Nicotinic antagonists Flashcards
nondepolarizing competitive antagonists MOA
hold the Nm receptor closed, preventing Na+ flow and depolarization–> no muscle contraction
effect of nondepolarizing blockers can be overcome with
ACh, as they are competitive antagonists
the only depolarizing blocker
succinylcholine
succinylcholine MOA
holds Nm open, continual flow of Na+ causes continual, longer than normal depolarization, which causes Nm to desensitize to subsequent ACh stimulation
neuromuscular blocking agents DO NOT
produce unconsciousness or anesthesia because they do not enter the brain
due to their high degree of ionization
neuromuscular blocking agents are NOT absorbed orally and do NOT enter CNS. IV ONLY.
nondepolarzing blockers interfere with the mobilization of ACh from the nerve terminal by
blocking pre-junctional sodium channels
endplate potential _______ when a nondepolarizing blocker is taken
decreases, an action potential can no longer be generated –> lack of muscle contraction (paralysis)
pharmacologic reversal for nondepolarizing blockers
cholinesterase inhibitors (increase ACh which can outcompete blockers)
muscles that are affected first by nondepolarizing blockers
small muscles followed by larger muscles
muscles that are affected last by nondepolarizing blockers
diaphragm, intercostal muscles
onset of action and recovery from succinylcholine are ________, so it’s used for
rapid
short procedures
succinylcholine’s action is terminated by
plama pseudocholinesterase
dibucaine
a local anesthetic that causes inhibition of AChE
abnormal dibucaine number
20%: abnormal cholinesterase acitivity, succinylcholine with last way too long