6. NM blockade and paralysis Flashcards
clinical use of NM blockade
surgery
prevent muscle contractions
maintain muscle relaxation/ paralysis without deep general anaesthesia
cosmetic surgery
what does the patient experience during NM blockade
slow methodical paralysis in Skm
extrinsic muscles of eye first, then small muscles of face, hands followed by muscles of pharynx, respiratory muscles last
individuals still experience pain
sites of action
- prevent synthesis: block Ch uptake- slow, no clinical use and slow to reverse, hemicholonium
- prevent release- botulinum toxin, black widow spider venom
3, block receptor activation- nicotinic receptor antagonist - increase reuptake- AchE inhibitor reverses NM blockade
black widow spider venom
explosive Ach release- spasms, paralysis
Botulinum toxin: bacteria
produced by bacterium Clostridium botulinum
Botox clinical uses
cervical dystonia (NM movement disorder of head and neck)
blepharospasm: involuntary contraction of eye muscles
severe primary axillary hyperhidrosis: excessive sweating
non-depolarising
nAchR antagonist
useful for surgery
features of non depolarising block
high freq. stimulation causes tetanus with duration slightly longer than twitch
occupy without stimulating post-synaptic nACh receptors
additive effect of similar drugs
block is competitive
onset action 3-5 mins, duration typically 30+ min
how do you stop non-depolarising antagonist
agents that depolarise muscle membrane
drugs that increase Ach release as some receptors are still active
reversed by anticholinesterase (neostigmine)
Depolarising
nAchR agonist persistent activation of nAchR-> inactivation of vg sodium channels rapid onset of action (<1min) short duration (<5 mins) ideal for intubation, ECT, dislocations
features of depolarising agonist
block preceded by muscle twitches
during block tension tetanus is depressed but doesnt fade
AchE do no reverse block
block summates with other depolarising drugs
drugs with weak curare like action antagonise block
dual block
phase II depolarising block
in some individuals: assume characteristics of non-depolarising block
nAChR agonist/ depolarising blocker drugs
suxamethonium, dexamethonium
nAChR antagonist/ non-depolarising blocker drug
atracurium, vecuronium, gallamine
ACh- esterase inhibitor (anticholinesterase)
phsyiostigmine, neostigmine