Neuromuscular relaxants Flashcards
What do NMB produce?
paralysis
Do NMB produce amnesia or analgesia?
NO
What are the pharm effects of NMB?
-interrupt nerve impulses at the NMJ -similar structure to the endogenous neurotransmitter acetylcholine (Ach) - provides muscle relaxation
Ca channels and nicotinic receptors are embedded where?
lipid bilayer
Are nicotinic receptors presynapic or postsynaptic?
POSTsynaptic
Describe the neuromuscular transmission release of Ach from nerve terminal…

AP and depolarizing of nerve terminal Ca channels open ca diffuses down gradient to nerve terminal Ach spills out into synaptic cleft Presynaptic nicotinic receptor responds to Ach by increasing in the synthesis and release of Ache
Describe the events at postsynaptic membrane

Ach combines with nicotinic receptors Both nicotinic receptors occupied. Channels open Na, Ca diffuse into cell and K diffuse out. Motor end plate depolarizes AP potentiated Skeletal muscle contracts
What is terminated by neurotransmitter action?
acetylcholinesterase (AChe) The choline is transported back to the nerve terminal and reconverted to Ach
Acetylcholine receptor _ protein subunits Central core for _ channeling Ach must bind to both _ subunits to open the core A subunits are the site of agonism and antagonism
Acetylochline receptor 5 protein subunits central core for cation channeling Ach must bind to both A subunits to open the core “A” subunits are the site of agonism and antagonism
Nondepolarizing BLOCK Nondepolarizing agents are competitive _. _ can not attach to the receptor Channels can not _ _ _ effect on the channel
inhibitors Ach open no direct
Depolarizing BLOCK _ binds to _ receptors, channel opens, motor endplate depolarizes _ contraction occurs Sch not metabolized by _ _ _ cannot be initiated
Succs, nicotinic single true acetylcholinesterases - channels stay open until Sch diffuses back into the circulation AP
What is a depolarizing muscle relaxant?
Succinylcholine
What are nondepolarizing muscle relaxants? (acd mpp rrv)
Mivacurium Rapacuronium Rocuronium Vecuronium Atracurium Cisatracurium Pipecuronium Pancuronium Doxacurium (ACD MPP RRV)
Succs: is there a reversal agent?
no
Succs: metabolism: rapid hydrolysis by _
pseudocholinesterase = plasma cholinesterase = an enzyme of the liver and plasma
How is a Sch block terminated?
by diffusion of Sch away from the neuromuscular junction
What are the Sch side effects for pediatrics?
contraindicated in routine mgmt d/t side effects MHAUS strongly advises against Sch use in children IV atropine 0.02mg/kg
What does the black box warning about Sch say for pediatrics?
-IV bolus admin may result in Malignant ventricular arrythmias and cardiac arrest 2 to actue rhado with HYPERkalemia. - IV bolus may result in profound bradycardia/asystole. Bradycardia is higher following a 2nd dose of succs. The occurrence of bradyarrhythmias may be reduced by pretreatment with atropine.
What are the side effects of Sch?
HYPERkalemia = increased with burns, trauma, nerve damage, neuromuscular disease, renal failure Muscle pains (fasciculations) INCREASED ICP, IOP, IGP =intragastric pressure (IGP) Massester spasm =jaw muscle rigidity in assoc with limb flaccidity Potent MH trigger agent
Dibucaine is a _ _ inhibits normal _ # indicates _ makeup of a person with regard to _ # is _ NOT _
Dibucaine is a local anesthetic inhibits normal pseudocholinesterase genetic makeup of a person with regard to pseduocholinesterase is qualitative NOT quanitative
Describe the incidence, dibucaine number, duration of homozygous typical…
incidence: normal Dibucaine #: 70-80 duration: 4-6 minutes
Describe the incidence, dibucaine number, duration of heterozygous atypical…
incidence: 1/50 patients Dibucaine #: 50-60 duration: 20-30 minutes
Describe the incidence, dibucaine number, duration of homozygous atypical…
incidence: 1/3000 Dibucaine #: 20-30 duration: 4-8 hours
Chemical properties of NonDepolarMR __ ammonium Steroid derivatives of _ Benzylisoquinolines are _ soluble Principle route of elimination is __ excretion
quaternary ammonium steroid derivatives of benzylisquinolines Benzylisoquinolines are water soluble = inhibits uptake into hepatocytes leads to lack of liver elimination = exception is steroid based relaxants Priniciple route of elimination is urinary excretion