscle.
two alpha-subunits; Na+
What are the type types of nicotinic acetylcholine receptors at the neuromuscular junction?
prejunctional Nn receptor is present on the presynaptic nerve (n= nerve)
postsynaptic Nm receptor is present at the motor endplate on the muscle cell (m= muscle)
What are the subunits of the postsynaptic nicotinic receptor?
2 alpha
1 beta
1 delta
1 epsilon
At rest, the inside of the muscle cell is ____ relative to the outside of the cell.
negative
Why don’t anions (like Cl-) pass through the postsynaptic nicotinic receptor channel?
they’re repelled by the negative charge in the channel
How is the action of Ach terminated at the post-junctional nicotinic receptor?
- Ach is metabolized by acetylcholinesterase to choline and acetate
- it diffuses away from the receptor
All of the following statements regarding extrajunctional nicotinic receptors are true EXCEPT:
a. it’s opened by choline
b. an epsilon subunit replaces a gamma subunit
c. it opens for a longer period of time
d. denervation allows for its proliferation
b. an epsilon subunit replaces a gamma subunit
______________ or ______________ can lead to the proliferation of extrajunctional receptors
Denervation injury or prolonged immobility
In the absence of extrajunctional receptors, succinylcholine can transiently increase serum potassium by ________________ for up to ____________.
0.5-1.0 mEq/L for up to 10-15 minutes
The presence of extrajunctional receptors predisposes the patient to _________ following succinylcholine administration.
hyperkalemia
As a general rule, in the event of a denervation injury, succinylcholine is best avoided ______________ following the injury and at least ______________
24-48 hours and at least one year after
Treatment of succinylcholine-induced hyperkalemia includes
IV calcium chloride
hyperventilation
glucose+ insulin
sodium bicarbonate
Patients with upregulation of extrajunctional receptors are ______________ to nondepolarizers.
resistant
this reduces the potency of these drugs
How many pathologic variants of the nicotinic receptor are there?
two
What are the two pathologic variants of the nicotinic receptor?
The a7 subtype consists of five alpha subunits
The a2B1… subtype has a gamma subunit instead of an epsilon subunit
What conditions represent contraindications to the use of succinylcholine?
upper or lower motor neuron injury
spinal cord injury
burns
skeletal muscle trauma
cerebrovascular accident
tetanus
severe sepsis
muscular dystrophy
prolonged chemical denervation (magnesium, long term NMB infusion, clostridial toxin)
________ may be an exception to this rule, as risk of hyperkalemia can persist for several years after
Burns
Fade during train-of-four stimulation is caused by:
a. agonism of presynaptic nicotinic receptors
b. antagonism of presynaptic nicotinic receptors
c. impaired presynaptic acetylcholine reuptake
d. decreased acetylcholine synthesis
b. antagonism of presynaptic nicotinic receptors
Fade during train-of-four stimulation is most likely caused by
antagonism of presynaptic Nn receptors