Local Anesthetics Flashcards
what characteristic of local anesthetics allows them to cross cell membranes
they’re amphipathic- both lipophilic and hydrophilic characteristics
are ester linked or amide linked local anesthetics more prone to rapid hydrolysis and inactivation
ester
are ester linked or amide linked local anesthetics at high risk for causing hypersensitivity
ester
are ester linked or amide linked local anesthetics used more on mucous surfaces
ester
what is the mechanism of action of local anesthetics
bind with cytoplasmic receptors and inhibit VGNaC, prolonging the channel in the inactive form
do local anesthetics have high affinity for resting, activated, or inactivated VGNaC
inactivated
the effects of local anesthetics are pronounced in __ and not in __
in rapidly firing axons
not in resting neurons
how many nodes of ranvier are sufficient to induce local anesthesia
2-3
does an increase in extracellular calcium increase of decrease the effects of local anesthesia
increase
tetrodotoxin comes from __
puffer fish
saxitoxin comes from __
algae
ciguatoxin comes from __
exotic fish
batrachotoxin comes from __
frogs
what is the order of blockage between motor, sensory, and autonomic fibers
autonomic first, then sensory and motor
what is the order of recovery between motor, sensory, and autonomic fibers
motor, sensory, then autonomics
are smaller or larger fibers more sensitive to blockade
small
are myelinated or unmyelinated fibers more sensitive to blockade
myelinated
what fibers, A/B/C, are affected first due to their response to low concentration of local anesthetic
B
what is an example of a differential blockade in which local anesthetics block sensory impulses while sparing motor and proprioception
labor analgesia
diffusion of local anesthetics is in the __ (unionized basic or charged) form, which is then converted to the __ (unionized basic or charged) form inside the axon
diffusion= unionized basic
converted to charged
what is the relationship between local anesthetic effect and inflammation
inflammation produces lactic acid products. acidification of tissues slows the local anesthetic effectiveness
the anesthetic becomes charged and is unable to penetrate the nerve cell membrane
what can be done to eliminate the effect of increased acidity with inflammation when giving a local anesthetic
enhance with sodium bicarbonate to increase the pH
amide linked local anesthetics use is cautioned in those with __, __, and those taking __
hepatic disease
congestive heart failure
beta blockers
local anesthetics have drug-drug interaction with what 2 classes of drug
alpha 2 agonist
opioids